An interleukin-1 subtype that is synthesized as an inactive membrane-bound pro-protein. Proteolytic processing of the precursor form by CASPASE 1 results in release of the active form of interleukin-1beta from the membrane.
An 11-kDa protein associated with the outer membrane of many cells including lymphocytes. It is the small subunit of the MHC class I molecule. Association with beta 2-microglobulin is generally required for the transport of class I heavy chains from the endoplasmic reticulum to the cell surface. Beta 2-microglobulin is present in small amounts in serum, csf, and urine of normal people, and to a much greater degree in the urine and plasma of patients with tubular proteinemia, renal failure, or kidney transplants.
One of two major pharmacologically defined classes of adrenergic receptors. The beta adrenergic receptors play an important role in regulating CARDIAC MUSCLE contraction, SMOOTH MUSCLE relaxation, and GLYCOGENOLYSIS.
An integrin beta subunit of approximately 85-kDa in size which has been found in INTEGRIN ALPHAIIB-containing and INTEGRIN ALPHAV-containing heterodimers. Integrin beta3 occurs as three alternatively spliced isoforms, designated beta3A-C.
A factor synthesized in a wide variety of tissues. It acts synergistically with TGF-alpha in inducing phenotypic transformation and can also act as a negative autocrine growth factor. TGF-beta has a potential role in embryonal development, cellular differentiation, hormone secretion, and immune function. TGF-beta is found mostly as homodimer forms of separate gene products TGF-beta1, TGF-beta2 or TGF-beta3. Heterodimers composed of TGF-beta1 and 2 (TGF-beta1.2) or of TGF-beta2 and 3 (TGF-beta2.3) have been isolated. The TGF-beta proteins are synthesized as precursor proteins.
An integrin found in FIBROBLASTS; PLATELETS; MONOCYTES, and LYMPHOCYTES. Integrin alpha5beta1 is the classical receptor for FIBRONECTIN, but it also functions as a receptor for LAMININ and several other EXTRACELLULAR MATRIX PROTEINS.
Also known as CD104 antigen, this protein is distinguished from other beta integrins by its relatively long cytoplasmic domain (approximately 1000 amino acids vs. approximately 50). Five alternatively spliced isoforms have been described.
This intrgrin is a key component of HEMIDESMOSOMES and is required for their formation and maintenance in epithelial cells. Integrin alpha6beta4 is also found on thymocytes, fibroblasts, and Schwann cells, where it functions as a laminin receptor (RECEPTORS, LAMININ) and is involved in wound healing, cell migration, and tumor invasiveness.
Integrin beta chains combine with integrin alpha chains to form heterodimeric cell surface receptors. Integrins have traditionally been classified into functional groups based on the identity of one of three beta chains present in the heterodimer. The beta chain is necessary and sufficient for integrin-dependent signaling. Its short cytoplasmic tail contains sequences critical for inside-out signaling.
A 44-kDa highly glycosylated plasma protein that binds phospholipids including CARDIOLIPIN; APOLIPOPROTEIN E RECEPTOR; membrane phospholipids, and other anionic phospholipid-containing moieties. It plays a role in coagulation and apoptotic processes. Formerly known as apolipoprotein H, it is an autoantigen in patients with ANTIPHOSPHOLIPID ANTIBODIES.
Integrin alpha4beta1 is a FIBRONECTIN and VCAM-1 receptor present on LYMPHOCYTES; MONOCYTES; EOSINOPHILS; NK CELLS and thymocytes. It is involved in both cell-cell and cell- EXTRACELLULAR MATRIX adhesion and plays a role in INFLAMMATION, hematopoietic cell homing and immune function, and has been implicated in skeletal MYOGENESIS; NEURAL CREST migration and proliferation, lymphocyte maturation and morphogenesis of the PLACENTA and HEART.
An integrin found on fibroblasts, platelets, endothelial and epithelial cells, and lymphocytes where it functions as a receptor for COLLAGEN and LAMININ. Although originally referred to as the collagen receptor, it is one of several receptors for collagen. Ligand binding to integrin alpha2beta1 triggers a cascade of intracellular signaling, including activation of p38 MAP kinase.
A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The adrenergic beta-2 receptors are more sensitive to EPINEPHRINE than to NOREPINEPHRINE and have a high affinity for the agonist TERBUTALINE. They are widespread, with clinically important roles in SKELETAL MUSCLE; LIVER; and vascular, bronchial, gastrointestinal, and genitourinary SMOOTH MUSCLE.
A family of transmembrane glycoproteins (MEMBRANE GLYCOPROTEINS) consisting of noncovalent heterodimers. They interact with a wide variety of ligands including EXTRACELLULAR MATRIX PROTEINS; COMPLEMENT, and other cells, while their intracellular domains interact with the CYTOSKELETON. The integrins consist of at least three identified families: the cytoadhesin receptors(RECEPTORS, CYTOADHESIN), the leukocyte adhesion receptors (RECEPTORS, LEUKOCYTE ADHESION), and the VERY LATE ANTIGEN RECEPTORS. Each family contains a common beta-subunit (INTEGRIN BETA CHAINS) combined with one or more distinct alpha-subunits (INTEGRIN ALPHA CHAINS). These receptors participate in cell-matrix and cell-cell adhesion in many physiologically important processes, including embryological development; HEMOSTASIS; THROMBOSIS; WOUND HEALING; immune and nonimmune defense mechanisms; and oncogenic transformation.
A soluble factor produced by MONOCYTES; MACROPHAGES, and other cells which activates T-lymphocytes and potentiates their response to mitogens or antigens. Interleukin-1 is a general term refers to either of the two distinct proteins, INTERLEUKIN-1ALPHA and INTERLEUKIN-1BETA. The biological effects of IL-1 include the ability to replace macrophage requirements for T-cell activation.
Integrin beta-1 chains which are expressed as heterodimers that are noncovalently associated with specific alpha-chains of the CD49 family (CD49a-f). CD29 is expressed on resting and activated leukocytes and is a marker for all of the very late activation antigens on cells. (from: Barclay et al., The Leukocyte Antigen FactsBook, 1993, p164)
A cell surface receptor mediating cell adhesion to the EXTRACELLULAR MATRIX and to other cells via binding to LAMININ. It is involved in cell migration, embryonic development, leukocyte activation and tumor cell invasiveness. Integrin alpha6beta1 is the major laminin receptor on PLATELETS; LEUKOCYTES; and many EPITHELIAL CELLS, and ligand binding may activate a number of signal transduction pathways. Alternative splicing of the cytoplasmic domain of the alpha6 subunit (INTEGRIN ALPHA6) results in the formation of A and B isoforms of the heterodimer, which are expressed in a tissue-specific manner.
A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The adrenergic beta-1 receptors are equally sensitive to EPINEPHRINE and NOREPINEPHRINE and bind the agonist DOBUTAMINE and the antagonist METOPROLOL with high affinity. They are found in the HEART, juxtaglomerular cells, and in the central and peripheral nervous systems.
Integrin alpha1beta1 functions as a receptor for LAMININ and COLLAGEN. It is widely expressed during development, but in the adult is the predominant laminin receptor (RECEPTORS, LAMININ) in mature SMOOTH MUSCLE CELLS, where it is important for maintenance of the differentiated phenotype of these cells. Integrin alpha1beta1 is also found in LYMPHOCYTES and microvascular endothelial cells, and may play a role in angiogenesis. In SCHWANN CELLS and neural crest cells, it is involved in cell migration. Integrin alpha1beta1 is also known as VLA-1 and CD49a-CD29.
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.
Established cell cultures that have the potential to propagate indefinitely.
A glycogen synthase kinase that was originally described as a key enzyme involved in glycogen metabolism. It regulates a diverse array of functions such as CELL DIVISION, microtubule function and APOPTOSIS.
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.
One of the ESTROGEN RECEPTORS that has greater affinity for ISOFLAVONES than ESTROGEN RECEPTOR ALPHA does. There is great sequence homology with ER alpha in the DNA-binding domain but not in the ligand binding and hinge domains.
A subtype of transforming growth factor beta that is synthesized by a wide variety of cells. It is synthesized as a precursor molecule that is cleaved to form mature TGF-beta 1 and TGF-beta1 latency-associated peptide. The association of the cleavage products results in the formation a latent protein which must be activated to bind its receptor. Defects in the gene that encodes TGF-beta1 are the cause of CAMURATI-ENGELMANN SYNDROME.
The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.
A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The beta-3 adrenergic receptors are the predominant beta-adrenergic receptor type expressed in white and brown ADIPOCYTES and are involved in modulating ENERGY METABOLISM and THERMOGENESIS.
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
Adherence of cells to surfaces or to other cells.
Brain waves with frequency between 15-30 Hz seen on EEG during wakefulness and mental activity.
Drugs that selectively bind to and activate beta-adrenergic receptors.
A DNA repair enzyme that catalyzes DNA synthesis during base excision DNA repair. EC
Proteins prepared by recombinant DNA technology.
Compounds bind to and activate ADRENERGIC BETA-2 RECEPTORS.
A multi-functional catenin that participates in CELL ADHESION and nuclear signaling. Beta catenin binds CADHERINS and helps link their cytoplasmic tails to the ACTIN in the CYTOSKELETON via ALPHA CATENIN. It also serves as a transcriptional co-activator and downstream component of WNT PROTEIN-mediated SIGNAL TRANSDUCTION PATHWAYS.
Cell-surface proteins that bind transforming growth factor beta and trigger changes influencing the behavior of cells. Two types of transforming growth factor receptors have been recognized. They differ in affinity for different members of the transforming growth factor beta family and in cellular mechanisms of action.
Compounds and molecular complexes that consist of very large numbers of atoms and are generally over 500 kDa in size. In biological systems macromolecular substances usually can be visualized using ELECTRON MICROSCOPY and are distinguished from ORGANELLES by the lack of a membrane structure.
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.
The parts of a macromolecule that directly participate in its specific combination with another molecule.
Any of the processes by which nuclear, cytoplasmic, or intercellular factors influence the differential control (induction or repression) of gene action at the level of transcription or translation.
The rate dynamics in chemical or physical systems.
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.
AMINO ALCOHOLS containing the propanolamine (NH2CH2CHOHCH2) group and its derivatives.
Receptors such as INTEGRIN ALPHAVBETA3 that bind VITRONECTIN with high affinity and play a role in cell migration. They also bind FIBRINOGEN; VON WILLEBRAND FACTOR; osteopontin; and THROMBOSPONDINS.
The introduction of a phosphoryl group into a compound through the formation of an ester bond between the compound and a phosphorus moiety.
Single chains of amino acids that are the units of multimeric PROTEINS. Multimeric proteins can be composed of identical or non-identical subunits. One or more monomeric subunits may compose a protomer which itself is a subunit structure of a larger assembly.
Nucleocytoplasmic transport molecules that bind to ALPHA KARYOPHERINS in the CYTOSOL and are involved in transport of molecules through the NUCLEAR PORE COMPLEX. Once inside the CELL NUCLEUS beta karyopherins interact with RAN GTP-BINDING PROTEIN and dissociate from alpha karyopherins. Beta karyopherins bound to RAN GTP-BINDING PROTEIN are then re-transported to the cytoplasm where hydrolysis of the GTP of RAN GTP-BINDING PROTEIN causes release of karyopherin beta.
A phosphoinositide phospholipase C subtype that is primarily regulated by its association with HETEROTRIMERIC G-PROTEINS. It is structurally related to PHOSPHOLIPASE C DELTA with the addition of C-terminal extension of 400 residues.
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.
The phenotypic manifestation of a gene or genes by the processes of GENETIC TRANSCRIPTION and GENETIC TRANSLATION.
Drugs that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. Adrenergic beta-antagonists are used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches, and anxiety.
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.
Glycoproteins found on the surfaces of cells, particularly in fibrillar structures. The proteins are lost or reduced when these cells undergo viral or chemical transformation. They are highly susceptible to proteolysis and are substrates for activated blood coagulation factor VIII. The forms present in plasma are called cold-insoluble globulins.
The relationship between the dose of an administered drug and the response of the organism to the drug.
Compounds that bind to and activate ADRENERGIC BETA-3 RECEPTORS.
A forkhead transcription factor that regulates expression of metabolic GENES and is involved in EMBRYONIC DEVELOPMENT. Mutations in HNF-3beta have been associated with CONGENITAL HYPERINSULINISM.
Any detectable and heritable change in the genetic material that causes a change in the GENOTYPE and which is transmitted to daughter cells and to succeeding generations.
Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques.
Identification of proteins or peptides that have been electrophoretically separated by blot transferring from the electrophoresis gel to strips of nitrocellulose paper, followed by labeling with antibody probes.
The characteristic 3-dimensional shape of a protein, including the secondary, supersecondary (motifs), tertiary (domains) and quaternary structure of the peptide chain. PROTEIN STRUCTURE, QUATERNARY describes the conformation assumed by multimeric proteins (aggregates of more than one polypeptide chain).
An integrin that binds to a variety of plasma and extracellular matrix proteins containing the conserved RGD amino acid sequence and modulates cell adhesion. Integrin alphavbeta3 is highly expressed in OSTEOCLASTS where it may play role in BONE RESORPTION. It is also abundant in vascular smooth muscle and endothelial cells, and in some tumor cells, where it is involved in angiogenesis and cell migration. Although often referred to as the vitronectin receptor there is more than one receptor for vitronectin (RECEPTORS, VITRONECTIN).
Non-antibody proteins secreted by inflammatory leukocytes and some non-leukocytic cells, that act as intercellular mediators. They differ from classical hormones in that they are produced by a number of tissue or cell types rather than by specialized glands. They generally act locally in a paracrine or autocrine rather than endocrine manner.
Cells grown in vitro from neoplastic tissue. If they can be established as a TUMOR CELL LINE, they can be propagated in cell culture indefinitely.
Serum glycoprotein produced by activated MACROPHAGES and other mammalian MONONUCLEAR LEUKOCYTES. It has necrotizing activity against tumor cell lines and increases ability to reject tumor transplants. Also known as TNF-alpha, it is only 30% homologous to TNF-beta (LYMPHOTOXIN), but they share TNF RECEPTORS.
A type of pancreatic cell representing about 50-80% of the islet cells. Beta cells secrete INSULIN.
One of the two major classes of cholinergic receptors. Nicotinic receptors were originally distinguished by their preference for NICOTINE over MUSCARINE. They are generally divided into muscle-type and neuronal-type (previously ganglionic) based on pharmacology, and subunit composition of the receptors.
A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)
Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures.
A hepatocyte nuclear factor that is closely related to HEPATOCYTE NUCLEAR FACTOR 1-ALPHA but is only weakly expressed in the LIVER. Mutations in hepatocyte nuclear factor 1-beta are associated with renal CYSTS and MATURITY-ONSET DIABETES MELLITUS type 5.
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 degree of similarity between sequences of amino acids. This information is useful for the analyzing genetic relatedness of proteins and species.
A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.
Recombinant proteins produced by the GENETIC TRANSLATION of fused genes formed by the combination of NUCLEIC ACID REGULATORY SEQUENCES of one or more genes with the protein coding sequences of one or more genes.
Elements of limited time intervals, contributing to particular results or situations.
The sequence of carbohydrates within POLYSACCHARIDES; GLYCOPROTEINS; and GLYCOLIPIDS.
The beta subunit of human CHORIONIC GONADOTROPIN. Its structure is similar to the beta subunit of LUTEINIZING HORMONE, except for the additional 30 amino acids at the carboxy end with the associated carbohydrate residues. HCG-beta is used as a diagnostic marker for early detection of pregnancy, spontaneous abortion (ABORTION, SPONTANEOUS); ECTOPIC PREGNANCY; HYDATIDIFORM MOLE; CHORIOCARCINOMA; or DOWN SYNDROME.
The biosynthesis of RNA carried out on a template of DNA. The biosynthesis of DNA from an RNA template is called REVERSE TRANSCRIPTION.
PKC beta encodes two proteins (PKCB1 and PKCBII) generated by alternative splicing of C-terminal exons. It is widely distributed with wide-ranging roles in processes such as B-cell receptor regulation, oxidative stress-induced apoptosis, androgen receptor-dependent transcriptional regulation, insulin signaling, and endothelial cell proliferation.
Histochemical localization of immunoreactive substances using labeled antibodies as reagents.
The movement of cells from one location to another. Distinguish from CYTOKINESIS which is the process of dividing the CYTOPLASM of a cell.
Antibodies produced by a single clone of cells.
Laboratory mice that have been produced from a genetically manipulated EGG or EMBRYO, MAMMALIAN.
High energy POSITRONS or ELECTRONS ejected from a disintegrating atomic nucleus.
Cell-surface glycoprotein beta-chains that are non-covalently linked to specific alpha-chains of the CD11 family of leukocyte-adhesion molecules (RECEPTORS, LEUKOCYTE-ADHESION). A defect in the gene encoding CD18 causes LEUKOCYTE-ADHESION DEFICIENCY SYNDROME.
Conversion of an inactive form of an enzyme to one possessing metabolic activity. It includes 1, activation by ions (activators); 2, activation by cofactors (coenzymes); and 3, conversion of an enzyme precursor (proenzyme or zymogen) to an active enzyme.
Short sequences (generally about 10 base pairs) of DNA that are complementary to sequences of messenger RNA and allow reverse transcriptases to start copying the adjacent sequences of mRNA. Primers are used extensively in genetic and molecular biology techniques.
A TGF-beta subtype that was originally identified as a GLIOBLASTOMA-derived factor which inhibits the antigen-dependent growth of both helper and CYTOTOXIC T LYMPHOCYTES. It is synthesized as a precursor molecule that is cleaved to form mature TGF-beta2 and TGF-beta2 latency-associated peptide. The association of the cleavage products results in the formation a latent protein which must be activated to bind its receptor.
Structurally related forms of an enzyme. Each isoenzyme has the same mechanism and classification, but differs in its chemical, physical, or immunological characteristics.
Different forms of a protein that may be produced from different GENES, or from the same gene by ALTERNATIVE SPLICING.
A long pro-domain caspase that has specificity for the precursor form of INTERLEUKIN-1BETA. It plays a role in INFLAMMATION by catalytically converting the inactive forms of CYTOKINES such as interleukin-1beta to their active, secreted form. Caspase 1 is referred as interleukin-1beta converting enzyme and is frequently abbreviated ICE.
Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.
A deoxyribonucleotide polymer that is the primary genetic material of all cells. Eukaryotic and prokaryotic organisms normally contain DNA in a double-stranded state, yet several important biological processes transiently involve single-stranded regions. DNA, which consists of a polysugar-phosphate backbone possessing projections of purines (adenine and guanine) and pyrimidines (thymine and cytosine), forms a double helix that is held together by hydrogen bonds between these purines and pyrimidines (adenine to thymine and guanine to cytosine).
Irregular microscopic structures consisting of cords of endocrine cells that are scattered throughout the PANCREAS among the exocrine acini. Each islet is surrounded by connective tissue fibers and penetrated by a network of capillaries. There are four major cell types. The most abundant beta cells (50-80%) secrete INSULIN. Alpha cells (5-20%) secrete GLUCAGON. PP cells (10-35%) secrete PANCREATIC POLYPEPTIDE. Delta cells (~5%) secrete SOMATOSTATIN.
Domesticated bovine animals of the genus Bos, usually kept on a farm or ranch and used for the production of meat or dairy products or for heavy labor.
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.
Large, noncollagenous glycoprotein with antigenic properties. It is localized in the basement membrane lamina lucida and functions to bind epithelial cells to the basement membrane. Evidence suggests that the protein plays a role in tumor invasion.
Peptides generated from AMYLOID BETA-PEPTIDES PRECURSOR. An amyloid fibrillar form of these peptides is the major component of amyloid plaques found in individuals with Alzheimer's disease and in aged individuals with trisomy 21 (DOWN SYNDROME). The peptide is found predominantly in the nervous system, but there have been reports of its presence in non-neural tissue.
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.
The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.
Serum proteins with an electrophoretic mobility that falls between ALPHA-GLOBULINS and GAMMA-GLOBULINS.
Genetically engineered MUTAGENESIS at a specific site in the DNA molecule that introduces a base substitution, or an insertion or deletion.
Connective tissue cells which secrete an extracellular matrix rich in collagen and other macromolecules.
A positive regulatory effect on physiological processes at the molecular, cellular, or systemic level. At the molecular level, the major regulatory sites include membrane receptors, genes (GENE EXPRESSION REGULATION), mRNAs (RNA, MESSENGER), and proteins.
Progressive restriction of the developmental potential and increasing specialization of function that leads to the formation of specialized cells, tissues, and organs.
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.
The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.
In vitro method for producing large amounts of specific DNA or RNA fragments of defined length and sequence from small amounts of short oligonucleotide flanking sequences (primers). The essential steps include thermal denaturation of the double-stranded target molecules, annealing of the primers to their complementary sequences, and extension of the annealed primers by enzymatic synthesis with DNA polymerase. The reaction is efficient, specific, and extremely sensitive. Uses for the reaction include disease diagnosis, detection of difficult-to-isolate pathogens, mutation analysis, genetic testing, DNA sequencing, and analyzing evolutionary relationships.
Differentiation antigens residing on mammalian leukocytes. CD stands for cluster of differentiation, which refers to groups of monoclonal antibodies that show similar reactivity with certain subpopulations of antigens of a particular lineage or differentiation stage. The subpopulations of antigens are also known by the same CD designation.
DNA sequences which are recognized (directly or indirectly) and bound by a DNA-dependent RNA polymerase during the initiation of transcription. Highly conserved sequences within the promoter include the Pribnow box in bacteria and the TATA BOX in eukaryotes.
Peptides composed of between two and twelve amino acids.
Electrophoresis in which a polyacrylamide gel is used as the diffusion medium.
Proteins which bind to DNA. The family includes proteins which bind to both double- and single-stranded DNA and also includes specific DNA binding proteins in serum which can be used as markers for malignant diseases.
Regulatory proteins that act as molecular switches. They control a wide range of biological processes including: receptor signaling, intracellular signal transduction pathways, and protein synthesis. Their activity is regulated by factors that control their ability to bind to and hydrolyze GTP to GDP. EC 3.6.1.-.
A TGF-beta subtype that plays role in regulating epithelial-mesenchymal interaction during embryonic development. It is synthesized as a precursor molecule that is cleaved to form mature TGF-beta3 and TGF-beta3 latency-associated peptide. The association of the cleavage products results in the formation a latent protein which must be activated to bind its receptor.
A negative regulatory effect on physiological processes at the molecular, cellular, or systemic level. At the molecular level, the major regulatory sites include membrane receptors, genes (GENE EXPRESSION REGULATION), mRNAs (RNA, MESSENGER), and proteins.
A cell line derived from cultured tumor cells.
Endogenous substances, usually proteins, which are effective in the initiation, stimulation, or termination of the genetic transcription process.
Technique using an instrument system for making, processing, and displaying one or more measurements on individual cells obtained from a cell suspension. Cells are usually stained with one or more fluorescent dyes specific to cell components of interest, e.g., DNA, and fluorescence of each cell is measured as it rapidly transverses the excitation beam (laser or mercury arc lamp). Fluorescence provides a quantitative measure of various biochemical and biophysical properties of the cell, as well as a basis for cell sorting. Other measurable optical parameters include light absorption and light scattering, the latter being applicable to the measurement of cell size, shape, density, granularity, and stain uptake.
AMINO ALCOHOLS containing the ETHANOLAMINE; (-NH2CH2CHOH) group and its derivatives.
A cytokine that stimulates the growth and differentiation of B-LYMPHOCYTES and is also a growth factor for HYBRIDOMAS and plasmacytomas. It is produced by many different cells including T-LYMPHOCYTES; MONOCYTES; and FIBROBLASTS.
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.
Drugs that bind to and block the activation of ADRENERGIC BETA-3 RECEPTORS.
One of the type I interferons produced by fibroblasts in response to stimulation by live or inactivated virus or by double-stranded RNA. It is a cytokine with antiviral, antiproliferative, and immunomodulating activity.
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.
Lipid-containing polysaccharides which are endotoxins and important group-specific antigens. They are often derived from the cell wall of gram-negative bacteria and induce immunoglobulin secretion. The lipopolysaccharide molecule consists of three parts: LIPID A, core polysaccharide, and O-specific chains (O ANTIGENS). When derived from Escherichia coli, lipopolysaccharides serve as polyclonal B-cell mitogens commonly used in laboratory immunology. (From Dorland, 28th ed)
Transport proteins that carry specific substances in the blood or across cell membranes.
A ligand that binds to but fails to activate the INTERLEUKIN 1 RECEPTOR. It plays an inhibitory role in the regulation of INFLAMMATION and FEVER. Several isoforms of the protein exist due to multiple ALTERNATIVE SPLICING of its mRNA.
A species of the Beta genus. Cultivars are used as a source of beets (root) or chard (leaves).
Lymphocytes responsible for cell-mediated immunity. Two types have been identified - cytotoxic (T-LYMPHOCYTES, CYTOTOXIC) and helper T-lymphocytes (T-LYMPHOCYTES, HELPER-INDUCER). They are formed when lymphocytes circulate through the THYMUS GLAND and differentiate to thymocytes. When exposed to an antigen, they divide rapidly and produce large numbers of new T cells sensitized to that antigen.
Carbohydrates consisting of between two (DISACCHARIDES) and ten MONOSACCHARIDES connected by either an alpha- or beta-glycosidic link. They are found throughout nature in both the free and bound form.
The level of protein structure in which regular hydrogen-bond interactions within contiguous stretches of polypeptide chain give rise to alpha helices, beta strands (which align to form beta sheets) or other types of coils. This is the first folding level of protein conformation.
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
Collagen receptors are cell surface receptors that modulate signal transduction between cells and the EXTRACELLULAR MATRIX. They are found in many cell types and are involved in the maintenance and regulation of cell shape and behavior, including PLATELET ACTIVATION and aggregation, through many different signaling pathways and differences in their affinities for collagen isoforms. Collagen receptors include discoidin domain receptors, INTEGRINS, and glycoprotein VI.
A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638)
The fission of a CELL. It includes CYTOKINESIS, when the CYTOPLASM of a cell is divided, and CELL NUCLEUS DIVISION.
The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.
One of the mechanisms by which CELL DEATH occurs (compare with NECROSIS and AUTOPHAGOCYTOSIS). Apoptosis is the mechanism responsible for the physiological deletion of cells and appears to be intrinsically programmed. It is characterized by distinctive morphologic changes in the nucleus and cytoplasm, chromatin cleavage at regularly spaced sites, and the endonucleolytic cleavage of genomic DNA; (DNA FRAGMENTATION); at internucleosomal sites. This mode of cell death serves as a balance to mitosis in regulating the size of animal tissues and in mediating pathologic processes associated with tumor growth.
Glycoproteins with the electrophoretic mobility of BETA-GLOBULINS, secreted by the placental TROPHOBLASTS into the maternal bloodstream during PREGNANCY. They can be detected 18 days after OVULATION and reach 200 mg/ml at the end of pregnancy. They are associated with fetal well-being.
Detection of RNA that has been electrophoretically separated and immobilized by blotting on nitrocellulose or other type of paper or nylon membrane followed by hybridization with labeled NUCLEIC ACID PROBES.
Thymosin. A family of heat-stable, polypeptide hormones secreted by the thymus gland. Their biological activities include lymphocytopoiesis, restoration of immunological competence and enhancement of expression of T-cell characteristics and function. They have therapeutic potential in patients having primary or secondary immunodeficiency diseases, cancer or diseases related to aging.
The process by which two molecules of the same chemical composition form a condensation product or polymer.
Serologic tests in which a positive reaction manifested by visible CHEMICAL PRECIPITATION occurs when a soluble ANTIGEN reacts with its precipitins, i.e., ANTIBODIES that can form a precipitate.
DNA sequences encoding the beta chain of the T-cell receptor. The genomic organization of the TcR beta genes is essentially the same in all species and is similar to the organization of Ig genes.
The regulatory subunits of large-conductance calcium-activated potassium channels.
Heterotrimeric GTP-binding protein subunits that tightly associate with GTP-BINDING PROTEIN GAMMA SUBUNITS. A dimer of beta and gamma subunits is formed when the GTP-BINDING PROTEIN ALPHA SUBUNIT dissociates from the GTP-binding protein heterotrimeric complex. The beta-gamma dimer can play an important role in signal transduction by interacting with a variety of second messengers.
A 51-amino acid pancreatic hormone that plays a major role in the regulation of glucose metabolism, directly by suppressing endogenous glucose production (GLYCOGENOLYSIS; GLUCONEOGENESIS) and indirectly by suppressing GLUCAGON secretion and LIPOLYSIS. Native insulin is a globular protein comprised of a zinc-coordinated hexamer. Each insulin monomer containing two chains, A (21 residues) and B (30 residues), linked by two disulfide bonds. Insulin is used as a drug to control insulin-dependent diabetes mellitus (DIABETES MELLITUS, TYPE 1).
A superfamily of proteins containing the globin fold which is composed of 6-8 alpha helices arranged in a characterstic HEME enclosing structure.
The characteristic 3-dimensional shape of a carbohydrate.
Immunologic method used for detecting or quantifying immunoreactive substances. The substance is identified by first immobilizing it by blotting onto a membrane and then tagging it with labeled antibodies.
Ubiquitous, inducible, nuclear transcriptional activator that binds to enhancer elements in many different cell types and is activated by pathogenic stimuli. The NF-kappa B complex is a heterodimer composed of two DNA-binding subunits: NF-kappa B1 and relA.
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.
Naturally occurring or experimentally induced animal diseases with pathological processes sufficiently similar to those of human diseases. They are used as study models for human diseases.
Theoretical representations that simulate the behavior or activity of biological processes or diseases. For disease models in living animals, DISEASE MODELS, ANIMAL is available. Biological models include the use of mathematical equations, computers, and other electronic equipment.
The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements.
A short-acting beta-2 adrenergic agonist that is primarily used as a bronchodilator agent to treat ASTHMA. Albuterol is prepared as a racemic mixture of R(-) and S(+) stereoisomers. The stereospecific preparation of R(-) isomer of albuterol is referred to as levalbuterol.
Surface ligands, usually glycoproteins, that mediate cell-to-cell adhesion. Their functions include the assembly and interconnection of various vertebrate systems, as well as maintenance of tissue integration, wound healing, morphogenic movements, cellular migrations, and metastasis.
An adrenergic beta-2 agonist that is used as a bronchodilator and tocolytic.
A characteristic feature of enzyme activity in relation to the kind of substrate on which the enzyme or catalytic molecule reacts.
A calcium-binding protein that is 92 AA long, contains 2 EF-hand domains, and is concentrated mainly in GLIAL CELLS. Elevation of S100B levels in brain tissue correlates with a role in neurological disorders.
A blood plasma glycoprotein that mediates cell adhesion and interacts with proteins of the complement, coagulation, and fibrinolytic cascade. (From Segen, Dictionary of Modern Medicine, 1992)
The part of a cell that contains the CYTOSOL and small structures excluding the CELL NUCLEUS; MITOCHONDRIA; and large VACUOLES. (Glick, Glossary of Biochemistry and Molecular Biology, 1990)
CELL LINES derived from the CV-1 cell line by transformation with a replication origin defective mutant of SV40 VIRUS, which codes for wild type large T antigen (ANTIGENS, POLYOMAVIRUS TRANSFORMING). They are used for transfection and cloning. (The CV-1 cell line was derived from the kidney of an adult male African green monkey (CERCOPITHECUS AETHIOPS).)
Enzymes that catalyze the transfer of N-acetylglucosamine from a nucleoside diphosphate N-acetylglucosamine to an acceptor molecule which is frequently another carbohydrate. EC 2.4.1.-.
A polypeptide substance comprising about one third of the total protein in mammalian organisms. It is the main constituent of SKIN; CONNECTIVE TISSUE; and the organic substance of bones (BONE AND BONES) and teeth (TOOTH).
The arrangement of two or more amino acid or base sequences from an organism or organisms in such a way as to align areas of the sequences sharing common properties. The degree of relatedness or homology between the sequences is predicted computationally or statistically based on weights assigned to the elements aligned between the sequences. This in turn can serve as a potential indicator of the genetic relatedness between the organisms.
Conjugated protein-carbohydrate compounds including mucins, mucoid, and amyloid glycoproteins.
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
The relatively long-lived phagocytic cell of mammalian tissues that are derived from blood MONOCYTES. Main types are PERITONEAL MACROPHAGES; ALVEOLAR MACROPHAGES; HISTIOCYTES; KUPFFER CELLS of the liver; and OSTEOCLASTS. They may further differentiate within chronic inflammatory lesions to EPITHELIOID CELLS or may fuse to form FOREIGN BODY GIANT CELLS or LANGHANS GIANT CELLS. (from The Dictionary of Cell Biology, Lackie and Dow, 3rd ed.)
Glycoproteins which contain sialic acid as one of their carbohydrates. They are often found on or in the cell or tissue membranes and participate in a variety of biological activities.
A group of hereditary hemolytic anemias in which there is decreased synthesis of one or more hemoglobin polypeptide chains. There are several genetic types with clinical pictures ranging from barely detectable hematologic abnormality to severe and fatal anemia.
Platelet membrane glycoprotein complex important for platelet adhesion and aggregation. It is an integrin complex containing INTEGRIN ALPHAIIB and INTEGRIN BETA3 which recognizes the arginine-glycine-aspartic acid (RGD) sequence present on several adhesive proteins. As such, it is a receptor for FIBRINOGEN; VON WILLEBRAND FACTOR; FIBRONECTIN; VITRONECTIN; and THROMBOSPONDINS. A deficiency of GPIIb-IIIa results in GLANZMANN THROMBASTHENIA.
Hormonally active polypeptides that can induce the transformed phenotype when added to normal, non-transformed cells. They have been found in culture fluids from retrovirally transformed cells and in tumor-derived cells as well as in non-neoplastic sources. Their transforming activities are due to the simultaneous action of two otherwise unrelated factors, TRANSFORMING GROWTH FACTOR ALPHA and TRANSFORMING GROWTH FACTOR BETA.
Spectroscopic method of measuring the magnetic moment of elementary particles such as atomic nuclei, protons or electrons. It is employed in clinical applications such as NMR Tomography (MAGNETIC RESONANCE IMAGING).
The sum of the weight of all the atoms in a molecule.
An immunoassay utilizing an antibody labeled with an enzyme marker such as horseradish peroxidase. While either the enzyme or the antibody is bound to an immunosorbent substrate, they both retain their biologic activity; the change in enzyme activity as a result of the enzyme-antibody-antigen reaction is proportional to the concentration of the antigen and can be measured spectrophotometrically or with the naked eye. Many variations of the method have been developed.
The species Oryctolagus cuniculus, in the family Leporidae, order LAGOMORPHA. Rabbits are born in burrows, furless, and with eyes and ears closed. In contrast with HARES, rabbits have 22 chromosome pairs.
Cells that line the inner and outer surfaces of the body by forming cellular layers (EPITHELIUM) or masses. Epithelial cells lining the SKIN; the MOUTH; the NOSE; and the ANAL CANAL derive from ectoderm; those lining the RESPIRATORY SYSTEM and the DIGESTIVE SYSTEM derive from endoderm; others (CARDIOVASCULAR SYSTEM and LYMPHATIC SYSTEM) derive from mesoderm. Epithelial cells can be classified mainly by cell shape and function into squamous, glandular and transitional epithelial cells.
A species of gram-negative, facultatively anaerobic, rod-shaped bacteria (GRAM-NEGATIVE FACULTATIVELY ANAEROBIC RODS) commonly found in the lower part of the intestine of warm-blooded animals. It is usually nonpathogenic, but some strains are known to produce DIARRHEA and pyogenic infections. Pathogenic strains (virotypes) are classified by their specific pathogenic mechanisms such as toxins (ENTEROTOXIGENIC ESCHERICHIA COLI), etc.
A meshwork-like substance found within the extracellular space and in association with the basement membrane of the cell surface. It promotes cellular proliferation and provides a supporting structure to which cells or cell lysates in culture dishes adhere.
Enzymes that catalyze the transfer of galactose from a nucleoside diphosphate galactose to an acceptor molecule which is frequently another carbohydrate. EC 2.4.1.-.
The 17-beta-isomer of estradiol, an aromatized C18 steroid with hydroxyl group at 3-beta- and 17-beta-position. Estradiol-17-beta is the most potent form of mammalian estrogenic steroids.
Large, phagocytic mononuclear leukocytes produced in the vertebrate BONE MARROW and released into the BLOOD; contain a large, oval or somewhat indented nucleus surrounded by voluminous cytoplasm and numerous organelles.
The outward appearance of the individual. It is the product of interactions between genes, and between the GENOTYPE and the environment.
The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM.
A group of enzymes that catalyzes the phosphorylation of serine or threonine residues in proteins, with ATP or other nucleotides as phosphate donors.
Test for tissue antigen using either a direct method, by conjugation of antibody with fluorescent dye (FLUORESCENT ANTIBODY TECHNIQUE, DIRECT) or an indirect method, by formation of antigen-antibody complex which is then labeled with fluorescein-conjugated anti-immunoglobulin antibody (FLUORESCENT ANTIBODY TECHNIQUE, INDIRECT). The tissue is then examined by fluorescence microscopy.
An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH.
The study of crystal structure using X-RAY DIFFRACTION techniques. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
Diffusible gene products that act on homologous or heterologous molecules of viral or cellular DNA to regulate the expression of proteins.
Normal adult human hemoglobin. The globin moiety consists of two alpha and two beta chains.
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).
Cell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and contain an integral membrane chloride channel. Each receptor is assembled as a pentamer from a pool of at least 19 different possible subunits. The receptors belong to a superfamily that share a common CYSTEINE loop.
A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.
Ordered rearrangement of T-cell variable gene regions coding for the beta-chain of antigen receptors.
All of the processes involved in increasing CELL NUMBER including CELL DIVISION.
A member of the tumor necrosis factor receptor superfamily. It has specificity for LYMPHOTOXIN ALPHA1, BETA2 HETEROTRIMER and TUMOR NECROSIS FACTOR LIGAND SUPERFAMILY MEMBER 14. The receptor plays a role in regulating lymphoid ORGANOGENESIS and the differentiation of certain subsets of NATURAL KILLER T-CELLS. Signaling of the receptor occurs through its association with TNF RECEPTOR-ASSOCIATED FACTORS.
Drugs that bind to and activate nicotinic cholinergic receptors (RECEPTORS, NICOTINIC). Nicotinic agonists act at postganglionic nicotinic receptors, at neuroeffector junctions in the peripheral nervous system, and at nicotinic receptors in the central nervous system. Agents that function as neuromuscular depolarizing blocking agents are included here because they activate nicotinic receptors, although they are used clinically to block nicotinic transmission.
Within a eukaryotic cell, a membrane-limited body which contains chromosomes and one or more nucleoli (CELL NUCLEOLUS). The nuclear membrane consists of a double unit-type membrane which is perforated by a number of pores; the outermost membrane is continuous with the ENDOPLASMIC RETICULUM. A cell may contain more than one nucleus. (From Singleton & Sainsbury, Dictionary of Microbiology and Molecular Biology, 2d ed)
Small double-stranded, non-protein coding RNAs (21-31 nucleotides) involved in GENE SILENCING functions, especially RNA INTERFERENCE (RNAi). Endogenously, siRNAs are generated from dsRNAs (RNA, DOUBLE-STRANDED) by the same ribonuclease, Dicer, that generates miRNAs (MICRORNAS). The perfect match of the siRNAs' antisense strand to their target RNAs mediates RNAi by siRNA-guided RNA cleavage. siRNAs fall into different classes including trans-acting siRNA (tasiRNA), repeat-associated RNA (rasiRNA), small-scan RNA (scnRNA), and Piwi protein-interacting RNA (piRNA) and have different specific gene silencing functions.

A gain-of-function polymorphism in a G-protein coupling domain of the human beta1-adrenergic receptor. (1/608)

The beta1-adrenergic receptor (beta1AR) is a key cell surface signaling protein expressed in the heart and other organs that mediates the actions of catecholamines of the sympathetic nervous system. A polymorphism in the intracellular cytoplasmic tail near the seventh transmembrane-spanning segment of the human beta1AR has been identified in a cohort of normal individuals. At amino acid position 389, Gly or Arg can be found (allele frequencies 0.26 and 0. 74, respectively), the former previously considered as the human wild-type beta1AR. Using site-directed mutagenesis to mimic the two variants, CHW-1102 cells were permanently transfected to express the Gly-389 and Arg-389 receptors. In functional studies with matched expression, the Arg-389 receptors had slightly higher basal levels of adenylyl cyclase activities (10.7 +/- 1.2 versus 6.1 +/- 0.4 pmol/min/mg). However, maximal isoproterenol-stimulated levels were markedly higher for the Arg-389 as compared to the Gly-389 receptor (63.3 +/- 6.1 versus 20.9 +/- 2.0 pmol/min/mg). Agonist-promoted [35S]guanosine 5'-O-(thiotriphosphate) binding was also increased with the Arg-389 receptor consistent with enhanced coupling to Gs and increased adenylyl cyclase activation. In agonist competition studies carried out in the absence of guanosine 5'-(beta, gamma-imido)triphosphate, high affinity binding could not be resolved with the Gly-389 receptor, whereas Arg-389 displayed an accumulation of the agonist high affinity receptor complex (RH = 26%). Taken together, these data indicate that this polymorphic variation of the human beta1AR results in alterations of receptor-Gs interaction with functional signal transduction consequences, consistent with its localization in a putative G-protein binding domain. The genetic variation of beta1AR at this locus may be the basis of interindividual differences in pathophysiologic characteristics or in the response to therapeutic betaAR agonists and antagonists in cardiovascular and other diseases.  (+info)

beta2-adrenergic cAMP signaling is uncoupled from phosphorylation of cytoplasmic proteins in canine heart. (2/608)

BACKGROUND: Recent studies of beta-adrenergic receptor (beta-AR) subtype signaling in in vitro preparations have raised doubts as to whether the cAMP/protein kinase A (PKA) signaling is activated in the same manner in response to beta2-AR versus beta1-AR stimulation. METHODS AND RESULTS: The present study compared, in the intact dog, the magnitude and characteristics of chronotropic, inotropic, and lusitropic effects of cAMP accumulation, PKA activation, and PKA-dependent phosphorylation of key effector proteins in response to beta-AR subtype stimulation. In addition, many of these parameters and L-type Ca2+ current (ICa) were also measured in single canine ventricular myocytes. The results indicate that although the cAMP/PKA-dependent phosphorylation cascade activated by beta1-AR stimulation could explain the resultant modulation of cardiac function, substantial beta2-AR-mediated chronotropic, inotropic, and lusitropic responses occurred in the absence of PKA activation and phosphorylation of nonsarcolemmal proteins, including phospholamban, troponin I, C protein, and glycogen phosphorylase kinase. However, in single canine myocytes, we found that beta2-AR-stimulated increases in both ICa and contraction were abolished by PKA inhibition. Thus, the beta2-AR-directed cAMP/PKA signaling modulates sarcolemmal L-type Ca2+ channels but does not regulate PKA-dependent phosphorylation of cytoplasmic proteins. CONCLUSIONS: These results indicate that the dissociation of beta2-AR signaling from cAMP regulatory systems is only apparent and that beta2-AR-stimulated cAMP/PKA signaling is uncoupled from phosphorylation of nonsarcolemmal regulatory proteins involved in excitation-contraction coupling.  (+info)

Cardiovascular and metabolic alterations in mice lacking both beta1- and beta2-adrenergic receptors. (3/608)

The activation state of beta-adrenergic receptors (beta-ARs) in vivo is an important determinant of hemodynamic status, cardiac performance, and metabolic rate. In order to achieve homeostasis in vivo, the cellular signals generated by beta-AR activation are integrated with signals from a number of other distinct receptors and signaling pathways. We have utilized genetic knockout models to test directly the role of beta1- and/or beta2-AR expression on these homeostatic control mechanisms. Despite total absence of beta1- and beta2-ARs, the predominant cardiovascular beta-adrenergic subtypes, basal heart rate, blood pressure, and metabolic rate do not differ from wild type controls. However, stimulation of beta-AR function by beta-AR agonists or exercise reveals significant impairments in chronotropic range, vascular reactivity, and metabolic rate. Surprisingly, the blunted chronotropic and metabolic response to exercise seen in beta1/beta2-AR double knockouts fails to impact maximal exercise capacity. Integrating the results from single beta1- and beta2-AR knockouts as well as the beta1-/beta2-AR double knock-out suggest that in the mouse, beta-AR stimulation of cardiac inotropy and chronotropy is mediated almost exclusively by the beta1-AR, whereas vascular relaxation and metabolic rate are controlled by all three beta-ARs (beta1-, beta2-, and beta3-AR). Compensatory alterations in cardiac muscarinic receptor density and vascular beta3-AR responsiveness are also observed in beta1-/beta2-AR double knockouts. In addition to its ability to define beta-AR subtype-specific functions, this genetic approach is also useful in identifying adaptive alterations that serve to maintain critical physiological setpoints such as heart rate, blood pressure, and metabolic rate when cellular signaling mechanisms are perturbed.  (+info)

Progressive hypertrophy and heart failure in beta1-adrenergic receptor transgenic mice. (4/608)

Stimulation of cardiac beta1-adrenergic receptors is the main mechanism that increases heart rate and contractility. Consequently, several pharmacological and gene transfer strategies for the prevention of heart failure aim at improving the function of the cardiac beta-adrenergic receptor system, whereas current clinical treatment favors a reduction of cardiac stimulation. To address this controversy, we have generated mice with heart-specific overexpression of beta1-adrenergic receptors. Their cardiac function was investigated in organ bath experiments as well as in vivo by cardiac catheterization and by time-resolved NMR imaging. The transgenic mice had increased cardiac contractility at a young age but also developed marked myocyte hypertrophy (3.5-fold increase in myocyte area). This increase was followed by progressive heart failure with functional and histological deficits typical for humans with heart failure. Contractility was reduced by approximately 50% in 35-week-old mice, and ejection fraction was reduced down to a minimum of approximately 20%. We conclude that overexpression of beta1-adrenergic receptors in the heart may lead to a short-lived improvement of cardiac function, but that increased beta1-adrenergic receptor signalling is ultimately detrimental.  (+info)

Potent and selective human beta(3)-adrenergic receptor antagonists. (5/608)

Although the functional presence of beta(3)-adrenergic receptors (beta(3)-AR) in rodents is well established, its significance in human adipose tissue has been controversial. One of the issues confounding the experimental data has been the lack of potent and selective human beta(3)-AR ligands analogous to the rodent-specific agonist BRL37344. Recently, we described a new class of aryloxypropanolamine beta(3)-AR agonists that potently and selectively activate lipolysis in rhesus isolated adipocytes and stimulate the metabolic rate in rhesus monkeys in vivo. In this article, we describe novel and selective beta(3)-AR antagonists with high affinity for the human receptor. L-748,328 and L-748,337 bind the human cloned beta(3)-AR expressed in Chinese hamster ovary (CHO) cells with an affinity of 3.7 +/- 1.4 and 4.0 +/- 0.4 nM, respectively. They display an affinity of 467 +/- 89 and 390 +/- 154 nM for the human beta(1)-AR. Their selectivity for human beta(3)-AR versus beta(2)-AR is greater than 20-fold (99 +/- 43 nM) and 45-fold (204 +/- 75 nM), respectively. These compounds are competitive antagonists capable of inhibiting the functional activation of agonists in a dose-dependent manner in cells expressing human cloned beta(3)-AR. Moreover, both L-748,328 and L-748,337 inhibit the lipolytic response elicited by the beta(3)-AR agonist L-742,791 in isolated nonhuman primate adipocytes. The aryloxypropanolamine benzenesulfonamide ligands illustrated here and elsewhere demonstrate high-affinity human beta(3)-AR binding. In addition, we describe specific 3'-phenoxy substitutions that transform these compounds from potent agonists into selective antagonists.  (+info)

Inducible cyclic AMP early repressor protein in rat pinealocytes: a highly sensitive natural reporter for regulated gene transcription. (6/608)

Rhythmic activity of arylalkylamine N-acetyltransferase (AANAT) determines melatonin synthesis in rat pineal gland. The transcriptional regulation of AANAT involves the activating and inhibiting transcription factors of the cyclic AMP (cAMP)-signaling pathway, cAMP response element-binding protein and inducible cAMP early repressor (ICER), respectively. Activation of this pathway is centered around norepinephrine, stimulating beta(1)-adrenergic receptors, but various other transmitters can modulate melatonin biosynthesis. To compare the transcriptional impact of norepinephrine with that of other neurotransmitters on melatonin synthesis, we determined ICER protein levels in pinealocytes and, in parallel, hormone secretion. The dose-dependent inductions of ICER protein by norepinephrine, the beta(1)-adrenergic receptor agonist isoproterenol, vasoactive intestinal peptide, pituitary adenylate cyclase-activating polypeptide, and adenosine are correlated to regulatory dynamics in melatonin production. Importantly, ICER protein induction required lower ligand concentrations than the induction of melatonin biosynthesis. Although neuropeptide Y, glutamate, and vasopressin altered norepinephrine-stimulated hormone production without affecting ICER levels, the activation of voltage-gated cation channels increased ICER without affecting hormone synthesis. Sensitivity and versatility of ICER induction in pinealocytes make these neuroendocrine cells a valuable model system in which to study molecular interactions determining a regulated gene expression.  (+info)

Inverse agonist activities of beta-adrenoceptor antagonists in rat myocardium. (7/608)

1. Negative inotropic effects of several beta-adrenoceptor (betaAR) antagonists on electrically-stimulated right atria, left atria, right ventricles and left ventricular papillary muscles from reserpine-treated rats were used as a measure of their inverse agonist activities. 2. Beta1AR antagonists acebutolol, atenolol and metoprolol, beta2AR antagonist ICI-181,551 and nonselective betaAR antagonists alprenolol, nadolol, propranolol and timolol produced negative inotropic effects, which were most marked on the right atria. 3. The nonselective betaAR antagonist pindolol did not exhibit inverse agonist activity but inhibited the negative inotropic activities of ICI-118,551, atenolol and propranolol. 4. The negative inotropic effects of lidocaine, nifedipine and pentobarbitone were similar on all the four myocardial preparations. 5. The positive inotropic efficacy of salbutamol on right and left atria but not on right ventricles and papillary muscles was comparable to that of isoprenaline. The antagonist activity of ICI-118,551 against isoprenaline was greater on right atria than on other cardiac regions. 6. Beta1AR proteins were expressed in all regions of the heart but of beta2AR were primarily localized in the right atrium. 7. It is concluded that beta2AR play a greater role in right atria than in other cardiac regions and almost all betaAR antagonists behave as inverse agonists.  (+info)

Characterization of beta-adrenoceptor mediated smooth muscle relaxation and the detection of mRNA for beta1-, beta2- and beta3-adrenoceptors in rat ileum. (8/608)

1. Functional and molecular approaches were used to characterize the beta-AR subtypes mediating relaxation of rat ileal smooth muscle. 2. In functional studies, (-)-isoprenaline relaxation was unchanged by CGP20712A (beta1-AR antagonist) or ICI118551 (beta2-AR antagonist) but shifted by propranolol (pKB=6.69). (+/-)-Cyanopindolol, CGP12177 and ICID7114 did not cause relaxation but antagonized (-)-isoprenaline relaxation. 3. BRL37344 (beta3-AR agonist) caused biphasic relaxation. The high affinity component was shifted with low affinity by propranolol, (+/-)-cyanopindolol, tertatolol and alprenolol. CL316243 (beta3-AR agonist) relaxation was unaffected by CGP20712A or ICI118551 but blocked by SR58894A (beta3-AR antagonist; pA2 = 7.80). Enhanced relaxation after exposure to forskolin and pertussis toxin showed that beta3-AR relaxation can be altered by manipulation of components of the adenylate cyclase signalling pathway. 4. The beta-AR agonist RO363 relaxed the ileum (pEC50=6.18) and was blocked by CGP20712A. Relaxation by the beta2-AR agonist zinterol (pEC50=5.71) was blocked by SR58894A but not by ICI118551. 5. In rat ileum, beta1-, beta2- and beta3-AR mRNA was detected. Comparison of tissues showed that beta3-AR mRNA expression was greatest in WAT>colon=ileum >cerebral cortex>soleus; beta1-AR mRNA was most abundant in cerebral cortex > WAT > ileum = colon > soleus; beta2-AR mRNA was expressed in soleus > WAT > ileum = colon > cerebral cortex. 6. These results show that beta3-ARs are the predominant beta-AR subtype mediating rat ileal relaxation while beta1-ARs may produce a small relaxation. The beta2-AR agonist zinterol produces relaxation through beta3-ARs and there was no evidence for the involvement of beta2-ARs in relaxation despite the detection of beta2-AR mRNA.  (+info)

We11,12 and others13-15 have shown that βAR stimulation in cardiac myocytes results in apoptosis that is mediated by ROS-dependent activation of JNK and the mitochondrial death pathway.16 This study demonstrates that βAR-stimulated JNK activation and apoptosis in ARVMs require Rac1. We further show for the first time that statins inhibit βAR-stimulated JNK activation and apoptosis and that these effects are due to inhibition of βAR-stimulated Rac1 activation.. A new finding of this study is that βAR stimulation causes Rac1 activation. Furthermore, adenoviral overexpression of the N17Rac1 dominant-negative mutant inhibited βAR-stimulated apoptosis and 3 known steps in the signaling pathway leading to βAR-stimulated apoptosis: JNK activation, cytochrome C release, and caspase-3 activation. Thus, in cardiac myocytes, βAR stimulation couples to Rac1 activation, which is upstream of JNK in the mitochondrial death pathway and necessary for βAR-stimulated apoptosis.. Little is known about the ...
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TY - JOUR. T1 - Expression of β3‐adrenoceptor mRNA in rat brain. AU - Summers, R. J.. AU - Papaioannou, M.. AU - Harris, S.. AU - Evans, B. A.. PY - 1995/1/1. Y1 - 1995/1/1. N2 - The reverse transcription/polymerase chain reaction was used to demonstrate β3‐adrenoceptor mRNA in rat brain regions. Levels were highest in hippocampus, cerebral cortex and striatum and lower in hypothalamus, brainstem and cerebellum. 1995 British Pharmacological Society. AB - The reverse transcription/polymerase chain reaction was used to demonstrate β3‐adrenoceptor mRNA in rat brain regions. Levels were highest in hippocampus, cerebral cortex and striatum and lower in hypothalamus, brainstem and cerebellum. 1995 British Pharmacological Society. KW - polymerase chain reaction. KW - rat brain. KW - β ‐Adrenoceptor. UR - U2 - 10.1111/j.1476-5381.1995.tb17205.x. DO - 10.1111/j.1476-5381.1995.tb17205.x. M3 - Article. C2 - ...
Genomics has significantly improved our understanding of chronic obstructive pulmonary disease (COPD) over the past decade. Genome-wide association studies have identified a number of genetic variants associated with lung function and susceptibility to COPD,1 2 and have helped explain why only some smokers develop COPD and why never-smokers can also be affected by the disease. Once COPD is diagnosed, reducing the burden of respiratory exacerbations is a clinical priority because these events are associated with accelerated lung function decline3 and increased mortality.4 However, not all patients with COPD experience exacerbations.5 6 Therefore, identifying individuals at increased risk of exacerbations may help target management and improve outcomes. Beyond the susceptibility to COPD, genomics may also help inform the morbidity of COPD. A previously reported twin study suggests that more than 60% of the risk of severe COPD exacerbations can be attributed to genetic factors.7 Among those, ...
Adrenergic receptors are cell‐surface receptors for two major catecholamine hormones and neurotransmitters that regulate key physiological responses, including cardiovascular and pulmonary functions
alpha 2a Adrenergic Receptor兔多克隆抗体(ab92650)可与小鼠, 大鼠, 人样本反应并经IHC实验严格验证。所有产品均提供质保服务,中国75%以上现货。
Heart failure remains one of the most highly prevalent and costly syndromes that leads to morbidity and mortality in the United States and increasingly around t...
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alpha 1 Adrenergic Receptor ELISA Kits für viele Reaktivitäten. Huhn, Rind (Kuh), Hund und weitere. alpha 1 Adrenergic Receptor ELISA Kits vergleichen und bestellen.
alpha 2C Adrenergic Receptor兔多克隆抗体(ab123368)可与人样本反应并经WB实验严格验证。所有产品均提供质保服务,中国75%以上现货。
Background: Genetic variation in the β2 (ADRB2) and β3 (ADRB3) adrenergic receptor genes are associated with obesity and insulin resistance. To further elucidate the role of these genes in the pathophysiology of obesity ...
Goat polyclonal beta 1 Adrenergic Receptor antibody validated for WB, IHC and tested in Human and Rat. Referenced in 4 publications and 2 independent reviews…
Can you pick the Adrenergic Receptor Blockers Test your knowledge on this science quiz to see how you do and compare your score to others. Quiz by poorvichhabra
Some biologically plausible mechanisms may explain the p53-AAbs possibly immediate or oblique protecting partMCE Chemical SB-220453 in ovarian most cancers.
Gene-based approach:Empirical P-value = 0.003(EAAO versus HC); Empirical P-value = 0.81(LAAO versus HC); ADRB2 (beta-2adrenoreceptor) gene region that is specifically associated with the early onset form of BD ...
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Background: Although endothelial cell protein C receptor (EPCR) gene Ser219Gly polymorphism has been associated with venous thromboembolism (VTE) susceptibility, no clear consensus has yet been reached. Objective and methods: A meta-analysis of 9,494 subjects from 13 individual studies was conducted to better elucidate the potential relationship between the EPCR gene Ser219Gly polymorphism and VTE. Pooled odds ratios (ORs) and their corresponding 95% confidence intervals (CIs) were evaluated by using fixed or random effect models.Results: The current meta-analysis suggested that there was a significant association between EPCR gene Ser219Gly polymorphism and VTE under allelic (OR: 1.42, 95% CI: 1.21-1.66, P=1.30×10-5), recessive (OR: 2.02, 95% CI: 1.44-2.85, P=5.35×10-5), homozygous (OR: 2.24, 95% CI: 1.59-3.16, P=3.66×10-6), and additive genetic models (OR: 1.63, 95% CI: 1.30-2.04, P=2.24×10-5). Conclusions: EPCR gene Ser219Gly polymorphism was associated with an elevated risk of VTE and the Gly
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TY - JOUR. T1 - b1-Adrenoceptors compensate for b3-adrenoceptors in ileum from b3-adrenoceptor knock-out mice. AU - Hutchinson, Dana Sabine. AU - Evans, Bronwyn A. AU - Summers, Roger J. PY - 2001. Y1 - 2001. M3 - Article. VL - 132. SP - 433. EP - 442. JO - British Journal of Pharmacology. JF - British Journal of Pharmacology. SN - 1476-5381. IS - 2. ER - ...
Results of a new study led by Johns Hopkins researchers offer new evidence for a strong link between angiotensin receptor autoantibodies and increased risk of frailty.
The Paper, Which Describes Pharmacogenetic Enhancement of Effectiveness for Prevention of Atrial Flutter, Was Also Published in the Journal of Cardiac Failure. Westminster, CO, September 9, 2015 - ARCA biopharma, Inc. (Nasdaq: ABIO), a biopharmaceutical company developing genetically-targeted therapies for cardiovascular diseases, today announced that the paper Bucindolol Prevents Atrial Flutter via the Beta-1 389 Arg/Gly Adrenergic Receptor Polymorphism will be presented at the 19th annual Scientific Meeting of the Heart Failure Society of America (HFSA) to be held in Washington, D.C. September 26-29, 2015. The paper was recently published in the Journal of Cardiac Failure, the official journal of the Heart Failure Society of America and the Japanese Heart Failure Society. The lead author on the paper is cardiologist-electrophysiologist Ryan G. Aleong of the University of Colorado, Anschutz Medical Campus, and a co-author on the ...
Background: Neuraxial blockade is used as primary anesthetic technique in one third of surgical procedures. The authors tested whether bisoprolol would protect patients at risk for cardiovascular complications undergoing surgery with spinal block. Methods: The authors performed a double-blinded, placebo-controlled, multicenter trial to compare the effect of bisoprolol with that of placebo on 1-yr composite outcome including cardiovascular mortality, nonfatal myocardial infarction, unstable angina, congestive heart failure, and cerebrovascular insult. Bisoprolol was given orally before and after surgery for a maximum of 10 days. Adrenergic receptor polymorphisms and safety outcome measures of bisoprolol therapy were also determined. Results: A total of 224 patients were enrolled. Spinal block could not be established in 5 patients. One hundred ten patients were assigned to the bisoprolol group, and 109 patients were assigned to the placebo group. The mean duration of treatment was 4.9 days in the ...
Adrenergic receptor trafficking is an active physiological process where adrenergic receptors are relocated from one region of the cell to another or from one type of cell to another. Discover the latest research on adrenergic receptor trafficking here. ...
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Data from the Clinical Study BEST Indicate That in the Study Norepinephrine Lowering and Clinical Therapeutic Responses to Bucindolol Were Strongly Influenced b
BioAssay record AID 288801 submitted by ChEMBL: Displacement of [3H]CGP12177 from human beta-2 adrenergic receptor expressed in HEK293 cells.
This study assessed the role of adrenergic receptors on the regulation of the uptake of L-dopa and the production of dopamine by… Expand ...
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Mechanism of Action In vitro studies and in vivo pharmacologic studies have demonstrated that albuterol has a preferential effect on beta2-adrenergic receptors compared with isoproterenol. While it is recognized that beta2-adrenergic receptors are the predominant receptors on bronchial smooth muscle, data indicate that there is a population of beta2-receptors in the human heart existing in a concentration between 10% and 50% of cardiac beta-adrenergic receptors. The precise function of these receptors has not been established. (See WARNINGS, Cardiovascular Effects section.). Activation of beta2-adrenergic receptors on airway smooth muscle leads to the activation of adenylcyclase and to an increase in the intracellular concentration of cyclic-3,5-adenosine monophosphate (cyclic AMP). This increase of cyclic AMP leads to the activation of protein kinase A, which inhibits the phosphorylation of myosin and lowers intracellular ionic calcium concentrations, resulting in relaxation. Albuterol ...
Looking for online definition of Alpha adrenergic receptor in the Medical Dictionary? Alpha adrenergic receptor explanation free. What is Alpha adrenergic receptor? Meaning of Alpha adrenergic receptor medical term. What does Alpha adrenergic receptor mean?
The aim of the present study was to evaluate the efficacy and β2-adrenoceptor (AR) selectivity of KUR-1246, a new uterine relaxant. Inhibition of spontaneous or drug-induced uterine contractions by KUR-1246 was evaluated in pregnant rats and rabbits by an organ bath method or by a balloon method. The selectivity of KUR-1246 was assessed simultaneously in organs isolated from late-pregnant rats. The affinity of KUR-1246 for human β1-, β2-, and β3-ARs was determined using two radioligands. KUR-1246 suppressed both spontaneous and drug-induced contractions in isolated uteri, the rank order of potency being isoproterenol , KUR-1246 , terbutaline , ritodrine. ICI-118551 (selective β2-AR antagonist) competitively antagonized the KUR-1246-induced inhibition of spontaneous uterine contractions, but CGP-20712A (selective β1-AR antagonist) and SR-58894A (selective β3-AR antagonist) did not. All β-AR agonists tested produced significant inhibition of spontaneous uterine contractions in vivo: ED30 ...
Adrenergic receptors are a class of G protein-coupled receptors. They are the targets for epinephrine and norepinephrine and thus represent a critical component in the sympathetic nervous system for maintenance of homeostasis and response to disease. Adrenergic receptors carry out signaling via coupling to guanine nucleotide binding proteins (G-proteins).
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The ß-adrenergic receptors are linked to G proteins. The ß-receptor has three known subtypes. Beta-1 receptors primarily regulate myocardial tissue and affect the rate of contraction via impulse conduction. Beta-2 receptors regulate smooth muscle tone and influence vascular and bronchiolar rela...
Synonyms for ADRB2 in Free Thesaurus. Antonyms for ADRB2. 175 synonyms for bar: public house, pub, counter, inn, local, lounge, saloon, tavern, canteen, watering hole, boozer, roadhouse, hostelry, alehouse, taproom.... What are synonyms for ADRB2?
Lack of Association of the Trp64Arg Polymorphism of β_3-Adrenergic Receptor Gene with Energy Expenditure in Response to Caffeine Among Young Healthy Women (2008 ...
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In vitro studies and in vivo pharmacologic studies have demonstrated that albuterol has a preferential effect on beta2-adrenergic receptors compared with isoproterenol. While it is recognized that beta2-adrenergic receptors are the predominant receptors in bronchial smooth muscle, data indicate that there is a population of beta2-receptors in the human heart existing in a concentration between 10% and 50%. The precise function of these receptors has not been established (see WARNINGS).. The pharmacologic effects of beta-adrenergic agonist drugs, including albuterol, are at least in part attributable to stimulation through beta-adrenergic receptors of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3,5-adenosine monophosphate (cyclic AMP). Increased cyclic AMP levels are associated with relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast ...
A non‐invasive intrinsic fluorescence sensing of the early stages of Alzheimers beta amyloid peptide aggregation in the presence of copper ions is reported. By using time‐resolved fluorescence techniques the formation of beta amyloid‐copper complexes and the accelerated peptide aggregation are demonstrated. The shifts in the emission spectral peaks indicate that the peptides exhibit different aggregation pathways than in the absence of copper.. ...
Summary Beta-1 adrenergic receptors are G-protein coupled receptors associated with a Gs protein subunit. Activation of the Gs subunit increases cAMP and PKA levels, leading to the phosphorylation of various intracellular proteins. Beta-1 receptors are primarily located on the heart, where their signalling causes increased heart rate and contractility. The other main function of beta-1 receptors is renin release at the kidney. Pharmacologically, beta-1 antagonists are important in the chronic management of high blood pressure and heart failure, while beta-1 agonists treat shock and decompensated heart failure in the acute setting. Key Points - Beta-1 ReceptorsSignalingUse the Gs signaling pathwayOutcomesIncreased heart rate / contractilityIncreased renin releaseIncreased lipolysis (lower yield) - SignalingUse the Gs signaling pathway - Use the Gs signaling pathway - OutcomesIncreased heart rate / contractilityIncreased renin releaseIncreased lipolysis (lower yield) - Increased heart rate /
The β2-AR is a major lipolytic receptor in human fat cells. With the notion that the β2-AR polymorphisms might play a role in obesity, Large et al. (1997)genotyped 140 women with a large variation in body fat mass. The Glu27 homozygotes had an average fat mass excess of 20 kg (Large et al., 1997, Table 1). Neither allele at the Arg16Gly polymorphism was linked to obesity. An investigation of obese men did not give a similar result (Hellstrom et al., 1999). These findings in women will probably stimulate further work and may be applied to the known interethnic variability in obesity.. The codon 164 threonine/isoleucine polymorphism of β2-AR has not received much attention in humans because of the comparative rarity of the less frequent (isoleucine) allele. To investigate the functional significance of this polymorphism in the myocardium, Turki et al. (1996) prepared transgenic mice expressing 45 times the normal endogenous β2-AR. Mice with the mutant 164 Ile and mice with the wild-type ...
Dr. Lee E. Limbird Limbirds research evaluates the structure and function of alpha2-adrenergic receptors and the mechanisms by which they influence multiple physiological functions. Alpha2-adrenergic receptors are molecules on the cell surface that bind the hormones epinephrine or norepinephrine and evoke such physiological functions as the regulation of hormone and neurotransmitter release, platelet aggregation and secretion, vascular contractility, and smooth muscle tone. Limbird and her colleagues are also examining the mechanisms by which alpha2-adrenergic receptors achieve their delivery to specialized domains on the surface of target cells. Limbird earned an undergraduate degree in chemistry from the College of Wooster in Wooster, Ohio, in 1970. She received a Ph.D. in biochemistry from the University of North Carolina, Chapel Hill, in 1973. Before moving to Vanderbilt, Limbird was a member of the departments of medicine and biochemistry at Duke University. From 1979 to 1985 she rose ...
Concentration of β-adrenergic receptor from small antral (SA), preovulatory (PO) and cystic follicular wall. The β-receptor concentration is expressed as fmol
What is ADRA2A? ADRA2A, located on chromosome 10, encodes the α-2A adrenergic receptor, a norepinephrine receptor that is the primary site of action for α-2A agonists. The α-2A adrenergic receptor…. ...
DI-fusion, le Dépôt institutionnel numérique de lULB, est loutil de référencementde la production scientifique de lULB.Linterface de recherche DI-fusion permet de consulter les publications des chercheurs de lULB et les thèses qui y ont été défendues.
The present study was carried out to determine, first, the cardiac beta -adrenergic receptor characteristics of normal chickens and chickens with heart failure and, second, the characteristics of myocardial beta -adrenergic receptors in non-hypertrophied hearts in broilers exposed to two different altitude and temperature programmes. The density of beta -adrenergic receptors was significantly lower in myocardial cells in right ventricular failure birds compared with healthy birds. The binding capacity of beta -adrenergic receptors was reduced in the non-hypertrophied ventricles after exposure to high altitude in the younger but not in older chickens. At both altitudes, beta -adrenergic receptor binding capacity was not significantly different in low temperature compared with normal temperature birds. These data support the hypothesis of beta -adrenergic receptor downregulation as one of the mechanisms of cardiac cell adaptation to hypertrophy or hypoxia. Second, the acclimatization to high ...
Both beta(1)- and beta(2)-adrenergic receptors (beta(1)- and beta(2)-AR) have important roles in heart function mainly in response to catecholamines. Some specific polymorphisms in the beta(1)- and beta(2)-AR genes, named ADRB1 and ADRB2, respectively, have been implicated in several cardiovascular and noncardiovascular phenotypes. In this study, we aimed to investigate the possible relationship between Ser49Gly and Arg389Gly polymorphisms of the ADRB1 and Arg16Gly and Gln27Glu polymorphisms of the ADRB2 gene with ST elevation myocardial infarction (MI) in a Turkish population. One hundred patients with ST elevation MI and 100 healthy control subjects were genotyped using the PCR-RFLP method. Although the Arg389 allele of the ADRB1 gene was associated with an elevated risk of MI, the Glu27 allele of the ADRB2 gene was associated with a decreased risk of MI. Carriers of the ADRB1 Arg389 allele (heterozygotes + homozygotes) had an approximately 3.5-fold increased risk for MI than Gly389 ...
In this paper, we have used the β-adrenoceptor agonist isoproterenol for all the in vivo and in vitro studies. We have extensively shown (Chernogubova et al., 2004, 2005; Hutchinson and Bengtsson, 2006; Dallner et al., 2006) that the β3-adrenoceptor is the only β-adrenoceptor subtype that increases glucose uptake via increased de novo synthesis of GLUT1 in brown adipocytes from wild-type mice in vitro through the use of specific agonists and antagonists (Chernogubova et al., 2004, 2005; Dallner et al., 2006). The exception occurs in β3-adrenoceptor knockout mice, where there is compensation by both the α1- and β1-adrenoceptors that is not evident in cultures derived from wild-type mice (Chernogubova et al., 2005). Hence we strongly believe that the effects of isoproterenol in vitro are due solely to activation of β3-adrenoceptors. With respect to glucose uptake in vivo, isoproterenol is still effective in promoting glucose uptake into BAT in β1β2-adrenoceptor knockout mice (Fig. 4 A), ...
Adverse drug reactions associated with the use of beta blockers include: nausea, diarrhea, bronchospasm, dyspnea, cold extremities, exacerbation of Raynauds syndrome, bradycardia, hypotension, heart failure, heart block, fatigue, dizziness, alopecia (hair loss), abnormal vision, hallucinations, insomnia, nightmares, sexual dysfunction, erectile dysfunction and/or alteration of glucose and lipid metabolism. Mixed α1/β-antagonist therapy is also commonly associated with orthostatic hypotension. Carvedilol therapy is commonly associated with edema.[44] Due to the high penetration across the blood-brain barrier, lipophilic beta blockers, such as propranolol and metoprolol, are more likely than other less lipophilic beta blockers to cause sleep disturbances, such as insomnia, vivid dreams and nightmares.[45] Adverse effects associated with β2-adrenergic receptor antagonist activity (bronchospasm, peripheral vasoconstriction, alteration of glucose and lipid metabolism) are less common with ...
beta-1 Adrenergic Receptors: A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The adrenergic beta-1 receptors are equally sensitive to EPINEPHRINE and NOREPINEPHRINE and bind the agonist DOBUTAMINE and the antagonist METOPROLOL with high affinity. They are found in the HEART, juxtaglomerular cells, and in the central and peripheral nervous systems.
TY - JOUR. T1 - β-arrestin-biased agonism of β-adrenergic receptor regulates Dicer-mediated microRNA maturation to promote cardioprotective signaling. AU - Teoh, Jian Peng. AU - Bayoumi, Ahmed S.. AU - Aonuma, Tatsuya. AU - Xu, Yanyan. AU - Johnson, John A.. AU - Su, Huabo. AU - Weintraub, Neal L.. AU - Tang, Yaoliang. AU - Kim, Il Man. PY - 2018/5. Y1 - 2018/5. N2 - Rationale: MicroRNAs (miRs) are small, non-coding RNAs that function to post-transcriptionally regulate target genes. First transcribed as primary miR transcripts (pri-miRs), they are enzymatically processed by Drosha into premature miRs (pre-miRs) and further cleaved by Dicer into mature miRs. Initially discovered to desensitize β-adrenergic receptor (βAR) signaling, β-arrestins are now well-appreciated to modulate multiple pathways independent of G protein signaling, a concept known as biased signaling. Using the β-arrestin-biased βAR ligand carvedilol, we previously showed that β-arrestin1 (not β-arrestin2)-biased β1AR ...
Stimulation of beta2-adrenergic receptors on the cell surface by adrenaline or noradrenaline leads to alterations in the metabolism, excitability, differentiation and growth of many cell types. These effects have traditionally been thought to be mediated exclusively by receptor activation of intrace …
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Background: β1-adrenergic receptor blockers are an important drugs recommended as first-line treatment of Heart Failure (HF) as they improve survival in left ventric..
The mechanisms of desensitization and resensitization of the dopamine D1 receptor are not well understood. Although the high homology of the D1 receptor with the β2-adrenergic receptor might indicate that similar mechanisms regulate the responsiveness of the receptors, even subtypes of β-adrenergic receptors differ substantially in this respect (Shiina et al., 2000). For β-adrenergic receptors, a distinction has been made between desensitization that is homologous (resulting from stimulation of the same receptor) or heterologous (resulting from stimulation of a different receptor subtype, or nonreceptor-mediated activation of a second messenger) (Harden, 1983). A mechanism for heterologous desensitization is phosphorylation of the receptor by PKA (Clark et al., 1989; Hausdorff et al., 1989), whereas homologous desensitization of the β2-adrenergic receptor involves phosphorylation of the agonist-occupied receptor by both GRK (Benovic et al., 1986) and PKA (Post et al., 1996; Moffett et al., ...
BioAssay record AID 36627 submitted by ChEMBL: Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells.
Wei, W.,Ming, X.,Yi, Z. Y.,et al. Autoimmunity Mediated Down-regulation Of B 2-adrenergic Receptor In COPD[J]. AMERICAN JOURNAL OF RESPIRATORY AND CRITICAL CARE MEDICINE,2010,181 ...
ADRB3, the β3-adrenergic receptor, has been connected to obesity and metabolic conditions. The Trp64Arg variant is a susceptibility gene polymorphism for T2D. [PMID 24972470] ...
Reaktivität: Hund, Meerschweinchen, Human and more. 48 verschiedene ADRB1 Antikörper vergleichen. Alle direkt auf antikörper-online bestellbar!
Purpose: Propranolol, a non-selective β-adrenergic receptor blocker, has been used for the treatment of the patients with hypertension for more than 50 years. There are several in vitro and in vivo evidences that β-adrenergic ...
... is a beta adrenergic receptor antagonist. Ban, T; Sada, S; Takahashi, Y; Sada, H; Fujita, T (1985). "Effects of para- ... Beta blockers, Carbamates, N-isopropyl-phenoxypropanolamines, Methyl esters, All stub articles, Cardiovascular system drug ... substituted beta-adrenoceptor blocking agents and methyl-substituted phenoxypropanolamine derivatives on maximum upstroke ... 329 (1): 77-85. doi:10.1007/bf00695196. PMID 2582279. S2CID 6067337. v t e (Articles without EBI source, Articles without KEGG ...
Implications for beta2-adrenergic receptor regulation". The Journal of Biological Chemistry. 274 (16): 10677-80. doi:10.1074/ ... "The AMPA receptor GluR2 C terminus can mediate a reversible, ATP-dependent interaction with NSF and alpha- and beta-SNAPs". ... Another neuronal role for NSF is indicated by its direct binding to the GluR2 subunit of AMPA type glutamate receptors (which ... McDonald PH, Cote NL, Lin FT, Premont RT, Pitcher JA, Lefkowitz RJ (Apr 1999). "Identification of NSF as a beta-arrestin1- ...
... dopamine mainly triggers dopamine receptors and β1-adrenergic receptors while at high doses it works via α-adrenergic receptors ... Dopamine binds to beta-1, beta-2, alpha-1 and dopaminergic receptors. Portal: Medicine (CS1: long volume value, Articles with ... and β2 adrenergic receptors. Cruickshank, Laura; Kennedy, Alan R.; Shankland, Norman (2013). "Tautomeric and ionisation forms ... Mediated through myocardial beta-1 adrenergic receptors, dopamine increase heart rate and force, thereby increasing cardiac ...
... is a beta-adrenergic receptor inhibitor (beta blocker). It is indicated for intraocular pressure reduction in ... Levobetaxolol inhibits the beta-1-adrenergic receptor. When applied topically, it reduces intra-ocular pressure (IOP) by 16-23 ... Levobetaxolol has fewer cardiovascular side effects than other beta blockers. Levobetaxolol should not be used by people who ... Beta blockers, N-isopropyl-phenoxypropanolamines, Enantiopure drugs, Isopropyl compounds, Cyclopropanes). ...
... a new beta adrenergic receptor probe". Journal of Cyclic Nucleotide Research. 7 (1): 13-26. PMID 6265511. v t e (Articles ... Iodopindolol is a beta-adrenergic selective antagonist tagged with radioactive iodine-125. It has been used to map beta ... Beta blockers, Radiopharmaceuticals, Organoiodides, Isopropyl compounds, N-isopropyl-phenoxypropanolamines, Indoles, All stub ... receptors in cellular experiments. Pindolol Ezrailson EG, Garber AJ, Munson PJ, Swartz TL, Birnbaumer L, Entman ML (1981). "[ ...
Métrich M, Lucas A, Gastineau M, Samuel JL, Heymes C, Morel E, Lezoualc'h F (Apr 2008). "Epac mediates beta-adrenergic receptor ... In heart, chronic stimulation of β-adrenergic receptor is known to progress to arrhythmia through an Epac2-dependent mechanism ... and is involved in the development of hypertrophic events by chronic cAMP stimulation through β-adrenergic receptors. In ... ryanodine receptor, and IP3 receptor. In neurons, Epac is involved in neurotransmitter release in glutamatergic synapses from ...
Williams, L. T.; Snyderman, R.; Lefkowitz, R. J. (1976-01-01). "Identification of beta-adrenergic receptors in human ... Williams, L T; Snyderman, R; Pike, M C; Lefkowitz, R J (1977-03-01). "Specific receptor sites for chemotactic peptides on human ... 1 (6): 521-525. doi:10.1128/IAI.1.6.521-525.1970. PMC 415936. PMID 16557770. Snyderman, R.; Goetzl, E. J. (1981-08-21). " ... 57 (1): 149-155. doi:10.1172/JCI108254. PMC 436634. PMID 1245597. Snyderman, Ralph; Phillips, Jean; Mergenhagen, Stephan E. ( ...
... is a short-acting beta adrenergic receptor antagonist. Acylation of glycidol (2) with the acid chloride 1 produces ... beta.-blockers with ultrashort duration of action". Journal of Medicinal Chemistry. 27 (8): 1007. doi:10.1021/jm00374a013. PMID ... Beta blockers, Fluoroarenes, Benzoate esters, Ureas, All stub articles, Cardiovascular system drug stubs). ... 1-dimethylethylenediamine with urea, gives flestolol (5). Quon, CY; Stampfli, HF (1993). "Biochemical characterization of ...
Schindler, C; Dobrev, D; Grossmann, M; Francke, K; Pittrow, D; Kirch, W (January 2004). "Mechanisms of beta-adrenergic receptor ... Some sympathetic stimulation of arterioles in skeletal muscle is mediated by epinephrine acting on β-adrenergic receptors of ... The vasodilating action of activation of beta-2 receptors (such as by adrenaline) appears to be endothelium-independent. ... Angiotensin II receptor blockers ACE inhibitors Calcium channel blockers Drugs that appear to work by activating the α2A ...
"Identification of adenylate cyclase-coupled beta-adrenergic receptors with radiolabeled beta-adrenergic antagonists". ... NRGs bind to the ERBB receptors to promote phosphorylation of specific tyrosine residues on the C-terminal link of the receptor ... Neuregulins are ligands of the ERBB-family receptors, while NRG1 and NRG2 are able to bind and activate both ERBB3 and ERBB4, ... NRGs bind to the ERBB3 and ERBB4 tyrosine kinase receptors; they then form homodimers or heterodimers, often consisting of ...
"Identification of adenylate cyclase-coupled beta-adrenergic receptors with radiolabeled beta-adrenergic antagonists". ... 78 (1): B37-B47. Bibcode:2013Geop...78B..37W. doi:10.1190/geo2011-0061.1. ISSN 0016-8033. Lefkowitz, R. J. (1975-09-15). " ... 13 (1): 2-3. Bibcode:2020NatGe..13....2D. doi:10.1038/s41561-019-0519-z. ISSN 1752-0894. S2CID 209380663. Akamatsu, N.; ... doi:10.1016/0006-2952(75)90013-1. ISSN 0006-2952. PMID 15. Eisner, Leo; Williams-Stroud, Sherilyn; Hill, Andrew; Duncan, Peter ...
... its humoral mediators and alpha-beta adrenergic receptors". Chest. 71 (2 suppl): 249-251. doi:10.1378/chest.71.2_Supplement.249 ... such as transient receptor potential canonical 6 (TRPC6) channels, and transient receptor potential vanilloid 4 (TRPV4) ... "Classical transient receptor potential channel 6 (TRPC6) is essential for hypoxic pulmonary vasoconstriction and alveolar gas ... 262 (4 Pt 1): C882-890. doi:10.1152/ajpcell.1992.262.4.C882. ISSN 0002-9513. PMID 1566816. Yuan, X. J.; Goldman, W. F.; Tod, M ...
"Excitatory alpha1-adrenergic receptors predominate over inhibitory beta-receptors in rabbit dorsal detrusor". The Journal of ... Their substrates are, e.g., MARCKS proteins, MAP kinase, transcription factor inhibitor IκB, the vitamin D3 receptor VDR, Raf ... Upon activation, protein kinase C enzymes are translocated to the plasma membrane by RACK proteins (membrane-bound receptor for ... Anderson PW, McGill JB, Tuttle KR (Sep 2007). "Protein kinase C beta inhibition: the promise for treatment of diabetic ...
Bylund DB, Snyder SH (1976). "Beta adrenergic receptor binding in membrane preparations from mammalian brain". Mol. Pharmacol. ... Wander TJ, Nelson A, Okazaki H, Richelson E (1986). "Antagonism by antidepressants of serotonin S1 and S2 receptors of normal ... ISBN 0-89603-121-7. Tran VT, Chang RS, Snyder SH (1978). "Histamine H1 receptors identified in mammalian brain membranes with [ ... Richelson E, Nelson A (1984). "Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro". J. ...
Different studies have indicated that adrenocortical carcinoma have beta-adrenergic receptor-binding sites that are not usually ... Bylund DB, Snyder SH (July 1976). "Beta adrenergic receptor binding in membrane preparations from mammalian brain". Molecular ... Williams LT, Gore TB, Lefkowitz RJ (February 1977). "Ectopic beta-adrenergic receptor binding sites. possible molecular basis ... which is used to label beta-adrenergic receptors for isolation. It has a XLogP3 value of 3.4. Its hydrogen bond donor count is ...
Bylund DB, Snyder SH (1976). "Beta adrenergic receptor binding in membrane preparations from mammalian brain". Mol. Pharmacol. ... It is now thought that changes occur in receptor sensitivity in the cerebral cortex and hippocampus. The hippocampus is part of ... Wander TJ, Nelson A, Okazaki H, Richelson E (1986). "Antagonism by antidepressants of serotonin S1 and S2 receptors of normal ... Richelson E, Nelson A (1984). "Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro". J. ...
It works by binding to the β1 adrenergic receptor. It is a 3rd generation adrenergic β receptor partial agonist. It provides ... Marlow HF (1989). "Xamoterol, a beta 1-adrenoceptor partial agonist: review of the clinical efficacy in heart failure". British ... Beta1-adrenergic agonists, Cardiac stimulants, Inotropic agents, Morpholines, Phenol ethers, Phenols, All stub articles, ... 28 Suppl 1: 23S-30S. doi:10.1111/j.1365-2125.1989.tb03570.x. PMC 1379873. PMID 2572251. Rang HP, Dale MM, Ritter JM, Moore PK ( ...
Jefferson, James W. (1974). "Beta-Adrenergic Receptor Blocking Drugs in Psychiatry". Archives of General Psychiatry. 31 (5): ... Beta blockers reduce anxiety by decreasing heart rate and preventing shaking. Beta blockers include propranolol, oxprenolol, ... Benzodiazepines bind selectively to the GABA receptor, which is the receptor protein found in the nervous system and is in ... Its mechanism of action is poorly-defined, with GABAergic, NGF and BDNF release promoting, MT1 receptor agonism, MT3 receptor ...
... alpha-2 and beta-2 adrenergic receptors,. The main endogenous agonist of these cell receptors is norepinephrine (NE). The ... beta-2 receptors. Agonism of beta-2 receptors causes vasodilation and low blood pressure (i.e. the effect is opposite of the ... See also receptor antagonist) alpha-2 receptors. Agonists of alpha-2 receptors in the vascular smooth muscle lead to ... Vascular smooth muscle is innervated primarily by the sympathetic nervous system through adrenergic receptors (adrenoceptors). ...
... alpha inhibitory and beta inhibitory adrenergic receptors in the guinea-pig stomach". Archives Internationales de ... S. Guimarães, W. Osswald (1969). "Adrenergic receptors in the veins of the dog". European Journal of Pharmacology. 5 (2): 188- ... beta blockers might bring release down to normal levels. The pharmacology of angiotensin und adenosine, their receptors and ... "Crosstalk between presynaptic angiotensin receptors, bradykinin receptors and α2-autoreceptors in sympathetic neurons: a study ...
Beta2-adrenergic agonists act on beta-2 receptors to drive potassium into the cells. Therefore, beta blockers can raise ... and noradrenaline have a protective effect on the cardiac electrophysiology because they bind to beta 2 adrenergic receptors, ... Examples of medications that can cause hyperkalemia include ACE inhibitors, angiotensin receptor blockers, non-selective beta ... Examples of drugs that can raise the serum potassium are non-selective beta-blockers such as propranolol and labetalol. Beta-1 ...
Johnson, M (2006). "Molecular mechanisms of beta(2)-adrenergic receptor function, response, and regulation". J Allergy Clin ... β1 receptors make up to 75% of all beta receptors and are predominantly located in the heart. β2 receptors are found in ... Beta2-adrenergic agonist Alpha-adrenergic agonist Asthma Beta blocker Beta-1 adrenergic receptor Beta-2 adrenergic receptor ... It also influences the specificity for the β-receptor subtypes. Direct-acting analog binds the β-adrenergic receptors directly ...
"Molecular mechanisms of beta(2)-adrenergic receptor function, response, and regulation". The Journal of Allergy and Clinical ... Pulmonary stretch receptors in the smooth muscle of the airways initiate a reflex known as the Hering-Breuer reflex that ... The lungs also have a sympathetic tone from norepinephrine acting on the beta 2 adrenoceptors in the respiratory tract, which ... 34 (1): 63-87. doi:10.1016/j.asd.2004.11.002. Burggren, Warren W.; McMahon, Brian R. (1988). Biology of the Land Crabs. ...
... stimulates beta-2 adrenergic receptors and peripheral dopamine receptor D1 and dopamine receptor D2. It also ... It works by stimulating beta-2 adrenergic receptors and peripheral dopamine receptor D1 and dopamine receptor D2. It also ... Beta-adrenergic agonists, Cardiac stimulants, Catecholamines, D1-receptor agonists, D2-receptor agonists, Norepinephrine ... Effects of depexamine may be suppressed by concomitant use with ß2-adrenergic and dopamine receptor antagonists requires ...
Norepinephrine acts more on alpha receptors than the beta receptors. Norepinephrine is the INN while noradrenaline is the BAN. ... It stimulates α1 and α2 adrenergic receptors to cause blood vessel contraction, thus increases peripheral vascular resistance ... Norepinephrine works by binding and activating alpha adrenergic receptors. Norepinephrine was discovered in 1946 and was ... Norepinephrine acts on beta-1 adrenergic receptors, causing increase in heart rate and cardiac output. However, the elevation ...
PH domains of beta-adrenergic receptor kinase and beta-spectrin to WD40/beta-transducin repeat containing regions of the beta- ... G protein receptor kinases (GRK) of GRK2 subfamily (beta-adrenergic receptor kinases): GRK2 and GRK3. Spectrin/pleckstrin-like ... Non-receptor tyrosine kinases belonging to the Btk/Itk/Tec subfamily. Insulin receptor substrate 1 (IRS-1). Regulators of small ... Wang DS, Shaw G (December 1995). "The association of the C-terminal region of beta I sigma II spectrin to brain membranes is ...
... is highly selective for postsynaptic alpha1- adrenergic, and non-selective for beta-adrenergic receptors. It is about ... Labetalol is a dual alpha (α1) and beta (β1/β2) adrenergic receptor blocker and competes with other Catecholamines for binding ... Labetalol was the first drug created that combined both alpha- and beta- adrenergic receptor blocking properties. It was ... Labetalol acts by blocking alpha and beta adrenergic receptors, resulting in decreased peripheral vascular resistance without ...
Non-selective beta blockers are known to facilitate bronchospasm as well. Beta blockers bind into the β2 receptors and block ... Beta2-adrenergic agonists are recommended for bronchospasm. Short acting (SABA) Terbutaline Salbutamol Levosalbutamol Long ... all of which act as receptor antagonists of muscarinic acetylcholine receptors) are effective for treating asthma and COPD- ... Bronchospasms are a possible side effect of some drugs: pilocarpine, beta blockers (used to treat hypertension), a paradoxical ...
Feldman RD, Hunninghake GW, McArdle WL (1987). "Beta-adrenergic-receptor-mediated suppression of interleukin 2 receptors in ... 36 (1): 40-5. doi:10.1038/ng1285. PMID 14702039. Gerhard DS, Wagner L, Feingold EA, et al. (2004). "The status, quality, and ... 138 (1-2): 171-4. doi:10.1016/0378-1119(94)90802-8. PMID 8125298. Suzuki Y, Yoshitomo-Nakagawa K, Maruyama K, et al. (1997). " ... 200 (1-2): 149-56. doi:10.1016/S0378-1119(97)00411-3. PMID 9373149. Hartley JL, Temple GF, Brasch MA (2001). "DNA cloning using ...
Labetalol - an alpha- and beta-adrenergic blocker, given as an intravenous bolus or infusion. Bolus followed by infusion. ... converting enzyme inhibitor or angiotensin II receptor blocker, which can interfere with renal autoregulation and produce acute ... 2 (6 Pt 1): 486-92. doi:10.1093/ajh/2.6.486. PMID 2757806. Tamaki, K.; Sadoshima, S.; Baumbach, G. L.; Iadecola, C.; Reis, D. J ... 7 (7 Pt 1): 623-8. doi:10.1093/ajh/7.7.623. PMID 7946164. Angeli P, Chiesa M, Caregaro L, et al. (1991). "Comparison of ...
Sellinger, M.; Frazer, A.; Mendels, J. CENTRAL BETA-ADRENERGIC RECEPTOR SUBSENSITIVITY DEVELOPS AFTER REPEATED ADMINISTRATION ... Altres estudis proven que diferents antidepressius produeixen efectes variats sobre els receptors del còrtex i de l'hipocamp.[ ... Estudis demostren que l'ús d'antidepressius involucra una adaptació neural que comporta una regulació a la baixa dels receptors ... ISBN 978-1-904671-85-5. [Pàgina?] *↑ «Initial severity and antidepressant benefits: A meta-analysis of data submitted to the ...
BMY-7,378 is a 5-HT1A receptor weak partial agonist/antagonist and α1D-adrenergic receptor antagonist.[1] ... Beta blockers (e.g., alprenolol, carteolol, cyanopindolol, iodocyanopindolol, isamoltane, oxprenolol, penbutolol, pindobind, ... "BMY 7378 is a selective antagonist of the D subtype of alpha 1-adrenoceptors". European Journal of Pharmacology. 272 (2-3): R5- ... 8-(2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl)-8-azaspiro[4.5]decane-7,9-dione ...
Adrenergic. *Adrenergic receptor agonist (α. *β (1. *2)). *Adrenergic receptor antagonist (α (1 ... Two conformers of dopamine have been identified as alpha- and beta-conformers in which the catechol ring is coplanar with the ... Non-ergoline dopamine receptor agonists have higher binding affinity to dopamine D3-receptors than dopamine D2-receptors. This ... A dopamine agonist (DA) is a compound that activates dopamine receptors. There are two families of dopamine receptors, D2-like ...
This is sensed by stretch receptors in the walls of vessels in the carotid sinus and aortic arch.[9] These receptors then ... The next stage is the adrenergic response. If there is underlying fear or anxiety (e.g., social circumstances), or acute fear ( ... Various medications, such as beta blockers, may cause bradycardia induced syncope.[17] ... 16 (4): 1-22, quiz 22-23. PMID 25105200.. *^ a b c d Ruwald, MH (August 2013). "Epidemiological studies on syncope - a register ...
... adrenergic receptor signaling to L-type Ca(2+) channels". Biophys. J. 79 (5): 2547-56. PMC 1301137 . PMID 11053129. doi:10.1016 ... Desenzitizacija beta-1-receptora. *UMich orijentacija proteina u membranama protein/pdbid-2rh1 - 3D struktura beta-2 ... Gq spregnuti receptor) i α2 (Gi spregnuti receptor). Fenilefrin je selektivni agonist α receptora. ... Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A ...
Molecular characterization of the mouse beta 3-adrenergic receptor: relationship with the atypical receptor of adipocytes.". ... Beta-3 adrenergički receptor (β3 adrenoreceptor), takođe poznat kao ADRB3, je beta-adrenergički receptor. ADRB3 je takođe ... Krief S, Lönnqvist F, Raimbault S, et al. (1993). „Tissue distribution of beta 3-adrenergic receptor mRNA in man.". J. Clin. ... Lelias JM, Kaghad M, Rodriguez M, et al. (1993). „Molecular cloning of a human beta 3-adrenergic receptor cDNA.". FEBS Lett. ...
... receptors, and functions as a full agonist at all sites except the 5-HT2A receptor, where it acts as a weak partial agonist or ... Beta blockers (e.g., alprenolol, carteolol, cyanopindolol, iodocyanopindolol, isamoltane, oxprenolol, penbutolol, pindobind, ... Robertson DW, Bloomquist W, Wong DT, Cohen ML (1992). "mCPP but not TFMPP is an antagonist at cardiac 5HT3 receptors". Life ... See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ...
Tolkovsky AM, Levitzki A (1978). "Mode of coupling between the beta-adrenergic receptor and adenylate cyclase in turkey ... These include receptor antagonists, neurotransmitters, neurotransmitter reuptake, G protein-coupled receptors, G proteins, ... When a ligand activates the G protein-coupled receptor, it induces a conformational change in the receptor that allows the ... Phosducin- transducin beta-gamma complex. Beta and gamma subunits of G-protein are shown by blue and red, respectively. ...
... is a potent and selective serotonin 5-HT1D receptor antagonist which has been used in research to study the function ... Beta blockers (e.g., alprenolol, carteolol, cyanopindolol, iodocyanopindolol, isamoltane, oxprenolol, penbutolol, pindobind, ... June 2004). "The role of the 5-HT1D receptor as a presynaptic autoreceptor in the guinea pig". European Journal of Pharmacology ... LY-456220 lacks significant affinity for the 5-HT1B, α1 adrenergic, and dopamine D2 receptors.[1][2] ...
"Rapid down regulation of beta adrenergic receptors by combining antidepressant drugs with forced swim: a model of ... Antidepressant drugs, such as those that cause down regulation of β-adrenergic receptors, can cause rapid neural adaptations in ... Neural receptor cells that process and receive stimulation go through constant changes for mammals and other living organisms ... The mechanoreception of sound requires a specific set of receptor cells called hair cells that allow for gradient signals to ...
beta β GLRB Ionotropic glutamate receptors[edit]. The ionotropic glutamate receptors bind the neurotransmitter glutamate. They ... Adrenergic. *Adrenergic receptor agonist (α. *β (1. *2)). *Adrenergic receptor antagonist (α (1 ... The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (also known as AMPA receptor, or quisqualate receptor) is a ... The N-methyl-D-aspartate receptor (NMDA receptor) - a type of ionotropic glutamate receptor - is a ligand-gated ion channel ...
Beyond these general permissive effects, dopamine (acting via D1 receptors) and norepinephrine (acting at several receptors) ... 4-Hydroxyamphetamine has been shown to be metabolized into 4-hydroxynorephedrine by dopamine beta-hydroxylase (DBH) in vitro ... See also: Receptor/signaling modulators • Monoamine reuptake inhibitors • Adrenergics • Dopaminergics • Serotonergics • ... and beta-hydroxylation, N-oxidation, N-dealkylation, and deamination.[82][88] The known metabolic pathways, detectable ...
α-2 adrenergic receptor[22]. *5-HT1 receptor[22]. PLC may also be activated by MAP kinase. Activators of this pathway include ... 1-4160-2328-3. .. *^ a b c d e f Walter F., PhD. Boron (2003). Medical Physiology: A Cellular And Molecular Approaoch. Elsevier ... 1-4160-2328-3. .. *^ a b c d e f Walter F., PhD. Boron (2003). Medical Physiology: A Cellular And Molecular Approaoch. Elsevier ... 1-4160-2328-3. .. *^ a b Trappe TA, Liu SZ (2013). "Effects of prostaglandins and COX-inhibiting drugs on skeletal muscle ...
Stimulatory factors: Beta-adrenergic agents, cholinergic agents, gastrin-releasing peptide (GRP) Inhibitory factor: ... This is done both directly on the parietal cell[failed verification] and indirectly via binding onto CCK2/gastrin receptors on ... Gastrin binds to cholecystokinin B receptors to stimulate the release of histamines in enterochromaffin-like cells, and it ... hypercalcemia (via calcium-sensing receptors) Gastrin release is inhibited by: the presence of acid (primarily the secreted HCl ...
... has also been found to induce anticonvulsant and antihypnotic effects involving alpha 2-adrenergic receptors, as well ... known as beta oxidation). Carnitine is mainly absorbed from the diet, but can be formed through biosynthesis. To produce ... oxide production via stimulation of the M3 muscarinic acetylcholine receptor or specific gamma-butyrobetaine ester receptors. ... fatty acid transport is reduced and the accumulation of cytotoxic intermediate products of fatty acid beta-oxidation in ...
Also, androgens, but not estrogens, increase beta adrenergic receptors while decreasing alpha adrenergic receptors- which ... nuclear translocation of androgen receptor complex with beta-catenin and T-cell factor 4 may bypass canonical Wnt signaling to ... norepinephrine then acting on lipolysis-inducing beta receptors. Males typically have more skeletal muscle mass than females. ... Zuloaga DG, Puts DA, Jordan CL, Breedlove SM (May 2008). "The role of androgen receptors in the masculinization of brain and ...
... a protein that regulates beta-adrenergic receptor function". Science. 248 (4962): 1547-50. Bibcode:1990Sci...248.1547L. doi: ... Lefkowitz RJ, Shenoy SK (April 2005). "Transduction of receptor signals by beta-arrestins". Science. 308 (5721): 512-7. Bibcode ... Increased accessibility of these sites in receptor-bound arrestin targets the arrestin-receptor complex to the coated pit. ... Arrestin binding to the receptor blocks further G protein-mediated signaling and targets receptors for internalization, and ...
These smooth muscle cells have muscarinic M3 receptors on their membrane. The activation of these receptors by acetylcholine ... These medications include short-acting beta agonists (SABAs) such as albuterol which typically last 4-6 hours, and long-acting ... Rau, JL (Jul 2000). "Inhaled adrenergic bronchodilators: historical development and clinical application". Respir Care. 45 (7 ... B-receptor agonists: Medications that stimulate the β2 receptor subtype on pulmonary smooth muscle will result in smooth muscle ...
... mesylate (Tornalate) is a short-acting β2 adrenergic receptor agonist used for the relief of bronchospasm in ... Walker, Susannah B.; Kradjan, Wayne A.; Bierman, C. Warren (6 May 1985). "Bitolterol Mesylate: A Beta-adrenergic Agent; ... Beta2-adrenergic agonists, Benzoate esters, Prodrugs, Withdrawn drugs, Tert-butyl compounds, Phenylethanolamines, 4-Tolyl ... 73 (1 Pt 1): 32-43. doi:10.1016/0091-6749(84)90481-0. PMID 6693665. v t e (Articles with short description, Short description ...
... a selective alpha2-adrenergic and imidazoline receptor agonist, produces spinal antinociception in mice". The Journal of ... If concomitant treatment with a beta blocker has to be stopped, the beta blocker should be discontinued first, then moxonidine ... Alpha-2 adrenergic receptor agonists, Antihypertensive agents, Chloroarenes, Chloropyrimidines, Imidazolines, Phenol ethers, ... moxonidine binds with much greater affinity to the imidazoline I1-receptor than to the α2-receptor. In contrast, clonidine ...
... beta-2 microglobulin - beta adrenergic receptor - beta sheet - beta-1 adrenergic receptor - beta-2 adrenergic receptor - beta- ... alpha-2 adrenergic receptor - alpha-beta T-cell antigen receptor - alpha-fetoprotein - alpha-globulin - alpha-macroglobulin - ... transforming growth factor beta - transforming growth factor beta receptor - transient receptor potential - translation ( ... interferon receptor - interferon type I - interferon type II - interferon-alpha - interferon-beta - interleukin receptor - ...
"Differential distribution of beta-adrenergic receptor subtypes in blood vessels of knockout mice lacking beta(1)- or beta(2)- ... van Brummelen P, Jie K, van Zwieten PA (1986). "Alpha-adrenergic receptors in human blood vessels". British Journal of Clinical ... However, when catecholamines active the beta receptor, the blood vessel dilates (gets larger) and allows for increased blood ... Clark BK (May 1992). "Beta-adrenergic blocking agents: their current status". AACN Clinical Issues in Critical Care Nursing. 3 ...
Topical beta-adrenergic receptor antagonists, such as timolol, levobunolol, and betaxolol, decrease aqueous humor production by ... Alpha2-adrenergic agonists, such as brimonidine and apraclonidine, work by a dual mechanism, decreasing aqueous humor ... Beta-blockers, such as timolol, work by decreasing aqueous formation. Carbonic anhydrase inhibitors decrease bicarbonate ... other major innovations in pharmacological glaucoma therapy were the introduction of beta blocker eye drops in the 1970s and of ...
... a target of beta-adrenergic signaling, regulates gene expression that controls oxidative metabolism in skeletal muscle". ... The nuclear receptor 4A3 (NR4A3) (nuclear receptor subfamily 4, group A, member 3) also known as neuron-derived orphan receptor ... a target of beta-adrenergic signaling, regulates gene expression that controls oxidative metabolism in skeletal muscle". ... is a target of beta-adrenergic signaling in skeletal muscle". Endocrinology. 147 (11): 5217-27. doi:10.1210/en.2006-0447. PMID ...
... while the ACTH receptor and the β2 adrenergic receptor are relatively distantly-related with a sequence identity of ... melanocortin-2 receptor (MC2R)] by human MC2R accessory protein isoforms alpha and beta in isogenic human embryonic kidney 293 ... The adrenocorticotropic hormone receptor or ACTH receptor also known as the melanocortin receptor 2 or MC2 receptor is a type ... ACTH receptors are the shortest of the melanocortin receptor family and are the smallest known G-coupled receptors. Both human ...
... beta blockers (ICI Pharmaceuticals, 1964) ACE inhibitors, and angiotensin receptor blockers. ACE inhibitors reduce the risk of ... Black JW, Crowther AF, Shanks RG, Smith LH, Dornhorst AC (1964). "A new adrenergic betareceptor antagonist". The Lancet. 283 ( ... 122 (1 Suppl): S3-S14. doi:10.1016/j.amjmed.2008.10.013. PMID 19110086. Gaddam KK, Verma A, Thompson M, Amin R, Ventura H (May ... ISBN 978-1-4000-8213-1. "All Nobel Prizes in Physiology or Medicine". The Nobel Prize. Retrieved 22 July 2022. Cutler, David M ...
Gq proteins couple to G protein-coupled receptors to activate beta-type phospholipase C (PLC-β) enzymes. PLC-β in turn ... When the receptor binds an activating ligand outside the cell (such as a hormone or neurotransmitter), the activated receptor ... The common polybasic domain in the C-tail of Gq-coupled receptors appears necessary for this receptor¬G protein preassembly. ... The following G protein-coupled receptors couple to Gq subunits: 5-HT2 serotonergic receptors Alpha-1 adrenergic receptor ...
... or by cross-coupling with beta-amino organozinc reagents, or reacting a brominated arene with beta-aminoethyl organolithium ... Phenethylamine has been shown to bind to human trace amine-associated receptor 1 (hTAAR1) as an agonist. β-PEA is also an ... "Dissociation Constants of Adrenergic Amines". Journal of the American Chemical Society. 73 (6): 2611-3. doi:10.1021/ja01150a055 ... Yang, HY; Neff, NH (1973). "Beta-phenylethylamine: A specific substrate for type B monoamine oxidase of brain". The Journal of ...
"Human fat cell beta-adrenergic receptors: beta-agonist-dependent lipolytic responses and characterization of beta-adrenergic ... ICI-118,551 is a selective β2 adrenergic receptor (adrenoreceptor) antagonist or beta blocker. ICI binds to the β2 subtype with ... Hillman KL, Doze VA, Porter JE (August 2005). "Functional characterization of the beta-adrenergic receptor subtypes expressed ... "Molecular characterization of the human beta 3-adrenergic receptor". Science. 245 (4922): 1118-21. Bibcode:1989Sci...245.1118E ...
In contrast to dopamine, fenoldopam is a selective D1 receptor agonist with no effect on beta adrenoceptors, although there is ... Since fenoldopam is an intravenous agent with minimal adrenergic effects that improves renal perfusion, in theory it could be ... Concomitant use of fenoldopam with a beta-blocker should be avoided if possible, as unexpected hypotension can result from beta ... D1 receptor stimulation activates adenylyl cyclase and raises intracellular cyclic AMP, resulting in vasodilation of most ...
Propranolol is a nonselective beta-adrenergic receptor blocking agent. It has been found to relieve exaggerated startle ... Beta-blockers. Class Summary. Beta-blockers such as propranolol are useful in controlling some symptoms of PTSD caused by ... Alpha-2 Adrenergic Agonists. Class Summary. Agents in this class may decrease vasomotor tone and heart rate by stimulating ... Clonidine is a central alpha-adrenergic agonist that is commonly used as an antihypertensive agent. It stimulates alpha2- ...
IRS-1 and beta 3 adrenergic-receptor gene mutations in NIDDM patients with or without insulin resistance and dyslipidaemia in ... IRS-1 and beta 3 adrenergic-receptor gene mutations in NIDDM patients with or without insulin resistance and dyslipidaemia in ...
The beta-2 adrenergic receptor (beta2AR) has a carboxyl terminus motif that can interact with PSD-95/discs-large/ZO1 homology ( ... Beta-2 adrenergic receptor mediated ERK activation is regulated by interaction with MAGI-3 FEBS Lett. 2010 Jun 3;584(11):2207- ... The beta-2 adrenergic receptor (beta2AR) has a carboxyl terminus motif that can interact with PSD-95/discs-large/ZO1 homology ( ... Xiaomei Yang 1 , Junfang Zheng, Ying Xiong, Hui Shen, Licui Sun, Yan Huang, Chaoyuan Sun, Yang Li, Junqi He ...
Beta-adrenergic receptor blockers. Class Summary. Relief of adrenergic symptoms, especially cardiac and neurologic. Propranolol ... Nonselective beta-adrenergic receptor blocker. Also blocks peripheral conversion of T4 to T3. Used along with antithyroid drugs ... Beta blockers. Beta blockers should be considered for patients with resting heart rates over 90 bpm or coexistent ... but they block the beta-adrenergic peripheral manifestations of the hyperthyroid state. Propranolol has an effect in decreasing ...
... beta-ARK) phosphorylates G protein coupled receptors in an agonist-dependent manner. Since the exact sites of receptor ... phosphorylation by beta-ARK are poorly defined, the identification of substrate amino acids that are critical to ... The beta-adrenergic receptor kinase (beta-ARK) phosphorylates G protein coupled receptors in an agonist-dependent manner. Since ... Role of acidic amino acids in peptide substrates of the beta-adrenergic receptor kinase and rhodopsin kinase Biochemistry. 1991 ...
Adrenergic, beta-2-, receptor, surface. 5q31-q32. rs1042713. Ex1+265G,A. Gly16Arg ... Angiotensin-converting enzyme degrades Alzheimer amyloid beta-peptide (A beta); retards A beta aggregation, deposition, fibril ... Alessi MC, Juhan-Vague I. PAI-1 and the metabolic syndrome: links, causes, and consequences. Arterioscler Thromb Vasc Biol 2006 ... Serpin peptidase inhibitor, clade E (nexin, plasminogen activator inhibitor type 1), member 1 ...
This study was aimed to evaluate beta-2 adrenergic agonist (Beta-2 Adrenergic Agonist, BAA) Salmeterol and beta blocker (Beta ... the mRNA expressions of follicular beta-2 adrenergic receptor (Beta-2 Adrenergic Receptor, β2ADR), cyclooxygenases ( ... The stimulation and inhibition of beta-2 adrenergic signaling could reduce ovarian inflammatory condition in addition to ... Cyclooxygenases, COX) 1 and 2, and cytokines were measured by real-time PCR. The plasma concentration of ovarian hormones, ...
Beta-adrenergic receptor binding: synaptic localization in rat brain. ... Beta-adrenergic receptor binding: synaptic localization in rat brain. Journal Article (Journal Article) ...
... a new adrenergic beta receptor antagonist. Indian Journal of Medical Research. 1970 Feb; 58(2): 246-52. ... 1-Feb-1970. Citation: Madan BR, Gupta RS, Santani DD. Cardiopulmonary actions of 1-isopropylamino-3-(3-tolyloxy)-2-propanol ... Cardiopulmonary actions of 1-isopropylamino-3-(3-tolyloxy)-2-propanol hydrochloride: a new adrenergic beta receptor antagonist. ...
Recombinant Saccharomyces cerevisiae Alpha-galactosidase 1 (MEL1) from Cusabio. Cat Number: CSB-YP356371SAC. USA, UK & Europe ... Recombinant Mouse Beta-adrenergic receptor kinase 1 (Grk2) , CSB-EP858153MO , CusabioAlternative Name(s): G-protein-coupled ... Recombinant Mouse Beta-adrenergic receptor kinase 1 (Grk2) , CSB-EP858153MO Cusabio Mouse Recombinants ... Recombinant Human Beta-1 adrenergic receptor (ADRB1) , CSB-CF001391HU(A4) Cusabio Human Recombinants ...
Candidate genes in these regions include beta-3 adrenergic receptor and leptin, respectively. Between the two parity groups, 3 ... No single 1-Mb window explained a significant proportion of the TGVM for RFI; however, analyses identified adjacent regions ... and MBW using the Bayes B method in GenSel version 4.0 with prior assumption that 1% of SNP have a non-zero effect. One ...
Beta-2 adrenergic receptor. A. 469. Escherichia virus T4, Homo sapiens. This entity is chimeric. Mutation(s): 7 Gene Names: E, ... Covalent agonists for studying G protein-coupled receptor activation.. Weichert, D., Kruse, A.C., Manglik, A., Hiller, C., ... Structural studies on G protein-coupled receptors (GPCRs) provide important insights into the architecture and function of ... Structural studies on G protein-coupled receptors (GPCRs) provide important insights into the architecture and function of ...
One of these is called the beta-1 adrenergic receptor. Among other things, it is responsible for palpitation, the racing pulse ... New insights into the workings of important drug receptorsMany medical drugs operate on specific receptors located in the outer ... Joël Mesots third term of office will start on 1 August 2016, Konrad Steffens second term of office on 1 July 2016. ... Researchers at the Paul Scherrer Institute (PSI) created a synthetic material out of 1 billion tiny magnets. Astonishingly, it ...
It specifically competes with beta-adrenergic receptor stimulating agents for available receptor sites. When access to beta‑ ... The effects of propranolol are due to selective blockade of beta-adrenergic receptors, leaving alpha-adrenergic responses ... Beta-adrenergic receptor blockade can cause reduction of intraocular pressure. Patients should be told that propranolol might ... Beta2-adrenergic receptors are found predominantly in smooth muscle-vascular, bronchial, gastrointestinal and genitourinary. ...
Beta-2 adrenergic receptor,Endolysin,Beta-2 adrenergic receptor. A. 500. Homo sapiens, Escherichia virus T4. Mutation(s): 1 ... the β 2 -adrenergic G protein-coupled receptor (β 2 AR), the peptide transporter (PepT St ), diacylglycerol kinase (DgkA), the ... beta-D-glucopyranose. B 2. N/A. Oligosaccharides Interaction. ... 1,4-BUTANEDIOL. C4 H10 O2. WERYXYBDKMZEQL-UHFFFAOYSA-N. Ligand ... 2S)-1-(9H-Carbazol-4-yloxy)-3-(isopropylamino)propan-2-ol. C18 H22 N2 O2. BQXQGZPYHWWCEB-ZDUSSCGKSA-N. Ligand Interaction. ...
Adrenergic receptor and Beta blocker have in common. Hyperleap helps uncover and suggest relationships using custom algorithms. ... Adrenergic receptor. Beta blockers are competitive antagonists that block the receptor sites for the endogenous catecholamines ... The adrenergic receptors or adrenoceptors are a class of G protein-coupled receptors that are targets of many catecholamines ... on adrenergic beta receptors, of the sympathetic nervous system, which mediates the fight-or-flight response. ...
... beta-adrenergic receptors) and peripheral tone (alpha-adrenergic receptors) is attempted. ... nonselective beta blocker use in the setting of acute cocaine intoxication may result in unopposed alpha-adrenergic receptor ... In addition, stimulation of the alpha-adrenergic receptors, which leads to increased peripheral vascular tone, increases the ... Potentiation of cocaine-induced coronary vasoconstriction by beta-adrenergic blockade. Ann Intern Med. 1990 Jun 15. 112(12):897 ...
Beta Blocker News and Research. RSS Beta-adrenergic receptor blocking agents (beta-blockers) are drugs with multiple actions on ... Blockade of beta-1 receptors results in slowing of heart rate, reduction in myocardial contractility, and lowering of systemic ... Furthermore, beta-blockers may reduce the risk of ventricular arrhythmias, which are an important cause of death following AMI ...
Molecular characterization of the mouse beta 3-adrenergic receptor: relationship with the atypical receptor of adipocytes.". ... Beta-3 adrenergički receptor (β3 adrenoreceptor), takođe poznat kao ADRB3, je beta-adrenergički receptor. ADRB3 je takođe ... Krief S, Lönnqvist F, Raimbault S, et al. (1993). „Tissue distribution of beta 3-adrenergic receptor mRNA in man.". J. Clin. ... Lelias JM, Kaghad M, Rodriguez M, et al. (1993). „Molecular cloning of a human beta 3-adrenergic receptor cDNA.". FEBS Lett. ...
Beta-2 Adrenergic receptor gene variations and coping styles in twins. Biological Psychology 61 (1 - 2), pp. 97 - 109 (2002) ... GenomXPress: Informationen aus der Deutschen Genomforschung 2004 (1), pp. 17 - 19 (2004) ...
Some patients receiving beta-adrenergic receptor blocking agents have experienced protracted severe hypotension during ... Nonselective beta-adrenergic receptor blocker; reduces IOP by reducing production of aqueous humor ... Some authorities recommend gradual withdrawal of beta-adrenergic receptor blocking agents in patients undergoing elective ... In patients undergoing elective surgery; gradual withdrawal of beta-adrenergic receptor blocking agents recommended; in ...
Simons FE, Simons KJ, Frith EM "The pharmacokinetics and antihistaminic of the H1 receptor antagonist hydroxyzine." J Allergy ... In cardiac tissues, these agents may produce positive chronotropic and inotropic effects via stimulation of beta- 1 adrenergic ... Paton DM, Webster DR "Clinical pharmacokinetics of H1-receptor antagonists (the antihistamines)." Clin Pharmacokinet 10 (1985 ... "The effect of single-dose phenylpropanolamine on blood pressure in patients with hypertension controlled by beta blockers." ...
9. Angiotensin II Receptor Blockers (ARBs) Chapter 18 PIXORIZE Pharmacology 2021: 18. Reproductive Pharm (12). *1. Leuprolide ( ... Chapter 5 PIXORIZE Pharmacology 2021: 5. Alpha and Beta Blockers (7). *1. Phenoxybenzamine ... PIXORIZE Pharmacology 2021: 5. Alpha and Beta Blockers (7). Chapter No 5 ... Chapter 1 PIXORIZE Pharmacology 2021: 1. General Pharm (15). *1. Gs - Gi Signaling Pathway ...
It is a beta-2-adrenergic receptor agonist. Bitolterol was withdrawn from the market by Elan Pharmaceuticals in 2001. ... The beta-2-adrenergic receptor binds epinephrine with an approximately .... Gene Name. ADRB2. Uniprot ID. P07550. Uniprot Name ... Agonism of the beta-2 adrenergic receptors by bitolterol leads to a relaxation of the smooth muscles surrounding these airway ... It is a beta-2-adrenergic receptor agonist. Bitolterol was withdrawn from the market by Elan Pharmaceuticals in 2001. ...
... adrenergic receptor: evidence for interaction with distinct conformations of beta(1)-adrenergic receptors. ... Pharmacological responses to aryloxypropanolamines were examined in cells expressing rat or human beta(1)-adrenergic receptors ... Aryloxypropanolamine and catecholamine ligand interactions with the beta(1)- ...
Behavioral effects of beta adrenergic agonists and antidepressant drugs after down-regulation of beta-2 adrenergic receptors by ... Beta adrenergic receptors facilitate norepinephrine release from rat hypothalamic and hippocampal slices. Res Commun Mol Pathol ... ODonnell JM, Wolfe BB, Frazer A. Agonist interactions with beta adrenergic receptors in rat brain. J Pharmacol Exp Ther. 1984 ... ODonnell JM, Frazer A. Effects of clenbuterol and antidepressant drugs on beta adrenergic receptor/N-protein coupling in the ...
IKs restricts excessive beat-to-beat variability of repolarization during beta-adrenergic receptor stimulation (2010-01) ... Altered adrenergic response in myocytes bordering a chronic myocardial infarction underlies in vivo triggered activity and ... Hyperactive ryanodine receptors in human heart failure and ischaemic cardiomyopathy reside outside of couplons (2018-09-01) ... Functional Mapping of the Transient Receptor Potential Vanilloid 1 Intracellular Binding Site (2006-09-01) Johnson, Daniel M.; ...
Learn Adrenergic Receptor Pharmacology in Pharmacology - USMLE Step 1 for Medicine faster and easier with Picmonics ... Beta-2 Agonists. Short-term Treatment. Terbutaline. Asthma. Tocolysis. Albuterol. Asthma. Long-term Treatment. Salmeterol. ... Blocks Alpha2 Receptor. Antagonist at 5-HT receptors. Side Effects. Sedation. Weight gain. Increased Serum Cholesterol. ... Selective Beta-1 Blockers. Characteristics. "-olol" Suffix. Drug Names. Beta-1 selective. Atenolol. Esmolol. Metoprolol. ...
Beta-Adrenergic Receptor Kinase 1 (ARBK1) Antibody. 20-abx013440 Abbexa * EUR 314.00 ... Parathyroid hormone/parathyroid hormone-related peptide receptor Rabbit Polyclonal Antibody. *Caspase-3 Rabbit Polyclonal ... rabbit by using as an immunogen synthesized peptide derived from part region of human ARBK1 protein at amino acid sequence of 1 ...
  • The adrenergic receptors or adrenoceptors are a class of G protein-coupled receptors that are targets of many catecholamines like norepinephrine (noradrenaline) and epinephrine (adrenaline) produced by the body, but also many medications like beta blockers , beta-2 (β2) agonists and alpha-2 (α2) agonists, which are used to treat high blood pressure and asthma, for example. (
  • Brimonidine belongs to a group of drugs called alpha-2 adrenergic receptor agonists. (
  • Long-acting beta 2 -adrenergic agonists (LABA) increase the risk of asthma-related death. (
  • Beta-Adrenergic Receptor Blocking Agents: Beta-blockers not only block the pulmonary effect of beta-agonists, but may also produce severe bronchospasm in patients with asthma or COPD. (
  • Diuretics: The ECG changes and/or hypokalemia that may result from the administration of non-potassium-sparing diuretics (such as loop or thiazide diuretics) can be acutely worsened by beta-agonists. (
  • In cells, the association of full-length beta2AR with MAGI-3 occurs constitutively and is enhanced by agonist stimulation of the receptor. (
  • The beta-adrenergic receptor kinase (beta-ARK) phosphorylates G protein coupled receptors in an agonist-dependent manner. (
  • The effects of beta(3)-adrenoceptor agonist CL-316,243 on adiponectin, adiponectin receptors and tumor necrosis factor-alpha expressions in adipose tissues of obese diabetic KKAy mice. (
  • It is a beta-2-adrenergic receptor agonist. (
  • Bitolterol is an adrenergic beta-2 agonist. (
  • Isoprenaline HCl (NCI-c55630,Isoproterenol hydrochloride) is a non-selective beta-adrenergic receptor agonist, used for the treatment of bradycardia and heart block. (
  • Data from a large placebo-controlled US study that compared the safety of another longacting beta 2 -adrenergic agonist (salmeterol) or placebo added to usual asthma therapy showed an increase in asthma-related deaths in patients receiving salmeterol. (
  • The adrenergic beta-1 receptors are equally sensitive to EPINEPHRINE and NOREPINEPHRINE and bind the agonist DOBUTAMINE and the antagonist METOPROLOL with high affinity. (
  • Selective alpha-adrenergic agonist (alpha2) without significant local anesthetic activity. (
  • Salmeterol is a selective, long-acting beta2-adrenergic agonist. (
  • 6-Chloromelatonin is a potent melatonin receptor agonist with greater metabolic stability than melatonin. (
  • Our data also demonstrated that beta2AR-stimulated extracellular signal-regulated kinase-1/2 (ERK1/2) activation was substantially retarded by MAGI-3 expression. (
  • Since the exact sites of receptor phosphorylation by beta-ARK are poorly defined, the identification of substrate amino acids that are critical to phosphorylation by the kinase are also unknown. (
  • The general applicability of the method is demonstrated with five integral membrane proteins: the β 2 -adrenergic G protein-coupled receptor (β 2 AR), the peptide transporter (PepT St ), diacylglycerol kinase (DgkA), the alginate transporter (AlgE) and the cystic fibrosis transmembrane conductance regulator (CFTR). (
  • Insulin exocytosis can be potentiated by the peptide hormones PACAP and GLP-1, through activation of protein kinase A. Moreover, transplanted bone marrow cells stimulate replication of endogenous beta-cells and have beneficial effects on blood glucose. (
  • G protein receptor kinase 4 polymorphisms: ß-blocker pharmacogenetics and treatment-related outcomes in hypertension. (
  • CHIR-99021 is a glycogen synthase kinase 3 beta inhibitor that has antiproliferative activity in vitro and in vivo. (
  • IMSEAR at SEARO: Cardiopulmonary actions of 1-isopropylamino-3-(3-tolyloxy)-2-propanol hydrochloride: a new adrenergic beta receptor antagonist. (
  • Za SR 59230A se mislilo da je selektivni β 3 antagonist [11] ali je naknadno utvrđeno da je takođe antagonist α 1 receptora. (
  • A cardioselective competitive beta-1 adrenergic receptor antagonist with antihypertensive properties and devoid of intrinsic sympathomimetic activity. (
  • The tartrate salt form of metoprolol, a cardioselective competitive beta-1 adrenergic receptor antagonist with antihypertensive properties and devoid of intrinsic sympathomimetic activity. (
  • 2004). Further, in non-habituated rats administration of a \(\beta\)-adrenoceptor antagonist immediately after the object recognition training blocked the corticosterone-induced memory enhancement (Roozendaal et al. (
  • SB-334867 is a selective orexin-1 (OX1) receptor antagonist. (
  • Phentolamine Mesylate(Phentolamine methanesulfonate) is a reversible and nonselective alpha-adrenergic receptor antagonist, used for the prevention or control of hypertensive episodes. (
  • At doses greater than required for beta blockade, propranolol also exerts a quinidine-like or anesthetic-like membrane action, which affects the cardiac action potential. (
  • Blockade of cardiac beta 1 -adrenergic receptors leads to a decrease in the activity of both normal and ectopic pacemaker cells and a decrease in A-V nodal conduction velocity. (
  • Blockade of cardiac beta 1 ‑adrenergic receptors also decreases the myocardial force of contraction and may provoke cardiac decompensation in patients with minimal cardiac reserve. (
  • In cardiac tissues, these agents may produce positive chronotropic and inotropic effects via stimulation of beta- 1 adrenergic receptors. (
  • Metoprolol antagonizes beta 1-adrenergic receptors in the myocardium, thereby reducing the rate and force of myocardial contraction leading to a reduction in cardiac output. (
  • Metoprolol tartrate antagonizes beta 1-adrenergic receptors in the myocardium, thereby reducing the rate and force of myocardial contraction, and consequently a diminished cardiac output. (
  • Cardiac myocytes express at least six subtypes of adrenergic receptor (AR) which include three subtypes of beta-AR (beta-1, beta-2, beta-3) and three subtypes of the alpha-1-AR (alpha-1A, alpha-1B, and alpha-1C). (
  • 1 The causes of low cardiac output after cardiac surgery are multifactorial. (
  • Surgical repair of cardiac malformation exposes the myocardial tissue to prolonged periods of myocardial ischaemia 1 and cardioplegia 2 . (
  • Localization of beta adrenergic receptors, and effects of noradrenaline and cyclic nucleotides on action potentials, ionic currents and tension in mammalian cardiac muscle. (
  • Increased cardiac sympathetic drive and reduced vagal modulation following endothelin receptor antagonism in healthy conscious rats. (
  • 1] Inversin, the product of the inv locus, may have a specific role in cardiac morphogenesis (especially in the development of IPS) in addition to its contribution to situs determination. (
  • Beta-blockers such as propranolol are useful in controlling some symptoms of PTSD caused by hyperarousal. (
  • Beta blockers should be considered for patients with resting heart rates over 90 bpm or coexistent cardiovascular disease. (
  • Beta blockers may be used during lactation. (
  • Beta blockers are used if symptomatic tremor or palpitations require their use. (
  • Beta blockers should not be used in the presence of bronchospasm, even the beta1-selective agents. (
  • Beta blockers are competitive antagonists that block the receptor sites for the endogenous catecholamines epinephrine (adrenaline) and norepinephrine (noradrenaline) on adrenergic beta receptors , of the sympathetic nervous system, which mediates the fight-or-flight response. (
  • Beta blockers , which counter some of the effects of noradrenaline by blocking their receptors, are frequently used to treat glaucoma, migraine, and a range of cardiovascular problems. (
  • Beta-adrenergic receptor blocking agents (beta-blockers) are drugs with multiple actions on the heart. (
  • Furthermore, beta-blockers may reduce the risk of ventricular arrhythmias, which are an important cause of death following AMI. (
  • Timolol belongs to a group of drugs called beta-adrenergic receptor blockers ( beta-blockers ). (
  • Many agents are available for lowering of IOP, including topical beta-blockers, adrenergic agents, and topical and systemic carbonic anhydrase inhibitors. (
  • Calcium channel blockers and beta blockers are poor choices because they will exacerbate hypotension. (
  • The effects of propranolol are due to selective blockade of beta-adrenergic receptors, leaving alpha-adrenergic responses intact. (
  • The memory-modulating effects of glucocorticoids appear to involve the selective activation of the low-affinity glucocorticoid receptor. (
  • Propranolol HCl (AY-64043, ICI-45520, NCS-91523) is a competitive non-selective beta-adrenergic receptors inhibitor with IC50 of 12 nM. (
  • Selective alpha2-receptor that reduces aqueous humor formation and possibly increases uveoscleral outflow. (
  • Role of non-selective adenosine receptor blockade and phosphodiesterase inhibition in cisplatin-induced nephrogonadal toxicity in rats. (
  • It is less well known, but equally important, that loss of selective fat pads (or absence of adipose tissue altogether) is also associated with severe forms of insulin resistance ( 1 - 3 ). (
  • Blockade of these receptors results in constriction. (
  • Blockade of beta-1 receptors results in slowing of heart rate, reduction in myocardial contractility, and lowering of systemic blood pressure. (
  • The positive inotropic responses in the denervated animal were abolished by beta receptor blockade but were unaffected by adrenalectomy. (
  • 1. The present study evaluated changes in autonomic control of the cardiovascular system in conscious rats following blockade of endothelin (ET) receptors with bosentan. (
  • 1. An R-wave in lead aVR greater than 3 mm, or an R/S ratio greater than 0.7, is highly suspicious for sodium channel blockade, which is the most important of the many toxicities of TCA overdose. (
  • If the diagnosis is unclear, narrowing of a widened QRS on ECG following sodium bicarbonate administration (1-2meq/kg) adds further support that pharmacologic sodium blockade is present. (
  • The beta-2 adrenergic receptor (beta2AR) has a carboxyl terminus motif that can interact with PSD-95/discs-large/ZO1 homology (PDZ) domain-containing proteins. (
  • We demonstrate that the tool compounds presented herein display an efficient covalent binding mode and that the respective covalent ligand-receptor complexes activate G proteins comparable to the natural neurotransmitters. (
  • [2] [3] Many membrane receptors include transmembrane proteins . (
  • Adra2a mediates adrenergic inhibition of insulin secretion, and both pharmacological receptor antagonism and adra2a gene silencing accomplished full normalization of insulin release. (
  • Beta-2 Adrenergic receptor gene variations and coping styles in twins. (
  • Glucocorticoids act through intracellular and intranuclear receptors and can affect gene transcription by direct binding of receptor homodimers to DNA . (
  • This illuminates a novel disease mechanism for beta-cell dysfunction and introduces adra2a as a candidate gene for defective insulin secretion. (
  • Effect of Bisoprolol on Heart Rate Variability in Patients With Coronary Atherosclerosis: Dependence on Polymorphisms of -1 Adrenergic Receptor Gene]. (
  • Association of beta-1 and beta-2 adrenergic receptor gene polymorphisms with myocardial infarction. (
  • beta-adrenergic receptor gene polymorphisms and beta-blocker treatment outcomes in hypertension. (
  • Adrenergic gene polymorphisms and cardiovascular risk in the NHLBI-sponsored Women's Ischemia Syndrome Evaluation. (
  • beta-2-adrenergic receptor gene polymorphism confers susceptibility to Graves disease. (
  • 1, 6, 7 Currently, array technology is usually most useful in establishing broad patterns of gene expression and in screening for differential gene expression. (
  • The main mechanism of action proposed for local anesthetics (LAs) is related to the binding of these substances to sodium channels receptors (Na+), leading to the reduction or elimination of the permeability of these ions and interruption of the nervous conduction 3-4 . (
  • Mechanism of its action is to prevent the chemicals transmitting nervous signal between nerves such as norepinephrine and adrenaline to bind receptors on nerves. (
  • Two current models have been proposed to explain transmembrane receptors mechanism, dimerization considered as current standard. (
  • Antagonism of central and peripheral muscarinic acetylcholine receptors (leads to delirium) d. (
  • Beta-3 adrenergički receptor (β 3 adrenoreceptor), takođe poznat kao ADRB3 , je beta-adrenergički receptor . (
  • Bitolterol, an adrenergic bronchodilator, is a prodrug that widens constricted airways in the lungs by relaxing the smooth muscles that surround the bronchial passages. (
  • Formoterol fumarate dihydrate is a beta 2 -adrenergic bronchodilator. (
  • A pilot study revealed propranolol is effective for decreasing physiological signs of hyperarousal for up to 1 week when used shortly after patients with PTSD reexperience their traumatic event. (
  • Propranolol is a nonselective beta-adrenergic receptor blocking agent. (
  • Propranolol Hydrochloride, USP is a synthetic beta-adrenergic receptor blocking agent chemically described as (+)-1-(isopropylamino)-3-(1-naphthyloxy)-2-propanol hydrochloride. (
  • Each mL contains 1 mg of Propranolol Hydrochloride, USP in Water for Injection, USP. (
  • Propranolol is a nonselective beta-adrenergic receptor blocking agent possessing no other autonomic nervous system activity. (
  • When access to beta‑receptor sites is blocked by propranolol, chronotropic, inotropic, and vasodilator responses to beta-adrenergic stimulation are decreased proportionately. (
  • The ß-adrenergic receptor blocker and anti-inflammatory drug propranolol mitigates brain cytokine expression in a long-term model of Gulf War Illness. (
  • In this study, a peptide whose sequence is present in a portion of the third intracellular loop region of the human platelet alpha 2-adrenergic receptor is shown to serve as a substrate for beta-ARK. (
  • The beta-2-adrenergic receptor is a Gs protein-coupled receptor, which activates adenylyl cyclase and raises intracellular cAMP. (
  • The muscarinic-M3 receptor is a Gq protein-coupled receptor which activates adenylyl cyclase and raises intracellular cAMP. (
  • In other receptors, the transmembrane domains undergo a conformational change upon binding, which effects intracellular conditions. (
  • The intracellular (or cytoplasmic ) domain of the receptor interacts with the interior of the cell or organelle, relaying the signal. (
  • With enzyme-linked receptors , the intracellular domain has enzymatic activity . (
  • Nonselective beta-adrenergic blocking agent that lowers IOP by reducing aqueous humor production. (
  • In a specifically designed congenic animal model of defective insulin secretion, we were able to identify two genetic loci on rat chromosome 1 that confer impaired beta-cell glucose metabolism and. (
  • In conclusion, defective insulin secretion in diabetes involves distinct functional defects in beta-cell exocytosis and glucose metabolism, conferred by two different genetic subloci. (
  • they react with the receptor to induce changes in the metabolism and activity of a cell. (
  • Fatal cases of ketoacidosis have been reported in patients with type 1 and type 2 diabetes mellitus receiving sodium glucose co-transporter-2 (SGLT2) inhibitors, including dapagliflozin. (
  • What do Norepinephrine, Adrenergic receptor and Beta. (
  • Regardless of how and where it is released, norepinephrine acts on target cells by binding to and activating adrenergic receptors located on the cell surface. (
  • The brain then transfers neurotransmitters throughout the body and also norepinephrine to speed up the receptors in the brain. (
  • However, glucocorticoids may also act more rapidly by interacting with membrane receptors and/or potentiating the efficacy of the norepinephrine-signal cascade via an interaction with G-protein-mediated actions. (
  • At high doses, BT produces a direct positive inotropic effect, probably through stimulation of beta adrenergic receptors. (
  • The authors conclude that the observed responses can be explained by the fact that isoproterenol stimulates beta adrenergic receptors, leading to a relaxation of airway smooth muscle. (
  • They may be used even as clinical investigation is ongoing because they have no effect on thyroid gland function, but they block the beta-adrenergic peripheral manifestations of the hyperthyroid state. (
  • In the peripheral vasculature, vasoconstriction may occur via stimulation of alpha-1 adrenergic receptors. (
  • 1959). The memory modulation is initiated, at least in part, by activation of peripheral \(\beta\)-adrenoceptors located on vagal afferents that project to the nucleus of the solitary tract (NTS) in the brain stem. (
  • Blocks beta1- and beta2-receptors and has mild intrinsic sympathomimetic effects. (
  • Candidate genes in these regions include beta-3 adrenergic receptor and leptin, respectively. (
  • Rodent and human beta 3-adrenergic receptor genes contain an intron within the protein-coding block. (
  • The association of eight potentially functional polymorphisms in five adrenergic receptor-encoding genes with myocardial infarction risk in Han Chinese. (
  • Glucocorticoids are highly lipophilic and, thus, readily enter the brain and bind directly to mineralocorticoid receptors and glucocorticoid receptors. (
  • Glucocorticoids alter the sensitivity of epinephrine in influencing memory consolidation and, conversely, adrenergic activation induced by emotional arousal appears to be essential in enabling glucocorticoid modulation of memory consolidation. (
  • Hence, among other factors, it is important for local anesthetics to show rapid onset of action, provide adequate duration of anesthesia, and be composed by substances (i.e. local anesthetics, vasoconstrictors) with minimal or no systemic toxicity 1-2 . (
  • Arg389Gly polymorphism of the human beta1-adrenergic receptor in patients with nonfatal acute myocardial infarction. (
  • Beta-adrenergic receptor binding: synaptic localization in rat brain. (
  • BAT consists of a group of specialized cells with abundant uncoupling protein 1 (UCP1) in the inner mitochondrial membrane and also fulfills endocrine functions. (
  • Nebivolol shows high affinity and selectivity for beta 1-adrenergic receptor sites in a rabbit lung membrane preparation (K i value = 0.9 nM and beta 2/beta 1 ratio = 50). (
  • Cell surface receptors ( membrane receptors , transmembrane receptors ) are receptors at the surface of a cell (built into its cell membrane ) that act in cell signaling by receiving (binding to) extracellular molecules . (
  • Each cell membrane can have several kinds of membrane receptor, in varying surface distribution. (
  • A specific receptor may also be differently distributed on different membrane surfaces, depending on the membrane sort and cell function. (
  • Since receptors usually cluster on the membrane surface, [4] [5] the placement of every receptor on each membrane surface is heterogeneous. (
  • Rotation Model: Ligand binding to the extracellular part of the receptor induces the rotation of the receptor's transmembrane region inside the cell membrane, in doing so regulate it's activity inside the cell. (
  • Like any integral membrane protein, a transmembrane receptor may be divided into three domains. (
  • In certain receptors, such as the nicotinic acetylcholine receptor , the transmembrane domain forms a protein pore through the membrane, or around the ion channel . (
  • A family of peptides was synthesized to further study the role of acidic amino acids in peptide substrates of beta-ARK. (
  • [1] Nebivolol displays β1-adrenoceptor selectivity with the K i (β2)/K i (β1) value of 40.7 judged by competition experiments to 3 H-CGP 12.1777 in the presence of CGP 207.12 A (300 nM, K i β2) or ICI 118.551 (50 nM, K i β1). (
  • A , RT/PCR assay with total mRNA and ompA primers set 1 (nucleotides 1-1860). (
  • A molecular docking study revealed that the rac-5c analog showed higher affinities than propafenone in relation to beta 1 and beta 2 adrenergic receptors, as well as sodium channels. (
  • By kinetic analyses of the phosphorylation reactions, beta-ARK exhibited a marked preference for negatively charged amino acids localized to the NH2-terminal side of a serine or threonine residue. (
  • IQ 1 has many functions such as decreasing Wnt-stimulated phosphorylation, maintaining the pluripotency of murine ESCs, preventing PP2A/Nkd interaction and so on. (
  • IQ 1 decreased Wnt-stimulated phosphorylation of p300 at Ser-89. (
  • The binding of IQ 1 to PR72/130 leads to decreased phosphorylation of the coactivator protein p300 at Ser-89. (
  • Aryloxypropanolamine and catecholamine ligand interactions with the beta(1)-adrenergic receptor: evidence for interaction with distinct conformations of beta(1)-adrenergic receptors. (
  • Defective insulin secretion is a central feature in diabetes mellitus and results from reduced pancreatic beta-cell mass as well as aberrant beta-cell function. (
  • Impaired insulin release can be enhanced by the insulinotropic hormones PACAP and GLP-1. (
  • Patienter med typ 1-diabetes måste därför behandlas med insulin livet ut. (
  • 2015).It lowers the blood glucose acutely by stimulating the release of insulin from the pancreas, an effect dependent upon functioning beta cells in the pancreatic islets. (
  • Positive regulators of insulin secretion are stimulation of beta-2 and m3-acetylcholine receptors. (
  • GLP-1 increases glucose-dependent insulin release. (
  • The beta-2 receptor is present in pancreatic beta cells, and is responsible for stimulating insulin secretion. (
  • Muscarinic M3 receptors are part of the parasympathetic nervous system and can induce insulin secretion. (
  • The alpha-2 receptor is a part of the sympathetic system present in pancreatic beta cells and inhibits insulin secretion. (
  • It impacts the insulin axis more than other sympathetic receptors, including beta-2 receptors. (
  • GLP-1 works by binding to cell surface receptors coupled with G protein-adenylyl cyclase system and is degraded by dipeptidyl peptidase-4 (DPP-4). (
  • FFAs induce the activation of the peroxisome proliferator-activated receptor (PPAR)-alfa in the liver, resulting in the synthesis and release of FGF21. (
  • Bempedoic acid and its active metabolite, ESP15228, require coenzyme A (CoA) activation by very long?chain acyl-CoA synthetase 1 (ACSVL1) to ETC-1002-CoA and ESP15228-CoA, respectively. (
  • Requirement of beta-adrenergic receptor activation and protein synthesis for LTP-reinforcement by novelty in rat dentate gyrus. (
  • ICAM-1, VCAM-1, and MAdCAM-1 are expressed on choroid plexus epithelium but not endothelium and mediate binding of lymphocytes in vitro. (
  • Beta adrenergic receptors on cultured human retinal pigment epithelium. (
  • In the human heart the beta-1-AR is the pre- dominate receptor. (
  • 72 hours) inhibits, in a dose-dependent manner, forskolin-stimulated hCG-beta secretion in JEG-3 and BeWo cells but had no effect on basal human chorionic gonadotrophin (hCG-beta) levels [4] . (
  • Pharmacological characterization of human recombinant melatonin mt(1) and MT(2) receptors. (
  • Expression of melatoninergic receptors in human placental choriocarcinoma cell lines. (
  • CHIR 99021inhibits human GSK-3β with Ki values of 9.8 nM[1]. (
  • 25(1): 7-10 estimate autonomic nervous control of the in women with metabolic syndrome compared to cardiovascular system and reduced HRV significantly those without, while results in men were increases cardiovascular mortality9. (