Adenosine: A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter.Receptor, Adenosine A2A: A subclass of adenosine A2 receptors found in LEUKOCYTES, the SPLEEN, the THYMUS and a variety of other tissues. It is generally considered to be a receptor for ADENOSINE that couples to the GS, STIMULATORY G-PROTEIN.Receptor, Adenosine A1: A subtype of ADENOSINE RECEPTOR that is found expressed in a variety of tissues including the BRAIN and DORSAL HORN NEURONS. The receptor is generally considered to be coupled to the GI, INHIBITORY G-PROTEIN which causes down regulation of CYCLIC AMP.Adenosine A2 Receptor Antagonists: Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.Purinergic P1 Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.Adenosine A1 Receptor Antagonists: Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.Receptor, Adenosine A3: A subtype of ADENOSINE RECEPTOR that is found expressed in a variety of locations including the BRAIN and endocrine tissues. The receptor is generally considered to be coupled to the GI, INHIBITORY G-PROTEIN which causes down regulation of CYCLIC AMP.Adenosine Deaminase: An enzyme that catalyzes the hydrolysis of ADENOSINE to INOSINE with the elimination of AMMONIA.Interleukin 1 Receptor Antagonist Protein: 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.Receptor, Adenosine A2B: A subclass of adenosine A2 receptors found in the CECUM, the COLON, the BLADDER, and a variety of other tissues. It is generally considered to be a low affinity receptor for ADENOSINE that couples to the GS, STIMULATORY G-PROTEIN.Receptors, Purinergic P1: A class of cell surface receptors that prefer ADENOSINE to other endogenous PURINES. Purinergic P1 receptors are widespread in the body including the cardiovascular, respiratory, immune, and nervous systems. There are at least two pharmacologically distinguishable types (A1 and A2, or Ri and Ra).Receptors, Adenosine A2: A subclass of ADENOSINE RECEPTORS that are generally considered to be coupled to the GS, STIMULATORY G-PROTEIN which causes up regulation of CYCLIC AMP.Neurokinin-1 Receptor Antagonists: Compounds that inhibit or block the activity of NEUROKININ-1 RECEPTORS.Adenosine A2 Receptor Agonists: Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS.Adenosine Kinase: An enzyme that catalyzes the formation of ADP plus AMP from adenosine plus ATP. It can serve as a salvage mechanism for returning adenosine to nucleic acids. EC 2.7.1.20.Rats, Sprague-Dawley: 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.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.Xanthines: Purine bases found in body tissues and fluids and in some plants.Piperidines: A family of hexahydropyridines.Adenosine A1 Receptor Agonists: Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS.Purinergic P1 Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.Excitatory Amino Acid Antagonists: Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.Dopamine Antagonists: Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME.Angiotensin Receptor Antagonists: Agents that antagonize ANGIOTENSIN RECEPTORS. Many drugs in this class specifically target the ANGIOTENSIN TYPE 1 RECEPTOR.Serotonin 5-HT3 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT3 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT3 RECEPTOR AGONISTS.Muscarinic Antagonists: Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. Muscarinic antagonists have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system.Receptors, Serotonin: Cell-surface proteins that bind SEROTONIN and trigger intracellular changes which influence the behavior of cells. Several types of serotonin receptors have been recognized which differ in their pharmacology, molecular biology, and mode of action.Radioligand Assay: Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).Histamine H2 Antagonists: Drugs that selectively bind to but do not activate histamine H2 receptors, thereby blocking the actions of histamine. Their clinically most important action is the inhibition of acid secretion in the treatment of gastrointestinal ulcers. Smooth muscle may also be affected. Some drugs in this class have strong effects in the central nervous system, but these actions are not well understood.Rats, Wistar: A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.Serotonin 5-HT2 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT2 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT2 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more specific 5-HT2 receptor subtypes.Receptors, Endothelin: Cell surface proteins that bind ENDOTHELINS with high affinity and trigger intracellular changes which influence the behavior of cells.Adenosine A3 Receptor Antagonists: Compounds that selectively bind to and block the activation of ADENOSINE A3 RECEPTORS.Purinergic P2 Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.Serotonin Antagonists: Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.Hormone Antagonists: Chemical substances which inhibit the function of the endocrine glands, the biosynthesis of their secreted hormones, or the action of hormones upon their specific sites.Receptors, Somatostatin: Cell surface proteins that bind somatostatin and trigger intracellular changes which influence the behavior of cells. Somatostatin is a hypothalamic hormone, a pancreatic hormone, and a central and peripheral neurotransmitter. Activated somatostatin receptors on pituitary cells inhibit the release of growth hormone; those on endocrine and gastrointestinal cells regulate the absorption and utilization of nutrients; and those on neurons mediate somatostatin's role as a neurotransmitter.Adenosine-5'-(N-ethylcarboxamide): A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity.Receptors, Purinergic: Cell surface proteins that bind PURINES with high affinity and trigger intracellular changes which influence the behavior of cells. The best characterized classes of purinergic receptors in mammals are the P1 receptors, which prefer ADENOSINE, and the P2 receptors, which prefer ATP or ADP.Phenethylamines: A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)Adenosine Monophosphate: Adenine nucleotide containing one phosphate group esterified to the sugar moiety in the 2'-, 3'-, or 5'-position.Narcotic Antagonists: Agents inhibiting the effect of narcotics on the central nervous system.Cyclic AMP: 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.Theophylline: A methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant activities. Theophylline inhibits the 3',5'-CYCLIC NUCLEOTIDE PHOSPHODIESTERASE that degrades CYCLIC AMP thus potentiates the actions of agents that act through ADENYLYL CYCLASES and cyclic AMP.Receptor, Endothelin A: A subtype of endothelin receptor found predominantly in the VASCULAR SMOOTH MUSCLE. It has a high affinity for ENDOTHELIN-1 and ENDOTHELIN-2.Receptors, Muscarinic: One of the two major classes of cholinergic receptors. Muscarinic receptors were originally defined by their preference for MUSCARINE over NICOTINE. There are several subtypes (usually M1, M2, M3....) that are characterized by their cellular actions, pharmacology, and molecular biology.Serotonin Receptor Agonists: Endogenous compounds and drugs that bind to and activate SEROTONIN RECEPTORS. Many serotonin receptor agonists are used as ANTIDEPRESSANTS; ANXIOLYTICS; and in the treatment of MIGRAINE DISORDERS.Histamine Antagonists: Drugs that bind to but do not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists. Classical antihistaminics block the histamine H1 receptors only.Binding, Competitive: 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.Receptors, N-Methyl-D-Aspartate: A class of ionotropic glutamate receptors characterized by affinity for N-methyl-D-aspartate. NMDA receptors have an allosteric binding site for glycine which must be occupied for the channel to open efficiently and a site within the channel itself to which magnesium ions bind in a voltage-dependent manner. The positive voltage dependence of channel conductance and the high permeability of the conducting channel to calcium ions (as well as to monovalent cations) are important in excitotoxicity and neuronal plasticity.Histamine H1 Antagonists: Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.Guinea Pigs: A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.GABA Antagonists: Drugs that bind to but do not activate GABA RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.Pyridines: Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.GABA-A Receptor Antagonists: Drugs that bind to but do not activate GABA-A RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-A RECEPTOR AGONISTS.Cells, Cultured: 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.Benzazepines: Compounds with BENZENE fused to AZEPINES.Serotonin 5-HT1 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT1 RECEPTORS, thereby blocking the actions of SEROTONIN 5-HT1 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more of the specific 5-HT1 receptor subtypes.Nicotinic Antagonists: Drugs that bind to nicotinic cholinergic receptors (RECEPTORS, NICOTINIC) and block the actions of acetylcholine or cholinergic agonists. Nicotinic antagonists block synaptic transmission at autonomic ganglia, the skeletal neuromuscular junction, and at central nervous system nicotinic synapses.Adrenergic alpha-1 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.Receptors, Dopamine D2: A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D2-class receptor genes contain INTRONS, and the receptors inhibit ADENYLYL CYCLASES.Biphenyl CompoundsReceptors, Angiotensin: Cell surface proteins that bind ANGIOTENSINS and trigger intracellular changes influencing the behavior of cells.Peptides, Cyclic: Peptides whose amino and carboxy ends are linked together with a peptide bond forming a circular chain. Some of them are ANTI-INFECTIVE AGENTS. Some of them are biosynthesized non-ribosomally (PEPTIDE BIOSYNTHESIS, NON-RIBOSOMAL).Receptor, Endothelin B: A subtype of endothelin receptor found predominantly in the KIDNEY. It may play a role in reducing systemic ENDOTHELIN levels.Serotonin: A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator.Pirenzepine: An antimuscarinic agent that inhibits gastric secretion at lower doses than are required to affect gastrointestinal motility, salivary, central nervous system, cardiovascular, ocular, and urinary function. It promotes the healing of duodenal ulcers and due to its cytoprotective action is beneficial in the prevention of duodenal ulcer recurrence. It also potentiates the effect of other antiulcer agents such as CIMETIDINE and RANITIDINE. It is generally well tolerated by patients.Receptors, Neuropeptide Y: Cell surface proteins that bind neuropeptide Y with high affinity and trigger intracellular changes which influence the behavior of cells.RNA, Messenger: 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.Dizocilpine Maleate: A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.Neurons: 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.TetrazolesReceptors, Purinergic P2: A class of cell surface receptors for PURINES that prefer ATP or ADP over ADENOSINE. P2 purinergic receptors are widespread in the periphery and in the central and peripheral nervous system.Leukotriene Antagonists: A class of drugs designed to prevent leukotriene synthesis or activity by blocking binding at the receptor level.Sialoglycoproteins: 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.2-Chloroadenosine: 2-Chloroadenosine. A metabolically stable analog of adenosine which acts as an adenosine receptor agonist. The compound has a potent effect on the peripheral and central nervous system.Calcium: 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.Adenosine A3 Receptor Agonists: Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS.Indoles: Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.Adrenergic alpha-Antagonists: Drugs that bind to but do not activate alpha-adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists. Adrenergic alpha-antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma.Receptor, Muscarinic M3: A subclass of muscarinic receptor that mediates cholinergic-induced contraction in a variety of SMOOTH MUSCLES.Receptors, Prostaglandin E: Cell surface receptors which bind prostaglandins with a high affinity and trigger intracellular changes which influence the behavior of cells. Prostaglandin E receptors prefer prostaglandin E2 to other endogenous prostaglandins. They are subdivided into EP1, EP2, and EP3 types based on their effects and their pharmacology.Ketanserin: A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients.Purinergic Antagonists: Drugs that bind to and block the activation of PURINERGIC RECEPTORS.Endothelin-1: A 21-amino acid peptide produced in a variety of tissues including endothelial and vascular smooth-muscle cells, neurons and astrocytes in the central nervous system, and endometrial cells. It acts as a modulator of vasomotor tone, cell proliferation, and hormone production. (N Eng J Med 1995;333(6):356-63)Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.PyrrolidinesTime Factors: Elements of limited time intervals, contributing to particular results or situations.Signal Transduction: 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.Pyrazoles: Azoles of two nitrogens at the 1,2 positions, next to each other, in contrast with IMIDAZOLES in which they are at the 1,3 positions.Phenylisopropyladenosine: N-Isopropyl-N-phenyl-adenosine. Antilipemic agent. Synonym: TH 162.Behavior, Animal: The observable response an animal makes to any situation.Adrenergic alpha-2 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS.Azepines: Seven membered heterocyclic rings containing a NITROGEN atom.Receptors, Bradykinin: Cell surface receptors that bind BRADYKININ and related KININS with high affinity and trigger intracellular changes which influence the behavior of cells. The identified receptor types (B-1 and B-2, or BK-1 and BK-2) recognize endogenous KALLIDIN; t-kinins; and certain bradykinin fragments as well as bradykinin itself.PiperazinesQuinoxalinesReceptors, Vasopressin: Specific molecular sites or proteins on or in cells to which VASOPRESSINS bind or interact in order to modify the function of the cells. Two types of vasopressin receptor exist, the V1 receptor in the vascular smooth muscle and the V2 receptor in the kidneys. The V1 receptor can be subdivided into V1a and V1b (formerly V3) receptors.Receptors, Interleukin-1: Cell surface receptors that are specific for INTERLEUKIN-1. Included under this heading are signaling receptors, non-signaling receptors and accessory proteins required for receptor signaling. Signaling from interleukin-1 receptors occurs via interaction with SIGNAL TRANSDUCING ADAPTOR PROTEINS such as MYELOID DIFFERENTIATION FACTOR 88.Sulfonamides: A group of compounds that contain the structure SO2NH2.Receptors, Dopamine D1: A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D1-class receptor genes lack INTRONS, and the receptors stimulate ADENYLYL CYCLASES.Angiotensin II: An octapeptide that is a potent but labile vasoconstrictor. It is produced from angiotensin I after the removal of two amino acids at the C-terminal by ANGIOTENSIN CONVERTING ENZYME. The amino acid in position 5 varies in different species. To block VASOCONSTRICTION and HYPERTENSION effect of angiotensin II, patients are often treated with ACE INHIBITORS or with ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKERS.Receptor, Muscarinic M1: A specific subtype of muscarinic receptor that has a high affinity for the drug PIRENZEPINE. It is found in the peripheral GANGLIA where it signals a variety of physiological functions such as GASTRIC ACID secretion and BRONCHOCONSTRICTION. This subtype of muscarinic receptor is also found in neuronal tissues including the CEREBRAL CORTEX and HIPPOCAMPUS where it mediates the process of MEMORY and LEARNING.Drug Interactions: The action of a drug that may affect the activity, metabolism, or toxicity of another drug.Receptors, Cholecystokinin: Cell surface proteins that bind cholecystokinin (CCK) with high affinity and trigger intracellular changes influencing the behavior of cells. Cholecystokinin receptors are activated by GASTRIN as well as by CCK-4; CCK-8; and CCK-33. Activation of these receptors evokes secretion of AMYLASE by pancreatic acinar cells, acid and PEPSIN by stomach mucosal cells, and contraction of the PYLORUS and GALLBLADDER. The role of the widespread CCK receptors in the central nervous system is not well understood.Dioxanes: 1,4-Diethylene dioxides. Industrial solvents. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), dioxane itself may "reasonably be anticipated to be a carcinogen." (Merck Index, 11th ed)Endothelins: 21-Amino-acid peptides produced by vascular endothelial cells and functioning as potent vasoconstrictors. The endothelin family consists of three members, ENDOTHELIN-1; ENDOTHELIN-2; and ENDOTHELIN-3. All three peptides contain 21 amino acids, but vary in amino acid composition. The three peptides produce vasoconstrictor and pressor responses in various parts of the body. However, the quantitative profiles of the pharmacological activities are considerably different among the three isopeptides.Receptor, Muscarinic M2: A specific subtype of muscarinic receptor found in the lower BRAIN, the HEART and in SMOOTH MUSCLE-containing organs. Although present in smooth muscle the M2 muscarinic receptor appears not to be involved in contractile responses.Triazines: Heterocyclic rings containing three nitrogen atoms, commonly in 1,2,4 or 1,3,5 or 2,4,6 formats. Some are used as HERBICIDES.Substance P: An eleven-amino acid neurotransmitter that appears in both the central and peripheral nervous systems. It is involved in transmission of PAIN, causes rapid contractions of the gastrointestinal smooth muscle, and modulates inflammatory and immune responses.Receptor, Serotonin, 5-HT2A: A serotonin receptor subtype found widely distributed in peripheral tissues where it mediates the contractile responses of variety of tissues that contain SMOOTH MUSCLE. Selective 5-HT2A receptor antagonists include KETANSERIN. The 5-HT2A subtype is also located in BASAL GANGLIA and CEREBRAL CORTEX of the BRAIN where it mediates the effects of HALLUCINOGENS such as LSD.Molecular Sequence Data: 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.Cricetinae: A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.Imidazoles: Compounds containing 1,3-diazole, a five membered aromatic ring containing two nitrogen atoms separated by one of the carbons. Chemically reduced ones include IMIDAZOLINES and IMIDAZOLIDINES. Distinguish from 1,2-diazole (PYRAZOLES).CHO Cells: 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.Synaptic Transmission: The communication from a NEURON to a target (neuron, muscle, or secretory cell) across a SYNAPSE. In chemical synaptic transmission, the presynaptic neuron releases a NEUROTRANSMITTER that diffuses across the synaptic cleft and binds to specific synaptic receptors, activating them. The activated receptors modulate specific ion channels and/or second-messenger systems in the postsynaptic cell. In electrical synaptic transmission, electrical signals are communicated as an ionic current flow across ELECTRICAL SYNAPSES.Injections, Intraventricular: Injections into the cerebral ventricles.Receptors, Metabotropic Glutamate: Cell surface proteins that bind glutamate and act through G-proteins to influence second messenger systems. Several types of metabotropic glutamate receptors have been cloned. They differ in pharmacology, distribution, and mechanisms of action.Kinetics: The rate dynamics in chemical or physical systems.Receptors, Adrenergic, alpha-1: A subclass of alpha-adrenergic receptors that mediate contraction of SMOOTH MUSCLE in a variety of tissues such as ARTERIOLES; VEINS; and the UTERUS. They are usually found on postsynaptic membranes and signal through GQ-G11 G-PROTEINS.Receptors, GABA-A: 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.TriazolesBrain: 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.Receptors, Prostaglandin E, EP1 Subtype: A subtype of prostaglandin E receptors that specifically couples to GTP-BINDING PROTEIN ALPHA SUBUNIT, GQ and the subsequently activates TYPE C PHOSPHOLIPASES. Additional evidence has shown that the receptor can act through a calcium-dependent signaling pathway.Purinergic P2X Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P2X RECEPTORS. Included under this heading are antagonists for specific P2X receptor subtypes.Theobromine: 3,7-Dimethylxanthine. The principle alkaloid in Theobroma cacao (the cacao bean) and other plants. A xanthine alkaloid that is used as a bronchodilator and as a vasodilator. It has a weaker diuretic activity than THEOPHYLLINE and is also a less powerful stimulant of smooth muscle. It has practically no stimulant effect on the central nervous system. It was formerly used as a diuretic and in the treatment of angina pectoris and hypertension. (From Martindale, The Extra Pharmacopoeia, 30th ed, pp1318-9)Histamine: An amine derived by enzymatic decarboxylation of HISTIDINE. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and also a centrally acting neurotransmitter.Muscle, Smooth: Unstriated and unstriped muscle, one of the muscles of the internal organs, blood vessels, hair follicles, etc. Contractile elements are elongated, usually spindle-shaped cells with centrally located nuclei. Smooth muscle fibers are bound together into sheets or bundles by reticular fibers and frequently elastic nets are also abundant. (From Stedman, 25th ed)Receptors, Dopamine: Cell-surface proteins that bind dopamine with high affinity and trigger intracellular changes influencing the behavior of cells.Receptors, Neurokinin-1: A class of cell surface receptors for TACHYKININS with a preference for SUBSTANCE P. Neurokinin-1 (NK-1) receptors have been cloned and are members of the G protein coupled receptor superfamily. They are found on many cell types including central and peripheral neurons, smooth muscle cells, acinar cells, endothelial cells, fibroblasts, and immune cells.Receptors, Neurokinin-2: A class of cell surface receptors for tachykinins that prefers neurokinin A; (NKA, substance K, neurokinin alpha, neuromedin L), neuropeptide K; (NPK); or neuropeptide gamma over other tachykinins. Neurokinin-2 (NK-2) receptors have been cloned and are similar to other G-protein coupled receptors.Histamine H3 Antagonists: Drugs that selectively bind to but do not activate HISTAMINE H3 RECEPTORS. They have been used to correct SLEEP WAKE DISORDERS and MEMORY DISORDERS.Receptors, Prostaglandin E, EP4 Subtype: A subtype of prostaglandin E receptors that specifically couples to GS ALPHA GTP-BINDING PROTEIN SUBUNITS and subsequently activates ADENYLYL CYCLASES. The receptor may also signal through the activation of PHOSPHATIDYLINOSITOL 3-KINASE.Electric Stimulation: Use of electric potential or currents to elicit biological responses.Disease Models, Animal: 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.5'-Nucleotidase: A glycoprotein enzyme present in various organs and in many cells. The enzyme catalyzes the hydrolysis of a 5'-ribonucleotide to a ribonucleoside and orthophosphate in the presence of water. It is cation-dependent and exists in a membrane-bound and soluble form. EC 3.1.3.5.Mice, Inbred C57BLCimetidine: A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.Receptors, Corticotropin-Releasing Hormone: Cell surface proteins that bind corticotropin-releasing hormone with high affinity and trigger intracellular changes which influence the behavior of cells. The corticotropin releasing-hormone receptors on anterior pituitary cells mediate the stimulation of corticotropin release by hypothalamic corticotropin releasing factor. The physiological consequence of activating corticotropin-releasing hormone receptors on central neurons is not well understood.Receptors, Neurotransmitter: Cell surface receptors that bind signalling molecules released by neurons and convert these signals into intracellular changes influencing the behavior of cells. Neurotransmitter is used here in its most general sense, including not only messengers that act to regulate ion channels, but also those which act on second messenger systems and those which may act at a distance from their release sites. Included are receptors for neuromodulators, neuroregulators, neuromediators, and neurohumors, whether or not located at synapses.Receptors, Opioid: Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.Cell Line: Established cell cultures that have the potential to propagate indefinitely.BenzodiazepinonesNaltrexone: Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.Inosine: A purine nucleoside that has hypoxanthine linked by the N9 nitrogen to the C1 carbon of ribose. It is an intermediate in the degradation of purines and purine nucleosides to uric acid and in pathways of purine salvage. It also occurs in the anticodon of certain transfer RNA molecules. (Dorland, 28th ed)Receptor, Angiotensin, Type 2: An angiotensin receptor subtype that is expressed at high levels in fetal tissues. Many effects of the angiotensin type 2 receptor such as VASODILATION and sodium loss are the opposite of that of the ANGIOTENSIN TYPE 1 RECEPTOR.Adrenergic Antagonists: Drugs that bind to but do not activate ADRENERGIC RECEPTORS. Adrenergic antagonists block the actions of the endogenous adrenergic transmitters EPINEPHRINE and NOREPINEPHRINE.Blood Pressure: PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS.Bradykinin: A nonapeptide messenger that is enzymatically produced from KALLIDIN in the blood where it is a potent but short-lived agent of arteriolar dilation and increased capillary permeability. Bradykinin is also released from MAST CELLS during asthma attacks, from gut walls as a gastrointestinal vasodilator, from damaged tissues as a pain signal, and may be a neurotransmitter.Receptors, Dopamine D3: A subtype of dopamine D2 receptors that are highly expressed in the LIMBIC SYSTEM of the brain.Serotonin 5-HT4 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT4 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN RECEPTOR AGONISTS.Muscle Contraction: A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.Receptor, Angiotensin, Type 1: An angiotensin receptor subtype that is expressed at high levels in a variety of adult tissues including the CARDIOVASCULAR SYSTEM, the KIDNEY, the ENDOCRINE SYSTEM and the NERVOUS SYSTEM. Activation of the type 1 angiotensin receptor causes VASOCONSTRICTION and sodium retention.Glutamic Acid: A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.2-Amino-5-phosphonovalerate: The D-enantiomer is a potent and specific antagonist of NMDA glutamate receptors (RECEPTORS, N-METHYL-D-ASPARTATE). The L form is inactive at NMDA receptors but may affect the AP4 (2-amino-4-phosphonobutyrate; APB) excitatory amino acid receptors.Receptors, Thromboxane: Cell surface proteins that bind THROMBOXANES with high affinity and trigger intracellular changes influencing the behavior of cells. Some thromboxane receptors act via the inositol phosphate and diacylglycerol second messenger systems.Receptors, Histamine H3: A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H3 receptors were first recognized as inhibitory autoreceptors on histamine-containing nerve terminals and have since been shown to regulate the release of several neurotransmitters in the central and peripheral nervous systems. (From Biochem Soc Trans 1992 Feb;20(1):122-5)Oligopeptides: Peptides composed of between two and twelve amino acids.Ligands: 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)Rabbits: 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.Somatostatin: A 14-amino acid peptide named for its ability to inhibit pituitary GROWTH HORMONE release, also called somatotropin release-inhibiting factor. It is expressed in the central and peripheral nervous systems, the gut, and other organs. SRIF can also inhibit the release of THYROID-STIMULATING HORMONE; PROLACTIN; INSULIN; and GLUCAGON besides acting as a neurotransmitter and neuromodulator. In a number of species including humans, there is an additional form of somatostatin, SRIF-28 with a 14-amino acid extension at the N-terminal.GABA-B Receptor Antagonists: Drugs that bind to but do not activate GABA-B RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-B RECEPTOR AGONISTS.Receptors, Opioid, mu: A class of opioid receptors recognized by its pharmacological profile. Mu opioid receptors bind, in decreasing order of affinity, endorphins, dynorphins, met-enkephalin, and leu-enkephalin. They have also been shown to be molecular receptors for morphine.Dopamine: One of the catecholamine NEUROTRANSMITTERS in the brain. It is derived from TYROSINE and is the precursor to NOREPINEPHRINE and EPINEPHRINE. Dopamine is a major transmitter in the extrapyramidal system of the brain, and important in regulating movement. A family of receptors (RECEPTORS, DOPAMINE) mediate its action.Mice, Knockout: 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.Dogs: The domestic dog, Canis familiaris, comprising about 400 breeds, of the carnivore family CANIDAE. They are worldwide in distribution and live in association with people. (Walker's Mammals of the World, 5th ed, p1065)Receptors, Adrenergic, alpha-2: A subclass of alpha-adrenergic receptors found on both presynaptic and postsynaptic membranes where they signal through Gi-Go G-PROTEINS. While postsynaptic alpha-2 receptors play a traditional role in mediating the effects of ADRENERGIC AGONISTS, the subset of alpha-2 receptors found on presynaptic membranes signal the feedback inhibition of NEUROTRANSMITTER release.Hippocampus: A curved elevation of GRAY MATTER extending the entire length of the floor of the TEMPORAL HORN of the LATERAL VENTRICLE (see also TEMPORAL LOBE). The hippocampus proper, subiculum, and DENTATE GYRUS constitute the hippocampal formation. Sometimes authors include the ENTORHINAL CORTEX in the hippocampal formation.Dopamine Agonists: Drugs that bind to and activate dopamine receptors.Receptor, Metabotropic Glutamate 5: A type I G protein-coupled receptor mostly expressed post-synaptic pyramidal cells of the cortex and CENTRAL NERVOUS SYSTEM.Receptors, Nicotinic: 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.Muscarinic Agonists: Drugs that bind to and activate muscarinic cholinergic receptors (RECEPTORS, MUSCARINIC). Muscarinic agonists are most commonly used when it is desirable to increase smooth muscle tone, especially in the GI tract, urinary bladder and the eye. They may also be used to reduce heart rate.Bicuculline: An isoquinoline alkaloid obtained from Dicentra cucullaria and other plants. It is a competitive antagonist for GABA-A receptors.Vasoconstriction: The physiological narrowing of BLOOD VESSELS by contraction of the VASCULAR SMOOTH MUSCLE.Receptors, Tachykinin: Cell surface proteins that bind TACHYKININS with high affinity and trigger intracellular changes influencing the behavior of cells. Three classes of tachykinin receptors have been characterized, the NK-1; NK-2; and NK-3; which prefer, respectively, SUBSTANCE P; NEUROKININ A; and NEUROKININ B.Receptors, Prostaglandin: Cell surface receptors that bind prostaglandins with high affinity and trigger intracellular changes which influence the behavior of cells. Prostaglandin receptor subtypes have been tentatively named according to their relative affinities for the endogenous prostaglandins. They include those which prefer prostaglandin D2 (DP receptors), prostaglandin E2 (EP1, EP2, and EP3 receptors), prostaglandin F2-alpha (FP receptors), and prostacyclin (IP receptors).Receptors, G-Protein-Coupled: The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.Patch-Clamp Techniques: An electrophysiologic technique for studying cells, cell membranes, and occasionally isolated organelles. All patch-clamp methods rely on a very high-resistance seal between a micropipette and a membrane; the seal is usually attained by gentle suction. The four most common variants include on-cell patch, inside-out patch, outside-out patch, and whole-cell clamp. Patch-clamp methods are commonly used to voltage clamp, that is control the voltage across the membrane and measure current flow, but current-clamp methods, in which the current is controlled and the voltage is measured, are also used.Pyrilamine: A histamine H1 antagonist. It has mild hypnotic properties and some local anesthetic action and is used for allergies (including skin eruptions) both parenterally and locally. It is a common ingredient of cold remedies.Benzimidazoles: Compounds with a BENZENE fused to IMIDAZOLES.Receptors, Purinergic P2Y1: A subclass of purinergic P2Y receptors that have a preference for ATP and ADP. The activated P2Y1 receptor signals through the G-PROTEIN-coupled activation of PHOSPHOLIPASE C and mobilization of intracellular CALCIUM.N-Methylaspartate: An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).Receptor, Serotonin, 5-HT2B: A serotonin receptor subtype found in the BRAIN; HEART; LUNGS; PLACENTA and DIGESTIVE SYSTEM organs. A number of functions have been attributed to the action of the 5-HT2B receptor including the development of cardiac myocytes (MYOCYTES, CARDIAC) and the contraction of SMOOTH MUSCLE.Receptors, Opioid, kappa: A class of opioid receptors recognized by its pharmacological profile. Kappa opioid receptors bind dynorphins with a higher affinity than endorphins which are themselves preferred to enkephalins.Receptors, Prostaglandin E, EP2 Subtype: A subtype of prostaglandin E receptors that specifically couples to GS ALPHA GTP-BINDING PROTEIN SUBUNITS and subsequently activates ADENYLYL CYCLASES.Histamine Agonists: Drugs that bind to and activate histamine receptors. Although they have been suggested for a variety of clinical applications histamine agonists have so far been more widely used in research than therapeutically.Electrophysiology: The study of the generation and behavior of electrical charges in living organisms particularly the nervous system and the effects of electricity on living organisms.Receptor, Cannabinoid, CB1: A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.Norepinephrine: Precursor of epinephrine that is secreted by the adrenal medulla and is a widespread central and autonomic neurotransmitter. Norepinephrine is the principal transmitter of most postganglionic sympathetic fibers and of the diffuse projection system in the brain arising from the locus ceruleus. It is also found in plants and is used pharmacologically as a sympathomimetic.Bicyclo Compounds, Heterocyclic: A class of saturated compounds consisting of two rings only, having two or more atoms in common, containing at least one hetero atom, and that take the name of an open chain hydrocarbon containing the same total number of atoms. (From Riguady et al., Nomenclature of Organic Chemistry, 1979, p31)Receptor, Serotonin, 5-HT2C: A serotonin receptor subtype found primarily in the CENTRAL NERVOUS SYSTEM and the CHOROID PLEXUS. This receptor subtype is believed to mediate the anorectic action of SEROTONIN, while selective antagonists of the 5-HT2C receptor appear to induce ANXIETY. Several isoforms of this receptor subtype exist, due to adenine deaminase editing of the receptor mRNA.Devazepide: A derivative of benzodiazepine that acts on the cholecystokinin A (CCKA) receptor to antagonize CCK-8's (SINCALIDE) physiological and behavioral effects, such as pancreatic stimulation and inhibition of feeding.Capsaicin: An alkylamide found in CAPSICUM that acts at TRPV CATION CHANNELS.Adenylate Cyclase: An enzyme of the lyase class that catalyzes the formation of CYCLIC AMP and pyrophosphate from ATP. EC 4.6.1.1.Enzyme Inhibitors: Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.Receptors, Opioid, delta: A class of opioid receptors recognized by its pharmacological profile. Delta opioid receptors bind endorphins and enkephalins with approximately equal affinity and have less affinity for dynorphins.Motor Activity: The physical activity of a human or an animal as a behavioral phenomenon.QuinuclidinesAutoradiography: The making of a radiograph of an object or tissue by recording on a photographic plate the radiation emitted by radioactive material within the object. (Dorland, 27th ed)gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.

*Etazolate

... as an adenosine antagonist of the A1 and A2 subtypes, and as a phosphodiesterase inhibitor selective for the PDE4 isoform. It ... Zezula J, Slany A, Sieghart W (April 1996). "Interaction of allosteric ligands with GABAA receptors containing one, two, or ... ISBN 3-7643-1837-6. Williams M, Jarvis MF (February 1988). "Adenosine antagonists as potential therapeutic agents". ... It acts as a positive allosteric modulator of the GABAA receptor at the barbiturate binding site, ...

*Cartazolate

It is also known to act as an adenosine antagonist at the A1 and A2 subtypes and as a phosphodiesterase inhibitor. Cartazolate ... activity as antagonists of A1- and A2-adenosine receptors". Biochemical Pharmacology. 37 (4): 655-64. doi:10.1016/0006-2952(88) ... "Perturbation of benzodiazepine receptor binding by pyrazolopyridines involves picrotoxinin/barbiturate receptor sites". Journal ... O'Brien, Robert (1986). Receptor binding in drug research. New York: Dekker. p. 519. ISBN 0-8247-7548-1. US Patent 3966746 ...

*Adenosine A1 receptor

... an adenosine A1-receptor antagonist,on diuresis and renal function in patients with acute decompensated heart failure and renal ... "Localization of the adenosine A1 receptor subtype gene (ADORA1) to chromosome 1q32.1". Genomics. 26 (2): 423-5. doi:10.1016/ ... Caffeine may reduce cerebral blood flow in premature infants, it is presumed by blocking vascular A2 ARs. Thus, it may prove ... The adenosine A1 receptor is one member of the adenosine receptor group of G protein-coupled receptors with adenosine as ...

*Adenosine A2A receptor

"Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ... Older research on adenosine receptor function, and non-selective adenosine receptor antagonists such as aminophylline, focused ... "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ... As a result, Adenosine receptor A2A decreases activity in the Dopamine D2 receptors. The adenosine A2A receptor has also been ...

*DMPX

... is a caffeine analog which displays affinity to A2 adenosine receptors, in contrast to the A1 subtype receptors. DMPX had 28× ... a potent and selective in vivo antagonist of adenosine analogs. Life Sci. 1988;43(21):1671-84. PMID 3193854. ...

*Thromboregulation

TX2 effects are mediated by G protein-coupled receptors, subtypes TPα and TPβ. Both receptors mediate phospholipase C ... These signaling elements include thromboxane A2, receptor type α, phospholipase Cβ3, and IP3 receptors. Signalization in ... It belongs to the homologous family of glycoprotein IIb-IIa antagonists. Kistrin has an adhesion site that binds to GP IIb-IIIa ... cAMP, cyclic adenosine monophosphate, phosphorylate messengers via protein kinase A (PKA). ...

*Nociceptin receptor

"Modification of nociception and morphine tolerance by the selective opiate receptor-like orphan receptor antagonist (-)-cis-1- ... Fukuda K, Shoda T, Morikawa H, Kato S, Mima H, Mori K (1998). "Activation of phospholipase A2 by the nociceptin receptor ... In contrast to classical OPs, NOP also couples to Pertussis toxin (PTX)-insensitive subtypes Gαz, Gα14, and Gα16, as well as ... causing an intracellular decrease in cyclic adenosine monophosphate(cAMP) levels, an important second messenger for many signal ...

*Adenosine

All adenosine receptor subtypes (A1, A2A, A2B, and A3) are G-protein-coupled receptors. The four receptor subtypes are further ... The A1 receptors couple to Gi/o and decreases cAMP levels, while the A2 adenosine receptors couple to Gs, which stimulates ... This is being contended and it is now considered a relative contraindication (however, selective adenosine antagonists are ... Cellular signaling by adenosine occurs through four known adenosine receptor subtypes (A1, A2A, A2B, and A3). Extracellular ...

*Multiple electrode aggregometry

The GPIIb/IIIa antagonist blocks the binding of fibrinogen to the GPIIb/IIIa receptors, preventing the formation of platelet- ... Adenosine diphosphate (ADP) is a platelet agonist. When it is added to saline-diluted whole blood in the test cuvette, it ... This test can detect if vWF shows a stronger than normal tendency to aggregate platelets, which can be seen in a subtype of vWD ... and PGH2 is then converted to thromboxane A2 (TXA2) by thromboxane synthase. TXA2 increases platelet aggregation, promotes ...

*5-HT1D receptor

"Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ... mixed 5-HT1B/1D antagonist) LY-310,762 LY-367,642 LY-456,219 LY-456,220 5-HT1 receptor 5-HT receptor GRCh38: Ensembl release 89 ... 5-hydroxytryptamine (serotonin) receptor 1D, also known as HTR1D, is a 5-HT receptor, but also denotes the human gene encoding ... 5HT1D receptor is a G protein linked receptor that activates an intracellular messenger cascade to produce an inhibitory ...

*Molecular and epigenetic mechanisms of alcoholism

Nagy, J. (2004). The NR2B subtype of NMDA receptor: a potential target for the treatment of alcohol dependence. Curr Drug ... glutamate receptor antagonist on ethanol consumption by genetic drinking rats. Alcohol, 40, 494-497. Hodge, C.W., Miles, M.F., ... Katsura, M., Shibasaki, M., Hayashida, S., Torigoe, F., Tsujimura, A., Ohkuma, S. (2006) Increase in expression of a1 and a2/d1 ... Pandey, S.C., Roy, A., Zhang, H. (2003). The decreased phosphorylation of cyclic adenosine monophosphate (cAMP) response ...

*MicroRNA

Most commonly, enzymes known as adenosine deaminases acting on RNA (ADARs) catalyze adenosine to inosine (A to I) transitions. ... The specific microRNA, miR-506 has been found to work as a tumor antagonist in several studies. In a 2014 study, a significant ... miR-382 is the target for the dopamine receptor D1 (DRD1), and its overexpression results in the upregulation of DRD1 and delta ... December 2003). "High mobility group A2 protein and its derivatives bind a specific region of the promoter of DNA repair gene ...

*List of OMIM disorder codes

IGF1R Interleukin 1 receptor antagonist deficiency; 612852; IL1RN Interleukin-2 receptor, alpha chain, deficiency of; 606367; ... IHH Brachydactyly type A2; 112600; BMPR1B Brachydactyly type A2; 112600; GDF5 Brachydactyly type B1; 113000; ROR2 Brachydactyly ... APC Adenosine deaminase deficiency, partial; 102700; ADA Adenosine triphosphate, elevated, of erythrocytes; 102900; PKLR ... DDB-negative subtype; 278740; DDB2 Xeroderma pigmentosum group F; 278760; ERCC4 Xeroderma pigmentosum group G; 278780; ERCC5 ...
TY - JOUR. T1 - Chronic exposure to adenosine receptor agonists and antagonists reciprocally regulates the A1 adenosine receptor-adenylyl cyclase system in cerebellar granule cells. AU - Hettinger-Smith, Barbara D.. AU - Leid, Mark. AU - Murray, Thomas F.. PY - 1996/11. Y1 - 1996/11. N2 - Chronic treatment with the adenosine receptor antagonist caffeine evokes an ...
A concise synthesis of a series of N6-substituted adenosines with bicyclo[3.2.1]octan-6-yl and polycyclic N6-substituents has been developed. The adenosine A1 receptor (A1R) affinity and potency of these compounds was initially assessed using competitive binding assays and cyclic adenosine monophosphate (cAMP) accumulation assays in DDT1 MF-2 cells. The potency and receptor subtype selectivity of selected examples was ...
DESCRIPTION: (Adapted from the Investigators Abstract): Adenosine administered as an aerosol to asthmatics causes bronchoconstriction, while in non-asthmatics adenosine causes bronchodilation. This occurs because the activation of A2B adenosine receptors on sensitized mast cells triggers degranulation, releasing histamine, leukotrienes, and other allergic mediators. A2B ...
Iodotubercidin is an adenosine kinase inhibitor that through its ability to increase levels of endogenous adenosine can enhance adenosines receptor-mediated effects. We investigated whether iodotubercidin can inhibit [3H]adenosine accumulation by inhibiting transport processes in addition to inhibition of intracellular trapping of labeled adenine nucleotides. Under conditions in which extensive metabolism of intracellular adenosine ...
Objectives:. The overall goal of this proposal is to develop methods to achieve heart and vascular protection from ischemia and thus improve soldiers performance in adverse environment. The major hypothesis is that new approach and method can be developed to enhance resistance to stress-induced circulatory insufficiency and myocardial ischemia. The goals here are to determine whether a decreased adenosine transporter function is associated ...
Intravenously administered adenosine is rapidly cleared from the circulation via cellular uptake, primarily by erythrocytes and vascular endothelial cells. This process involves a specific transmembrane nucleoside carrier system that is reversible, nonconcentrative, and bidirectionally symmetrical. Intracellular adenosine is rapidly metabolized either via phosphorylation to adenosine monophosphate by ...
TY - JOUR. T1 - Attenuation of chronic pulmonary inflammation in A2B adenosine receptor knockout mice. AU - Zaynagetdinov, Rinat. AU - Ryzhov, Sergey. AU - Goldstein, Anna E.. AU - Yin, Huiyong. AU - Novitskiy, Sergey V.. AU - Goleniewska, Kasia. AU - Polosukhin, Vasiliy V.. AU - Newcomb, Dawn C.. AU - Mitchell, Daphne. AU - Morschl, Eva. AU - Zhou, Yang. AU - Blackburn, Michael R.. ...
Adenosine is a candidate sleep substance. It can be both a distress signal of importance in pathology and a physiological regulator. Key factors in determining which of these possibilities pertain are: (i) the number of receptors expressed, and (ii) the mechanisms that establish extracellular adenosine levels. The roles of adenosine are studied by means of antagonists and/or animals (mostly ...
Adenosine is a nucleoside that is composed of adenine and d-ribose. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. For instance, adenosine plays an important role in energy transfer - as adenosine triphosphate (ATP) and adenosine diphosphate (ADP). It also plays a role in ...
Previous in vitro studies have shown biphasic effects of adenosine on mast cell activity; however, the receptor subtypes that mediate the inhibitory effects of adenosine are still controversial (Peachell et al., 1991; Yip et al., 2009). Mast cells express two distinct Gs-coupled adenosine receptors; their biologic roles have not been comprehensively defined, especially in vivo. Since activation of Gs-coupled adenosine receptors increases ...
Having the ability to modulate lymphocyte entry into the central nervous system (CNS) would benefit patients with neuroinflammatory diseases. We have previously shown that extracellular adenosine regulates CNS entry of lymphocytes during experimental autoimmune encephalomyelitis (EAE), the animal model for the CNS inflammatory disease multiple sclerosis. For instance, while extracellular adenosine levels are vastly increased following ...
Vasodilator stress with adenosine or dipyridamole is an alternative to exercise stress with myocardial perfusion imaging for the detection of coronary artery disease. Although the safety of adenosine and dipyridamole has been well established, undesirable side effects including chest pain, headache, dyspnea, and atrioventricular conduction abnormalities do occur in a majority of patients.1-4 In addition, ...
Adenosine is the first drug of choice in the treatment of supraventricular arrhythmias. While the effects of adenosine on sympathetic nerve activity (SNA) have been investigated, no information is available on the effects on cardiac vagal nerve activity (VNA). We assessed in rats the responses of cardiac VNA, SNA and cardiovascular variables to intravenous bolus ...
We examined how the endogenous anticonvulsant adenosine might influence gamma-aminobutyric acid type A (GABA(A)) receptor stability and which adenosine receptors (ARs) were involved. Upon repetitive activation (GABA 500 microM), GABA(A) receptors, microtransplanted into Xenopus oocytes from neurosurgically resected epileptic human nervous tissues, exhibited an obvious ...
Introduction: Prior studies demonstrate that ischemic preconditioning (IP) alters adenosine metabolism. The significance of this effect is not fully understood, but evidence suggests that reduction in extracellular adenosine may represent use as an alternative fuel. Transformation into AMP/ADP may also replenish intracellular total adenine nucleotides (TAN), improving the potential high-energy phosphate bonds available in cells facing ...
To the Editor: Recently, Jeremias et al1 reported their studies comparing the vasodilator action of intracoronary injected adenosine with ATP in 6 healthy mongrel dogs. On the basis of a dose-response curve ranging from 10 to 100 μg, the authors conclude that adenosine and ATP are approximately equipotent vasodilators. Neither substance could induce maximal vasodilation, as assessed with postischemic hyperemia. Similar ...
Adenosine deaminase (ADA) is an enzyme involved in purine metabolism. It is needed for the breakdown of adenosine from food and for the turnover of nucleic acids in tissues. Present in virtually all mammalian cells, its primary function in humans is the development and maintenance of the immune system. Adenosine deaminase is considered one of the key enzymes of purine metabolism. Adenosine deaminase in humans is involved in the development ...
A review. The low affinity A2B adenosine receptor, like any other adenosine receptor subtype, belongs to the super-family of seven transmembrane domain G protein-coupled receptors (7TMs GPCR) and is classified by the GPCR database in the family of rhodopsin like receptors (Class A of GPCR). It has been cloned from various species, including rat and human, and its sequences are highly similar ...
We performed experiments to test the hypothesis that endogenous adenosine acts as an essential cofactor required for eliciting angiotensin II (Ang II)-induced afferent and/or efferent arteriolar vasoconstriction. Enalaprilat (2 mg IV) was administered to anesthetized rats to reduce endogenous Ang II levels. Kidneys and blood were harvested from these animals and used for study of renal microvascular function using the in vitro blood-perfused juxtamedullary ...
Preclinical studies have shown that the P2Y12 receptor antagonist ticagrelor can increase the extracellular concentration of the endogenous nucleoside adenosine by inhibiting the cellular uptake of adenosine via the equilibrative nucleoside transporter (ENT). This mechanism can contribute to the beneficial effects and to the side effects (dyspnea) of ticagrelor in patients with an acute myocardial infarction. In the current ...
The effect of (-)-N6-phenylisopropyl adenosine (PIA), a metabolically stable P1-receptor agonist, was investigated on guinea-pig isolated trachea. PIA showed two opposite effects: contraction, evident at low concentrations (10(-7) to 2-5 X 10(-6) M), and relaxation at higher doses. Relaxation by PIA was antagonized in an apparently competitive manner by two antagonists of ...
Preeclampsia is a prevalent pregnancy hypertensive disease with both maternal and fetal morbidity and mortality. Emerging evidence indicates that global placental DNA hypomethylation is observed in patients with preeclampsia and is linked to altered gene expression and disease development. However, the molecular basis underlying placental epigenetic changes in preeclampsia remains unclear. Using 2 independent ...
Pharmacologic stress with dipyridamole has provided useful diagnostic, as well as prognostic, information in patients undergoing thallium-201 myocardial perfusion imaging. With its ultrashort half-life and a potent and consistent vasodilator effect, adenosine may be the coronary vasodilator of choice with myocardial perfusion imaging.. Fifty-one healthy subjects and 93 patients with suspected coronary artery disease ...
Looking for online definition of adenosine deaminase in the Medical Dictionary? adenosine deaminase explanation free. What is adenosine deaminase? Meaning of adenosine deaminase medical term. What does adenosine deaminase mean?
Looking for online definition of cyclic adenosine monophosphate (cyclic AMP, cAMP, 3',5'-cAMP) in the Medical Dictionary? cyclic adenosine monophosphate (cyclic AMP, cAMP, 3',5'-cAMP) explanation free. What is cyclic adenosine monophosphate (cyclic AMP, cAMP, 3',5'-cAMP)? Meaning of cyclic adenosine monophosphate (cyclic AMP, cAMP, 3',5'-cAMP) medical term. What does cyclic adenosine ...
Adenosine monophosphate deaminase deficiency type 1, also called myoadenylate deaminase deficiency (MADD), is a recessive genetic metabolic disorder that affects approximately 1-2% of populations of European descent. It appears to be considerably rarer in Asian populations. The genetic form is caused by a defect in the gene for AMP deaminase though there is also an acquired form of AMP deficiency. ...
Purpose: : Traumatic optic neuropathy (TON) is an irreversible vision-threatening complication often found in head injuries. Following optic nerve trauma, the bodys innate immune cells scavenge the trauma site for debris while releasing cytokines that cause additional damage and cell death beyond that of the initial insult. While neuronal cell loss stemming directly from the initial insult is irreversible, the secondary inflammation from cytokine release may be prevented. The purpose of our ...
Synonyms for adenosine deaminase conjugated with polyethylene glycol in Free Thesaurus. Antonyms for adenosine deaminase conjugated with polyethylene glycol. 2 words related to adenosine: biochemistry, nucleoside. What are synonyms for adenosine deaminase conjugated with polyethylene glycol?
Concordant with data derived from A2A-null CD4+/CD25− (Fig. 4 D), proliferation responses of CD4+/CD25− T cells obtained from Cd39-null mice are exaggerated after 6 d of stimulation, which is coincident with the up-regulation of adenosine receptor A2A in CD4+/CD25− cells (Fig. 5 C). As a further confirmation of direct connections between CD39 expression and adenosine generation, effects of the addition of soluble exogenous NTPDases (apyrase grade VII) to Cd39-null T cell cultures were ...
TY - JOUR. T1 - Effect of adenosine and pertussis vaccine on lymphocyte response in vitro to phytohemmaglutinin in asthmatic and non-asthmatic subjects. AU - Hiratani, M.. AU - McCall, M. K.. AU - Chaperon, E. A.. AU - Townley, R. G.. PY - 1988/1/1. Y1 - 1988/1/1. N2 - Adenosine and pertussis vaccine each significantly suppresed the in vitro lymphocyte response to photohemagglutinin (PHA) in both asthmatic and non-asthmatic subjects. On the other hand, ...
The low-affinity A2B receptor is known to mediate proinflammatory effects of adenosine by up-regulating production of cytokines and growth factors. This view has been supported by a large body of evidence provided by pharmacological analysis of adenosine-dependent cytokine and growth factor secretion in various cells, tissues, and organs (8, 11, 13, 18, 31, 32, 33, 34, 35, 36, 37, 38). Pharmacological inhibition of A2B receptors ...
Lien vers Pubmed [PMID] - 25904549. J. Immunol. 2015 Jun;194(11):5312-9. Staphylococcus aureus is a common cause of bacterial infections in respiratory diseases. It secretes molecules to dampen host immunity, and the recently identified adenosine is one of these molecules. The type IIA secretory phospholipase A2 (sPLA2-IIA) is a host protein endowed with antibacterial properties, especially against Gram-positive bacteria such as S. aureus. However, the role of adenosine in ...
The mechanisms by which adenosine triphosphate, thrombin, and trypsin cause relaxation of vascular smooth muscle were investigated. Relaxation of the rat thoracic aorta with adenosine triphosphate, thrombin, and/or trypsin was associated with increased levels of cyclic guanosine monophosphate in both time- and concentration-dependent manners. Thrombin and trypsin did not alter cyclic adenosine monophosphate levels, ...
TY - JOUR. T1 - Excitation of rat locus coeruleus neurons by adenosine 5′-triphosphate. T2 - Ionic mechanism and receptor characterization. AU - Shen, Ke-Zhong. AU - North, R. A.. PY - 1993. Y1 - 1993. N2 - ATP and several congeners were applied to locus coeruleus neurons in slices cut from rat pons. Whole-cell recording of membrane current showed that ATP caused an inward current at -60 mV. Effective concentrations (applied by superfusion) were 3-300 μM, and the peak current ...
The uroepithelium lines the urinary bladder, urethra and the lower renal pelvis. It provides a tight blood-urine barrier that prevents the unregulated movement of solutes, ions and metabolites present in the urine. Apart from forming a robust barrier, a growing body of evidence supports the role of the uroepithelium as a sensory transducer that is sensitive to extracellular biochemical and mechanical stimuli. One of the mediators that is released from the uroepithelium and impacts ...
TY - JOUR. T1 - Conversion of a stem cell leukemia from a T-lymphoid to a myeloid phenotype induced by the adenosine deaminase inhibitor 2-deoxycoformycin. AU - Hershfield, M. S.. AU - Kurtzberg, J.. AU - Harden, E.. AU - Moore, J. O.. AU - Whang-Peng, J.. AU - Haynes, B. F.. PY - 1984/3/22. Y1 - 1984/3/22. N2 - Selective failure of lymphoid development occurs in genetic deficiency of adenosine deaminase (ADA). We examined the in vivo effects of a potent inhibitor of ADA, 2-deoxycoformycin, which was used to ...
A sensitive and robust LC-MS/MS method was developed to quantify basal adenosine concentrations in human plasma of patients undergoing on-pump coronary artery bypass grafting (CABG) surgery. A strong cation exchange (SCX) monolithic cartridge was used to enrich analyte, improve robustness, and reduce biological complexity. A simple modifier-free mobile phase was employed to improve sensitivity and reproducibility. This method exhibits consistent precision and ...
TY - JOUR. T1 - Increased adenosine in cerebrospinal fluid after severe traumatic brain injury in infants and children. T2 - Association with severity of injury and excitotoxicity. AU - Robertson, Courtney. AU - Bell, M. J.. AU - Kochanek, P. M.. AU - Adelson, P. D.. AU - Ruppel, R. A.. AU - Carcillo, J. A.. AU - Wisniewski, S. R.. AU - Mi, Z.. AU - Janesko, K. L.. AU - Clark, R. S B. AU - Marion, D. W.. AU - Graham, S. H.. ...
Exogenous administration of adenosine induces atrial fibrillation in up to 7.0% of patients. Animal studies affirm endogenous adenosine released in response to tissue hypoxia may play a mechanistic role in arrhythmias associated with myocardial ischaemia or hypoxia. Therefore, atrial fibrillation occurring early after the acute phase of myocardial infarction involving ...
Hereditary hemolytic anemia, a dominantly transmitted disorder, has affected 12 family members spanning three generations. The concentration of adenosine triphosphate in the red cells was about half that of comparably reticulocyte-rich blood. Since adenosine deaminase and adenosine kinase compete for a common substrate, the greatly increased activity of the former may interfere with nucleotide ...
Adenosine uptake via nucleoside transporters is inhibited when S49 and NG108-15 cell lines cells are exposed to ethanol. This inhibition leads to an accumulation of extracellular adenosine that binds to adenosine A2 receptors and increases cAMP production. Subsequently, there is a heterologous desensitization of receptors coupled to adenylyl cyclase for which adenosine also is required. There are multiple ...
In collaboration with Dr. Tarja Porkka-Heiskanen, we tested the role of nitric oxide (NO) in sleep homeostasis by using in vivo microdialysis to administer compounds into the rat basal forebrain that increase or decrease concentrations of NO. Consistent with our hypothesis, we found that nitric oxide production is required for the production of NREM recovery sleep following sleep deprivation. However, using specific inhibitors of nitric oxide synthases, we found that iNOS rather than nNOS produced the nitric oxide involved in homeostatic sleep regulation. The generation of ...
TY - JOUR. T1 - Structural basis for the growth factor activity of human adenosine deaminase ADA2. AU - Zavialov, Anton V.. AU - Yu, Xiaodi. AU - Spillmann, Dorothe. AU - Lauvau, Grégoire. AU - Zavialo, Andrey V.. PY - 2010/4/16. Y1 - 2010/4/16. N2 - Two distinct adenosine deaminases, ADA1 and ADA2, are found in humans. ADA1 has ...
The existence of a prejunctional adenosine receptor, termed A 3 , was originally proposed on the basis of antagonist effects in the frog neuromuscular junction by Riberio and Sebastiao [20}, since the rank-order activity of antagonists in this preparation did not correlate with either Al or Az receptor pharmacology. At the Purines 92 meeting in Milan (I5}, the evidence for the existence of this receptor was discussed and, ...
DZNep was previously reported to be a selective inhibitor of H3K27 and H4K20 trimethylation (13). However, that study focused only on the methylation of H3K27, H3K9, and H4K20, whereas we have expanded the study to include other histone methylation modifications. Our extended study shows that DZNep is not a selective inhibitor of H3K27me3 and H4K20me3 as previously reported (13). Instead DZNep was found to globally inhibit both repressive and active histone methylation marks. In addition, we tested other AdoHcy hydrolase and global ...
Incubation of human erythrocytes in medium containing inosine (10 mM), pyruvate (10 mM), phosphate (50 mM) and NaCl (75 mM) at pH 6.6 leads to a more than 1000-fold increase in the concentration of 5-phosphoribosyl 1-pyrophosphate (PRPP), as identified and quantified by 31P-n.m.r. spectroscopy. The accumulation is highly pH-dependent, with a maximum at extracellular pH 6.60, and the maximum value of 1.3-1.6 mmol/l of erythrocytes is attained within 1 h at 37 degrees C. PRPP was ...
Double-stranded RNA-specific adenosine deaminase is an enzyme that in humans is encoded by the ADAR gene (which stands for adenosine deaminase acting on RNA). Adenosine deaminases acting on RNA (ADAR) are enzymes responsible for binding to double stranded RNA (dsRNA) and converting adenosine (A) to inosine (I) by deamination. ADAR protein is a ...
The development, maintenance and repair of the skeletal system are dependent on the differentiation of both chondrocytes and osteoblasts from their common progenitor, the mesenchymal stem cell (MSC). The A2B adenosine receptor (A2BAR) is a G-protein-coupled receptor that signals by increasing cAMP and/or activating phospholipase C signaling. Considering the published roles of cAMP on MSC differentiation, and our finding that the expression of the ...
Abstract: RNA editing by the adenosine deaminase acting on RNA (ADAR) enzymes has been associated with many human neurological diseases including: epilepsy; suicidal depression; autism; pediatric glioblastoma; and ALS (Lou Gehrigs disease). RNA editing is ubiquitous in the animal kingdom. ADAR deaminates the RNA base adenosine (A) to inosine (I) in dsRNA ...
TY - JOUR. T1 - Adenosine and inosine exert cytoprotective effects in an in vitro model of liver ischemia-reperfusion injury. AU - Modis, Katalin. AU - Gero, Domokos. AU - Stangl, Rita. AU - Rosero, Olivér. AU - Szijártó, Attila. AU - Lotz, Gábor. AU - Mohácsik, Petra. AU - Szoleczky, Petra. AU - Coletta, Ciro. AU - Szabo, Csaba. PY - 2013/2. Y1 - 2013/2. N2 - Liver ischemia represents a common clinical problem. In the present study, using an in vitro model of hepatic ...
article{2286a0f7-5934-41f8-aed8-94b7a8b75a40, abstract = {Recent studies indicate a severely reduced coronary flow reserve (CFR) in neonates with congenital heart disease. The significance of these studies remains debatable, as the ability of the anatomically normal neonatal heart to increase coronary flow is currently unknown. This study was designed to establish normal values for CFR in newborns after ...
Perspective: Systemic right ventricles are at high risk of contractile dysfunction, the cause of which is still unclear. The chronic exposure of the morphological right ventricle to systemic pressure leads to significant hypertrophy. Ischaemia has been postulated to contribute to the right ventricular systolic dysfunction by a number of mechanisms. Supply demand mismatch from an inadequate coronary circulation to support the hypertrophied right ventricle may contribute. In addition, systemic arterial hypoxaemia in the ...
TY - JOUR. T1 - Regulation of hippocampal cannabinoid CB1 receptor actions by adenosine A1 receptors and chronic caffeine administration. T2 - implications for the effects of Δ9-tetrahydrocannabinol on spatial memory. AU - Sousa, Vasco C. AU - Assaife-Lopes, Natália. AU - Ribeiro, Joaquim A. AU - Pratt, Judith A. AU - Brett, Ros R. AU - ...
Methods Thirty-two male Sprague-Dawley rats (310-360 g) were anaesthetised and divided into four equal groups (n=8 each): Saline, Saline+MA, Theophylline, and Theophylline+MA. In the two MA groups, the sparrow-pecking MA technique was applied at 30 repetitions per min for 1 min to a depth of 15-18 mm using a stainless steel acupuncture needle (0.20×40 mm). The stimulus point was located on the right tibialis anterior (TA) muscle 7-8 mm below the knee. Animals in the two theophylline groups ...
... of procedure notching arbitrary due total ob or striking flood. Bini S, Khatod M, Cafri G, Chen Y, Paxton EW. Surgeon, read Adenosine, and above goals may reflect year in personal engine Protocols required for guilty metal. Gioe TJ, Novak C, Sinner scholarship, Ma W, Mehle S. Knee half in the previous insurance: fl in a n company. BMC Musculoskelet Disord 2014 Nov 22; 15:390. Department of Orthopaedic Surgery, Chang Gung Memorial Hospital, 6, West Section, Chia-Pu Road, Pu-Tz City, ...
Diadenosine triphosphate is present in platelet-dense granules and released quantitatively on platelet aggregation. We have found that intact porcine aortic endothelial cells can efficiently hydrolyze extracellular diadenosine triphosphate. The products of diadenosine triphosphate hydrolysis are adenosine monophosphate and adenosine diphosphate. Adenosine diphosphate is a ...
Adenosine is an important mediator of the endogenous defense against ischemia-induced injury in the heart. Adenosine can achieve cardioprotection by mediating the effect of ischemic preconditioning and by protecting against myocyte injury when it is present during the infarct-producing ischemia. A novel adenosine A3 receptor can mediate this protective function. One approach to achieve cardioprotection is to enhance ...
Introduction: The use of biological markers in the diagnosis of tuberculous pleural effusion (TPE) is a breakthrough. Demonstration of elevated levels of Pleural fluid Adenosine deaminase (ADA), interferon-gamma (IFN-γ), tuberculous proteins/antibodies lysozme etc. have been proposed. Adenosine deaminase (ADA) estimation in pleural fluid has been shown as reliable biomarker specially when there is suspicion of tuberculosis. Detection of mycobacterium ...
Smith, C., G.; Lee, S., J.; Marquardt, D., L., 1995: Effects of Tubercidin and its 5'-O-Methyl Ether on Adenosine Receptors and Mediator Release Functions in Mast Cells
Adenosine is an endogenously released purine nucleoside that signals through four widely expressed G protein-coupled receptors: A1, A2A, A2B, and A3. Of these, A2AR is recognized as mediating major adenosine anti-inflammatory activity. During cutaneous leishmaniasis, adenosine induces immunosuppression, which promotes the establishment of infection. Herein, we demonstrated that A2AR signaling is exploited by ...
Extracellular adenosine triphosphate: A potential regulator of vasa vasorum neovascularization in hypoxia-induced pulmonary vascular remodeling ...
TY - JOUR. T1 - Inhibition by adenosine A(2A) receptors of NMDA but not AMPA currents in rat neostriatal neurons. AU - Wirkner, Kerstin. AU - Assmann, Heike. AU - Köles, L.. AU - Gerevich, Zoltan. AU - Franke, Heike. AU - Nörenberg, Wolfgang. AU - Boehm, Rudolf. AU - Illes, Peter. PY - 2000. Y1 - 2000. N2 - 1. Whole-cell patch clamp experiments were used to investigate the transduction mechanism of adenosine A(2A) ...
Units of blood were divided into 5 aliquots and were stored at 4 C. in ACD without additive or supplemented with adenine, inosine, inosine adenine, or adenosine. Adenine and nucleoside were added in an amount of 0.75 and 15 micro moles per ml ACD-blood, respectively. After storage for 6 weeks, 24 hour post-transfusion survival of the erthrocytes was determined. Survival of the erthrocytes was significantly increased when the ACD was supplemented with any of the additives. There was, however, no ...
Clinical Application of the Adenosine Triphosphate-based Response Assay in Intravesical Chemotherapy for Superficial Bladder Cancer Adenosine triphosphate;chemotherapy response assay;superficial bladder cancer; Objective: To investigate correlations between adenosine triphosphate chemotherapy response assay (ATP-CRA) and clinical outcomes after ...
Myocardial perfusion reserve (hyperemic divided by basal myocardial blood flow) describes vasodilator responsiveness of coronaryresistive vessels. The effect of aging and gender on myocardial perfusion reserve remains controversial. Methods: We studied 56 normal volunteers (21 women, 35 men; aged 50 +/- 20 yr, range 21-86 yr) with O-15-water PET to measure myocardial blood flow during basal and hyperemic stales with intravenous dipyridamole (0.56 mg/kg, n = 46) or adenosine (140 mu g/kg/min, n = 10). For ...
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When given for the evaluation or treatment of a supraventricular tachycardia (SVT), the initial dose is 6 mg, given as a rapid parenteral infusion. Due to adenosines extremely short half-life, the IV line is started as proximal (near) to the heart as possible, such as the cubital fossa. The IV push is often followed with an immediate flush of 10-20 ccs of saline. If this has no effect (i.e., no evidence of transient AV block), a dose of 12 ...
In this study, we demonstrated that administration of exogenous adenosine or inhibition of ADA in the TMN suppressed the histaminergic arousal system and increased the amount of NREM sleep. This effect was mimicked by activation of A1R with its agonist CPA and abolished with the antagonist CPT. These findings clearly indicate that A1R mediates the inhibition of the TMN by adenosine to promote NREM sleep. Murillo-Rodriguez et al. (26) reported that ...
Alkylxanthine drugs, such as theophylline, block adenosine receptors, inhibit phosphodiesterases and other enzymes, and cause the release of calcium from intracellular stores. Adenosine receptor blockade occurs at low micromolar concentrations of the drugs, while other effects occur in the millimolar concentration range. The effects of theophylline were tested on spontaneous transmitter release at the frog cutaneous-pectoris neuromuscular junction (NMJ). A ...
The formation of new lymphatic vessels, or lymphangiogenesis, is a natural process involved in tissue repair and in the resolution of inflammatory reactions. In some cancers, this process is exploited by the tumor to promote its growth and its metastatic dissemination. Our group recently identified a role for the CD73-adenosine pathway in tumor angiogenesis. As angiogenesis and lymphangiogenesis are similar processes, often occurring in parallel, we suspect that the ...
A ketogenic diet (KD) is a high-fat, low-carbohydrate metabolic regimen; its effectiveness in the treatment of refractory epilepsy suggests that the mechanisms underlying its anticonvulsive effects differ from those targeted by conventional antiepileptic drugs. Recently, KD and analogous metabolic strategies have shown therapeutic promise in other neurologic disorders, such as reducing brain injury, pain, and inflammation. Here, we have shown that KD can reduce seizures in mice by increasing ...
Adenosine mediates many physiological functions via activation of extracellular receptors. The modulation of cell growth by adenosine was found to be receptor-mediated. In A431 cells adenosine evoked a biphasic response in which a low concentration (~10 μM) produced inhibition of colony formation but at higher concentrations (up to 100 μM) this inhibition was progressively reversed. Evidence for the involvement of A1 (inhibitory) and A2 ...
Diagnostic value of pleural fluid interferon-gamma and adenosine deaminase in patients with pleural tuberculosis in Qatar Fahmi Yousef Khan,1 Maha Hamza,2 Aisha Hussein Omran,2 Muhannad Saleh,2 Mona Lingawi,2 Adel Alnaqdy,3 Mohamed Osman Abdel Rahman,3 Hasan Syed Ahmedullah,4 Alan ...
The main conclusion of this prospective study is that in patients with adenosine-sensitive syncope, the mechanism of syncope is heterogeneous, although bradycardia is the most frequent finding. The causal relationship between ATP-induced AV block and syncope due to paroxysmal AV block is weak. Atrioventricular block induced by ATP predicts AV block as the mechanism of spontaneous syncope in only a few tilt-negative cases.. At the time of ILR-documented syncope, about ...
Both TAR DNA binding protein of 43kDa (TDP-43) pathology and failure of RNA editing at the glutamine/arginine (Q/R) site of GluA2, a subunit of the α-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptor, are the characteristic etiology-linked molecular abnormalities that concomitantly occur in the motor neurons of the majority of patients with amyotrophic lateral sclerosis (ALS), the most common adult-onset ...
Myocardial perfusion imaging (MPI), using single photon emission computed tomography (SPECT) is a validated method for detecting coronary artery disease. Transthoracic Doppler echocardiography (TTDE) of flow at rest and during adenosine provocation has previously been evaluated in selected patient groups. We therefore wanted to compare the diagnostic ability of TTDE in the left anterior descending coronary artery (LAD) to that of MPI in an unselected ...
Safety in using adenosine (Hello care moisturizing ampoule mask). astellas pharma inc. is making packaging and sale items of a series impedances of various drugs including adenosine. Safety in using adenosine (Dr. gloderm tabrx liftup mask).. Adenosine triphosphate can also be found in iniquity the catalog distributed by its producer astellas pharma us inc. Interactions are ...
Intra- and extracellular adenosine levels rise in response to physiological stimuli and with metabolic/energetic perturbations, inflammatory challenge and tissue injury. Extracellular adenosine engages members of the G-protein coupled adenosine receptor (AR) family to mediate generally beneficial acute and adaptive responses within all constituent cells of the heart. In this way the four AR sub-types - ...
Irritable bowel syndrome (IBS) is a functional gastrointestinal disorder, with the characteristic symptoms of chronic abdominal pain and altered bowel habits (diarrhea, constipation, or both). IBS is a highly prevalent condition, which negatively affects quality of life and is a significant burden on global healthcare costs. Although many pharmacological medicines have been proposed to treat IBS, including those targeting ...
PubMed comprises more than 30 million citations for biomedical literature from MEDLINE, life science journals, and online books. Citations may include links to full-text content from PubMed Central and publisher web sites.
immune Uncategorized 3-deazaneplanocin A HCl manufacture, Mouse monoclonal to CD106(PE) Background Successful reduction of malaria transmission to very low levels has made Isabel Province, Solomon Islands, a target for early elimination by 2014. qualitative research methods. Results Approximately 33% (8,554/26,221) 3-deazaneplanocin A HCl manufacture of the population of Isabel Province participated in the ...
Caffeine is a naturally occurring methylxanthine that acts as a non-selective adenosine receptor antagonist. Epidemiological studies demonstrated habitual coffee drinking to be significantly associated with liver cancer survival. We aimed to investigate the effects of caffeine and its analog CGS 15943 on hepatocellular carcinoma (HCC) and pancreatic cancer ...
TY - JOUR. T1 - Performance of computed tomography-derived fractional flow reserve using reduced-order modelling and static computed tomography stress myocardial perfusion imaging for detection of haemodynamically significant coronary stenosis. AU - Ihdayhid, Abdul Rahman. AU - Sakaguchi, Takuya. AU - Linde, Jesper J.. AU - Sørgaard, Mathias H.. AU - Kofoed, Klaus F.. AU - Fujisawa, Yasuko. ...
Adenosine is an endogenous nucleoside occurring in all cells of the body and is not chemically related to other antiarrhythmic drugs. Adenosine is indicated for the conversion to sinus rhythm of paroxysmal supraventricular tachycardia (PSVT), including that associated with accessory bypass tracts (Wolff-Parkinson-White Syndrome). Adenosine is antagonized competitively by methylxanthines such as caffeine and theophylline, and ...
Mediates both influx and efflux of nucleosides across the membrane (equilibrative transporter). It is sensitive (ES) to low concentrations of the inhibitor nitrobenzylmercaptopurine riboside (NBMPR) and is sodium-independent. It has a higher affinity for adenosine. Resistant to dipyridamole and dilazep inhibition (anticancer chemotherapeutics drugs).
The increases in choroidal thickness observed in the 7-MX-treated monkeys do not necessarily rule out the possibility that the primary site of action of 7-MX is the sclera. However, given that the choroid is a critical component in the vision-dependent cascade that mediates normal refractive development, it is possible that 7-MX affects refractive development by influencing or altering the operational properties of this emmetropization cascade. A large body of evidence supports the hypothesis that vision-dependent ...
We found that the modified nucleosides 5,6-dihydrouridine (DHU), Ψ, acp3U, 3-methylcytidine (m3C), 5-methyluridine (m5U), 3-methyluridine (m3U), xanthosine (X), 1-methylguanosine (m1G), m22G, N2,N2,7-trimethylguanosine (m2,2,7G), mcm5s2U, N6-threonylcarbamoyladenosine (t6A) and m6t6A are elevated in the supernatants of MCF-7 cells compared to those of MCF-10A cells. Therefore, we generally considered a compound level as "elevated" when the area ratio exceeds the mean value of the reference cell line by two standard ...
The bacterial 5-methylthioadenosine/S-adenosylhomocysteine nucleosidase (MTAN) enzyme is a multifunctional enzyme that catalyzes the hydrolysis of the N-ribosidic bond of at least four different adenosine-based metabolites: S-adenosylhomocysteine (S
TY - JOUR. T1 - Cardiac transplantation after prolonged graft preservation with the University of Wisconsin solution. AU - Jeevanandam, V.. AU - Auteri, J. S.. AU - Sanchez, J. A.. AU - Hsu, Daphne T.. AU - Marboe, C.. AU - Smith, C. R.. AU - Rose, E. A.. PY - 1992. Y1 - 1992. N2 - We tested the ability of University of Wisconsin solution to extend hypothermic preservation of the nonperfused heart during orthotopic baboon allotransplantation. Seven baboons ...
The 105,000 x g supernatant fluid (S[subscript HS]) from extracts of pea seedlings (Pisum sativum, var. Alaska) etiolated for 60 hours yielded a very potent adenosine triphosphatase activity. This activity was designated as an apyrase when the reaction stoichiometry indicated that adenosine triphosphate (ATP) was hydrolyzed to adenosine monophosphate (AMP) and two moles of inorganic ...
The report displayed here plans showcase players to make steady progress while adequately managing one of a kind difficulties in the worldwide Adenosine advertise. The examiners and analysts creating the report have thought about different elements anticipated to emphatically and contrarily sway the worldwide Adenosine advertise. The report incorporates SWOT and PESTLE investigations to give a more profound comprehension of ...
Synonyms for adenosine 5'-diphosphate in Free Thesaurus. Antonyms for adenosine 5'-diphosphate. 1 synonym for adenosine diphosphate: ADP. What are synonyms for adenosine 5'-diphosphate?
TY - JOUR. T1 - Adenosine 5′-triphosphate activates nuclear translocation of mitogen-activated protein kinases leading to the induction of early growth response 1 and Raf expression in human granulosa-luteal cells. AU - Tai, Chen Jei. AU - Chang, Shu Ju. AU - Leung, Peter C K. AU - Tzeng, Chii Ruey. PY - 2004/10. Y1 - 2004/10. N2 - With the stimulation of many types of cell surface receptors, MAPKs are activated. We have ...
Read A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics by with Rakuten Kobo. This book, with its 16 chapters, documents the present state of knowledge of the adenosine A receptor. It covers a wide ...
Treatments with Poly(adenosine diphosphate ribose) polymerase (PARP) inhibitors have offered patients carrying cancers with mutated BRCA1 or BRCA2 genes a new and in many cases effective option for disease control. There is potentially a large patient population that may also benefit from PARP inhibitor treatment, either in monotherapy or in combination with chemotherapy. Here, we describe the multifaceted role of PARP inhibitors and discuss ...
Zinc adenosine triphosphate - Surfactant - SAAPedia - SAAPedia(Surfactant.TOP),Surfactant,Anionic surfactants, Cationic surfactants, Non-ionic surfactants, Zwitterionic surfactants, Polymer Surfactants, Fluoro surfactants, Silicone surfactants, Biosurfactants, Natural surfactants, Special surfactants - Page1
Copper Adenosine Triphosphate - Surfactant - SAAPedia - SAAPedia(Surfactant.TOP),Surfactant,Anionic surfactants, Cationic surfactants, Non-ionic surfactants, Zwitterionic surfactants, Polymer Surfactants, Fluoro surfactants, Silicone surfactants, Biosurfactants, Natural surfactants, Special surfactants - Page1
[05-06-2011] The U.S. Food and Drug Administration (FDA) is alerting the healthcare community about syringe connection problems when certain needleless glass syringes containing the cardiac drugs adenosine and amiodarone are used with particular types of intravenous (IV) access systems.
A nucleoside that is composed of adenine and d-ribose. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter.
3-(2,4,4-trimethylpentan-2-ylamino)propanenitrile chemical properties, What are the chemical properties of 3-(2,4,4-trimethylpentan-2-ylamino)propanenitrile 86375-28-2, What are the physical properties of 3-(2,4,4-trimethylpentan-2-ylamino)propanenitrile ect.

Etazolate - WikipediaEtazolate - Wikipedia

... as an adenosine antagonist of the A1 and A2 subtypes, and as a phosphodiesterase inhibitor selective for the PDE4 isoform. It ... Zezula J, Slany A, Sieghart W (April 1996). "Interaction of allosteric ligands with GABAA receptors containing one, two, or ... ISBN 3-7643-1837-6. Williams M, Jarvis MF (February 1988). "Adenosine antagonists as potential therapeutic agents". ... It acts as a positive allosteric modulator of the GABAA receptor at the barbiturate binding site, ...
more infohttps://en.wikipedia.org/wiki/Etazolate

Activation of metabotropic glutamate receptors increases cAMP accumulation in hippocampus by potentiating responses to...Activation of metabotropic glutamate receptors increases cAMP accumulation in hippocampus by potentiating responses to...

Additionally, adenosine receptor antagonists blocked mGluR-mediated increases in cAMP accumulation with potencies that were ... highly correlated with their potencies at A2 adenosine receptors. Furthermore, we performed a series of studies that suggest ... ACPD activates an mGluR subtype that potentiates responses to agonists of other receptors that are coupled to adenylate cyclase ... We found that adenosine deaminase abolished 1S,3R-ACPD-stimulated cAMP accumulation whereas the adenosine uptake blocker ...
more infohttp://www.jneurosci.org/content/13/1/38.long

Activation of metabotropic glutamate receptors increases cAMP accumulation in hippocampus by potentiating responses to...Activation of metabotropic glutamate receptors increases cAMP accumulation in hippocampus by potentiating responses to...

Additionally, adenosine receptor antagonists blocked mGluR-mediated increases in cAMP accumulation with potencies that were ... highly correlated with their potencies at A2 adenosine receptors. Furthermore, we performed a series of studies that suggest ... ACPD activates an mGluR subtype that potentiates responses to agonists of other receptors that are coupled to adenylate cyclase ... We found that adenosine deaminase abolished 1S,3R-ACPD-stimulated cAMP accumulation whereas the adenosine uptake blocker ...
more infohttp://www.jneurosci.org/content/13/1/38

Cartazolate - WikipediaCartazolate - Wikipedia

It is also known to act as an adenosine antagonist at the A1 and A2 subtypes and as a phosphodiesterase inhibitor. Cartazolate ... activity as antagonists of A1- and A2-adenosine receptors". Biochemical Pharmacology. 37 (4): 655-64. doi:10.1016/0006-2952(88) ... "Perturbation of benzodiazepine receptor binding by pyrazolopyridines involves picrotoxinin/barbiturate receptor sites". Journal ... OBrien, Robert (1986). Receptor binding in drug research. New York: Dekker. p. 519. ISBN 0-8247-7548-1. US Patent 3966746 ...
more infohttps://en.wikipedia.org/wiki/Cartazolate

Adenozinski A2A receptor - WikipediaAdenozinski A2A receptor - Wikipedia

1992). "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor.". Genomics ... a potent and selective adenosine A2 receptor antagonist.". Eur. J. Pharmacol. 267 (3): 335-41. PMID 8088373. doi:10.1016/0922- ... "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics 11 (1): ... 1994). "Identification of adenosine A2 receptor-cAMP system in human aortic endothelial cells.". Biochem. Biophys. Res. Commun. ...
more infohttps://sh.wikipedia.org/wiki/Adenozinski_A2A_receptor

Local Antinociceptive and Hyperalgesic Effects in the Formalin Test After Peripheral Administration of Adenosine Analogues in...Local Antinociceptive and Hyperalgesic Effects in the Formalin Test After Peripheral Administration of Adenosine Analogues in...

On the other hand adenosine analogues have been shown to possess antinociceptive effects after peripheral and intrathecal ... Adenosine administered to humans has been reported to induce pain after intravenous administration. ... Adenosine A1 and A2 receptors: structure--function relationships. van Galen PJ, Stiles GL, Michaels G, Jacobson KA. van Galen ... Influences of different adenosine receptor subtypes on catalepsy in mice. Zarrindast MR, Modabber M, Sabetkasai M. Zarrindast ...
more infohttps://pubmed.ncbi.nlm.nih.gov/1438021/

Neurologic Effects of Caffeine: Overview, Consumption of Caffeine, Physiologic Effects of CaffeineNeurologic Effects of Caffeine: Overview, Consumption of Caffeine, Physiologic Effects of Caffeine

The A1 and A2a adenosine receptors are the subtypes primarily involved in the caffeine effect, with A2b and A3 receptors ... 13] Caffeine is an inhibitor of the adenosine A2 receptor and was shown to improves motor deficits in a mouse model of ... Thus, adenosine receptor blockade appears to be the predominant mode of action. Methylxanthines act as competitive antagonists ... The latter interaction might explain the adenosine receptor antagonist-induced increase in behaviors related to dopamine (eg, ...
more infohttps://emedicine.medscape.com/article/1182710-overview

NCI Drug Dictionary - National Cancer InstituteNCI Drug Dictionary - National Cancer Institute

NDMA receptor antagonists such as amitriptyline and ketamine interfere with the role of NMDA receptors in the process of ... In addition to activating adenosine A1 receptors and inhibiting the neuronal reuptake of norepinephrine and serotonin, ... which appear to be mediated through the modulation of multiple subtypes of glutamate receptors including the N-methyl D- ... Ketoprofen also causes a decrease in the formation of thromboxane A2 synthesis, by thromboxane synthase, thereby inhibiting ...
more infohttps://www.cancer.gov/publications/dictionaries/cancer-drug?expand=K

Frontiers | Dopamine Signaling in reward-related behaviors | Frontiers in Neural CircuitsFrontiers | Dopamine Signaling in reward-related behaviors | Frontiers in Neural Circuits

... with an overview of the role of D1 and D2 receptors in the control of reward-associated behaviors. ... with an overview of the role of D1 and D2 receptors in the control of reward-associated behaviors. ... Localization of dopamine receptor subtypes occupied by intra-accumbens antagonists that reverse cocaine-induced locomotion. ... Onali, P., Oliansa, M. C., and Bunse, B. (1988). Evidence that adenosine A2 and dopamine autoreceptors antagonistically ...
more infohttps://www.frontiersin.org/articles/10.3389/fncir.2013.00152/full

Plus itPlus it

... the AMPA Receptor Antagonist Treatment in Ischemic Stroke Trial (ARTIST+) and AMPA Receptor Antagonist Treatment in Ischemic ... Metabotropic Glutamate Receptor (MGLUR) Modulators.-. There are eight subtypes of MGLUR, divided into three groups. The group I ... Drugs targeting the endothelium such as serotonin antagonists and adenosine agonists were recently reviewed (116). Although ... á-Phenyl-tert-butyl-nitrone reduces cortical infarct and edema in rats subjected to focal ischemia. Brain Res 1994;644:267-272 ...
more infohttp://www.ajnr.org/content/25/2/181

WikiGenes - Adora2a - adenosine A2a receptorWikiGenes - Adora2a - adenosine A2a receptor

... an adenosine A2 receptor antagonist, did not affect taurine release [41].. *Persistent expression of human clotting factor IX ... Adenosine receptor subtypes and vasodilatation in rat skeletal muscle during systemic hypoxia: a role for A1 receptors. Bryan, ... Purinergic P2 receptors trigger adenosine release leading to adenosine A2A receptor activation and facilitation of long-term ... Purinergic P2 receptors trigger adenosine release leading to adenosine A2A receptor activation and facilitation of long-term ...
more infohttps://www.wikigenes.org/e/gene/e/25369.html

Comparative pharmacology of human adenosine receptor subtypes - characterization of stably transfected receptors in CHO cells.Comparative pharmacology of human adenosine receptor subtypes - characterization of stably transfected receptors in CHO cells.

In this study all human subtypes were stably transfected into Chinese hamster ovary (CHO) cells in order to be able to ... Four adenosine receptor subtypes of the family of G protein-coupled receptors, designated A1, A2A, A2B and A3 are currently ... as the most potent antagonist at this receptor subtype. The A3 receptor was characterized utilizing the nonselective agonist [ ... Next Document: The bovine thromboxane A2 receptor: molecular cloning, expression, and functional characterization.. ...
more infohttp://www.biomedsearch.com/nih/Comparative-pharmacology-human-adenosine-receptor/9459566.html

Pharmacology And Therapeutics - Coupled Receptors - GUWS MedicalPharmacology And Therapeutics - Coupled Receptors - GUWS Medical

Antagonist Elimination of parasympathetic tone. C01CA - Adrenergic and Dopaminergic Agents. Agonist Vasoconstriction (a1: a2) ... Note that receptor subtype distributions have not been indicated for all receptor classes (e.g., prostanoid receptors and ... Adenosine (A,aA) Adrenoceptors (ct2A/2a2c) Angiotensin (AT2) Neuropeptide Y(Yj) Prostanoid Vasopressin (V,) ... AT1 receptor antagonists inhibit the interaction of angiotensin II with its AT1 receptor, and have proven therapeutic efficacy ...
more infohttps://www.guwsmedical.info/coupled-receptors/pharmacology-and-therapeutics.html

5-HT1D receptor - Wikipedia5-HT1D receptor - Wikipedia

1992). "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor.". Genomics ... GR-127,935 (mešoviti 5-HT1B/1D antagonist). *LY-310,762. *LY-367,642 ... 5-HT1D receptor (5-hidroksitriptaminski (serotoninski) receptor 1D, HTR1D) je 5-HT receptor. On je kodiran istoimenim genom.[1] ... Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A • ...
more infohttps://sh.wikipedia.org/wiki/5-HT1D_receptor

Indobufen Sodium | Semantic ScholarIndobufen Sodium | Semantic Scholar

Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype. ... Binding of [3H]KF17837S, a selective adenosine A2 receptor antagonist, to rat brain membranes. ... The adenosine antagonist 9-chloro-2-(2-furanyl)[1,2,4]triazolo[1,5-c]quinazolin-5-amine (CGS15943) binds to human A3 receptors ... N3,N7-diaminophenothiazinium derivatives as antagonists of α7-nicotinic acetylcholine receptors expressed in Xenopus oocytes. ...
more infohttps://www.semanticscholar.org/topic/Indobufen-Sodium/5197831

A novel chemokine receptor for SDF-1 and I-TAC involved in cell survival, cell adhesion, and tumor development | JEMA novel chemokine receptor for SDF-1 and I-TAC involved in cell survival, cell adhesion, and tumor development | JEM

Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor. Genomics. 11:225- ... HHV8-encoded vMIP-I selectively engages chemokine receptor CCR8. Agonist and antagonist profiles of viral chemokines. J. Biol. ... Constitutively active Gq/11-coupled receptors enable signaling by co-expressed G(i/o)-coupled receptors. J. Biol. Chem. 279: ... Identification of an orphan receptor gene as a type 1 calcitonin gene-related peptide receptor. Biochem. Biophys. Res. Commun. ...
more infohttp://jem.rupress.org/content/203/9/2201

Frontiers | Purinergic Signaling in Mast Cell Degranulation and Asthma | PharmacologyFrontiers | Purinergic Signaling in Mast Cell Degranulation and Asthma | Pharmacology

... induced via the activation of G protein-coupled adenosine receptors and P2Y nucleotide receptors, as well as by ATP-gated P2X ... induced via the activation of G protein-coupled adenosine receptors and P2Y nucleotide receptors, as well as by ATP-gated P2X ... All three classes of receptors, adenosine, P2X and P2Y are involved in tracheal mucus secretion. This review will summarize the ... All three classes of receptors, adenosine, P2X and P2Y are involved in tracheal mucus secretion. This review will summarize the ...
more infohttps://www.frontiersin.org/articles/10.3389/fphar.2017.00947/full

Interactions of Hallucinogens with the Glutamatergic System: Permissive Network Effects Mediated Through Cortical Layer V...Interactions of Hallucinogens with the Glutamatergic System: Permissive Network Effects Mediated Through Cortical Layer V...

Ardayfio PA et al (2008) The 5-hydroxytryptamine2A receptor antagonist R-(+)-a-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl ... adenosine A1, or μ-opioid receptors, suppress these effects of 5-HT2A receptor stimulation. Furthermore, a range of mostly Gq/ ... Neto FL et al (2000) Differential distribution of metabotropic glutamate receptor subtype mRNAs in the thalamus of the rat. ... 2A receptors: Modulation by novel 5-HT2A/2C antagonists, D1 antagonists and 5-HT1A agonists. J Pharmacol Exp Ther 273:101-112 ...
more infohttps://link.springer.com/chapter/10.1007%2F7854_2017_480

Characterization of Adenosine Receptors Mediating Spinal Sensory Transmission Related to Nociceptive Information in the Rat |...Characterization of Adenosine Receptors Mediating Spinal Sensory Transmission Related to Nociceptive Information in the Rat |...

... a selective A2 adenosine receptor agonist directly labels A2 receptors in rat brain. J Pharmacol Exp Ther 1989; 251:888-93. ... The inhibitory effects of adenosine agonists were almost completely reversed by a prototypic adenosine receptor antagonist, ... Collis MG, Hourani SMO: Adenosine receptor subtypes. Trends Pharmacol Sci 1993; 14:360-6. ... two main types of receptors are believed to mediate the actions of adenosine: A1and A2types of adenosine receptors. They are ...
more infohttp://anesthesiology.pubs.asahq.org/article.aspx?articleid=1947864

A2A - Adenosine - GPCR - Receptors - ProductsA2A - Adenosine - GPCR - Receptors - Products

All four members are coupled to a G-protein (A1 and A3 subtypes to Gi, and A2 subtypes to Gs (GPCR-A18)). As a result, ... Adenosine A2A antagonist €90.00 2283 SCH 442416, Desmethyl Radioligand precursor of the adenosine A2A antagonist SCH 442416 € ... Four subtypes of adenosine receptors (ARs) have been identified among vertebrates so far (A1, A2A, A2B and A3). These receptors ... Adenosine receptor subtypes listed: A1, A2A, A3. [1] InternationalUnion of Basic and Clinical Pharmacology. LXXXI. Nomenclature ...
more infohttps://www.axonmedchem.com/products/receptors/gpcr/adenosine/a2a

Anti-inflammatory mechanisms of methotrexate in rheumatoid arthritis | Annals of the Rheumatic DiseasesAnti-inflammatory mechanisms of methotrexate in rheumatoid arthritis | Annals of the Rheumatic Diseases

Extracellular adenosine can bind to the seven transmembrane-spanning adenosine surface receptors types A1, A2α, A2β, A3, which ... The rank order of the affinity of adenosine binding to these receptor subtypes is A1,A2a,A2b.36 The adenosine A1 receptor is ... through adenosine increase and binding to A3 receptors, might promote the IL1 receptor antagonist (IL1ra) transcription and ... adenosine via A2 receptor binding increases secretion of IL6 and IL10.50 51 Binding of adenosine to A3 receptors leads to ...
more infohttps://ard.bmj.com/content/60/8/729

Pharmacologic Treatment of Acute Kidney Injury: Why Drugs Havent Worked and What Is on the Horizon | American Society of...Pharmacologic Treatment of Acute Kidney Injury: Why Drugs Haven't Worked and What Is on the Horizon | American Society of...

Adenosine binds to receptors, which are members of the G protein-coupled receptor family that includes four subtypes: A1, A2A, ... Jordan JE, Zhao Z, Sato H, Taft S, Vinten-Johansen J: Adenosine A2 receptor activation attenuates reperfusion injury by ... However, Wilhelm et al. (92) recently showed that tezosertan, a dual ET-1 receptor antagonist, attenuated renal injury even ... Linden J: Molecular approach to adenosine receptors: Receptor mediated mechanisms of tissue protection. Annu Rev Pharmacol ...
more infohttps://cjasn.asnjournals.org/node/893.full.print

NYOH - Drug DictionaryNYOH - Drug Dictionary

NDMA receptor antagonists such as amitriptyline and ketamine interfere with the role of NMDA receptors in the process of ... In addition to activating adenosine A1 receptors and inhibiting the neuronal reuptake of norepinephrine and serotonin, ... which appear to be mediated through the modulation of multiple subtypes of glutamate receptors including the N-methyl D- ... Ketoprofen also causes a decrease in the formation of thromboxane A2 synthesis, by thromboxane synthase, thereby inhibiting ...
more infohttps://newyorkoncology.com/disease-drug-info/drug-dictionary/K/

Free Fatty Acid ReceptorsFree Fatty Acid Receptors

Significantly higher amounts of dopamine receptor ligands including subtype selective [2], [4] and multi-subtype [16], [17] ... Pert C. B., Pasternak G., Snyder S. H. (1973) Opiate agonists and antagonists discriminated by receptor binding in human brain ... bradykinin and adenosine [31??]. Latest studies have exposed that EETs activate cell-surface receptors to improve the degrees ... from membrane phospholipids through the action of the phospholipase A2; (b) biotransformation of AA by cyclooxygenase within a ...
more infohttp://www.exposed-skin-care.net/category/free-fatty-acid-receptors/

Role of Plant Derived Alkaloids and Their Mechanism in Neurodegenerative DisordersRole of Plant Derived Alkaloids and Their Mechanism in Neurodegenerative Disorders

Caffeine portrays its activity as adenosine A2 receptor antagonist which results in enhanced loco motor activity in ... Five subtypes (M1-M5) of muscarinic receptor are widely distributed in the CNS which are chiefly involved in a vast variety of ... It directs the down-regulation of adenosine A2 receptors to counter the suppressive effect of adenosine on brain dopaminergic ... Rivera-Oliver M, Díaz-Ríos M. Using caffeine and other adenosine receptor antagonists and agonists as therapeutic tools against ...
more infohttp://www.ijbs.com/v14p0341.htm
  • In this study all human subtypes were stably transfected into Chinese hamster ovary (CHO) cells in order to be able to study their pharmacological profile in an identical cellular background utilizing radioligand binding studies (A1, A2A, A3) or adenylyl cyclase activity assays (A2B). (biomedsearch.com)
  • In competition with antagonist radioligand biphasic curves were observed for agonists. (biomedsearch.com)
  • The DRP is a gamma-aminobutyric acid A (GABA A ) receptor-mediated depolarization of primary afferent terminals, which reflects a feedback inhibition associated with analgesia. (asahq.org)
  • As a result, stimulation of A1 and A3 subtypes in general results in neurotransmission through the inhibition of adenylate cyclase and phospholipase C , whereas stimulation of the A2 subtypes leads to enhanced neurotransmission. (axonmedchem.com)
  • Bailey MA (2004) Inhibition of bicarbonate reabsorption in the rat proximal tubule by activation of luminal P2Y1 receptors. (springer.com)
  • 1. Inhibition of Nitrobenzylthioinosine-Sensitive Adenosine Transport by Elevated D-Glucose Involves Activation of P2Y2 Purinoceptors in Human Umbilical Vein Endothelial Cells Jorge Parodi, Carlos Flores, Claudio Aguayo, M. Isolde Rudolph, Paola Casanello, Luis SobreviaAbstract-Chronic incubation with elevated D-glucose reduces adenosine transport in endothelial cells. (slideshare.net)
  • Our findings demonstrate that inhibition of adenosine transport via hENT1 in endothelial cells cultured in 25 mmol/L D-glucose could be due to stimulation of P2Y2 purinoceptors by ATP, which is released from these cells in response to D-glucose. (slideshare.net)
  • Evidence implicates a number of brain regions in mediating these effects of serotonergic hallucinogens and G q/11 -coupled receptors including the midline and intralaminar thalamic nuclei, claustrum, and neurons in deep PFC. (springer.com)
  • Here, we highlight accomplishments made in the generation of dopaminergic and cholinergic neurons, the two subtypes most affected in Alzheimer's and Parkinson's diseases and indirectly affected in Huntington's disease. (hindawi.com)
  • Adenosine administered to humans has been reported to induce pain after intravenous administration. (nih.gov)
  • Both adenosine and ATP can induce degranulation and bronchoconstriction on their own and synergistically with allergens. (frontiersin.org)
  • ATP acts via P2X receptors (P2XRs), which are ligand-gated cation channels, to induce mast cell degranulation ( Bulanova and Bulfone-Paus, 2010 ). (frontiersin.org)
  • Recordings made from layer V (L5) pyramidal cells of the prefrontal cortex (PFC) and neocortex in rodent slice preparations have shown that serotonin (5-hydroxytryptamine, 5-HT) and serotonergic hallucinogens induce an increase in the frequency of spontaneous excitatory postsynaptic currents (EPSCs) in the apical dendritic field by activating 5-HT 2A receptors. (springer.com)
  • α 1 -adrenergic, and mGlu 5 receptors) similarly induce glutamate (Glu) release onto L5 pyramidal cells. (springer.com)
  • We found that adenosine deaminase abolished 1S,3R-ACPD-stimulated cAMP accumulation whereas the adenosine uptake blocker dipyridamole enhanced this response. (jneurosci.org)
  • diminished hENT1 mRNA levels, an effect mimicked by ATP It has been reported that ATP inhibits dipyridamole- and blocked by P2Y antagonists. (slideshare.net)
  • On the other hand adenosine analogues have been shown to possess antinociceptive effects after peripheral and intrathecal administration in animals. (nih.gov)
  • Effects of intrathecal injection of the adenosine receptor agonists R-phenylisopropyl-adenosine and N-ethylcarboxamide-adenosine on nociception and motor function in the rat. (nih.gov)
  • Unlike many other chemokine receptors, ligand activation of CXCR7 does not cause Ca 2+ mobilization or cell migration. (rupress.org)
  • Overall, the pharmacological characteristics of the human receptors are similar to other species with some species-specific characteristics. (biomedsearch.com)
  • A topical preparation containing the antidepressant amitriptyline and the excitatory amino acid antagonist ketamine with potential topical analgesic activity. (cancer.gov)
  • Beique J-C et al (2007) Mechanism of the 5-hydroxytryptamine 2A receptor-mediated facilitation of synaptic activity in prefrontal cortex. (springer.com)
  • We established that endothe-reduce the NBMPR-sensitive adenosine transport associated lial cells express the hENT1 isoform of nucleoside transporterswith increased protein levels and the activity of endothelial and that incubation with 25 mmol/L D-glucose leads to inhibitionNO synthase, intracellular Ca2 , PKC, and mitogen-activated of adenosine transport by a mechanism that involves the activa-protein kinases p42/p44mapk.6,10 Thus, hENT1 adenosine trans- tion of P2Y2 purinoceptors. (slideshare.net)
  • It is generally believed that SDF-1 mediates these many disparate processes via a single cell surface receptor known as chemokine receptor 4 (CXCR4). (rupress.org)
  • [8,Studies with in vivo models of nociception have suggested that the A 1 receptor plays an important role in spinal antinociception. (asahq.org)
  • Recently, clinical evidence was found for the A3 receptor to be involved in rheumatoid arthritis , among other myocardial functions. (axonmedchem.com)
  • During the past decade, adenosine has been widely accepted as a neuromodulator in the peripheral and central nervous systems. (asahq.org)
  • In addition to the receptor types shown in Figure 4.1, GPCRs in the central nervous system (such as a2-adrenoceptors that regulate the sympathetic nervous system), GPCRs located in endocrine organs (through regulation, for example, of renin release) and receptors involved in metabolic regulation exert profound effects on cardiovascular health and disease and may constitute therapeutic targets. (guwsmedical.info)
  • The important roles that some types of GPCRs have in cardiovascular diseases through effects mediated by receptors located on blood cells (e.g., many types of prostanoid receptors) or acting via enzymatic mechanisms (e.g., thrombin receptors) will not be discussed here. (guwsmedical.info)
  • These effects on 5-HT 2A receptors and related GPCRs appear to play a major role in the behavioral effects of serotonergic hallucinogens, such as head twitches in rodents and higher order behaviors such as rodent lever pressing on the differential-reinforcement-of-low rate 72-s (DRL 72-s) schedule. (springer.com)
  • Adenosine 5′-triphosphate (ATP, compound 3 in Figure 1 ) is abundant in mast cells, stored in granules and secreted upon activation. (frontiersin.org)
  • This implies that the effects of 5-HT 2A receptor activation on the activity of L5 pyramidal cells may be responsible for mediating a range of behaviors linked to limbic circuitry with connectivity between the PFC, striatum, thalamus, claustrum, striatum, amygdala, and the hippocampal formation. (springer.com)
  • Moreover, adenosine protects against renal ischemic reperfusion injury by the anti-inflammatory effect of enhancing the activity of regulatory T cell and by attenuating the inflammatory injury produced by neutrophils via A 2 AR activation. (springer.com)
  • Al-Mashhadi RH, Skott O, Vanhoutte PM et al (2009) Activation of A(2) adenosine receptors dilates cortical efferent arterioles in mouse. (springer.com)
  • Awad AS, Huang L, Ye H et al (2006) Adenosine A2A receptor activation attenuates inflammation and injury in diabetic nephropathy. (springer.com)
  • Babich V, Vadnagara K, Di Sole F (2015) Dual effect of adenosine a1 receptor activation on renal O2 consumption. (springer.com)
  • Beach RE, Watts BA 3rd, Good DW et al (1991) Effects of graded oxygen tension on adenosine release by renal medullary and thick ascending limb suspensions. (springer.com)
  • Because adenosine production increases in hypoxia, the issue of a role of the nucleoside in the renal injury following ischemia reperfusion has been studied extensively. (springer.com)
  • Experimental evidence supports the notion that adenosine protects against ischemia-induced acute kidney injury by directly acting on renal endothelial and tubular A 1 AR. (springer.com)
  • In this study, exposure of human umbilical vein endothelial cells to 25 mmol/L D-glucose or 100 mol/L ATP, ATP- -S, or UTP, but not ADP or , -methylene ATP, reduced adenosine transport with no change in transport affinity. (slideshare.net)
  • Closely related receptor subtypes may have very different anatomical distribution patterns and opposing functional effects in the cardiovascular system. (guwsmedical.info)
  • This review focuses on the role of the DA system in drug addiction and food motivation, with an overview of the role of D1 and D2 receptors in the control of reward-associated behaviors. (frontiersin.org)
  • In this review, I will provide a short summary of DA signaling in reward-related behaviors, with an overview of recent studies on cocaine-addiction behaviors as well as some on food reward in the context of the role of D1 and D2 receptors in regulating these behaviors. (frontiersin.org)
  • In this regard, adenosine is considered to play an important role in modifying nociceptive information in the spinal cord. (asahq.org)
  • With an expanded understanding of CCX-CKR2 properties, we now rename this receptor CXCR7 and provide evidence for its role in oncologic processes. (rupress.org)
  • More specifically, A1 and A2A receptors play a role in regulating myocardial oxygen consumption and coronary blood flow . (axonmedchem.com)
  • Interestingly, evidence is growing for a certain role of adenosine receptors in the field of oncology . (axonmedchem.com)
  • Abebe W, Hussain T, Olanrewaju H et al (1995) Role of nitric oxide in adenosine receptor-mediated relaxation of porcine coronary artery. (springer.com)
  • Besides, stimulation of the A1 receptor has a myocardial depressant effect by decreasing the conduction of electrical impulses and suppressing pacemaker cell function, resulting in a decrease in heart rate. (axonmedchem.com)