An organic cation transporter found in kidney. It is localized to the basal lateral membrane and is likely to be involved in the renal secretion of organic cations.
A family of proteins involved in the transport of organic cations. They play an important role in the elimination of a variety of endogenous substances, xenobiotics, and their metabolites from the body.
A group of membrane transport proteins that transport biogenic amine derivatives of catechol across the PLASMA MEMBRANE. Catecholamine plasma membrane transporter proteins regulate neural transmission as well as catecholamine metabolism and recycling.
Positively charged atoms, radicals or groups of atoms which travel to the cathode or negative pole during electrolysis.
An active neurotoxic metabolite of 1-METHYL-4-PHENYL-1,2,3,6-TETRAHYDROPYRIDINE. The compound reduces dopamine levels, inhibits the biosynthesis of catecholamines, depletes cardiac norepinephrine and inactivates tyrosine hydroxylase. These and other toxic effects lead to cessation of oxidative phosphorylation, ATP depletion, and cell death. The compound, which is related to PARAQUAT, has also been used as an herbicide.
A class of sodium-independent nucleoside transporters that mediate the facilitative transport of NUCLEOSIDES.
A potassium-selective ion channel blocker. (From J Gen Phys 1994;104(1):173-90)
A constituent of STRIATED MUSCLE and LIVER. It is an amino acid derivative and an essential cofactor for fatty acid metabolism.
The movement of materials (including biochemical substances and drugs) through a biological system at the cellular level. The transport can be across cell membranes and epithelial layers. It also can occur within intracellular compartments and extracellular compartments.
A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.
Proteins involved in the transport of organic anions. They play an important role in the elimination of a variety of endogenous substances, xenobiotics and their metabolites from the body.
A subclass of ORGANIC ANION TRANSPORTERS that do not rely directly or indirectly upon sodium ion gradients for the transport of organic ions.
A polyspecific transporter for organic cations found primarily in the kidney. It mediates the coupled exchange of alpha-ketoglutarate with organic ions such as P-AMINOHIPPURIC ACID.
Transport proteins that carry specific substances in the blood or across cell membranes.
A ubiquitously expressed octamer transcription factor that regulates GENETIC TRANSCRIPTION of SMALL NUCLEAR RNA; IMMUNOGLOBULIN GENES; and HISTONE H2B genes.
A biguanide hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. Metformin improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose. (From Martindale, The Extra Pharmacopoeia, 30th ed, p289)
Pyridinium compounds are organic salts formed when pyridine, a basic heterocyclic organic compound, reacts with acids, resulting in a positively charged nitrogen atom surrounded by aromatic rings.
Membrane proteins whose primary function is to facilitate the transport of molecules across a biological membrane. Included in this broad category are proteins involved in active transport (BIOLOGICAL TRANSPORT, ACTIVE), facilitated transport and ION CHANNELS.
Tetraethylammonium compounds refer to a group of organic salts containing the tetraethylammonium ion (N(C2H5)4+), which is characterized by four ethyl groups bonded to a central nitrogen atom, and are commonly used in research and medicine as pharmacological tools for studying ion channels.
Body organ that filters blood for the secretion of URINE and that regulates ion concentrations.
An acetic acid ester of CARNITINE that facilitates movement of ACETYL COA into the matrices of mammalian MITOCHONDRIA during the oxidation of FATTY ACIDS.
A competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.
Epithelial cell line originally derived from porcine kidneys. It is used for pharmacologic and metabolic studies.
The commonest and widest ranging species of the clawed "frog" (Xenopus) in Africa. This species is used extensively in research. There is now a significant population in California derived from escaped laboratory animals.
The movement of ions across energy-transducing cell membranes. Transport can be active, passive or facilitated. Ions may travel by themselves (uniport), or as a group of two or more ions in the same (symport) or opposite (antiport) directions.
A naturally occurring metabolite of HISTIDINE that has antioxidant properties.
Membrane transporters that co-transport two or more dissimilar molecules in the opposite direction across a membrane. Usually the transport of one ion or molecule is against its electrochemical gradient and is "powered" by the movement of another ion or molecule with its electrochemical gradient.
The movement of materials across cell membranes and epithelial layers against an electrochemical gradient, requiring the expenditure of metabolic energy.
Biogenic amines having only one amine moiety. Included in this group are all natural monoamines formed by the enzymatic decarboxylation of natural amino acids.
The renal tubule portion that extends from the BOWMAN CAPSULE in the KIDNEY CORTEX into the KIDNEY MEDULLA. The proximal tubule consists of a convoluted proximal segment in the cortex, and a distal straight segment descending into the medulla where it forms the U-shaped LOOP OF HENLE.
Proteins which are found in membranes including cellular and intracellular membranes. They consist of two types, peripheral and integral proteins. They include most membrane-associated enzymes, antigenic proteins, transport proteins, and drug, hormone, and lectin receptors.
The prototypical uricosuric agent. It inhibits the renal excretion of organic anions and reduces tubular reabsorption of urate. Probenecid has also been used to treat patients with renal impairment, and, because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy.
Agents that affect ION PUMPS; ION CHANNELS; ABC TRANSPORTERS; and other MEMBRANE TRANSPORT PROTEINS.
Membrane proteins whose primary function is to facilitate the transport of positively charged molecules (cations) across a biological membrane.
The glycine amide of 4-aminobenzoic acid. Its sodium salt is used as a diagnostic aid to measure effective renal plasma flow (ERPF) and excretory capacity.
Derivatives of ammonium compounds, NH4+ Y-, in which all four of the hydrogens bonded to nitrogen have been replaced with hydrocarbyl groups. These are distinguished from IMINES which are RN=CR2.
Positively charged atoms, radicals or groups of atoms with a valence of plus 2, which travel to the cathode or negative pole during electrolysis.
Established cell cultures that have the potential to propagate indefinitely.
A family of MEMBRANE TRANSPORT PROTEINS that require ATP hydrolysis for the transport of substrates across membranes. The protein family derives its name from the ATP-binding domain found on the protein.
The rate dynamics in chemical or physical systems.
Female germ cells derived from OOGONIA and termed OOCYTES when they enter MEIOSIS. The primary oocytes begin meiosis but are arrested at the diplotene state until OVULATION at PUBERTY to give rise to haploid secondary oocytes or ova (OVUM).
An adrenocortical steroid that has modest but significant activities as a mineralocorticoid and a glucocorticoid. (From Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed, p1437)
A histamine H1 antagonist. It has mild hypnotic properties and some local anesthetic action and is used for allergies (including skin eruptions) both parenterally and locally. It is a common ingredient of cold remedies.
An optical isomer of quinine, extracted from the bark of the CHINCHONA tree and similar plant species. This alkaloid dampens the excitability of cardiac and skeletal muscles by blocking sodium and potassium currents across cellular membranes. It prolongs cellular ACTION POTENTIALS, and decreases automaticity. Quinidine also blocks muscarinic and alpha-adrenergic neurotransmission.
Positively charged atoms, radicals or group of atoms with a valence of plus 1, which travel to the cathode or negative pole during electrolysis.
Accumulation of a drug or chemical substance in various organs (including those not relevant to its pharmacologic or therapeutic action). This distribution depends on the blood flow or perfusion rate of the organ, the ability of the drug to penetrate organ membranes, tissue specificity, protein binding. The distribution is usually expressed as tissue to plasma ratios.
RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
The uptake of naked or purified DNA by CELLS, usually meaning the process as it occurs in eukaryotic cells. It is analogous to bacterial transformation (TRANSFORMATION, BACTERIAL) and both are routinely employed in GENE TRANSFER TECHNIQUES.
Drugs used for their effects on the kidneys' regulation of body fluid composition and volume. The most commonly used are the diuretics. Also included are drugs used for their antidiuretic and uricosuric actions, for their effects on the kidneys' clearance of other drugs, and for diagnosis of renal function.
The normality of a solution with respect to HYDROGEN ions; H+. It is related to acidity measurements in most cases by pH = log 1/2[1/(H+)], where (H+) is the hydrogen ion concentration in gram equivalents per liter of solution. (McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)
A characteristic feature of enzyme activity in relation to the kind of substrate on which the enzyme or catalytic molecule reacts.
A cell line generated from human embryonic kidney cells that were transformed with human adenovirus type 5.
The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.
A basic constituent of lecithin that is found in many plants and animal organs. It is important as a precursor of acetylcholine, as a methyl donor in various metabolic processes, and in lipid metabolism.
A member of the alkali group of metals. It has the atomic symbol Na, atomic number 11, and atomic weight 23.
Drugs that selectively bind to but do not activate histamine H2 receptors, thereby blocking the actions of histamine. Their clinically most important action is the inhibition of acid secretion in the treatment of gastrointestinal ulcers. Smooth muscle may also be affected. Some drugs in this class have strong effects in the central nervous system, but these actions are not well understood.
An octamer transcription factor expressed primarily in B-LYMPHOCYTES and the developing CENTRAL NERVOUS SYSTEM that regulates GENETIC TRANSCRIPTION of IMMUNOGLOBULIN GENES.
A genus of the family Muridae consisting of eleven species. C. migratorius, the grey or Armenian hamster, and C. griseus, the Chinese hamster, are the two species used in biomedical research.
The domestic dog, Canis familiaris, comprising about 400 breeds, of the carnivore family CANIDAE. They are worldwide in distribution and live in association with people. (Walker's Mammals of the World, 5th ed, p1065)
CELL LINE derived from the ovary of the Chinese hamster, Cricetulus griseus (CRICETULUS). The species is a favorite for cytogenetic studies because of its small chromosome number. The cell line has provided model systems for the study of genetic alterations in cultured mammalian cells.
Human colonic ADENOCARCINOMA cells that are able to express differentiation features characteristic of mature intestinal cells, such as ENTEROCYTES. These cells are valuable in vitro tools for studies related to intestinal cell function and differentiation.
A 170-kDa transmembrane glycoprotein from the superfamily of ATP-BINDING CASSETTE TRANSPORTERS. It serves as an ATP-dependent efflux pump for a variety of chemicals, including many ANTINEOPLASTIC AGENTS. Overexpression of this glycoprotein is associated with multidrug resistance (see DRUG RESISTANCE, MULTIPLE).
An amine derived by enzymatic decarboxylation of HISTIDINE. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and also a centrally acting neurotransmitter.
The concentration of a compound needed to reduce population growth of organisms, including eukaryotic cells, by 50% in vitro. Though often expressed to denote in vitro antibacterial activity, it is also used as a benchmark for cytotoxicity to eukaryotic cells in culture.
The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.
The insertion of recombinant DNA molecules from prokaryotic and/or eukaryotic sources into a replicating vehicle, such as a plasmid or virus vector, and the introduction of the resultant hybrid molecules into recipient cells without altering the viability of those cells.
Membrane transporters that co-transport two or more dissimilar molecules in the same direction across a membrane. Usually the transport of one ion or molecule is against its electrochemical gradient and is "powered" by the movement of another ion or molecule with its electrochemical gradient.
The main structural component of the LIVER. They are specialized EPITHELIAL CELLS that are organized into interconnected plates called lobules.
A large lobed glandular organ in the abdomen of vertebrates that is responsible for detoxification, metabolism, synthesis and storage of various substances.
The relationship between the dose of an administered drug and the response of the organism to the drug.
An octamer transcription factor that is expressed primarily in totipotent embryonic STEM CELLS and GERM CELLS and is down-regulated during CELL DIFFERENTIATION.
A variation of the PCR technique in which cDNA is made from RNA via reverse transcription. The resultant cDNA is then amplified using standard PCR protocols.
The action of a drug that may affect the activity, metabolism, or toxicity of another drug.
A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.
Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.
Unstable isotopes of carbon that decay or disintegrate emitting radiation. C atoms with atomic weights 10, 11, and 14-16 are radioactive carbon isotopes.
Single-stranded complementary DNA synthesized from an RNA template by the action of RNA-dependent DNA polymerase. cDNA (i.e., complementary DNA, not circular DNA, not C-DNA) is used in a variety of molecular cloning experiments as well as serving as a specific hybridization probe.
A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.
A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator.
Organic compounds which contain platinum as an integral part of the molecule.
Characteristic restricted to a particular organ of the body, such as a cell type, metabolic response or expression of a particular protein or antigen.
The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.
A highly vascularized mammalian fetal-maternal organ and major site of transport of oxygen, nutrients, and fetal waste products. It includes a fetal portion (CHORIONIC VILLI) derived from TROPHOBLASTS and a maternal portion (DECIDUA) derived from the uterine ENDOMETRIUM. The placenta produces an array of steroid, protein and peptide hormones (PLACENTAL HORMONES).
Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.
Tritium is an isotope of hydrogen (specifically, hydrogen-3) that contains one proton and two neutrons in its nucleus, making it radioactive with a half-life of about 12.3 years, and is used in various applications including nuclear research, illumination, and dating techniques due to its low energy beta decay.
Substances which lower blood glucose levels.
An antiviral that is used in the prophylactic or symptomatic treatment of influenza A. It is also used as an antiparkinsonian agent, to treat extrapyramidal reactions, and for postherpetic neuralgia. The mechanisms of its effects in movement disorders are not well understood but probably reflect an increase in synthesis and release of dopamine, with perhaps some inhibition of dopamine uptake.
A single nucleotide variation in a genetic sequence that occurs at appreciable frequency in the population.
Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures.

The interaction of n-tetraalkylammonium compounds with a human organic cation transporter, hOCT1. (1/158)

Polyspecific organic cation transporters in epithelia play an important role in the elimination of many endogenous bioactive amines and therapeutically important drugs. Recently, the first human organic cation transporter (hOCT1) was cloned from liver. The purpose of the current study was to determine the effect of molecular size and hydrophobicity on the transport of organic cations by hOCT1. We studied the interaction of a series of n-tetraalkylammonium (n-TAA) compounds (alkyl chain length, N, ranging from 1 to 6 carbons) with hOCT1 in a transiently transfected human cell line, HeLa. [14C]tetraethylammonium (TEA) uptake was measured under different experimental conditions. Both cis-inhibition and trans-stimulation studies were carried out. With the exception of tetramethylammonium, all of the n-TAAs significantly inhibited [14C]TEA uptake. A reversed correlation of IC50 values (range, 3.0-260 microM) with alkyl chain lengths or partition coefficients (LogP) was observed. trans-Stimulation studies revealed that TEA, tetrapropylammonium, tetrabutylammonium, as well as tributylmethylammonium trans-stimulated TEA uptake mediated by hOCT1. In contrast, tetramethylammonium and tetrapentylammonium did not trans-stimulate [14C]TEA uptake, and tetrahexylammonium demonstrated an apparent "trans-inhibition" effect. These data indicate that with increasing alkyl chain lengths (N >/= 2), n-TAA compounds are more poorly translocated by hOCT1 although their potency of inhibition increases. Similar findings were obtained with nonaliphatic hydrocarbons. These data suggest that a balance between hydrophobic and hydrophilic properties is necessary for binding and subsequent translocation by hOCT1.  (+info)

Identity of the F52F12.1 gene product in Caenorhabditis elegans as an organic cation transporter. (2/158)

We describe here the cloning and functional characterization of an organic cation transporter from Caenorhabditis elegans (CeOCT1). The CeOCT1 cDNA is 1826 bp long and codes for a protein of 568 amino acids. The oct1 gene is approximately 3.2 kb in size and consists of 12 exons. The location of this gene corresponds to the F52F12.1 gene locus on chromosome I. The predicted protein contains 12 putative transmembrane domains. It exhibits significant homology to mammalian OCTs. When expressed in mammalian cells, CeOCT1 induces the transport of the prototypical organic cation tetraethylammonium. The Michaelis-Menten constant for this substrate is 80+/-16 microM. The substrate specificity of CeOCT1 is broad. This represents the first report on the cloning and functional characteristics of an organic cation transporter from C. elegans.  (+info)

Selective substrates for non-neuronal monoamine transporters. (3/158)

The recently identified transport proteins organic cation transporter 1 (OCT1), OCT2, and extraneuronal monoamine transporter (EMT) accept dopamine, noradrenaline, adrenaline, and 5-hydroxytryptamine as substrates and hence qualify as non-neuronal monoamine transporters. In the present study, selective transport substrates were identified that allow, by analogy to receptor agonists, functional discrimination of these transporters. To contrast efficiency of solute transport, stably transfected 293 cell lines, each expressing a single transporter, were examined side by side in uptake experiments with radiolabeled substrates. Normalized uptake rates indicate that tetraethylammonium, with a rate of about 0.5 relative to 1-methyl-4-phenylpyridinium (MPP+), is a good substrate for OCT1 and OCT2. It was not, however, accepted as substrate by EMT. Choline was transported exclusively by OCT1, with a rate of about 0.5 relative to MPP+. Histamine was a good substrate with a rate of about 0.6 relative to MPP+ for OCT2 and EMT, but was not transported by OCT1. Guanidine was an excellent substrate for OCT2, with a rate as high as that of MPP+. Transport of guanidine by OCT1 was low, and transport by EMT was negligible. With the guanidine derivatives cimetidine and creatinine, a pattern strikingly similar to guanidine was observed. Collectively, these substrates reveal key differences in solute recognition and turnover and thus challenge the concept of "polyspecific" organic cation transporters. In addition, our data, when compared with previous studies, suggest that OCT2 corresponds to the organic cation/H+ antiport mechanism in renal brush-border membrane vesicles, and that EMT corresponds to the guanidine/H+ antiport mechanism in membrane vesicles from placenta and intestine.  (+info)

Selectivity of the polyspecific cation transporter rOCT1 is changed by mutation of aspartate 475 to glutamate. (4/158)

After site-directed mutagenesis, the organic cation transporter rOCT1 was expressed in Xenopus laevis oocytes or human embryonic kidney cells and functionally characterized. rOCT1 belongs to a new family of polyspecific transporters that includes transporters for organic cations and anions and the Na(+)-carnitine cotransporter. When glutamate was substituted for Asp475 (middle of the proposed 11th transmembrane alpha-helix), the V(max) values for choline, tetraethylammonium (TEA), N(1)-methylnicotinamide, and 1-methyl-4-phenylpyridinium were reduced by 89 to 98%. The apparent K(m) values were also decreased (choline by 15-fold, TEA by 8-fold, N(1)-methylnicotinamide by 4-fold) or remained constant (1-methyl-4-phenylpyridinium). After the mutation, the membrane potential dependence of the K(m) value for [(3)H]choline uptake was abolished. The affinity of n-tetraalkyl ammonium compounds to inhibit TEA uptake was increased. This affinity and its increase by the D475E mutation were increased with the length of the n-alkyl chains. After expression in X. laevis oocytes, the IC(50) ratios of wild-type and D475E mutant were 1.7 (tetramethylammonium), 4.3 (TEA), 5.0 (tetrapropylammonium), 5.0 (tetrabutylammonium), and 65 (tetrapentylammonium). Cationic inhibitors with ring structures were differentially affected: the IC(50) value for TEA inhibition by cyanine 863 remained unchanged, whereas it was increased for quinine. The data suggest that rOCT1 contains a large cation-binding pocket with several interaction domains that may be responsible for high-affinity binding of structurally different cations and that Asp475 is located close to one of these interaction domains.  (+info)

Interactions of HIV protease inhibitors with a human organic cation transporter in a mammalian expression system. (5/158)

Recently, we cloned a human organic cation transporter, hOCT1, which is expressed primarily in the liver. hOCT1 plays an important role in the cellular uptake and elimination of various xenobiotics including therapeutically important drugs. HIV protease inhibitors are a new class of therapeutic agents. The purpose of this study was to elucidate the interactions of HIV protease inhibitors with hOCT1 and to determine whether hOCT1 is involved in the elimination of these compounds. We studied the interactions of HIV protease inhibitors with hOCT1 in a transiently transfected human cell line, HeLa. Uptake studies were carried out 40 h post-transfection using the radiolabeled model organic cation, [(14)C]tetraethylammonium (TEA), under different experimental conditions. In cis-inhibition studies, all of the HIV protease inhibitors tested, i.e., indinavir (IC(50) of 62 microM), nelfinavir (IC(50) of 22 microM), ritonavir (IC(50) of 5.2 microM), and saquinavir (IC(50) of 8.3 microM) inhibited TEA uptake in HeLa cells expressing hOCT1. However, none of the HIV protease inhibitors trans-stimulated [(14)C]TEA uptake, suggesting that they are poorly translocated by hOCT1. Nelfinavir, ritonavir, and saquinavir demonstrated an apparent "trans-inhibition" effect. No enhanced uptake of [(14)C]saquinavir was observed in hOCT1 DNA-transfected cells versus empty vector-transfected cells. These data suggest that HIV protease inhibitors are potent inhibitors, but poor substrates, of hOCT1. Some HIV protease inhibitors may potently inhibit the uptake and elimination of cationic drugs that are substrates for hOCT1, leading to potential drug-drug interactions. Other transporters, e.g., MDR1 and MRP1, in HIV-targeted cells may control the intracellular concentrations of HIV protease inhibitors.  (+info)

Kinetic and selectivity differences between rodent, rabbit, and human organic cation transporters (OCT1). (6/158)

Organic cation transporters play an important role in the absorption, distribution, and elimination of clinical agents, toxic substances, and endogenous compounds. In kidney preparations, significant differences in functional characteristics of organic cation transport between various species have been reported. However, the underlying molecular mechanisms responsible for these interspecies differences are not known. The goal of this study was to determine the kinetics and substrate selectivities of organic cation transporter (OCT1) homologs from mouse, rat, rabbit, and human that may contribute to interspecies differences in the renal and hepatic handling of organic cations. With a series of n-tetraalkylammonium (nTAA) compounds, a correlation between increasing alkyl chain length and affinity for the four OCT1 homologs was observed. However, the apparent affinity constants (K(i)) differed among the species homologs. For the mouse homolog mOCT1, apparent K(i) values ranged from 7 microM for tetrabutylammonium to 2000 microM for tetramethylammonium. In contrast, the human homolog hOCT1 exhibited weaker interactions with the nTAA compounds. Trans-stimulation studies and current measurements in voltage-clamped oocytes demonstrated that larger nTAA compounds were transported at greater rates in oocytes expressing hOCT1, whereas smaller nTAAs were transported at greater rates in oocytes expressing mOCT1 or rOCT1. The rabbit homolog rbOCT1 exhibited intermediate properties in its interactions with nTAAs compared with its rodent and human counterparts. This report demonstrates that the human OCT1 homolog has functional properties distinct from those of the rodent and rabbit OCT1 homologs. The study underscores potential difficulties in extrapolating data from preclinical studies in animal models to humans.  (+info)

Developmentally regulated expression of organic ion transporters NKT (OAT1), OCT1, NLT (OAT2), and Roct. (7/158)

Several xenobiotic (organic cation and anion) transporters have recently been identified, although their endogenous substrates, if such exist, remain unknown. When we initially identified NKT, also known as OAT1, the first member of the organic anion transporter (OAT) family (Lopez-Nieto CE, You G, Bush KT, Barros EJ, Beier DR, and Nigam SK. J Biol Chem 272: 6471-6478, 1997), we noted its expression in the embryonic kidney. We have now demonstrated its transporter function and more fully examined the spatiotemporal expression patterns of representative organic ion transporters, [NKT (OAT1), Roct, OCT1, and NLT, also known as OAT2] during murine development. In the kidney, NKT (OAT1), OCT1, and Roct transcripts appeared at midgestation, coinciding with proximal tubule differentiation, and gradually increased during nephron maturation. A similar pattern was observed for NLT (OAT2) in the liver and kidney, although, in the kidney, NLT (OAT2) transcription did not increase as dramatically. The roughly cotemporal expression of these related transporters in the developing proximal tubule may indicate common transcriptional regulation. Expression during embryogenesis in extrarenal sites could suggest a role in the formation and maintenance of nonrenal tissues. Importantly, all four genes were expressed in unexpected places during nonrenal organogenesis: Roct in the fetal liver (temporally coinciding with the onset of hematopoiesis) and neural tissue; NKT (OAT1) in the fetal brain; OCT1 in the ascending aorta and atrium; and NLT (OAT2) in the fetal lung, intestine, skin, and developing bone. Because these gene products mediate the transport of a broad range of metabolites and toxins, it seems likely that, apart from their known functions, these transporters play a role in transport of organic molecules, perhaps including those with morphogenetic activity. These genes could also play important developmental roles independent of transport function.  (+info)

The affinity of the organic cation transporter rOCT1 is increased by protein kinase C-dependent phosphorylation. (8/158)

Members of the organic cation transporter (OCT) family are mainly expressed in kidney, liver, intestine, and brain. The regulation of the OCT type 1 from rat (rOCT1) stably transfected in HEK293 cells was examined using a fluorimetric technique, 1-[(3)H]methyl-4-phenylpyridinium uptake studies, and fast-whole-cell patch-clamp recordings. For the fluorescence measurements, the cation 4-(4-(dimethylamino)styryl)-N-methylpyridinium iodide (ASP(+)) was used as substrate. Uptake of ASP(+) via rOCT1 was electrogenic, and its inhibition by other organic cations was consistent with previously reported radioactive tracer flux measurements. The inhibitor quinine was not translocated by the organic cation transporter in contrast to tetraethylammonium. Stimulation of diacyl glycerol-dependent protein kinase C (PKC) by sn-1,2-dioctanoyl glycerol (1 microM) resulted in an increase in initial ASP(+) uptake rate by 216 +/- 28% (n = 29). The effect was completely antagonized by the PKC inhibitor tamoxifen (20 microM, n = 22). Forskolin (1 microM), which activates adenylate cyclase and thereby protein kinase A (PKA), stimulated the initial rate of ASP(+) accumulation by 51 +/- 6% (n = 19). This effect was inhibited by the specific PKA inhibitor KT5720 (1 microM, n = 12). Inhibition of tyrosine kinases by aminogenestein (10 microM) reduced ASP(+) uptake by 63 +/- 7% (n = 7), while genestein or tyrphostin AG1295 (each 10 microM) were without significant effects. Incubation of the cells with sn-1, 2-dioctanoyl glycerol (1 microM) increased the affinities of the transporter to tetraethylammonium, tetrapenthylammonium, and quinine by a factor of 58, 14.5, and 2.4, respectively. Western blot analysis revealed that rOCT1 protein was phosphorylated at a serine residue upon stimulation of PKC. In conclusion, it has been demonstrated that the organic cation transport by rOCT1 is stimulated by PKC, PKA, and endogenous tyrosine kinase activation. The PKC phosphorylates rOCT1 and leads to a conformational change at the substrate binding site.  (+info)

Organic Cation Transporter 1 (OCT1) is a protein that belongs to the solute carrier family 22 (SLC22A). It is primarily expressed in the liver and plays an essential role in the uptake and elimination of various organic cations, including many drugs, from the systemic circulation into hepatocytes. OCT1 also transports some endogenous substances such as neurotransmitters and hormones. Mutations or variants in the OCT1 gene can affect drug response and disposition, making it an important factor to consider in personalized medicine.

Organic cation transport proteins (OCTs) are a group of membrane transporters that facilitate the movement of organic cations across biological membranes. These transporters play an essential role in the absorption, distribution, and elimination of various endogenous and exogenous substances, including drugs and toxins.

There are four main types of OCTs, namely OCT1, OCT2, OCT3, and OCTN1 (also known as novel organic cation transporter 1 or OCT6). These proteins belong to the solute carrier (SLC) family, specifically SLC22A.

OCTs have a broad substrate specificity and can transport various organic cations, such as neurotransmitters (e.g., serotonin, dopamine, histamine), endogenous compounds (e.g., creatinine, choline), and drugs (e.g., metformin, quinidine, morphine). The transport process is typically sodium-independent and can occur in both directions, depending on the concentration gradient of the substrate.

OCTs are widely expressed in various tissues, including the liver, kidney, intestine, brain, heart, and placenta. Their expression patterns and functions vary among different OCT types, contributing to their diverse roles in physiology and pharmacology. Dysfunction of OCTs has been implicated in several diseases, such as drug toxicity, neurodegenerative disorders, and cancer.

In summary, organic cation transport proteins are membrane transporters that facilitate the movement of organic cations across biological membranes, playing crucial roles in the absorption, distribution, and elimination of various substances, including drugs and toxins.

Catecholamine plasma membrane transport proteins, also known as neurotransmitter transporters or simply transporters, are a type of membrane protein responsible for the reuptake of catecholamines (such as dopamine, norepinephrine, and epinephrine) from the synaptic cleft back into the presynaptic neuron. These proteins play a crucial role in regulating neurotransmitter concentrations in the synapse and terminating neurotransmission. They are targets for various psychoactive drugs, including antidepressants, psychostimulants, and cocaine.

A cation is a type of ion, which is a charged particle, that has a positive charge. In chemistry and biology, cations are formed when a neutral atom loses one or more electrons during chemical reactions. The removal of electrons results in the atom having more protons than electrons, giving it a net positive charge.

Cations are important in many biological processes, including nerve impulse transmission, muscle contraction, and enzyme function. For example, sodium (Na+), potassium (K+), calcium (Ca2+), and magnesium (Mg2+) are all essential cations that play critical roles in various physiological functions.

In medical contexts, cations can also be relevant in the diagnosis and treatment of various conditions. For instance, abnormal levels of certain cations, such as potassium or calcium, can indicate specific diseases or disorders. Additionally, medications used to treat various conditions may work by altering cation concentrations or activity within the body.

1-Methyl-4-phenylpyridinium (MPP+) is a neurotoxic compound that is widely used in scientific research to study Parkinson's disease and other neurological disorders. MPP+ is an ionic form of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), which is a lipophilic compound that can cross the blood-brain barrier and be converted to MPP+ by monoamine oxidase B (MAO-B) in glial cells.

MPP+ is taken up by dopaminergic neurons through the dopamine transporter (DAT), where it inhibits complex I of the electron transport chain, leading to mitochondrial dysfunction and energy depletion. This results in the death of dopaminergic neurons, which are the primary cells affected in Parkinson's disease.

MPP+ has been used as a model compound to study the mechanisms of neurodegeneration in Parkinson's disease and other neurological disorders, and it has also been used in the development of potential therapeutic strategies for these conditions.

Equilibrative nucleoside transport proteins (ENTs) are a type of membrane transporter that regulate the bidirectional movement of nucleosides across the cell membrane. They facilitate the diffusion of nucleosides down their concentration gradient, hence the term "equilibrative." These transport proteins play a crucial role in maintaining intracellular nucleoside concentrations and ensuring proper nucleotide synthesis for various cellular processes, including DNA replication, repair, and gene expression. There are two major families of ENTs: the human equilibrative nucleoside transporters (hENTs) and the concentrative nucleoside transporters (CNTs). The hENT family includes four members (hENT1-4), while the CNT family consists of three members (CNT1-3). These transport proteins have been identified as potential targets for cancer therapy, as inhibiting their function can selectively sensitize tumor cells to nucleoside analog-based chemotherapies.

Tetraethylammonium (TEA) is not typically defined in the context of medical terminology, but rather it is a chemical compound with the formula (C2H5)4N+. It is used in research and development, particularly in the field of electrophysiology where it is used as a blocking agent for certain types of ion channels.

Medically, TEA may be mentioned in the context of its potential toxicity or adverse effects on the human body. Exposure to TEA can cause symptoms such as nausea, vomiting, diarrhea, abdominal pain, headache, dizziness, and confusion. Severe exposure can lead to more serious complications, including seizures, respiratory failure, and cardiac arrest.

Therefore, while Tetraethylammonium is not a medical term per se, it is important for healthcare professionals to be aware of its potential health hazards and take appropriate precautions when handling or working with this compound.

Carnitine is a naturally occurring substance in the body that plays a crucial role in energy production. It transports long-chain fatty acids into the mitochondria, where they can be broken down to produce energy. Carnitine is also available as a dietary supplement and is often used to treat or prevent carnitine deficiency.

The medical definition of Carnitine is:

"A quaternary ammonium compound that occurs naturally in animal tissues, especially in muscle, heart, brain, and liver. It is essential for the transport of long-chain fatty acids into the mitochondria, where they can be oxidized to produce energy. Carnitine also functions as an antioxidant and has been studied as a potential treatment for various conditions, including heart disease, diabetes, and kidney disease."

Carnitine is also known as L-carnitine or levocarnitine. It can be found in foods such as red meat, dairy products, fish, poultry, and tempeh. In the body, carnitine is synthesized from the amino acids lysine and methionine with the help of vitamin C and iron. Some people may have a deficiency in carnitine due to genetic factors, malnutrition, or certain medical conditions, such as kidney disease or liver disease. In these cases, supplementation may be necessary to prevent or treat symptoms of carnitine deficiency.

Biological transport refers to the movement of molecules, ions, or solutes across biological membranes or through cells in living organisms. This process is essential for maintaining homeostasis, regulating cellular functions, and enabling communication between cells. There are two main types of biological transport: passive transport and active transport.

Passive transport does not require the input of energy and includes:

1. Diffusion: The random movement of molecules from an area of high concentration to an area of low concentration until equilibrium is reached.
2. Osmosis: The diffusion of solvent molecules (usually water) across a semi-permeable membrane from an area of lower solute concentration to an area of higher solute concentration.
3. Facilitated diffusion: The assisted passage of polar or charged substances through protein channels or carriers in the cell membrane, which increases the rate of diffusion without consuming energy.

Active transport requires the input of energy (in the form of ATP) and includes:

1. Primary active transport: The direct use of ATP to move molecules against their concentration gradient, often driven by specific transport proteins called pumps.
2. Secondary active transport: The coupling of the movement of one substance down its electrochemical gradient with the uphill transport of another substance, mediated by a shared transport protein. This process is also known as co-transport or counter-transport.

Cimetidine is a histamine-2 (H2) receptor antagonist, which is a type of medication that reduces the production of stomach acid. It works by blocking the action of histamine on the H2 receptors in the stomach, which are responsible for stimulating the release of stomach acid. By blocking these receptors, cimetidine reduces the amount of stomach acid produced and can help to relieve symptoms such as heartburn, indigestion, and stomach ulcers.

Cimetidine is available by prescription in various forms, including tablets, capsules, and liquid. It is typically taken two or three times a day, depending on the specific condition being treated. Common side effects of cimetidine may include headache, dizziness, diarrhea, and constipation.

In addition to its use in treating stomach acid-related conditions, cimetidine has also been studied for its potential anti-cancer properties. Some research suggests that it may help to enhance the immune system's response to cancer cells and reduce the growth of certain types of tumors. However, more research is needed to confirm these effects and determine the optimal dosage and duration of treatment.

Organic anion transporters (OATs) are membrane transport proteins that are responsible for the cellular uptake and excretion of various organic anions, such as drugs, toxins, and endogenous metabolites. They are found in various tissues, including the kidney, liver, and brain, where they play important roles in the elimination and detoxification of xenobiotics and endogenous compounds.

In the kidney, OATs are located in the basolateral membrane of renal tubular epithelial cells and mediate the uptake of organic anions from the blood into the cells. From there, the anions can be further transported into the urine by other transporters located in the apical membrane. In the liver, OATs are expressed in the sinusoidal membrane of hepatocytes and facilitate the uptake of organic anions from the blood into the liver cells for metabolism and excretion.

There are several isoforms of OATs that have been identified, each with distinct substrate specificities and tissue distributions. Mutations in OAT genes can lead to various diseases, including renal tubular acidosis, hypercalciuria, and drug toxicity. Therefore, understanding the function and regulation of OATs is important for developing strategies to improve drug delivery and reduce adverse drug reactions.

Organic anion transporters (OATs) are membrane transport proteins that facilitate the movement of organic anions across biological membranes. The term "sodium-independent" refers to the fact that these particular OATs do not require the presence of sodium ions for their transport function.

Sodium-independent OATs are a subgroup of the larger family of organic anion transporters, which also includes sodium-dependent OATs. These transporters play important roles in the elimination and distribution of various endogenous and exogenous organic anions, including drugs, toxins, and metabolic waste products.

In the kidney, for example, sodium-independent OATs are located in the basolateral membrane of renal tubular epithelial cells and are involved in the secretion and reabsorption of organic anions. They help maintain the balance of these compounds in the body by facilitating their movement into and out of cells, often in conjunction with other transport proteins that move these compounds across the apical membrane of the tubular epithelial cells.

Overall, sodium-independent OATs are important for the proper functioning of various physiological processes, including drug disposition, toxin elimination, and waste product clearance.

Organic anion transport protein 1 (OATP1) is not a specific medical term, but it refers to a type of membrane transporter protein that is involved in the cellular uptake of organic anions, such as drugs, toxins, and endogenous compounds. It is primarily expressed in the liver and plays a crucial role in the hepatic clearance of these substances.

The official medical definition of OATP1 may vary depending on the specific context or source, but it generally refers to a member of the solute carrier organic anion transporter family (SLCO), specifically SLCO1A2, which is also known as OATP1B1. This protein is responsible for the transport of various drugs and their metabolites, including statins, antibiotics, and antiviral agents, into hepatocytes for further metabolism and elimination.

It's worth noting that there are several other members of the OATP family with different tissue distributions and substrate specificities, such as OATP1B3 (SLCO1B3) and OATP2B1 (SLCO2B1). Therefore, it is essential to specify which particular protein is being referred to when using the term "OATP1."

Carrier proteins, also known as transport proteins, are a type of protein that facilitates the movement of molecules across cell membranes. They are responsible for the selective and active transport of ions, sugars, amino acids, and other molecules from one side of the membrane to the other, against their concentration gradient. This process requires energy, usually in the form of ATP (adenosine triphosphate).

Carrier proteins have a specific binding site for the molecule they transport, and undergo conformational changes upon binding, which allows them to move the molecule across the membrane. Once the molecule has been transported, the carrier protein returns to its original conformation, ready to bind and transport another molecule.

Carrier proteins play a crucial role in maintaining the balance of ions and other molecules inside and outside of cells, and are essential for many physiological processes, including nerve impulse transmission, muscle contraction, and nutrient uptake.

Octamer Transcription Factor-1 (OTF-1 or Oct-1) is a protein that, in humans, is encoded by the OCT1 gene. It belongs to the class of transcription factors known as POU domain proteins, which are characterized by a highly conserved DNA-binding domain called the POU domain.

Oct-1 binds to the octamer motif (ATGCAAAT) in the regulatory regions of many genes and plays a crucial role in regulating their expression. It can act as both an activator and repressor of transcription, depending on the context and the interactions with other proteins. Oct-1 is widely expressed in various tissues and is involved in several cellular processes, including cell cycle regulation, differentiation, and DNA damage response.

Metformin is a type of biguanide antihyperglycemic agent used primarily in the treatment of type 2 diabetes mellitus. It works by decreasing glucose production in the liver, reducing glucose absorption in the gut, and increasing insulin sensitivity in muscle and fat tissue. By lowering both basal and postprandial plasma glucose levels, metformin helps to control blood sugar levels and improve glycemic control. It is also used off-label for various other indications such as polycystic ovary syndrome (PCOS) and gestational diabetes. Common side effects include diarrhea, nausea, vomiting, and abdominal discomfort. Lactic acidosis is a rare but serious side effect that requires immediate medical attention.

Pyridinium compounds are organic salts that contain a positively charged pyridinium ion. Pyridinium is a type of cation that forms when pyridine, a basic heterocyclic organic compound, undergoes protonation. The nitrogen atom in the pyridine ring accepts a proton (H+) and becomes positively charged, forming the pyridinium ion.

Pyridinium compounds have the general structure of C5H5NH+X-, where X- is an anion or negatively charged ion. These compounds are often used in research and industry, including as catalysts, intermediates in chemical synthesis, and in pharmaceuticals. Some pyridinium compounds have been studied for their potential therapeutic uses, such as in the treatment of bacterial infections or cancer. However, it is important to note that some pyridinium compounds can also be toxic or reactive, so they must be handled with care.

Membrane transport proteins are specialized biological molecules, specifically integral membrane proteins, that facilitate the movement of various substances across the lipid bilayer of cell membranes. They are responsible for the selective and regulated transport of ions, sugars, amino acids, nucleotides, and other molecules into and out of cells, as well as within different cellular compartments. These proteins can be categorized into two main types: channels and carriers (or pumps). Channels provide a passive transport mechanism, allowing ions or small molecules to move down their electrochemical gradient, while carriers actively transport substances against their concentration gradient, requiring energy usually in the form of ATP. Membrane transport proteins play a crucial role in maintaining cell homeostasis, signaling processes, and many other physiological functions.

Tetraethylammonium compounds refer to chemical substances that contain the tetraethylammonium cation (N(C2H5)4+). This organic cation is derived from tetraethylammonium hydroxide, which in turn is produced by the reaction of ethyl alcohol with ammonia and then treated with a strong acid.

Tetraethylammonium compounds are used in various biomedical research applications as they can block certain types of ion channels, making them useful for studying neuronal excitability and neurotransmission. However, these compounds have also been associated with toxic effects on the nervous system and other organs, and their use is therefore subject to strict safety regulations.

A kidney, in medical terms, is one of two bean-shaped organs located in the lower back region of the body. They are essential for maintaining homeostasis within the body by performing several crucial functions such as:

1. Regulation of water and electrolyte balance: Kidneys help regulate the amount of water and various electrolytes like sodium, potassium, and calcium in the bloodstream to maintain a stable internal environment.

2. Excretion of waste products: They filter waste products from the blood, including urea (a byproduct of protein metabolism), creatinine (a breakdown product of muscle tissue), and other harmful substances that result from normal cellular functions or external sources like medications and toxins.

3. Endocrine function: Kidneys produce several hormones with important roles in the body, such as erythropoietin (stimulates red blood cell production), renin (regulates blood pressure), and calcitriol (activated form of vitamin D that helps regulate calcium homeostasis).

4. pH balance regulation: Kidneys maintain the proper acid-base balance in the body by excreting either hydrogen ions or bicarbonate ions, depending on whether the blood is too acidic or too alkaline.

5. Blood pressure control: The kidneys play a significant role in regulating blood pressure through the renin-angiotensin-aldosterone system (RAAS), which constricts blood vessels and promotes sodium and water retention to increase blood volume and, consequently, blood pressure.

Anatomically, each kidney is approximately 10-12 cm long, 5-7 cm wide, and 3 cm thick, with a weight of about 120-170 grams. They are surrounded by a protective layer of fat and connected to the urinary system through the renal pelvis, ureters, bladder, and urethra.

Acetyl-L-carnitine, also known as ALCAR, is a form of the amino acid carnitine. It is a naturally occurring substance in the body that plays a crucial role in energy production in cells, particularly within mitochondria, the "powerhouses" of the cell.

Acetyl-L-carnitine is involved in the transport of fatty acids into the mitochondria, where they can be broken down to produce energy. It also functions as an antioxidant, helping to protect cells from damage caused by free radicals.

This compound has been studied for its potential benefits in various medical conditions, including neurological disorders, cardiovascular diseases, and liver diseases. Some research suggests that Acetyl-L-carnitine may help improve cognitive function, reduce fatigue, and alleviate pain. However, more studies are needed to confirm these findings and establish the optimal dosage and safety profiles for different medical conditions.

It is important to note that while Acetyl-L-carnitine is available as a dietary supplement, its use should be discussed with a healthcare provider before starting any new supplement regimen, especially if you have a medical condition or are taking medication.

Famotidine is a type of medication called an H2 blocker, or histamine-2 receptor antagonist. It works by reducing the amount of acid produced in the stomach. Famotidine is commonly used to treat and prevent ulcers in the stomach and intestines, and to manage conditions where the stomach produces too much acid, such as Zollinger-Ellison syndrome. It is also used to treat gastroesophageal reflux disease (GERD) and other conditions in which acid backs up from the stomach into the esophagus, causing heartburn.

Famotidine is available by prescription and over-the-counter in various forms, including tablets, capsules, and liquid. It is important to take famotidine exactly as directed by a healthcare professional, and to talk to them about any potential risks or side effects.

I'm sorry for any confusion, but "LLC-PK1 cells" is not a widely recognized medical term or abbreviation in the field of medicine. LLC-PK1 is a specific type of cell line that is used in scientific research, particularly in the field of biology and pharmacology.

To be more precise, LLC-PK1 is a continuous porcine kidney cell line that is often used in laboratory experiments. It was established by fusing primary pig kidney cells with a heteroploid cell line. These cells are commonly used as a model system to study various biological and pharmacological processes, including the effects of drugs on kidney function, because of their ability to grow and divide indefinitely under controlled conditions.

However, without more specific context, it's difficult to provide a more detailed medical definition for "LLC-PK1 cells." If you have more information about how this term is being used, I may be able to give a more precise explanation.

"Xenopus laevis" is not a medical term itself, but it refers to a specific species of African clawed frog that is often used in scientific research, including biomedical and developmental studies. Therefore, its relevance to medicine comes from its role as a model organism in laboratories.

In a broader sense, Xenopus laevis has contributed significantly to various medical discoveries, such as the understanding of embryonic development, cell cycle regulation, and genetic research. For instance, the Nobel Prize in Physiology or Medicine was awarded in 1963 to John R. B. Gurdon and Sir Michael J. Bishop for their discoveries concerning the genetic mechanisms of organism development using Xenopus laevis as a model system.

Ion transport refers to the active or passive movement of ions, such as sodium (Na+), potassium (K+), chloride (Cl-), and calcium (Ca2+) ions, across cell membranes. This process is essential for various physiological functions, including nerve impulse transmission, muscle contraction, and maintenance of resting membrane potential.

Ion transport can occur through several mechanisms, including:

1. Diffusion: the passive movement of ions down their concentration gradient, from an area of high concentration to an area of low concentration.
2. Facilitated diffusion: the passive movement of ions through specialized channels or transporters in the cell membrane.
3. Active transport: the energy-dependent movement of ions against their concentration gradient, requiring the use of ATP. This process is often mediated by ion pumps, such as the sodium-potassium pump (Na+/K+-ATPase).
4. Co-transport or symport: the coupled transport of two or more different ions or molecules in the same direction, often driven by an electrochemical gradient.
5. Counter-transport or antiport: the coupled transport of two or more different ions or molecules in opposite directions, also often driven by an electrochemical gradient.

Abnormalities in ion transport can lead to various medical conditions, such as cystic fibrosis (which involves defective chloride channel function), hypertension (which may be related to altered sodium transport), and certain forms of heart disease (which can result from abnormal calcium handling).

Ergothioneine is a naturally occurring antioxidant compound that is found in various foods such as mushrooms, some types of beans, and certain grains. It is also produced by some bacteria that live in the human body. Ergothioneine has been shown to have potential health benefits due to its antioxidant properties, which help protect cells from damage caused by free radicals. Some studies suggest that ergothioneine may have neuroprotective effects and could play a role in preventing neurodegenerative diseases such as Parkinson's and Alzheimer's. However, more research is needed to fully understand the potential health benefits of this compound.

Antiporters, also known as exchange transporters, are a type of membrane transport protein that facilitate the exchange of two or more ions or molecules across a biological membrane in opposite directions. They allow for the movement of one type of ion or molecule into a cell while simultaneously moving another type out of the cell. This process is driven by the concentration gradient of one or both of the substances being transported. Antiporters play important roles in various physiological processes, including maintaining electrochemical balance and regulating pH levels within cells.

Biological transport, active is the process by which cells use energy to move materials across their membranes from an area of lower concentration to an area of higher concentration. This type of transport is facilitated by specialized proteins called transporters or pumps that are located in the cell membrane. These proteins undergo conformational changes to physically carry the molecules through the lipid bilayer of the membrane, often against their concentration gradient.

Active transport requires energy because it works against the natural tendency of molecules to move from an area of higher concentration to an area of lower concentration, a process known as diffusion. Cells obtain this energy in the form of ATP (adenosine triphosphate), which is produced through cellular respiration.

Examples of active transport include the uptake of glucose and amino acids into cells, as well as the secretion of hormones and neurotransmitters. The sodium-potassium pump, which helps maintain resting membrane potential in nerve and muscle cells, is a classic example of an active transporter.

Biogenic monoamines are a type of neurotransmitter, which are chemical messengers that transmit signals in the brain and other parts of the nervous system. They are called "biogenic" because they are derived from biological substances, and "monoamines" because they contain one amine group (-NH2) and are derived from the aromatic amino acids: tryptophan, tyrosine, and phenylalanine.

Examples of biogenic monoamines include:

1. Serotonin (5-hydroxytryptamine or 5-HT): synthesized from the amino acid tryptophan and plays a crucial role in regulating mood, appetite, sleep, memory, and learning.
2. Dopamine: formed from tyrosine and is involved in reward, motivation, motor control, and reinforcement of behavior.
3. Norepinephrine (noradrenaline): also derived from tyrosine and functions as a neurotransmitter and hormone that modulates attention, arousal, and stress responses.
4. Epinephrine (adrenaline): synthesized from norepinephrine and serves as a crucial hormone and neurotransmitter in the body's fight-or-flight response to stress or danger.
5. Histamine: produced from the amino acid histidine, it acts as a neurotransmitter and mediates allergic reactions, immune responses, and regulates wakefulness and appetite.

Imbalances in biogenic monoamines have been linked to various neurological and psychiatric disorders, such as depression, anxiety, Parkinson's disease, and schizophrenia. Therefore, medications that target these neurotransmitters, like selective serotonin reuptake inhibitors (SSRIs) for depression or levodopa for Parkinson's disease, are often used in the treatment of these conditions.

The proximal kidney tubule is the initial portion of the renal tubule in the nephron of the kidney. It is located in the renal cortex and is called "proximal" because it is closer to the glomerulus, compared to the distal tubule. The proximal tubule plays a crucial role in the reabsorption of water, electrolytes, and nutrients from the filtrate that has been formed by the glomerulus. It also helps in the secretion of waste products and other substances into the urine.

The proximal tubule is divided into two segments: the pars convoluta and the pars recta. The pars convoluta is the curved portion that receives filtrate from the Bowman's capsule, while the pars recta is the straight portion that extends deeper into the renal cortex.

The proximal tubule is lined with a simple cuboidal epithelium, and its cells are characterized by numerous mitochondria, which provide energy for active transport processes. The apical surface of the proximal tubular cells has numerous microvilli, forming a brush border that increases the surface area for reabsorption.

In summary, the proximal kidney tubule is a critical site for the reabsorption of water, electrolytes, and nutrients from the glomerular filtrate, contributing to the maintenance of fluid and electrolyte balance in the body.

Membrane proteins are a type of protein that are embedded in the lipid bilayer of biological membranes, such as the plasma membrane of cells or the inner membrane of mitochondria. These proteins play crucial roles in various cellular processes, including:

1. Cell-cell recognition and signaling
2. Transport of molecules across the membrane (selective permeability)
3. Enzymatic reactions at the membrane surface
4. Energy transduction and conversion
5. Mechanosensation and signal transduction

Membrane proteins can be classified into two main categories: integral membrane proteins, which are permanently associated with the lipid bilayer, and peripheral membrane proteins, which are temporarily or loosely attached to the membrane surface. Integral membrane proteins can further be divided into three subcategories based on their topology:

1. Transmembrane proteins, which span the entire width of the lipid bilayer with one or more alpha-helices or beta-barrels.
2. Lipid-anchored proteins, which are covalently attached to lipids in the membrane via a glycosylphosphatidylinositol (GPI) anchor or other lipid modifications.
3. Monotopic proteins, which are partially embedded in the membrane and have one or more domains exposed to either side of the bilayer.

Membrane proteins are essential for maintaining cellular homeostasis and are targets for various therapeutic interventions, including drug development and gene therapy. However, their structural complexity and hydrophobicity make them challenging to study using traditional biochemical methods, requiring specialized techniques such as X-ray crystallography, nuclear magnetic resonance (NMR) spectroscopy, and single-particle cryo-electron microscopy (cryo-EM).

Probenecid is a medication that is primarily used to treat gout and hyperuricemia (high levels of uric acid in the blood). It works by decreasing the production of uric acid in the body and increasing its excretion through the kidneys.

In medical terms, probenecid is a uricosuric agent, which means it increases the urinary excretion of urate, the salt form of uric acid. It does this by inhibiting the reabsorption of urate in the proximal tubules of the kidneys, thereby promoting its elimination in the urine.

Probenecid is also used in conjunction with certain antibiotics, such as penicillin and cephalosporins, to increase their concentration in the body by reducing their excretion by the kidneys. This is known as probenecid-antibiotic interaction.

It's important to note that probenecid should be used under the supervision of a healthcare provider, and its use may be contraindicated in certain medical conditions or in combination with specific medications.

Membrane transport modulators refer to a class of molecules that affect the movement of ions, nutrients, and other substances across cell membranes by interacting with membrane transport proteins. These proteins, also known as transporters or carriers, facilitate the passive or active transport of molecules in and out of cells.

Membrane transport modulators can either inhibit or enhance the activity of these transport proteins. They play a crucial role in pharmacology and therapeutics, as they can influence drug absorption, distribution, metabolism, and excretion (ADME). Examples of membrane transport modulators include ion channel blockers, inhibitors of efflux pumps like P-glycoprotein, and enhancers of nutrient uptake transporters.

It is important to note that the term "membrane transport modulator" can encompass a wide range of molecules with varying mechanisms and specificities, so further characterization is often necessary for a more precise understanding of their effects.

Cation transport proteins are a type of membrane protein that facilitate the movement of cations (positively charged ions) across biological membranes. These proteins play a crucial role in maintaining ion balance and electrical excitability within cells, as well as in various physiological processes such as nutrient uptake, waste elimination, and signal transduction.

There are several types of cation transport proteins, including:

1. Ion channels: These are specialized protein structures that form a pore or channel through the membrane, allowing ions to pass through rapidly and selectively. They can be either voltage-gated or ligand-gated, meaning they open in response to changes in electrical potential or binding of specific molecules, respectively.

2. Ion pumps: These are active transport proteins that use energy from ATP hydrolysis to move ions against their electrochemical gradient, effectively pumping them from one side of the membrane to the other. Examples include the sodium-potassium pump (Na+/K+-ATPase) and calcium pumps (Ca2+ ATPase).

3. Ion exchangers: These are antiporter proteins that facilitate the exchange of one ion for another across the membrane, maintaining electroneutrality. For example, the sodium-proton exchanger (NHE) moves a proton into the cell in exchange for a sodium ion being moved out.

4. Symporters: These are cotransporter proteins that move two or more ions together in the same direction, often coupled with the transport of a solute molecule. An example is the sodium-glucose cotransporter (SGLT), which facilitates glucose uptake into cells by coupling its movement with that of sodium ions.

Collectively, cation transport proteins help maintain ion homeostasis and contribute to various cellular functions, including electrical signaling, enzyme regulation, and metabolic processes. Dysfunction in these proteins can lead to a range of diseases, such as neurological disorders, cardiovascular disease, and kidney dysfunction.

p-Aminohippuric acid (PAH) is a small organic compound that is primarily used as a diagnostic agent in measuring renal plasma flow. It is freely filtered by the glomeruli and almost completely secreted by the proximal tubules of the kidney. This makes it an ideal candidate for measuring effective renal plasma flow, as changes in its clearance can indicate alterations in renal function.

In a medical context, PAH is often used in conjunction with other tests to help diagnose and monitor kidney diseases or conditions that affect renal function. The compound is typically administered intravenously, and its clearance is then measured through blood or urine samples collected over a specific period. This information can be used to calculate the renal plasma flow and assess the overall health of the kidneys.

It's important to note that while PAH is a valuable tool in clinical nephrology, it should be used as part of a comprehensive diagnostic workup and interpreted in conjunction with other test results and clinical findings.

Quaternary ammonium compounds (QACs) are a group of disinfectants and antiseptics that contain a nitrogen atom surrounded by four organic groups, resulting in a charged "quat" structure. They are widely used in healthcare settings due to their broad-spectrum activity against bacteria, viruses, fungi, and spores. QACs work by disrupting the cell membrane of microorganisms, leading to their death. Common examples include benzalkonium chloride and cetyltrimethylammonium bromide. It is important to note that some microorganisms have developed resistance to QACs, and they may not be effective against all types of pathogens.

Divalent cations are ions that carry a positive charge of +2. They are called divalent because they have two positive charges. Common examples of divalent cations include calcium (Ca²+), magnesium (Mg²+), and iron (Fe²+). These ions play important roles in various biological processes, such as muscle contraction, nerve impulse transmission, and bone metabolism. They can also interact with certain drugs and affect their absorption, distribution, and elimination in the body.

A cell line is a culture of cells that are grown in a laboratory for use in research. These cells are usually taken from a single cell or group of cells, and they are able to divide and grow continuously in the lab. Cell lines can come from many different sources, including animals, plants, and humans. They are often used in scientific research to study cellular processes, disease mechanisms, and to test new drugs or treatments. Some common types of human cell lines include HeLa cells (which come from a cancer patient named Henrietta Lacks), HEK293 cells (which come from embryonic kidney cells), and HUVEC cells (which come from umbilical vein endothelial cells). It is important to note that cell lines are not the same as primary cells, which are cells that are taken directly from a living organism and have not been grown in the lab.

ATP-binding cassette (ABC) transporters are a family of membrane proteins that utilize the energy from ATP hydrolysis to transport various substrates across extra- and intracellular membranes. These transporters play crucial roles in several biological processes, including detoxification, drug resistance, nutrient uptake, and regulation of cellular cholesterol homeostasis.

The structure of ABC transporters consists of two nucleotide-binding domains (NBDs) that bind and hydrolyze ATP, and two transmembrane domains (TMDs) that form the substrate-translocation pathway. The NBDs are typically located adjacent to each other in the cytoplasm, while the TMDs can be either integral membrane domains or separate structures associated with the membrane.

The human genome encodes 48 distinct ABC transporters, which are classified into seven subfamilies (ABCA-ABCG) based on their sequence similarity and domain organization. Some well-known examples of ABC transporters include P-glycoprotein (ABCB1), multidrug resistance protein 1 (ABCC1), and breast cancer resistance protein (ABCG2).

Dysregulation or mutations in ABC transporters have been implicated in various diseases, such as cystic fibrosis, neurological disorders, and cancer. In cancer, overexpression of certain ABC transporters can contribute to drug resistance by actively effluxing chemotherapeutic agents from cancer cells, making them less susceptible to treatment.

In the context of medicine and pharmacology, "kinetics" refers to the study of how a drug moves throughout the body, including its absorption, distribution, metabolism, and excretion (often abbreviated as ADME). This field is called "pharmacokinetics."

1. Absorption: This is the process of a drug moving from its site of administration into the bloodstream. Factors such as the route of administration (e.g., oral, intravenous, etc.), formulation, and individual physiological differences can affect absorption.

2. Distribution: Once a drug is in the bloodstream, it gets distributed throughout the body to various tissues and organs. This process is influenced by factors like blood flow, protein binding, and lipid solubility of the drug.

3. Metabolism: Drugs are often chemically modified in the body, typically in the liver, through processes known as metabolism. These changes can lead to the formation of active or inactive metabolites, which may then be further distributed, excreted, or undergo additional metabolic transformations.

4. Excretion: This is the process by which drugs and their metabolites are eliminated from the body, primarily through the kidneys (urine) and the liver (bile).

Understanding the kinetics of a drug is crucial for determining its optimal dosing regimen, potential interactions with other medications or foods, and any necessary adjustments for special populations like pediatric or geriatric patients, or those with impaired renal or hepatic function.

An oocyte, also known as an egg cell or female gamete, is a large specialized cell found in the ovary of female organisms. It contains half the number of chromosomes as a normal diploid cell, as it is the product of meiotic division. Oocytes are surrounded by follicle cells and are responsible for the production of female offspring upon fertilization with sperm. The term "oocyte" specifically refers to the immature egg cell before it reaches full maturity and is ready for fertilization, at which point it is referred to as an ovum or egg.

Corticosterone is a hormone produced by the adrenal gland in many animals, including humans. It is a type of glucocorticoid steroid hormone that plays an important role in the body's response to stress, immune function, metabolism, and regulation of inflammation. Corticosterone helps to regulate the balance of sodium and potassium in the body and also plays a role in the development and functioning of the nervous system. It is the primary glucocorticoid hormone in rodents, while cortisol is the primary glucocorticoid hormone in humans and other primates.

Pyrilamine is an antihistamine drug that is primarily used to relieve allergic symptoms such as sneezing, itching, watery eyes, and runny nose. It works by blocking the action of histamine, a substance naturally produced by the body during an allergic reaction. Pyrilamine may also be used to treat motion sickness and to help with tension headaches or migraines.

Pyrilamine is available in various forms, including tablets, capsules, and syrup, and it can be taken with or without food. Common side effects of pyrilamine include dizziness, dry mouth, and drowsiness. It is important to avoid activities that require mental alertness, such as driving or operating heavy machinery, until you know how pyrilamine affects you.

Like all medications, pyrilamine should be taken under the supervision of a healthcare provider, who can determine the appropriate dosage and monitor for any potential side effects or interactions with other drugs. It is essential to follow the instructions provided by your healthcare provider carefully and not exceed the recommended dose.

Quinidine is a Class IA antiarrhythmic medication that is primarily used to treat and prevent various types of cardiac arrhythmias (abnormal heart rhythms). It works by blocking the rapid sodium channels in the heart, which helps to slow down the conduction of electrical signals within the heart and stabilize its rhythm.

Quinidine is derived from the bark of the Cinchona tree and has been used for centuries as a treatment for malaria. However, its antiarrhythmic properties were discovered later, and it became an important medication in cardiology.

In addition to its use in treating arrhythmias, quinidine may also be used off-label for other indications such as the treatment of nocturnal leg cramps or myasthenia gravis. It is available in various forms, including tablets and injectable solutions.

It's important to note that quinidine has a narrow therapeutic index, meaning that there is only a small difference between an effective dose and a toxic one. Therefore, it must be carefully monitored to ensure that the patient is receiving a safe and effective dose. Common side effects of quinidine include gastrointestinal symptoms such as nausea, vomiting, and diarrhea, as well as visual disturbances, headache, and dizziness. More serious side effects can include QT prolongation, which can lead to dangerous arrhythmias, and hypersensitivity reactions.

A monovalent cation is a type of ion that has a single positive charge. In the context of medical and biological sciences, monovalent cations are important because they play crucial roles in various physiological processes, such as maintaining electrical neutrality in cells, facilitating nerve impulse transmission, and regulating fluid balance.

The most common monovalent cation is sodium (Na+), which is the primary cation in the extracellular fluid. Other examples of monovalent cations include potassium (K+), which is the main cation inside cells, and hydrogen (H+) ions, which are involved in acid-base balance.

Monovalent cations are typically measured in milliequivalents per liter (mEq/L) in clinical settings to express their concentration in biological fluids.

Tissue distribution, in the context of pharmacology and toxicology, refers to the way that a drug or xenobiotic (a chemical substance found within an organism that is not naturally produced by or expected to be present within that organism) is distributed throughout the body's tissues after administration. It describes how much of the drug or xenobiotic can be found in various tissues and organs, and is influenced by factors such as blood flow, lipid solubility, protein binding, and the permeability of cell membranes. Understanding tissue distribution is important for predicting the potential effects of a drug or toxin on different parts of the body, and for designing drugs with improved safety and efficacy profiles.

Messenger RNA (mRNA) is a type of RNA (ribonucleic acid) that carries genetic information copied from DNA in the form of a series of three-base code "words," each of which specifies a particular amino acid. This information is used by the cell's machinery to construct proteins, a process known as translation. After being transcribed from DNA, mRNA travels out of the nucleus to the ribosomes in the cytoplasm where protein synthesis occurs. Once the protein has been synthesized, the mRNA may be degraded and recycled. Post-transcriptional modifications can also occur to mRNA, such as alternative splicing and addition of a 5' cap and a poly(A) tail, which can affect its stability, localization, and translation efficiency.

Molecular sequence data refers to the specific arrangement of molecules, most commonly nucleotides in DNA or RNA, or amino acids in proteins, that make up a biological macromolecule. This data is generated through laboratory techniques such as sequencing, and provides information about the exact order of the constituent molecules. This data is crucial in various fields of biology, including genetics, evolution, and molecular biology, allowing for comparisons between different organisms, identification of genetic variations, and studies of gene function and regulation.

Transfection is a term used in molecular biology that refers to the process of deliberately introducing foreign genetic material (DNA, RNA or artificial gene constructs) into cells. This is typically done using chemical or physical methods, such as lipofection or electroporation. Transfection is widely used in research and medical settings for various purposes, including studying gene function, producing proteins, developing gene therapies, and creating genetically modified organisms. It's important to note that transfection is different from transduction, which is the process of introducing genetic material into cells using viruses as vectors.

"Renal agents" is not a standardized medical term with a single, widely accepted definition. However, in a general sense, renal agents could refer to medications or substances that have an effect on the kidneys or renal function. This can include drugs that are primarily used to treat kidney diseases or disorders (such as certain types of diuretics, ACE inhibitors, or ARBs), as well as chemicals or toxins that can negatively impact renal function if they are not properly eliminated from the body.

It's worth noting that the term "renal agent" is not commonly used in medical literature or clinical practice, and its meaning may vary depending on the context in which it is used. If you have any specific questions about a particular medication or substance and its effect on renal function, I would recommend consulting with a healthcare professional for more accurate information.

Hydrogen-ion concentration, also known as pH, is a measure of the acidity or basicity of a solution. It is defined as the negative logarithm (to the base 10) of the hydrogen ion activity in a solution. The standard unit of measurement is the pH unit. A pH of 7 is neutral, less than 7 is acidic, and greater than 7 is basic.

In medical terms, hydrogen-ion concentration is important for maintaining homeostasis within the body. For example, in the stomach, a high hydrogen-ion concentration (low pH) is necessary for the digestion of food. However, in other parts of the body such as blood, a high hydrogen-ion concentration can be harmful and lead to acidosis. Conversely, a low hydrogen-ion concentration (high pH) in the blood can lead to alkalosis. Both acidosis and alkalosis can have serious consequences on various organ systems if not corrected.

Substrate specificity in the context of medical biochemistry and enzymology refers to the ability of an enzyme to selectively bind and catalyze a chemical reaction with a particular substrate (or a group of similar substrates) while discriminating against other molecules that are not substrates. This specificity arises from the three-dimensional structure of the enzyme, which has evolved to match the shape, charge distribution, and functional groups of its physiological substrate(s).

Substrate specificity is a fundamental property of enzymes that enables them to carry out highly selective chemical transformations in the complex cellular environment. The active site of an enzyme, where the catalysis takes place, has a unique conformation that complements the shape and charge distribution of its substrate(s). This ensures efficient recognition, binding, and conversion of the substrate into the desired product while minimizing unwanted side reactions with other molecules.

Substrate specificity can be categorized as:

1. Absolute specificity: An enzyme that can only act on a single substrate or a very narrow group of structurally related substrates, showing no activity towards any other molecule.
2. Group specificity: An enzyme that prefers to act on a particular functional group or class of compounds but can still accommodate minor structural variations within the substrate.
3. Broad or promiscuous specificity: An enzyme that can act on a wide range of structurally diverse substrates, albeit with varying catalytic efficiencies.

Understanding substrate specificity is crucial for elucidating enzymatic mechanisms, designing drugs that target specific enzymes or pathways, and developing biotechnological applications that rely on the controlled manipulation of enzyme activities.

HEK293 cells, also known as human embryonic kidney 293 cells, are a line of cells used in scientific research. They were originally derived from human embryonic kidney cells and have been adapted to grow in a lab setting. HEK293 cells are widely used in molecular biology and biochemistry because they can be easily transfected (a process by which DNA is introduced into cells) and highly express foreign genes. As a result, they are often used to produce proteins for structural and functional studies. It's important to note that while HEK293 cells are derived from human tissue, they have been grown in the lab for many generations and do not retain the characteristics of the original embryonic kidney cells.

An amino acid sequence is the specific order of amino acids in a protein or peptide molecule, formed by the linking of the amino group (-NH2) of one amino acid to the carboxyl group (-COOH) of another amino acid through a peptide bond. The sequence is determined by the genetic code and is unique to each type of protein or peptide. It plays a crucial role in determining the three-dimensional structure and function of proteins.

Choline is an essential nutrient that is vital for the normal functioning of all cells, particularly those in the brain and liver. It is a water-soluble compound that is neither a vitamin nor a mineral, but is often grouped with vitamins because it has many similar functions. Choline is a precursor to the neurotransmitter acetylcholine, which plays an important role in memory, mood, and other cognitive processes. It also helps to maintain the structural integrity of cell membranes and is involved in the transport and metabolism of fats.

Choline can be synthesized by the body in small amounts, but it is also found in a variety of foods such as eggs, meat, fish, nuts, and cruciferous vegetables. Some people may require additional choline through supplementation, particularly if they follow a vegetarian or vegan diet, are pregnant or breastfeeding, or have certain medical conditions that affect choline metabolism.

Deficiency in choline can lead to a variety of health problems, including liver disease, muscle damage, and neurological disorders. On the other hand, excessive intake of choline can cause fishy body odor, sweating, and gastrointestinal symptoms such as diarrhea and vomiting. It is important to maintain adequate levels of choline through a balanced diet and, if necessary, supplementation under the guidance of a healthcare professional.

Sodium is an essential mineral and electrolyte that is necessary for human health. In a medical context, sodium is often discussed in terms of its concentration in the blood, as measured by serum sodium levels. The normal range for serum sodium is typically between 135 and 145 milliequivalents per liter (mEq/L).

Sodium plays a number of important roles in the body, including:

* Regulating fluid balance: Sodium helps to regulate the amount of water in and around your cells, which is important for maintaining normal blood pressure and preventing dehydration.
* Facilitating nerve impulse transmission: Sodium is involved in the generation and transmission of electrical signals in the nervous system, which is necessary for proper muscle function and coordination.
* Assisting with muscle contraction: Sodium helps to regulate muscle contractions by interacting with other minerals such as calcium and potassium.

Low sodium levels (hyponatremia) can cause symptoms such as confusion, seizures, and coma, while high sodium levels (hypernatremia) can lead to symptoms such as weakness, muscle cramps, and seizures. Both conditions require medical treatment to correct.

Histamine H2 antagonists, also known as H2 blockers, are a class of medications that work by blocking the action of histamine on the H2 receptors in the stomach. Histamine is a chemical that is released by the body during an allergic reaction and can also be released by certain cells in the stomach in response to food or other stimuli. When histamine binds to the H2 receptors in the stomach, it triggers the release of acid. By blocking the action of histamine on these receptors, H2 antagonists reduce the amount of acid produced by the stomach, which can help to relieve symptoms such as heartburn, indigestion, and stomach ulcers. Examples of H2 antagonists include ranitidine (Zantac), famotidine (Pepcid), and cimetidine (Tagamet).

Octamer Transcription Factor-2 (OCT-2, also known as OTF-2 or POU2F2) is a protein that, in humans, is encoded by the POU2F2 gene. It belongs to the class II family of POU domain transcription factors, which are characterized by a highly conserved DNA-binding domain called the POU domain.

The OCT-2 protein plays crucial roles in the development and function of the nervous system, particularly in the differentiation and maintenance of neurons. It is involved in regulating the expression of various genes that are essential for neural functions, such as neurotransmitter synthesis, synaptic plasticity, and neuronal survival.

OCT-2 forms homodimers or heterodimers with other transcription factors to bind to specific DNA sequences called octamer motifs, which typically have the consensus sequence ATGCAAAT. The binding of OCT-2 to these motifs influences the transcriptional activity of the target genes, either activating or repressing their expression.

Dysregulation of OCT-2 has been implicated in several neurological disorders and cancers, making it a potential therapeutic target for these conditions.

"Cricetulus" is a genus of rodents that includes several species of hamsters. These small, burrowing animals are native to Asia and have a body length of about 8-15 centimeters, with a tail that is usually shorter than the body. They are characterized by their large cheek pouches, which they use to store food. Some common species in this genus include the Chinese hamster (Cricetulus griseus) and the Daurian hamster (Cricetulus dauuricus). These animals are often kept as pets or used in laboratory research.

I believe there might be a misunderstanding in your question. "Dogs" is not a medical term or condition. It is the common name for a domesticated carnivore of the family Canidae, specifically the genus Canis, which includes wolves, foxes, and other extant and extinct species of mammals. Dogs are often kept as pets and companions, and they have been bred in a wide variety of forms and sizes for different purposes, such as hunting, herding, guarding, assisting police and military forces, and providing companionship and emotional support.

If you meant to ask about a specific medical condition or term related to dogs, please provide more context so I can give you an accurate answer.

CHO cells, or Chinese Hamster Ovary cells, are a type of immortalized cell line that are commonly used in scientific research and biotechnology. They were originally derived from the ovaries of a female Chinese hamster (Cricetulus griseus) in the 1950s.

CHO cells have several characteristics that make them useful for laboratory experiments. They can grow and divide indefinitely under appropriate conditions, which allows researchers to culture large quantities of them for study. Additionally, CHO cells are capable of expressing high levels of recombinant proteins, making them a popular choice for the production of therapeutic drugs, vaccines, and other biologics.

In particular, CHO cells have become a workhorse in the field of biotherapeutics, with many approved monoclonal antibody-based therapies being produced using these cells. The ability to genetically modify CHO cells through various methods has further expanded their utility in research and industrial applications.

It is important to note that while CHO cells are widely used in scientific research, they may not always accurately represent human cell behavior or respond to drugs and other compounds in the same way as human cells do. Therefore, results obtained using CHO cells should be validated in more relevant systems when possible.

Caco-2 cells are a type of human epithelial colorectal adenocarcinoma cell line that is commonly used in scientific research, particularly in the field of drug development and toxicology. These cells are capable of forming a monolayer with tight junctions, which makes them an excellent model for studying intestinal absorption, transport, and metabolism of drugs and other xenobiotic compounds.

Caco-2 cells express many of the transporters and enzymes that are found in the human small intestine, making them a valuable tool for predicting drug absorption and bioavailability in humans. They are also used to study the mechanisms of drug transport across the intestinal epithelium, including passive diffusion and active transport by various transporters.

In addition to their use in drug development, Caco-2 cells are also used to study the toxicological effects of various compounds on human intestinal cells. They can be used to investigate the mechanisms of toxicity, as well as to evaluate the potential for drugs and other compounds to induce intestinal damage or inflammation.

Overall, Caco-2 cells are a widely used and valuable tool in both drug development and toxicology research, providing important insights into the absorption, transport, metabolism, and toxicity of various compounds in the human body.

P-glycoprotein (P-gp) is a type of membrane transport protein that plays a crucial role in the efflux (extrusion) of various substrates, including drugs and toxins, out of cells. It is also known as multidrug resistance protein 1 (MDR1).

P-gp is encoded by the ABCB1 gene and is primarily located on the apical membrane of epithelial cells in several tissues, such as the intestine, liver, kidney, and blood-brain barrier. Its main function is to protect these organs from harmful substances by actively pumping them out of the cells and back into the lumen or bloodstream.

In the context of pharmacology, P-gp can contribute to multidrug resistance (MDR) in cancer cells. When overexpressed, P-gp can reduce the intracellular concentration of various anticancer drugs, making them less effective. This has led to extensive research on inhibitors of P-gp as potential adjuvants for cancer therapy.

In summary, P-glycoprotein is a vital efflux transporter that helps maintain homeostasis by removing potentially harmful substances from cells and can impact drug disposition and response in various tissues, including the intestine, liver, kidney, and blood-brain barrier.

Histamine is defined as a biogenic amine that is widely distributed throughout the body and is involved in various physiological functions. It is derived primarily from the amino acid histidine by the action of histidine decarboxylase. Histamine is stored in granules (along with heparin and proteases) within mast cells and basophils, and is released upon stimulation or degranulation of these cells.

Once released into the tissues and circulation, histamine exerts a wide range of pharmacological actions through its interaction with four types of G protein-coupled receptors (H1, H2, H3, and H4 receptors). Histamine's effects are diverse and include modulation of immune responses, contraction and relaxation of smooth muscle, increased vascular permeability, stimulation of gastric acid secretion, and regulation of neurotransmission.

Histamine is also a potent mediator of allergic reactions and inflammation, causing symptoms such as itching, sneezing, runny nose, and wheezing. Antihistamines are commonly used to block the actions of histamine at H1 receptors, providing relief from these symptoms.

Inhibitory Concentration 50 (IC50) is a measure used in pharmacology, toxicology, and virology to describe the potency of a drug or chemical compound. It refers to the concentration needed to reduce the biological or biochemical activity of a given substance by half. Specifically, it is most commonly used in reference to the inhibition of an enzyme or receptor.

In the context of infectious diseases, IC50 values are often used to compare the effectiveness of antiviral drugs against a particular virus. A lower IC50 value indicates that less of the drug is needed to achieve the desired effect, suggesting greater potency and potentially fewer side effects. Conversely, a higher IC50 value suggests that more of the drug is required to achieve the same effect, indicating lower potency.

It's important to note that IC50 values can vary depending on the specific assay or experimental conditions used, so they should be interpreted with caution and in conjunction with other measures of drug efficacy.

A cell membrane, also known as the plasma membrane, is a thin semi-permeable phospholipid bilayer that surrounds all cells in animals, plants, and microorganisms. It functions as a barrier to control the movement of substances in and out of the cell, allowing necessary molecules such as nutrients, oxygen, and signaling molecules to enter while keeping out harmful substances and waste products. The cell membrane is composed mainly of phospholipids, which have hydrophilic (water-loving) heads and hydrophobic (water-fearing) tails. This unique structure allows the membrane to be flexible and fluid, yet selectively permeable. Additionally, various proteins are embedded in the membrane that serve as channels, pumps, receptors, and enzymes, contributing to the cell's overall functionality and communication with its environment.

Molecular cloning is a laboratory technique used to create multiple copies of a specific DNA sequence. This process involves several steps:

1. Isolation: The first step in molecular cloning is to isolate the DNA sequence of interest from the rest of the genomic DNA. This can be done using various methods such as PCR (polymerase chain reaction), restriction enzymes, or hybridization.
2. Vector construction: Once the DNA sequence of interest has been isolated, it must be inserted into a vector, which is a small circular DNA molecule that can replicate independently in a host cell. Common vectors used in molecular cloning include plasmids and phages.
3. Transformation: The constructed vector is then introduced into a host cell, usually a bacterial or yeast cell, through a process called transformation. This can be done using various methods such as electroporation or chemical transformation.
4. Selection: After transformation, the host cells are grown in selective media that allow only those cells containing the vector to grow. This ensures that the DNA sequence of interest has been successfully cloned into the vector.
5. Amplification: Once the host cells have been selected, they can be grown in large quantities to amplify the number of copies of the cloned DNA sequence.

Molecular cloning is a powerful tool in molecular biology and has numerous applications, including the production of recombinant proteins, gene therapy, functional analysis of genes, and genetic engineering.

A symporter is a type of transmembrane protein that functions to transport two or more molecules or ions across a biological membrane in the same direction, simultaneously. This process is called co-transport and it is driven by the concentration gradient of one of the substrates, which is usually an ion such as sodium (Na+) or proton (H+).

Symporters are classified based on the type of energy that drives the transport process. Primary active transporters, such as symporters, use the energy from ATP hydrolysis or from the electrochemical gradient of ions to move substrates against their concentration gradient. In contrast, secondary active transporters use the energy stored in an existing electrochemical gradient of one substrate to drive the transport of another substrate against its own concentration gradient.

Symporters play important roles in various physiological processes, including nutrient uptake, neurotransmitter reuptake, and ion homeostasis. For example, the sodium-glucose transporter (SGLT) is a symporter that co-transports glucose and sodium ions across the intestinal epithelium and the renal proximal tubule, contributing to glucose absorption and regulation of blood glucose levels. Similarly, the dopamine transporter (DAT) is a symporter that co-transports dopamine and sodium ions back into presynaptic neurons, terminating the action of dopamine in the synapse.

Hepatocytes are the predominant type of cells in the liver, accounting for about 80% of its cytoplasmic mass. They play a key role in protein synthesis, protein storage, transformation of carbohydrates, synthesis of cholesterol, bile salts and phospholipids, detoxification, modification, and excretion of exogenous and endogenous substances, initiation of formation and secretion of bile, and enzyme production. Hepatocytes are essential for the maintenance of homeostasis in the body.

The liver is a large, solid organ located in the upper right portion of the abdomen, beneath the diaphragm and above the stomach. It plays a vital role in several bodily functions, including:

1. Metabolism: The liver helps to metabolize carbohydrates, fats, and proteins from the food we eat into energy and nutrients that our bodies can use.
2. Detoxification: The liver detoxifies harmful substances in the body by breaking them down into less toxic forms or excreting them through bile.
3. Synthesis: The liver synthesizes important proteins, such as albumin and clotting factors, that are necessary for proper bodily function.
4. Storage: The liver stores glucose, vitamins, and minerals that can be released when the body needs them.
5. Bile production: The liver produces bile, a digestive juice that helps to break down fats in the small intestine.
6. Immune function: The liver plays a role in the immune system by filtering out bacteria and other harmful substances from the blood.

Overall, the liver is an essential organ that plays a critical role in maintaining overall health and well-being.

A dose-response relationship in the context of drugs refers to the changes in the effects or symptoms that occur as the dose of a drug is increased or decreased. Generally, as the dose of a drug is increased, the severity or intensity of its effects also increases. Conversely, as the dose is decreased, the effects of the drug become less severe or may disappear altogether.

The dose-response relationship is an important concept in pharmacology and toxicology because it helps to establish the safe and effective dosage range for a drug. By understanding how changes in the dose of a drug affect its therapeutic and adverse effects, healthcare providers can optimize treatment plans for their patients while minimizing the risk of harm.

The dose-response relationship is typically depicted as a curve that shows the relationship between the dose of a drug and its effect. The shape of the curve may vary depending on the drug and the specific effect being measured. Some drugs may have a steep dose-response curve, meaning that small changes in the dose can result in large differences in the effect. Other drugs may have a more gradual dose-response curve, where larger changes in the dose are needed to produce significant effects.

In addition to helping establish safe and effective dosages, the dose-response relationship is also used to evaluate the potential therapeutic benefits and risks of new drugs during clinical trials. By systematically testing different doses of a drug in controlled studies, researchers can identify the optimal dosage range for the drug and assess its safety and efficacy.

Octamer Transcription Factor-3 (OTF-3 or Oct3) is a specific protein that belongs to the class of POU domain transcription factors. These proteins play crucial roles in the regulation of gene expression during cell growth, development, and differentiation. The "POU" name refers to the presence of two conserved domains - a POU-specific domain and a POU homeodomain - that recognize and bind to specific DNA sequences called octamer motifs, which are involved in controlling the transcription of target genes.

Oct3, encoded by the Pou2f1 gene, is widely expressed in various tissues, including lymphoid cells, neurons, and embryonic stem cells. It has been shown to regulate the expression of several genes that are essential for cell survival, proliferation, and differentiation. Dysregulation of Oct3 has been implicated in several diseases, such as cancers and neurological disorders.

In summary, Octamer Transcription Factor-3 (Oct3) is a POU domain transcription factor that binds to octamer motifs in DNA and regulates the expression of target genes involved in cell growth, development, and differentiation.

Reverse Transcriptase Polymerase Chain Reaction (RT-PCR) is a laboratory technique used in molecular biology to amplify and detect specific DNA sequences. This technique is particularly useful for the detection and quantification of RNA viruses, as well as for the analysis of gene expression.

The process involves two main steps: reverse transcription and polymerase chain reaction (PCR). In the first step, reverse transcriptase enzyme is used to convert RNA into complementary DNA (cDNA) by reading the template provided by the RNA molecule. This cDNA then serves as a template for the PCR amplification step.

In the second step, the PCR reaction uses two primers that flank the target DNA sequence and a thermostable polymerase enzyme to repeatedly copy the targeted cDNA sequence. The reaction mixture is heated and cooled in cycles, allowing the primers to anneal to the template, and the polymerase to extend the new strand. This results in exponential amplification of the target DNA sequence, making it possible to detect even small amounts of RNA or cDNA.

RT-PCR is a sensitive and specific technique that has many applications in medical research and diagnostics, including the detection of viruses such as HIV, hepatitis C virus, and SARS-CoV-2 (the virus that causes COVID-19). It can also be used to study gene expression, identify genetic mutations, and diagnose genetic disorders.

A drug interaction is the effect of combining two or more drugs, or a drug and another substance (such as food or alcohol), which can alter the effectiveness or side effects of one or both of the substances. These interactions can be categorized as follows:

1. Pharmacodynamic interactions: These occur when two or more drugs act on the same target organ or receptor, leading to an additive, synergistic, or antagonistic effect. For example, taking a sedative and an antihistamine together can result in increased drowsiness due to their combined depressant effects on the central nervous system.
2. Pharmacokinetic interactions: These occur when one drug affects the absorption, distribution, metabolism, or excretion of another drug. For example, taking certain antibiotics with grapefruit juice can increase the concentration of the antibiotic in the bloodstream, leading to potential toxicity.
3. Food-drug interactions: Some drugs may interact with specific foods, affecting their absorption, metabolism, or excretion. An example is the interaction between warfarin (a blood thinner) and green leafy vegetables, which can increase the risk of bleeding due to enhanced vitamin K absorption from the vegetables.
4. Drug-herb interactions: Some herbal supplements may interact with medications, leading to altered drug levels or increased side effects. For instance, St. John's Wort can decrease the effectiveness of certain antidepressants and oral contraceptives by inducing their metabolism.
5. Drug-alcohol interactions: Alcohol can interact with various medications, causing additive sedative effects, impaired judgment, or increased risk of liver damage. For example, combining alcohol with benzodiazepines or opioids can lead to dangerous levels of sedation and respiratory depression.

It is essential for healthcare providers and patients to be aware of potential drug interactions to minimize adverse effects and optimize treatment outcomes.

Sprague-Dawley rats are a strain of albino laboratory rats that are widely used in scientific research. They were first developed by researchers H.H. Sprague and R.C. Dawley in the early 20th century, and have since become one of the most commonly used rat strains in biomedical research due to their relatively large size, ease of handling, and consistent genetic background.

Sprague-Dawley rats are outbred, which means that they are genetically diverse and do not suffer from the same limitations as inbred strains, which can have reduced fertility and increased susceptibility to certain diseases. They are also characterized by their docile nature and low levels of aggression, making them easier to handle and study than some other rat strains.

These rats are used in a wide variety of research areas, including toxicology, pharmacology, nutrition, cancer, and behavioral studies. Because they are genetically diverse, Sprague-Dawley rats can be used to model a range of human diseases and conditions, making them an important tool in the development of new drugs and therapies.

"Cells, cultured" is a medical term that refers to cells that have been removed from an organism and grown in controlled laboratory conditions outside of the body. This process is called cell culture and it allows scientists to study cells in a more controlled and accessible environment than they would have inside the body. Cultured cells can be derived from a variety of sources, including tissues, organs, or fluids from humans, animals, or cell lines that have been previously established in the laboratory.

Cell culture involves several steps, including isolation of the cells from the tissue, purification and characterization of the cells, and maintenance of the cells in appropriate growth conditions. The cells are typically grown in specialized media that contain nutrients, growth factors, and other components necessary for their survival and proliferation. Cultured cells can be used for a variety of purposes, including basic research, drug development and testing, and production of biological products such as vaccines and gene therapies.

It is important to note that cultured cells may behave differently than they do in the body, and results obtained from cell culture studies may not always translate directly to human physiology or disease. Therefore, it is essential to validate findings from cell culture experiments using additional models and ultimately in clinical trials involving human subjects.

Carbon radioisotopes are radioactive isotopes of carbon, which is an naturally occurring chemical element with the atomic number 6. The most common and stable isotope of carbon is carbon-12 (^12C), but there are also several radioactive isotopes, including carbon-11 (^11C), carbon-14 (^14C), and carbon-13 (^13C). These radioisotopes have different numbers of neutrons in their nuclei, which makes them unstable and causes them to emit radiation.

Carbon-11 has a half-life of about 20 minutes and is used in medical imaging techniques such as positron emission tomography (PET) scans. It is produced by bombarding nitrogen-14 with protons in a cyclotron.

Carbon-14, also known as radiocarbon, has a half-life of about 5730 years and is used in archaeology and geology to date organic materials. It is produced naturally in the atmosphere by cosmic rays.

Carbon-13 is stable and has a natural abundance of about 1.1% in carbon. It is not radioactive, but it can be used as a tracer in medical research and in the study of metabolic processes.

Complementary DNA (cDNA) is a type of DNA that is synthesized from a single-stranded RNA molecule through the process of reverse transcription. In this process, the enzyme reverse transcriptase uses an RNA molecule as a template to synthesize a complementary DNA strand. The resulting cDNA is therefore complementary to the original RNA molecule and is a copy of its coding sequence, but it does not contain non-coding regions such as introns that are present in genomic DNA.

Complementary DNA is often used in molecular biology research to study gene expression, protein function, and other genetic phenomena. For example, cDNA can be used to create cDNA libraries, which are collections of cloned cDNA fragments that represent the expressed genes in a particular cell type or tissue. These libraries can then be screened for specific genes or gene products of interest. Additionally, cDNA can be used to produce recombinant proteins in heterologous expression systems, allowing researchers to study the structure and function of proteins that may be difficult to express or purify from their native sources.

Cricetinae is a subfamily of rodents that includes hamsters, gerbils, and relatives. These small mammals are characterized by having short limbs, compact bodies, and cheek pouches for storing food. They are native to various parts of the world, particularly in Europe, Asia, and Africa. Some species are popular pets due to their small size, easy care, and friendly nature. In a medical context, understanding the biology and behavior of Cricetinae species can be important for individuals who keep them as pets or for researchers studying their physiology.

Serotonin, also known as 5-hydroxytryptamine (5-HT), is a monoamine neurotransmitter that is found primarily in the gastrointestinal (GI) tract, blood platelets, and the central nervous system (CNS) of humans and other animals. It is produced by the conversion of the amino acid tryptophan to 5-hydroxytryptophan (5-HTP), and then to serotonin.

In the CNS, serotonin plays a role in regulating mood, appetite, sleep, memory, learning, and behavior, among other functions. It also acts as a vasoconstrictor, helping to regulate blood flow and blood pressure. In the GI tract, it is involved in peristalsis, the contraction and relaxation of muscles that moves food through the digestive system.

Serotonin is synthesized and stored in serotonergic neurons, which are nerve cells that use serotonin as their primary neurotransmitter. These neurons are found throughout the brain and spinal cord, and they communicate with other neurons by releasing serotonin into the synapse, the small gap between two neurons.

Abnormal levels of serotonin have been linked to a variety of disorders, including depression, anxiety, schizophrenia, and migraines. Medications that affect serotonin levels, such as selective serotonin reuptake inhibitors (SSRIs), are commonly used to treat these conditions.

Organoplatinum compounds are a group of chemical substances that contain at least one carbon-platinum bond. These compounds have been widely studied and used in the field of medicine, particularly in cancer chemotherapy. The most well-known organoplatinum compound is cisplatin, which is a platinum-based drug used to treat various types of cancers such as testicular, ovarian, bladder, and lung cancers. Cisplatin works by forming crosslinks with the DNA of cancer cells, disrupting their ability to replicate and ultimately leading to cell death. Other examples of organoplatinum compounds used in cancer treatment include carboplatin and oxaliplatin.

Organ specificity, in the context of immunology and toxicology, refers to the phenomenon where a substance (such as a drug or toxin) or an immune response primarily affects certain organs or tissues in the body. This can occur due to various reasons such as:

1. The presence of specific targets (like antigens in the case of an immune response or receptors in the case of drugs) that are more abundant in these organs.
2. The unique properties of certain cells or tissues that make them more susceptible to damage.
3. The way a substance is metabolized or cleared from the body, which can concentrate it in specific organs.

For example, in autoimmune diseases, organ specificity describes immune responses that are directed against antigens found only in certain organs, such as the thyroid gland in Hashimoto's disease. Similarly, some toxins or drugs may have a particular affinity for liver cells, leading to liver damage or specific drug interactions.

A base sequence in the context of molecular biology refers to the specific order of nucleotides in a DNA or RNA molecule. In DNA, these nucleotides are adenine (A), guanine (G), cytosine (C), and thymine (T). In RNA, uracil (U) takes the place of thymine. The base sequence contains genetic information that is transcribed into RNA and ultimately translated into proteins. It is the exact order of these bases that determines the genetic code and thus the function of the DNA or RNA molecule.

The placenta is an organ that develops in the uterus during pregnancy and provides oxygen and nutrients to the growing baby through the umbilical cord. It also removes waste products from the baby's blood. The placenta attaches to the wall of the uterus, and the baby's side of the placenta contains many tiny blood vessels that connect to the baby's circulatory system. This allows for the exchange of oxygen, nutrients, and waste between the mother's and baby's blood. After the baby is born, the placenta is usually expelled from the uterus in a process called afterbirth.

A "knockout" mouse is a genetically engineered mouse in which one or more genes have been deleted or "knocked out" using molecular biology techniques. This allows researchers to study the function of specific genes and their role in various biological processes, as well as potential associations with human diseases. The mice are generated by introducing targeted DNA modifications into embryonic stem cells, which are then used to create a live animal. Knockout mice have been widely used in biomedical research to investigate gene function, disease mechanisms, and potential therapeutic targets.

Tritium is not a medical term, but it is a term used in the field of nuclear physics and chemistry. Tritium (symbol: T or 3H) is a radioactive isotope of hydrogen with two neutrons and one proton in its nucleus. It is also known as heavy hydrogen or superheavy hydrogen.

Tritium has a half-life of about 12.3 years, which means that it decays by emitting a low-energy beta particle (an electron) to become helium-3. Due to its radioactive nature and relatively short half-life, tritium is used in various applications, including nuclear weapons, fusion reactors, luminous paints, and medical research.

In the context of medicine, tritium may be used as a radioactive tracer in some scientific studies or medical research, but it is not a term commonly used to describe a medical condition or treatment.

Hypoglycemic agents are a class of medications that are used to lower blood glucose levels in the treatment of diabetes mellitus. These medications work by increasing insulin sensitivity, stimulating insulin release from the pancreas, or inhibiting glucose production in the liver. Examples of hypoglycemic agents include sulfonylureas, meglitinides, biguanides, thiazolidinediones, DPP-4 inhibitors, SGLT2 inhibitors, and GLP-1 receptor agonists. It's important to note that the term "hypoglycemic" refers to a condition of abnormally low blood glucose levels, but in this context, the term is used to describe agents that are used to treat high blood glucose levels (hyperglycemia) associated with diabetes.

Amantadine is an antiviral medication that is primarily used to prevent and treat certain types of influenza (flu). It works by stopping the virus from multiplying in your body. In addition to its antiviral properties, amantadine also has central nervous system (CNS) stimulant and dopaminergic effects, which make it useful in the treatment of Parkinson's disease and various movement disorders.

The medical definition of Amantadine is:

A synthetic symmetrical tricyclic amine used as an antiviral agent to treat and prevent influenza A infection and as an anti-parkinsonian drug to control extrapyramidal symptoms caused by neuroleptic agents. The antiviral effect may be due to interference with viral uncoating or replication. The anti-parkinsonian effect may be due to a combination of dopamine agonist and NMDA receptor antagonist properties. (Stedman's Medical Dictionary, 28th edition)

Please note that the use of Amantadine for various medical conditions should always be under the supervision of a healthcare professional, as they will consider potential benefits and risks and provide appropriate guidance.

Single Nucleotide Polymorphism (SNP) is a type of genetic variation that occurs when a single nucleotide (A, T, C, or G) in the DNA sequence is altered. This alteration must occur in at least 1% of the population to be considered a SNP. These variations can help explain why some people are more susceptible to certain diseases than others and can also influence how an individual responds to certain medications. SNPs can serve as biological markers, helping scientists locate genes that are associated with disease. They can also provide information about an individual's ancestry and ethnic background.

Molecular models are three-dimensional representations of molecular structures that are used in the field of molecular biology and chemistry to visualize and understand the spatial arrangement of atoms and bonds within a molecule. These models can be physical or computer-generated and allow researchers to study the shape, size, and behavior of molecules, which is crucial for understanding their function and interactions with other molecules.

Physical molecular models are often made up of balls (representing atoms) connected by rods or sticks (representing bonds). These models can be constructed manually using materials such as plastic or wooden balls and rods, or they can be created using 3D printing technology.

Computer-generated molecular models, on the other hand, are created using specialized software that allows researchers to visualize and manipulate molecular structures in three dimensions. These models can be used to simulate molecular interactions, predict molecular behavior, and design new drugs or chemicals with specific properties. Overall, molecular models play a critical role in advancing our understanding of molecular structures and their functions.

Organic Cation Transporter Like-3 (ORCTL3) was first discovered as a result of a large-scale DNA sequencing project in search ... bearing homology to organic-cation transporters". Cytogenetic and Genome Research. 83 (3-4): 251-255. doi:10.1159/000015197. ... "Identification of a kidney-specific mouse organic cation transporter like-1 (mOCTL1)". Experimental & Molecular Medicine. 39 (6 ... ORCTL3 was decided upon because of its structural homology to proteins belonging to the family of organic cation transporters. ...
... serotonin transporter (SERT), vesicular monoamine transporter (VMAT2) and organic cation transporters (OCT1, 2 and EMT) in ... Polyspecific organic cation transporters in the liver, kidney, intestine, and other organs are critical for elimination of many ... Koehler MR, Wissinger B, Gorboulev V, Koepsell H, Schmid M (Jun 1998). "The two human organic cation transporter genes SLC22A1 ... "Entrez Gene: SLC22A1 solute carrier family 22 (organic cation transporter), member 1". Pryor, R; Cabreiro, F; Haberland, G (16 ...
... serotonin transporter (SERT), vesicular monoamine transporter (VMAT2) and organic cation transporters (OCT1, 2 and EMT) in ... Organic cation transporter 3 is a polyspecific transporter whose transport is independent of sodium. Known substrates for ... 2007). "The organic cation transporters (OCT1, OCT2, EMT) and the plasma membrane monoamine transporter (PMAT) show ... 1999). "Identity of the organic cation transporter OCT3 as the extraneuronal monoamine transporter (uptake2) and evidence for ...
Thiamine transport is not inhibited by other organic cations nor affected by sodium ion concentration; it is stimulated by a ... The thiamine transporter protein encoded by SLC19A2 has a 40% shared amino acid identity with the folate transporter SLC19A1. ... "Cloning of the human thiamine transporter, a member of the folate transporter family". The Journal of Biological Chemistry. 274 ... Thiamine transporter 1, also known as thiamine carrier 1 (TC1) or solute carrier family 19 member 2 (SLC19A2) is a protein that ...
2006). "A human transporter protein that mediates the final excretion step for toxic organic cations". Proc. Natl. Acad. Sci. U ... Chen Y, Zhang S, Sorani M, Giacomini KM (2007). "Transport of paraquat by human organic cation transporters and multidrug and ... 2007). "The MATE proteins as fundamental transporters of metabolic and xenobiotic organic cations". Trends Pharmacol. Sci. 27 ( ... "A human transporter protein that mediates the final excretion step for toxic organic cations". Proc. Natl. Acad. Sci. U.S.A. ...
The human organic cation transporter (hOCT2) recognizes the degree of substrate ionization. The Journal of Biological Chemistry ... Assessment of substrate-dependent ligand interactions at the organic cation transporter OCT2 using six model substrates. ... and organic cation transporter (OCT) 2 in rabbit renal proximal tubules. Journal of Pharmacology and Experimental Therapeutics ... Sex differences in the mRNA, protein, and functional expression of organic anion transporter (OAT) 1, OAT3, ...
Eraly SA, Hamilton BA, Nigam SK (Jan 2003). "Organic anion and cation transporters occur in pairs of similar and similarly ... Xuan W, Lamhonwah AM, Librach C, Jarvi K, Tein I (Jun 2003). "Characterization of organic cation/carnitine transporter family ... Kawasaki Y, Kato Y, Sai Y, Tsuji A (Dec 2004). "Functional characterization of human organic cation transporter OCTN1 single ... The first functional designation of this protein was OCTN1 ("organic cation transporter, novel, type 1"), but efficiency of ...
Roth B., M; Obaidat, A; Hagenbuch, B (March 2012). "OATPs, OATs and OCTs: the organic anion and cation transporters of the SLCO ... Organic cation transport proteins Organic anion-transporting polypeptide Solute carrier family Osmoregulation Organic anion ... "Transporter Classification Database: 2.A.82 The Organic Solute Transporter (OST) Family". tcdb.org. Ballatori, Nazzareno; ... "The heteromeric organic solute transporter alpha-beta, Ostalpha-Ostbeta, is an ileal basolateral bile acid transporter". J Biol ...
Zhu HJ, Appel DI, Gründemann D, Markowitz JS (July 2010). "Interaction of organic cation transporter 3 (SLC22A3) and ... Rytting E, Audus KL (January 2005). "Novel organic cation transporter 2-mediated carnitine uptake in placental choriocarcinoma ... The human serotonin transporter and norepinephrine transporter do not contain zinc binding sites. 4-Hydroxyamphetamine has been ... SLC1A1 is excitatory amino acid transporter 3 (EAAT3), a glutamate transporter located in neurons, SLC22A3 is an extraneuronal ...
Hsyu PH, Gisclon LG, Hui AC, Giacomini KM (January 1988). "Interactions of organic anions with the organic cation transporter ... Solute carrier family 22 (organic anion/cation transporter), member 12, also known as SLC22A12 and URAT1, is a protein which in ... "Entrez Gene: SLC22A12 solute carrier family 22 (organic anion/cation transporter), member 12". Enomoto A, Kimura H, ... "A common mutation in an organic anion transporter gene, SLC22A12, is a suppressing factor for the development of gout". ...
... such as being a transcriptional regulator of bile acid transporters in the intestine and kidneys. HNF-1α is involved in the ... promotion of hepatic organic cation transporters, which uptake certain classes of pharmaceuticals; hence, the loss of its ... including the involvement in GLUT1 and GLUT2 transporter expression in pancreatic β-cells and angiotensin-converting enzyme 2 ... HNF-1 protein is present in ovarian clear-cell carcinoma. In humans, mutations in HNF1A cause diabetes that responds to low ...
Human MATE1 (hMATE1) is an electroneutral H+/organic cation (OC) exchanger responsible for the final excretion step of ... These transporters may function together with auxiliary proteins that allow passage across just the cytoplasmic membrane or ... "Role of glutamate residues in substrate recognition by human MATE1 polyspecific H+/organic cation exporter". American Journal ... structurally unrelated toxic organic cations in kidney and liver. Glu273, Glu278, Glu300 and Glu389 are conserved in the ...
2002). "Human organic anion transporters and human organic cation transporters mediate renal transport of prostaglandins". J. ... "Entrez Gene: SLC22A11 solute carrier family 22 (organic anion/cation transporter), member 11". Maruyama K, Sugano S (1994). " ... 2002). "Interaction of human organic anion transporters 2 and 4 with organic anion transport inhibitors". J. Pharmacol. Exp. ... "Human renal organic anion transporter 4 operates as an asymmetric urate transporter". J Am Soc Nephrol. 18 (2): 430-9. doi: ...
Lamhonwah, A. M.; Skaug, J.; Scherer, S. W.; Tein, I. (2003). "A third human carnitine/organic cation transporter (OCTN3) as a ... Solute carrier family 22 (organic cation transporter), member 21 is a protein that in the house mouse is encoded by the ... "Solute carrier family 22 (organic cation transporter), member 21". Retrieved 2011-12-11. "Indirect calorimetry data for ... "Molecular and Functional Characterization of Organic Cation/Carnitine Transporter Family in Mice". Journal of Biological ...
... and human clarify the phylogeny of organic anion and cation transporters". Physiol. Genomics. 18 (1): 12-24. doi:10.1152/ ... Solute carrier family 22 member 25 (SLC22A25), also known as organic anion transporter UST6, is a protein that in humans is ... "Identification of six putative human transporters with structural similarity to the drug transporter SLC22 family". Genomics. ... Eraly SA; Monte JC; Nigam SK (2004). "Novel slc22 transporter homologs in fly, worm, ...
... organic cation transport proteins MeSH D12.776.157.530.450.250.812.500 - organic cation transporter 1 MeSH D12.776.157.530. ... organic anion transporters, sodium-dependent MeSH D12.776.157.530.450.074.500.781 - organic anion transporters, sodium- ... organic anion transporters MeSH D12.776.157.530.450.074.500.199 - dicarboxylic acid transporters MeSH D12.776.157.530.450.074. ... 500.400 - monocarboxylic acid transporters MeSH D12.776.157.530.450.074.500.500 - organic anion transporters, atp-dependent ...
... organic cation transport proteins MeSH D12.776.543.585.450.250.812.500 - organic cation transporter 1 MeSH D12.776.543.585. ... organic anion transporters, sodium-dependent MeSH D12.776.543.585.450.074.500.875 - organic anion transporters, sodium- ... organic anion transporters MeSH D12.776.543.585.450.074.500.149 - dicarboxylic acid transporters MeSH D12.776.543.585.450.074. ... 500.300 - monocarboxylic acid transporters MeSH D12.776.543.585.450.074.500.500 - organic anion transporters, atp-dependent ...
2002). "Human organic anion transporters and human organic cation transporters mediate renal transport of prostaglandins". J. ... organic anion transporter), member 7". Cropp CD, Komori T, Shima JE, et al. (2008). "Organic anion transporter 2 (SLC22A7) is a ... 2002). "Interaction of human organic anion transporters 2 and 4 with organic anion transport inhibitors". J. Pharmacol. Exp. ... Sun W, Wu RR, van Poelje PD, Erion MD (2001). "Isolation of a family of organic anion transporters from human liver and kidney ...
"A human transporter protein that mediates the final excretion step for toxic organic cations". Proceedings of the National ... "The MATE proteins as fundamental transporters of metabolic and xenobiotic organic cations". Trends in Pharmacological Sciences ... "Entrez Gene: MATE2 H+/organic cation antiporter". Morita Y, Kodama K, Shiota S, Mine T, Kataoka A, Mizushima T, Tsuchiya T ( ... organic cation antiporters". Biochemical Pharmacology. 74 (2): 359-71. doi:10.1016/j.bcp.2007.04.010. hdl:2433/124277. PMID ...
2006). "The MATE proteins as fundamental transporters of metabolic and xenobiotic organic cations". Trends in Pharmacological ... archaea and eukaryotes function as fundamental transporters of metabolic and xenobiotic organic cations. These proteins are ... NorM is nicknamed "Last of the multidrug transporters" because it is the last multidrug transporter discovered functionally as ... "Structure of a Cation-bound Multidrug and Toxic Compound Extrusion Transporter". Nature. 467 (7318): 991-994. Bibcode:2010Natur ...
hENT4 is uniquely selective for adenosine, and also transports a variety of organic cations. The generalized transport reaction ... Concentrative nucleoside transporter Nucleoside transporter Molina-Arcas M, Trigueros-Motos L, Casado FJ, Pastor-Anglada M (Jun ... Young, J. D.; Yao, S. Y. M.; Sun, L.; Cass, C. E.; Baldwin, S. A. (2008-07-01). "Human equilibrative nucleoside transporter ( ... Baldwin SA, Beal PR, Yao SY, King AE, Cass CE, Young JD (Feb 2004). "The equilibrative nucleoside transporter family, SLC29". ...
"Entrez Gene: SLC22A18 solute carrier family 22 (organic cation transporter), member 18". Akiyama S (December 2001). "[ ... an organic cation transporter expressed in the renal proximal tubules". FEBS Letters. 433 (3): 245-50. doi:10.1016/S0014-5793( ... an imprinted gene similar to polyspecific transporter and multi-drug resistance genes". Human Molecular Genetics. 7 (4): 597- ... 49 (1): 38-51. doi:10.1006/geno.1998.5221. PMID 9570947. Reece M, Prawitt D, Landers J, Kast C, Gros P, Housman D, Zabel BU, ...
... serotonin transporter (SERT), vesicular monoamine transporter (VMAT2) and organic cation transporters (OCT1, 2 and EMT) in ... Polyspecific organic cation transporters in the liver, kidney, intestine, and other organs are critical for elimination of many ... Solute carrier family 22 member 2 (also termed OCT2 or organic cation transporter-2) is a protein that in humans is encoded by ... Barendt WM, Wright SH (2002). "The human organic cation transporter (hOCT2) recognizes the degree of substrate ionization". J. ...
These transporters generally catalyze the export of cations. A representative list of proteins belonging to the PCC family can ... Anyatonwu GI, Ehrlich BE (August 2005). "Organic cation permeation through the channel formed by polycystin-2". The Journal of ... Polycystin-2 transports a variety of organic cations (dimethylamine, tetraethylammonium, tetrabutylammonium, ... The Polycystin Cation Channel (PCC) Family (TC# 1.A.5) consists of several transporters ranging in size from 500 to over 4000 ...
Decynium has been shown to have a very high affinity to organic cation transporters in a variety of species, including human, ... Hayer-Zillgen M, Brüss M, Bönisch H (2002). "Expression and pharmacological profile of the human organic cation transporters ... as well as all members of the organic cation transporter (OCT) family in both human and rat cells. However, it has little ... "Primary structure and functional expression of the apical organic cation transporter from kidney epithelial LLC-PK1 cells". J ...
... organic cation transporter), member 5 SLC26A2: solute carrier family 26 (sulfate transporter), member 2 SH3TC2: domain and ... Solute carrier organic anion transporter family member 4c1 SLU7: pre-mRNA-splicing factor SLU7 SMN1: survival motor neuron 1, ... diastrophic dysplasia sulfate transporter EIF4E1B: encoding protein Eukaryotic translation initiation factor 4E family member ... 103 (1): 63-8. doi:10.1002/ajmg.1513. PMID 11562936. Schmutz J, Martin J, Terry A, Couronne O, Grimwood J, Lowry S, et al. ( ...
... organic anion/cation transporter), member 9". Zhou F, Hong M, You G (2007). "Regulation of human organic anion transporter 4 by ... 2005). "Human organic anion transporter 4 is a renal apical organic anion/dicarboxylate exchanger in the proximal tubules". J. ... Shin HJ, Anzai N, Enomoto A, He X, Kim do K, Endou H, Kanai Y (Apr 2007). "Novel liver-specific organic anion transporter OAT7 ... Sun W, Wu RR, van Poelje PD, Erion MD (Apr 2001). "Isolation of a family of organic anion transporters from human liver and ...
"Mutations in novel organic cation transporter (OCTN2), an organic cation/carnitine transporter, with differential effects on ... "Functional characteristics and tissue distribution pattern of organic cation transporter 2 (OCTN2), an organic cation/carnitine ... Such polyspecific organic cation transporters in the liver, kidney, intestine, and other organs are critical for the ... The SLC22A5 gene codes for a plasma integral membrane protein which functions as both an organic cation transporter and a ...
... sodium-independent organic cation transport proteins (OCTs) and/or carnitine/organic cation transporters (OCTNs), and do not ... Lastly, choline may enter the cell through intermediate-affinity transporters, which include the choline transporter-like ... The uptake of choline is accomplished predominantly by the high-affinity, sodium dependent choline transporter (CHT) and ... 222 (1): 193-214. doi:10.1016/S0021-9258(19)50785-2. PMID 13366993. Michel V, Yuan Z, Ramsubir S, Bakovic M (May 2006). " ...
Along with the organic cation transporters and the ATP-binding cassette transporters, the OATPs play an important role in the ... Members of the Organo Anion Transporter (OAT) Family (organic-anion-transporting polypeptides, OATP) are membrane transport ... "Functional characterization of rat brain-specific organic anion transporter (Oatp14) at the blood-brain barrier: high affinity ... proteins or 'transporters' that mediate the transport of mainly organic anions across the cell membrane. Therefore, OATPs are ...
To study this vectorial transport of organic cations, we constructed a double-transfected Madin-Darby canine kidney strain II ( ... many of which are organic cations. To study this vectorial transport of organic cations, we constructed a double-transfected ... Vectorial transport of the plant alkaloid berberine by double-transfected cells expressing the human organic cation transporter ... Additionally, MDCKII single transfectants stably expressing OCT1, MDR1 P-gp, or human organic cation transporter 2 (OCT2, ...
Organic cation transporters (OCT) in the IUPHAR/BPS Guide to PHARMACOLOGY. ... EMT , Extraneuronal monoamine transporter , organic cation transporter 3 , solute carrier family 22 (organic cation transporter ... OCT2r , organic cation transporter 2 , solute carrier family 22 (organic cation transporter), member 2 , Orct2 , solute carrier ... Human organic anion transporters and human organic cation transporters mediate renal transport of prostaglandins. J Pharmacol ...
Organic Cation Transporter Like-3 (ORCTL3) was first discovered as a result of a large-scale DNA sequencing project in search ... bearing homology to organic-cation transporters". Cytogenetic and Genome Research. 83 (3-4): 251-255. doi:10.1159/000015197. ... "Identification of a kidney-specific mouse organic cation transporter like-1 (mOCTL1)". Experimental & Molecular Medicine. 39 (6 ... ORCTL3 was decided upon because of its structural homology to proteins belonging to the family of organic cation transporters. ...
8] "Comparison of type I and type II organic cation transport by organic cation transporters and organic anion-transporting ... GO:0015101 F:organic cation transmembrane transporter activity GO:0015651 F:quaternary ammonium group transmembrane transporter ... 12] "The human organic cation transporter-1 gene is transactivated by hepatocyte nuclear factor-4alpha." Saborowski M.et.al. ... 2] "Cloning and functional expression of a human liver organic cation transporter." Zhang L.et.al. 9187257. [3] "Molecular ...
Human Organic Cation Transporter 1 Protein Levels of Granulocytes Can Optimize Imatinib Therapy in Patients with Chronic ... Open the PDF for Human Organic Cation Transporter 1 Protein Levels of Granulocytes Can Optimize Imatinib Therapy in Patients ... View article titled, Human Organic Cation Transporter 1 Protein Levels of Granulocytes Can Optimize Imatinib Therapy in ... Chronic myeloid leukemia High-performance liquid chromatography and tandem mass spectrometry Human organic cation transporter 1 ...
Not a substrate for organic cation transporter (OCT) 2 in vitro. Inhibits OCT2, multidrug and toxin extrusion protein (MATE) 1 ... Not a substrate for or inhibitor of breast cancer resistance protein (BCRP). Not an inhibitor of organic anion transporter (OAT ... Directly inhibits calcium binding by oxalate and by organic stone matrix. Acts as a crystal poison at the interface, reducing ... Drugs Affected by Other Membrane Transporters. Substrates of OCT2, MATE1, and MATE2-K: Systemic exposure may be affected; ...
... and organic cation transporter (OCT)1. Dacomitinib does not inhibit organic anion transporters (OAT)1 and OAT3, OCT2, organic ... Effect of Dacomitinib on Transporter Systems: Dacomitinib is a substrate for the membrane transport protein P-glycoprotein (P- ... Grades 1 through 5 are included in All Grades.. ‡ One Grade 5 (fatal) event in the VIZIMPRO arm.. § Stomatitis includes mucosal ... 1 INDICATIONS AND USAGE 2 DOSAGE AND ADMINISTRATION 2.1 Patient Selection 2.2 Recommended Dosage 2.3 Dosage Modifications for ...
Citrus fruit-derived flavonoid naringenin and the expression of hepatic organic cation transporter 1 protein in diabetic rats ... Metformin reduces insulin doses in type 1 diabetes, but does not reduce the rate of glycated hemoglobin (HbA 1c), nor is it ... Pubmed Data : Sultan Qaboos Univ Med J. 2020 Feb ;20(1):e90-e94. Epub 2020 Mar 9. PMID: 32190375 ... clear whether the benefit is sustained beyone 1 year or has any benefit to cardiovascular or other key clinical outcomes. Jan ...
organic anion-transporting polypeptide. SLCO. solute carrier organic anion transporter. OCT1. organic cation transporter 1. DDI ... organic anion transporter 2, organic cation transporter 1, and monocarboxylate transporter 8. Cytochalasin B, which inhibits ... glucose transporter. CsA. cyclosporine A. AUC. area under the plasma concentration-time curve.. ... Digoxin is reported to be actively transported into human hepatocytes by the organic anion-transporting polypeptide 1B3 ( ...
Effect of genetic variation in the organic cation transporter 1 (OCT1) on metformin action. J Clin Invest 2007; 117: 1422-1431 ... Genetic Variants of the Organic Cation Transporter 2 Influence the Disposition of Metformin. Clin Pharmacol Ther 2008; 84: 559- ... 1 Faculty of Pharmaceutical Medicine, Jamia Hamdard, New Delhi, India. › Author Affiliations Further Information. Publication ... 1 Kirpichnikov D, McFarlane SI, Sowers JR. Metformin: an update. Ann Intern Med 2002; 137: 25-33 ...
... with a 1-week washout period between treatments. For each treatment, blood samples were collected before and at intervals up to ... Organic cation transporter OCTs (SLC22) and MATEs (SLC47) in the human kidney. AAPS J 2013; 15: 581-588. ... Organic cation transporter OCTs (SLC22) and MATEs (SLC47) in the human kidney. AAPS J 2013; 15: 581-588. ... Organic cation transporter OCTs (SLC22) and MATEs (SLC47) in the human kidney. AAPS J 2013; 15: 581-588. ...
Organic cation transporter 1 in complex with verapamil 3.45 Å (EMD-28588), processed by Dr. Yang Suo. ...
Human OCTN1(Organic Cation/Ergothioneine Transporter) ELISA Kit. Human Organic Cation/Ergothioneine Transporter (OCTN1) ELISA ... Rabbit Anti-Mouse Organic Cation Transporter homolog (OCTN1) IgG #1, aff pure. ... Rabbit Anti-Mouse Organic Cation Transporter homolog (OCTN2) IgG #1, aff pure. ... Rabbit Anti-Mouse Organic Cation Transporter homolog (OCTN3) IgG #1, aff pure. ...
Transporters such as organic anion-transporting polypeptide 1A2, P-glycoprotein, human organic cation transporter 1, and ... Coadministration of multivalent cation-containing drugs and LVX should be avoided. For patients receiving warfarin and LVX ... 1 Lu-Shan Yu,2 Su Zeng,2 Yu-Wen Huang,1 Quan Zhou11Department of Pharmacy, the Second Affiliated Hospital, School of Medicine, ... multidrug and toxin extrusion protein 1 are involved in the pharmacokinetics of LVX.Conclusion: Personalized LVX therapeutics ...
ORGANIC CATION TRANSPORTER (OCTN)-1 VARIANTS SHAPE INNATE IMMUNITY AND PREDICT INDIVIDUAL RESPONSE TO VEDOLIZUMAB IN ULCERATIVE ...
Bictegravir inhibits organic cation transporter 2 (OCT2) and multidrug and toxin extrusion transporter 1 (MATE1) in vitro. ... Bictegravir inhibits organic cation transporter 2 (OCT2) and multidrug and toxin extrusion transporter 1 (MATE1) in vitro. ... Bictegravir inhibits organic cation transporter 2 (OCT2) and multidrug and toxin extrusion transporter 1 (MATE1) in vitro. ... Bictegravir inhibits organic cation transporter 2 (OCT2) and multidrug and toxin extrusion transporter 1 (MATE1) in vitro. ...
Organic Cation Transporter 1 100% * Human 100% * Blood-Brain Barrier 100% * Mouse 100% ...
Organic Cation Transporters in Health and Disease Hermann Koepsell. Lynette C. Daws, ASSOCIATE EDITOR ... Solute Carrier Transporters as Potential Targets for the Treatment of Metabolic Disease Tina Schumann, Jörg König, Christine ... Pharmacological Reviews January 2020, 72 (1) 1-49; DOI: https://doi.org/10.1124/pr.118.016899 ... Pharmacological Reviews January 2020, 72 (1) 50-79; DOI: https://doi.org/10.1124/pr.118.016311 ...
Further differentiation of PSCs to the pancreatic progenitor (PP) stage resulted in a decreased proportion of PDX1/NKX6-1- ... Variation in the plasma membrane monoamine transporter (Pmat) (Encoded by Slc29a4) and organic cation transporter 1 (Oct1) ( ... SLC22A1 is a transmembrane protein working as a polyspecific organic cation transporter, mainly in the liver [52]. So far, it ... Dujic, T.; Zhou, K.; Donnelly, L.A.; Tavendale, R.; Palmer, C.N.; Pearson, E.R. Association of Organic Cation Transporter 1 ...
Transporter Systems: Abrocitinib is an inhibitor of organic cation transporter (OCT)1 but is not an inhibitor of organic anion ... The metabolites of abrocitinib, M1 and M2 are excreted predominantly in urine, and are substrates of OAT3 transporter. ... Table 1. Dosage Recommendations in Patients with Renal Impairment * Glomerular filtration rate was estimated by the ... Table 9. Efficacy Results of CIBINQO Monotherapy at Week 12 in Subjects with Moderate-to-Severe AD (Trial-AD-1 and Trial-AD-2) ...
The anticancer activity and the antitumor specificity of oxaliplatin mainly depend on human organic cation transporters (OCT) 1 ... "Organic cation transporters are determinants of oxaliplatin cytotoxicity." Cancer Res. 66: 8847-8857 (2006). ... This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese ... 1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New ...
... and 3A4 and drug transporters Na+-taurocholate-cotransporting polypeptide, organic cation transporter 1, and organic anion- ... 2012;1:e00049. [PubMed] [DOI] [Cited in This Article: ] [Cited by in Crossref: 1280] [Cited by in F6Publishing: 1370] [Article ... 2009;392:1-10. [PubMed] [DOI] [Cited in This Article: ] [Cited by in Crossref: 251] [Cited by in F6Publishing: 223] [Article ... 2019;1:120-130. [PubMed] [DOI] [Cited in This Article: ] [Cited by in Crossref: 25] [Cited by in F6Publishing: 19] [Article ...
... organic anion-transporting polypeptides (OATP) 1B1, OATP1B3, organic cation transporters (OCT)1 and OCT2, or multidrug and ... In vitro, raltegravir is a weak inhibitor of organic anion transporter (OAT) 1 (IC50 of 109 µM) and OAT3 (IC50 of 18.8 µM). ... chelation of metal cations). Given simultaneously iron salts are expected to reduce raltegravir plasma levels; taking iron ... chelation of metal cations). Aluminium and magnesium containing antacids reduce raltegravir plasma levels. Co-administration of ...
... an organic cation transporter [OCT]1, OCT2, and multi-drug and toxin extrusion [MATE]2-K substrate), and rosuvastatin (an ... No clinically significant differences in the pharmacokinetics of furosemide (an organic anion transporter [OAT]1 and OAT3 ... Transporter Systems. Cefiderocol is not an inhibitor of OATP1B1, MATE1, P-glycoprotein (P-gp), breast cancer resistance protein ... BCRP), or bile salt export pump transporters. Cefiderocol is not a substrate of OAT1, OAT3, OCT2, MATE1, MATE2-K, P-gp, or BCRP ...
... and organic cation transporters. Itrailey. The some radiopharmaceuticals are registered. Paediatr child health. The increase in ... W. 1.: 2. Pepi. Sammes. Accessed 21 march 2014 106. 5headache 55 references 5. Becker wj, findlay t, moga c, scott na, ... They may often consider themselves to studies lack- than 1(6 are studied. C. H. 1993. However, nonopioid analge- of atypical ... Hollister, l. 14., ci a).: .1. Transferrin receptors have specific agonists and antagonusx receptors exhibit the alternative ...
"Pharmacokinetics of Organic Cation Transporter 1 (OCT1) Substrates in Oct1/2 Knockout Mice and Species Difference in Hepatic ... The award recipient in the Pharmacokinetics/Drug Transporters category for 2020 is Bridget L. Morse, PharmD, PhD from Eli Lilly ... Her research team explores 1) the structural basis of allosteric ligand-receptor interactions; 2) the full scope of effects of ... and his recent work has delineated new mechanisms for therapeutically modulating G-protein coupled receptors such as the GLP-1 ...
... whereas only weak inhibitory effects were shown by substrates of typical organic cation transporters, such as ... Involvement of the H+/Organic Cation Antiporter in Nicotine Transport in Rat Liver. Yuma Tega, Shin-ichi Akanuma, Yoshiyuki ... The pattern of inhibition and ion dependence is suggestive of an H+/organic cation antiporter-mediated nicotine transport ... Involvement of the H+/Organic Cation Antiporter in Nicotine Transport in Rat Liver ...
... organic cation transporter), member 17 , solute carrier family 22 , solute carrier family 22 (organic cation transporter) ... organic cation transporter), member 18 , solute carrier family 22 , solute carrier family 22 (organic cation transporter) ... organic cation transporter), member 15 , solute carrier family 22 , solute carrier family 22 (organic anion/cation transporter ... organic cation transporter) , solute carrier family 22 (organic cation transporter), member 14 ...
Effect of genetic variation in the organic cation transporter 1 (OCT1) on metformin action. Author(s): Shu Y, Sheardown SA, ... Genetic variation in the organic cation transporter 1 is associated with metformin response in patients with diabetes mellitus ... HLA-A, -B, and -DR associations in type 1 diabetes mellitus with onset after age forty. Author(s): Pittman WB, Acton RT, Barger ... Genetic similarities between latent autoimmune diabetes in adults, type 1 diabetes, and type 2 diabetes. Author(s): Cervin C, ...
Renal organic cation transporter. Non-inhibitor. 0.944. CYP450 2C9 substrate. Non-substrate. 0.823. ... Organic compounds. Super Class. Organic acids and derivatives. Class. Carboxylic acids and derivatives. Sub Class. Amino acids ... This compound belongs to the class of organic compounds known as alpha amino acids. These are amino acids in which the amino ... Organic oxides / Monoalkylamines / Hydrocarbon derivatives / Carbonyl compounds. Substituents. 1-aminocyclopropane-1-carboxylic ...
  • To study this vectorial transport of organic cations, we constructed a double-transfected Madin-Darby canine kidney strain II (MDCKII) cell line permanently expressing the human organic cation transporter 1 (OCT1, SLC22A1) in the basolateral membrane and MDR1 P-glycoprotein (MDR1 P-gp, ABCB1), an adenosine triphosphate (ATP)-dependent efflux pump for organic cations, in the apical membrane. (nih.gov)
  • Additionally, MDCKII single transfectants stably expressing OCT1, MDR1 P-gp, or human organic cation transporter 2 (OCT2, SLC22A2) were generated. (nih.gov)
  • Antisera directed against OCT1 or OCT2 specifically detected OCT1 in the basolateral membrane of human hepatocytes, OCT2 in tubular epithelial cells of human kidney, and the respective recombinant transporter in the basolateral membrane of MDCKII transfectants. (nih.gov)
  • We identified the lipophilic organic cation berberine, a fluorescent plant alkaloid exhibiting a broad range of biological activities, as substrate of OCT1 and OCT2 with Michaelis-Menten constants of 14.8 microM and 4.4 microM, respectively. (nih.gov)
  • Berberine also inhibited the uptake of the prototypic cations tetraethylammonium and 1-methyl-4-phenylpyridinium by MDCK-OCT1 and MDCK-OCT2 transfectants. (nih.gov)
  • 2013) Role of the plasma membrane transporter of organic cations OCT1 and its genetic variants in modern liver pharmacology. (guidetopharmacology.org)
  • Amino acids in TMS1 confer major functional differences between human and mouse orthologs of the polyspecific membrane transporter, OCT1. (tcdb.org)
  • 11] "Metformin is a superior substrate for renal organic cation transporter OCT2 rather than hepatic OCT1. (tcdb.org)
  • 16] "Evolutionary conservation predicts function of variants of the human organic cation transporter, OCT1. (tcdb.org)
  • 18] "Seven novel single nucleotide polymorphisms in the human SLC22A1 gene encoding organic cation transporter 1 (OCT1). (tcdb.org)
  • The molecule of MF, a small hydrophilic cation, is transported from the extracellular space to the cytoplasm of the target cell through organic cation transporters-1 and -2 (OCT1, OCT2), multidrug and toxin extrusion transporters (MATE), and ATM (ataxia telangiectasia mutated) transporter, and OCT1 and OCT2 are considered as the main functional units of MF transmembrane transport [ 7 ] . (encyclopedia.pub)
  • Islatravir Didn't Inhibit Important Hepatic Transporters at Clinically Relevant Concentrations In recombinant cell lines, concentrations of islatravir of up to 300 did not inhibit the OATP1B1-, OATP1B3-, and OCT1-mediated uptake of pitavastatin, sulfobromophthalein, or metformin, respectively. (caspaseinhibitor.com)
  • This indicates IC50 values higher than 300 for OATP1B1, OATP1B3, and OCT1, and higher than one hundred for the other hepatic transporters tested (Table two). (caspaseinhibitor.com)
  • The main objective is to develop and validate the methodology to study the genetic polymorphism of Organic cation transporter (OCT1) rs622342. (pharmdinfo.com)
  • Bictegravir inhibits organic cation transporter 2 (OCT2) and multidrug and toxin extrusion transporter 1 (MATE1) in vitro. (medscape.com)
  • The anticancer activity and the antitumor specificity of oxaliplatin mainly depend on human organic cation transporters (OCT) 1 and OCT2. (lclabs.com)
  • Introduction: The human organic cation transporter 2 (OCT2) is involved in the transport of endogenous quaternary amines and positively charged drugs across the basolateral membrane of proximal tubular cells. (figshare.com)
  • Islatravir Did not Inhibit Key Renal Transporters at Clinically Relevant Concentrations OAT1-mediated cidofovir uptake in recombinant cell lines was not inhibited by concentrations of islatravir up to one hundred , whereas islatravir inhibited OAT3-mediated estrone sulfate uptake and OCT2-mediated metformin uptake by 31 and 15 at one hundred , respectively. (caspaseinhibitor.com)
  • 2. Gründemann D, Liebich G, Kiefer N, Köster S, Schömig E. (1999) Selective substrates for non-neuronal monoamine transporters. (guidetopharmacology.org)
  • Uptake of [ 3 H]digoxin in SCHH was not inhibited by a variety of substrates or inhibitors for OATP1B1, OATP1B3, OATP2B1, organic anion transporter 2, organic cation transporter 1, and monocarboxylate transporter 8. (aspetjournals.org)
  • Moreover, [ 3 H]nicotine uptake was strongly inhibited in the presence of cationic drugs, such as pyrilamine, whereas only weak inhibitory effects were shown by substrates of typical organic cation transporters, such as tetraethylammonium, 1-methyl-4-phenylpyridinium, choline, and l -carnitine. (aspetjournals.org)
  • Pombrio JM, Giangreco A, Li L, Wempe MF, Anders MW, Sweet DH, Pritchard JB, Ballatori N. Mercapturic acids (N-acetylcysteine S-conjugates) as endogenous substrates for the renal organic anion transporter-1. (ucdenver.edu)
  • 1. In the present study it was tested whether known P-glycoprotein (P-gp) substrates/MDR reversal agents interact with small (type 1) and bulky (type 2) cationic drugs at the level of biliary excretion in the rat isolated perfused liver model (IPRL). (nih.gov)
  • 4. MDR substrates/reversal agents like verapamil, quinine, quinidine and vinblastine strongly reduced both type 1 and type 2 organic cation excretion into bile. (nih.gov)
  • 1] "Cloning and characterization of two human polyspecific organic cation transporters. (tcdb.org)
  • A polyspecific transporter for organic cations found primarily in the kidney. (ucdenver.edu)
  • The purpose of this study was to investigate the hepatic uptake mechanisms of [ 3 H]digoxin using sandwich-cultured human hepatocytes (SCHH) and transporter-expressing cells. (aspetjournals.org)
  • The predicted interactions were assessed by cis-inhibition assay using [ 3 H]1-methyl-4-phenylpyridinium ([ 3 H]MPP + ) as a model substrate, or by measuring the uptake of radiolabeled ligands in intact cells. (figshare.com)
  • Discovered more than a century ago, interest in this low molecular weight thiol/ketone has reignited, partly due to its unique chemical properties (such as its unusual stability), as well as the recognition of a transporter, the organic cation transporter novel type 1 (OCTN1), responsible for the uptake and accumulation of ET in human tissues in our diet, as well as selective distribution into tissues due to differences in transporter expression. (biosynsis.com)
  • Metformin uptake into recombinant cell lines expressing the renal efflux transporters MATE1 or MAT. (caspaseinhibitor.com)
  • SLC22A16 is one of newly isolated organic cation transporters, which is responsible for uptake and transport of adriamycin into cells. (elsevierpure.com)
  • While [ 3 H]thiamine uptake was markedly inhibited by nonlabeled thiamine it was not inhibited by several organic cations in 100-fold excess. (elsevierpure.com)
  • While [3H]thiamine uptake was markedly inhibited by nonlabeled thiamine it was not inhibited by several organic cations in 100-fold excess. (elsevierpure.com)
  • 4. Kimura H, Takeda M, Narikawa S, Enomoto A, Ichida K, Endou H. (2002) Human organic anion transporters and human organic cation transporters mediate renal transport of prostaglandins. (guidetopharmacology.org)
  • 3] "Molecular cloning, functional characterization and genomic organization of four alternatively spliced isoforms of the human organic cation transporter 1 (hOCT1/SLC22A1). (tcdb.org)
  • 17] "Novel single nucleotide polymorphisms of organic cation transporter 1 (SLC22A1) affecting transport functions. (tcdb.org)
  • Transporters such as organic anion-transporting polypeptide 1A2, P-glycoprotein, human organic cation transporter 1, and multidrug and toxin extrusion protein 1 are involved in the pharmacokinetics of LVX. (dovepress.com)
  • Organic Anion Transport Protein 1" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (ucdenver.edu)
  • This graph shows the total number of publications written about "Organic Anion Transport Protein 1" by people in this website by year, and whether "Organic Anion Transport Protein 1" was a major or minor topic of these publications. (ucdenver.edu)
  • Below are the most recent publications written about "Organic Anion Transport Protein 1" by people in Profiles. (ucdenver.edu)
  • Severe arrhythmia as a result of the interaction of cetirizine and pilsicainide in a patient with renal insufficiency: first case presentation showing competition for excretion via renal multidrug resistance protein 1 and organic cation transporter 2. (druglib.com)
  • Hence this carrier has a high degree of specificity for vitamin B 1 . (elsevierpure.com)
  • 14] "The expression of the solute carriers NTCP and OCT-1 is regulated by cholesterol in HepG2 cells. (tcdb.org)
  • Recently, the use of naturally expressed and overexpressed OCTN1 in human cells has once again confirmed the selective preference of ET as the substrate for OCTN1, supporting the proposal to rename OCTN1 as the ergothione transporter (ET). (biosynsis.com)
  • The studies were performed with model compounds tri-n-butylmethylammonium (TBuMA) (a relatively small type 1 organic cation), rocuronium (Roc) (a bulky type 2 organic cation) and the classical P-gp substrate doxorubicin (Dox). (nih.gov)
  • Alternatively, multiple organic cation transport systems with separate substrate specificities may be involved in the biliary excretion of amphiphilic drugs. (nih.gov)
  • Primary carnitine deficiency is caused by a deficiency in the plasma membrane carnitine transporter, with urinary carnitine wasting causing systemic carnitine depletion. (medscape.com)
  • SLC22A5 mutations can affect carnitine transport by impairing maturation of transporters to the plasma membrane. (medscape.com)
  • Within mitochondria, metformin directly inhibits the function of complex 1, a cluster of proteins vital to the function of the electron transport chain. (lifespan.io)
  • Corticosterone and quinine are able to inhibit all three organic cation transporters. (guidetopharmacology.org)
  • Interestingly, type 2 compounds, such as rocuronium, clearly inhibited type 1 cationic drugs as well as Dox secretion into bile, whereas type 1 compounds did not significantly inhibit type 2 drug excretion into bile. (nih.gov)
  • Description: This is Double-antibody Sandwich Enzyme-linked immunosorbent assay for detection of Human Organic Cation/Ergothioneine Transporter (OCTN1) in Tissue homogenates, cell lysates and other biological fluids. (therabio.org)
  • Description: Enzyme-linked immunosorbent assay based on the Double-antibody Sandwich method for detection of Human Organic Cation/Ergothioneine Transporter (OCTN1) in samples from Tissue homogenates, cell lysates and other biological fluids with no significant corss-reactivity with analogues from other species. (therabio.org)
  • Description: A sandwich ELISA kit for detection of Organic Cation/Ergothioneine Transporter from Human in samples from blood, serum, plasma, cell culture fluid and other biological fluids. (therabio.org)
  • Organic cation transporter new type 1, Ergothioneine transporter? (biosynsis.com)
  • 7] "Functional characterization of an organic cation transporter (hOCT1) in a transiently transfected human cell line (HeLa). (tcdb.org)
  • In 2005, it was discovered that OCTN1 (encoded by the gene slc22a4) is mainly a transporter of ET, and its transport efficiency is higher than many other related metabolites. (biosynsis.com)
  • 2] "Cloning and functional expression of a human liver organic cation transporter. (tcdb.org)
  • 9] "Regulation of the human organic cation transporter hOCT1. (tcdb.org)
  • 12] "The human organic cation transporter-1 gene is transactivated by hepatocyte nuclear factor-4alpha. (tcdb.org)
  • 15] "Identification of genetic variations of the human organic cation transporter hOCT1 and their functional consequences. (tcdb.org)
  • ISENTRESS 600 mg film-coated tablets is indicated in combination with other anti-retroviral medicinal products for the treatment of human immunodeficiency virus (HIV-1) infection in adults, and paediatric patients weighing at least 40 kg (see sections 4.2, 4.4, 5.1 and 5.2). (medicines.org.uk)
  • 1 INDICATIONS AND USAGE Abacavir tablets, in combination with other antiretroviral agents, are indicated for the treatment of human immunodeficiency virus (HIV-1) infection. (drugcentral.org)
  • Abacavir tablets, nucleoside analogue human immunodeficiency virus (HIV-1) reverse transcriptase inhibitor, are indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection. (drugcentral.org)
  • These include extensive research revealing the relationship between blood ET levels and health and disease, cellular and tissue protective mechanisms, potential therapeutic applications of ET, transporter expression and tissue distribution, biosynthetic mechanisms, and more. (biosynsis.com)
  • Coadministration of multivalent cation-containing drugs and LVX should be avoided. (dovepress.com)
  • 13] "Differential pharmacological in vitro properties of organic cation transporters and regional distribution in rat brain. (tcdb.org)
  • In vitro fertilized (IVF) embryos were cultured in the presence of dimethyl sulfoxide or inhibitors of MAP2K (0.4 μM PD0325901) and GSK3 (3 μM CHIR99021) from the zygote (Day 1) stage. (bioone.org)
  • Acta Haematol (2023) 146 (1): 39-45. (karger.com)
  • 12(1): 7-16, 2023 01 30. (bvsalud.org)
  • Biomarker research 2023 7 11 (1): 73. (cdc.gov)
  • Nature communications 2023 4 14 (1): 1958. (cdc.gov)
  • 3. We found a mutual interaction between TBuMA and procainamidethobromide (PAEB), both type 1 cationic compounds during biliary excretion. (nih.gov)
  • Neuroprotection of quercetin on central neurons against chronic high glucose through enhancement of Nrf2/ARE/glyoxalase-1 pathway mediated by phosphorylation regulation. (ac.ir)
  • Metformin reduces insulin doses in type 1 diabetes, but does not reduce the rate of glycated hemoglobin (HbA 1c), nor is it clear whether the benefit is sustained beyone 1 year or has any benefit to cardiovascular or other key clinical outcomes. (greenmedinfo.com)
  • 1 Kirpichnikov D, McFarlane SI, Sowers JR. Metformin: an update. (thieme-connect.com)
  • Mean + SD serum metformin concentrations over time following IV (A) and oral (B) administration of a bolus dose of metformin hydrochloride to 7 mixed-breed dogs (phase 1) in a crossover experiment (interval of 1 week between treatments). (avma.org)
  • Mean + SD serum metformin concentrations over time following twice-daily oral administration of metformin (phase 2) to the 7 dogs in Figure 1 . (avma.org)
  • Koepsell H. (2013) The SLC22 family with transporters of organic cations, anions and zwitterions. (guidetopharmacology.org)
  • The blood pH needs to be constantly between 7.35 and 7.45, and in addition the blood needs to remain electrically neutral, which means that the total cations, or positively charged particles, equals the total anions, or negatively charged particles. (msdmanuals.com)
  • Now, not all of the ions are easy or convenient to measure, so typically the dominant cation, sodium Na+, which is typically around 137 mEq/L and the two dominant anions, chloride Cl−, which is about 104 mEq/L, and bicarbonate HCO3−, which is around 24 mEq/L, are measured. (msdmanuals.com)
  • FETROJA for injection is a white to off-white, sterile, lyophilized powder formulated with 1 gram of cefiderocol (equivalent to 1.6 grams of cefiderocol sulfate tosylate), sucrose (900 mg), sodium chloride (216 mg), and sodium hydroxide to adjust pH. (globalrph.com)
  • 8] "Comparison of 'type I' and 'type II' organic cation transport by organic cation transporters and organic anion-transporting polypeptides. (tcdb.org)
  • however, a significant component of clearance is due to multidrug resistance 1-mediated transport into bile. (aspetjournals.org)
  • The pattern of inhibition and ion dependence is suggestive of an H + /organic cation antiporter-mediated nicotine transport system. (aspetjournals.org)
  • In secondary carnitine deficiency, which is caused by other metabolic disorders (eg, fatty acid oxidation disorders, organic acidemias), carnitine depletion may be secondary to the formation of acylcarnitine adducts and the inhibition of carnitine transport in renal cells by acylcarnitines. (medscape.com)
  • Yin J, Wang J. (2016) Renal drug transporters and their significance in drug-drug interactions. (guidetopharmacology.org)
  • The accumulation ability of ET in the body and its selective distribution in tissues (through differential expression of transporters) indicate that ET plays an important physiological role. (biosynsis.com)
  • Organic cation transporter 1 in complex with verapamil 3.45 Å (EMD-28588), processed by Dr. Yang Suo. (unc.edu)
  • 1) Cancer is classified as a group of diseases, all of which are characterized by uncontrolled cell proliferation. (wikipedia.org)
  • Epidemiological studies have shown cancer to be a leading cause of death worldwide (Figure 1). (wikipedia.org)
  • 1 Department of Pharmacokinetics and Drug Delivery, Groningen Institute for Drug Studies, University of Groningen, The Netherlands. (nih.gov)
  • This compound belongs to the class of organic compounds known as alpha amino acids. (drugbank.com)
  • Consistent with recent attention to ET, publications mentioning this compound have shown exponential growth (Figure 1). (biosynsis.com)
  • N/A: Indicates Monoamine Oxidase Inhibitor web calculations usually are not relevant for transporter or enzyme place. (caspaseinhibitor.com)
  • 6. Our data are compatible with a potential involvement of P-glycoprotein in the hepatobiliary excretion of doxorubicin as well as of some type 1 and type 2 organic cations. (nih.gov)
  • The 3 areas of involvement include (1) the cardiac muscle, which is affected by progressive cardiomyopathy (by far, the most common form of presentation), (2) the CNS, which is affected by encephalopathy caused by hypoketotic hypoglycemia, and (3) the skeletal muscle, which is affected by myopathy. (medscape.com)
  • 2014) SLC22, SLC44, and SLC47 transporters--organic anion and cation transporters: molecular and cellular properties. (guidetopharmacology.org)