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.
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.
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.
An enzyme that catalyzes the hydrolysis of ADENOSINE to INOSINE with the elimination of AMMONIA.
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.
Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.
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.
Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.
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.
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.
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.
Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.
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).
Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS.
Purine bases found in body tissues and fluids and in some plants.
Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS.
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.
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.
Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.
Adenine nucleotide containing one phosphate group esterified to the sugar moiety in the 2'-, 3'-, or 5'-position.
A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity.
Compounds that inhibit or block the activity of NEUROKININ-1 RECEPTORS.
Compounds that selectively bind to and block the activation of ADENOSINE A3 RECEPTORS.
A cyclic nucleotide derivative that mimics the action of endogenous CYCLIC AMP and is capable of permeating the cell membrane. It has vasodilator properties and is used as a cardiac stimulant. (From Merck Index, 11th ed)
The relationship between the dose of an administered drug and the response of the organism to the drug.
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.
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.
A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)
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.
N-Isopropyl-N-phenyl-adenosine. Antilipemic agent. Synonym: TH 162.
A family of hexahydropyridines.
Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS.
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.
Drugs that bind to but do not activate SEROTONIN 5-HT3 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT3 RECEPTOR AGONISTS.
Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
A long-acting derivative of cyclic AMP. It is an activator of cyclic AMP-dependent protein kinase, but resistant to degradation by cyclic AMP phosphodiesterase.
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.
Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.
Agents that antagonize ANGIOTENSIN RECEPTORS. Many drugs in this class specifically target the ANGIOTENSIN TYPE 1 RECEPTOR.
Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.
An enzyme of the lyase class that catalyzes the formation of CYCLIC AMP and pyrophosphate from ATP. EC 4.6.1.1.
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)
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.
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.
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.
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.
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.
Enzymes that catalyze the hydrolysis of CYCLIC AMP to form adenosine 5'-phosphate. The enzymes are widely distributed in animal tissue and control the level of intracellular cyclic AMP. Many specific enzymes classified under this heading demonstrate additional spcificity for 3',5'-cyclic IMP and CYCLIC GMP.
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.
A potent cyclic nucleotide phosphodiesterase inhibitor; due to this action, the compound increases cyclic AMP and cyclic GMP in tissue and thereby activates CYCLIC NUCLEOTIDE-REGULATED PROTEIN KINASES
Agents inhibiting the effect of narcotics on the central nervous system.
An antibiotic purine ribonucleoside that readily substitutes for adenosine in the biological system, but its incorporation into DNA and RNA has an inhibitory effect on the metabolism of these nucleic acids.
The rate dynamics in chemical or physical systems.
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.
Elements of limited time intervals, contributing to particular results or situations.
A group of enzymes which catalyze the hydrolysis of ATP. The hydrolysis reaction is usually coupled with another function such as transporting Ca(2+) across a membrane. These enzymes may be dependent on Ca(2+), Mg(2+), anions, H+, or DNA.
Cell surface proteins that bind ENDOTHELINS with high affinity and trigger intracellular changes which influence the behavior of cells.
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.
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)
Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).
Drugs that bind to and block the activation of PURINERGIC RECEPTORS.
Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.
Drugs that bind to but do not activate GABA RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.
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.
Drugs that bind to but do not activate GABA-A RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-A RECEPTOR AGONISTS.
A group of enzymes that are dependent on CYCLIC AMP and catalyze the phosphorylation of SERINE or THREONINE residues on proteins. Included under this category are two cyclic-AMP-dependent protein kinase subtypes, each of which is defined by its subunit composition.
Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.
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.
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.
Compounds which inhibit or antagonize the biosynthesis or actions of phosphodiesterases.
A class of drugs designed to prevent leukotriene synthesis or activity by blocking binding at the receptor level.
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.
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.
Glycoproteins which contain sialic acid as one of their carbohydrates. They are often found on or in the cell or tissue membranes and participate in a variety of biological activities.
A subtype of endothelin receptor found predominantly in the VASCULAR SMOOTH MUSCLE. It has a high affinity for ENDOTHELIN-1 and ENDOTHELIN-2.
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.
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.
Catalyze the hydrolysis of nucleosides with the elimination of ammonia.
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.
A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin. (From AMA Drug Evaluations Annual, 1994, p752)
A group of compounds that contain the structure SO2NH2.
Drugs used to cause dilation of the blood vessels.
An amine derived by enzymatic decarboxylation of HISTIDINE. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and also a centrally acting neurotransmitter.
The 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.
Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding.
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.
Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.
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.
Inhibitor of phosphodiesterases.
A ribonucleoside antibiotic synergist and adenosine deaminase inhibitor isolated from Nocardia interforma and Streptomyces kaniharaensis. It is proposed as an antineoplastic synergist and immunosuppressant.
The increase in a measurable parameter of a PHYSIOLOGICAL PROCESS, including cellular, microbial, and plant; immunological, cardiovascular, respiratory, reproductive, urinary, digestive, neural, musculoskeletal, ocular, and skin physiological processes; or METABOLIC PROCESS, including enzymatic and other pharmacological processes, by a drug or other chemical.
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.
Compounds with BENZENE fused to AZEPINES.
A drug combination that contains THEOPHYLLINE and ethylenediamine. It is more soluble in water than theophylline but has similar pharmacologic actions. It's most common use is in bronchial asthma, but it has been investigated for several other applications.
Established cell cultures that have the potential to propagate indefinitely.
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.
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.
Guanosine cyclic 3',5'-(hydrogen phosphate). A guanine nucleotide containing one phosphate group which is esterified to the sugar moiety in both the 3'- and 5'-positions. It is a cellular regulatory agent and has been described as a second messenger. Its levels increase in response to a variety of hormones, including acetylcholine, insulin, and oxytocin and it has been found to activate specific protein kinases. (From Merck Index, 11th ed)
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)
A purine base and a fundamental unit of ADENINE NUCLEOTIDES.
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
The action of a drug that may affect the activity, metabolism, or toxicity of another drug.
A series of heterocyclic compounds that are variously substituted in nature and are known also as purine bases. They include ADENINE and GUANINE, constituents of nucleic acids, as well as many alkaloids such as CAFFEINE and THEOPHYLLINE. Uric acid is the metabolic end product of purine metabolism.
Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.
A class of enzymes that catalyze the hydrolysis of one of the two ester bonds in a phosphodiester compound. EC 3.1.4.
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.
Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS.
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.
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.
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.
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.
(11 alpha,13E,15S)-11,15-Dihydroxy-9-oxoprost-13-en-1-oic acid (PGE(1)); (5Z,11 alpha,13E,15S)-11,15-dihydroxy-9-oxoprosta-5,13-dien-1-oic acid (PGE(2)); and (5Z,11 alpha,13E,15S,17Z)-11,15-dihydroxy-9-oxoprosta-5,13,17-trien-1-oic acid (PGE(3)). Three of the six naturally occurring prostaglandins. They are considered primary in that no one is derived from another in living organisms. Originally isolated from sheep seminal fluid and vesicles, they are found in many organs and tissues and play a major role in mediating various physiological activities.
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.
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.
Compounds that bind to and block the stimulation of PURINERGIC P2X RECEPTORS. Included under this heading are antagonists for specific P2X receptor subtypes.
The muscle tissue of the HEART. It is composed of striated, involuntary muscle cells (MYOCYTES, CARDIAC) connected to form the contractile pump to generate blood flow.
A potent inhibitor of ADENOSINE DEAMINASE. The drug induces APOPTOSIS of LYMPHOCYTES, and is used in the treatment of many lymphoproliferative malignancies, particularly HAIRY CELL LEUKEMIA. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity.
Drugs that selectively bind to but do not activate HISTAMINE H3 RECEPTORS. They have been used to correct SLEEP WAKE DISORDERS and MEMORY DISORDERS.
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).
Seven membered heterocyclic rings containing a NITROGEN atom.
5'-Adenylic acid, monoanhydride with sulfuric acid. The initial compound formed by the action of ATP sulfurylase on sulfate ions after sulfate uptake. Synonyms: adenosine sulfatophosphate; APS.
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.
PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS.
One of two major pharmacologically defined classes of adrenergic receptors. The beta adrenergic receptors play an important role in regulating CARDIAC MUSCLE contraction, SMOOTH MUSCLE relaxation, and GLYCOGENOLYSIS.
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.
A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.
Drugs that bind to but do not activate GABA-B RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-B RECEPTOR AGONISTS.
An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.
Sulfhydryl analog of INOSINE that inhibits nucleoside transport across erythrocyte plasma membranes, and has immunosuppressive properties. It has been used similarly to MERCAPTOPURINE in the treatment of leukemia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p503)
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)
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.
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)
The observable response an animal makes to any situation.
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.
The most common and most biologically active of the mammalian prostaglandins. It exhibits most biological activities characteristic of prostaglandins and has been used extensively as an oxytocic agent. The compound also displays a protective effect on the intestinal mucosa.
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.
Conversion of an inactive form of an enzyme to one possessing metabolic activity. It includes 1, activation by ions (activators); 2, activation by cofactors (coenzymes); and 3, conversion of an enzyme precursor (proenzyme or zymogen) to an active enzyme.
A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.
Drugs that bind to but do not activate ADRENERGIC RECEPTORS. Adrenergic antagonists block the actions of the endogenous adrenergic transmitters EPINEPHRINE and NOREPINEPHRINE.
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.
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.
A pyridine nucleotide that mobilizes CALCIUM. It is synthesized from nicotinamide adenine dinucleotide (NAD) by ADP RIBOSE CYCLASE.
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).
A group of compounds with the heterocyclic ring structure of benzo(c)pyridine. The ring structure is characteristic of the group of opium alkaloids such as papaverine. (From Stedman, 25th ed)
A subtype of endothelin receptor found predominantly in the KIDNEY. It may play a role in reducing systemic ENDOTHELIN levels.
Systems in which an intracellular signal is generated in response to an intercellular primary messenger such as a hormone or neurotransmitter. They are intermediate signals in cellular processes such as metabolism, secretion, contraction, phototransduction, and cell growth. Examples of second messenger systems are the adenyl cyclase-cyclic AMP system, the phosphatidylinositol diphosphate-inositol triphosphate system, and the cyclic GMP system.
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.
Treatment process involving the injection of fluid into an organ or tissue.
The active sympathomimetic hormone from the ADRENAL MEDULLA. It stimulates both the alpha- and beta- adrenergic systems, causes systemic VASOCONSTRICTION and gastrointestinal relaxation, stimulates the HEART, and dilates BRONCHI and cerebral vessels. It is used in ASTHMA and CARDIAC FAILURE and to delay absorption of local ANESTHETICS.
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.
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.
Purine bases related to hypoxanthine, an intermediate product of uric acid synthesis and a breakdown product of adenine catabolism.
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.
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.
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.
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.
A purine and a reaction intermediate in the metabolism of adenosine and in the formation of nucleic acids by the salvage pathway.
The physiological widening of BLOOD VESSELS by relaxing the underlying VASCULAR SMOOTH MUSCLE.
Cell surface proteins that bind cyclic AMP with high affinity and trigger intracellular changes which influence the behavior of cells. The best characterized cyclic AMP receptors are those of the slime mold Dictyostelium discoideum. The transcription regulator CYCLIC AMP RECEPTOR PROTEIN of prokaryotes is not included nor are the eukaryotic cytoplasmic cyclic AMP receptor proteins which are the regulatory subunits of CYCLIC AMP-DEPENDENT PROTEIN KINASES.
A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.
Injections into the cerebral ventricles.
The action of a drug in promoting or enhancing the effectiveness of another drug.
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.
Compounds with a BENZENE fused to IMIDAZOLES.
Nucleotides in which the base moiety is substituted with one or more sulfur atoms.
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.
Use of electric potential or currents to elicit biological responses.
Drugs that bind to but do not activate SEROTONIN 5-HT4 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN RECEPTOR AGONISTS.
The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.
A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H2 receptors act via G-proteins to stimulate ADENYLYL CYCLASES. Among the many responses mediated by these receptors are gastric acid secretion, smooth muscle relaxation, inotropic and chronotropic effects on heart muscle, and inhibition of lymphocyte function. (From Biochem Soc Trans 1992 Feb;20(1):122-5)
A protein that has been shown to function as a calcium-regulated transcription factor as well as a substrate for depolarization-activated CALCIUM-CALMODULIN-DEPENDENT PROTEIN KINASES. This protein functions to integrate both calcium and cAMP signals.
A polyanionic compound with an unknown mechanism of action. It is used parenterally in the treatment of African trypanosomiasis and it has been used clinically with diethylcarbamazine to kill the adult Onchocerca. (From AMA Drug Evaluations Annual, 1992, p1643) It has also been shown to have potent antineoplastic properties.
Body organ that filters blood for the secretion of URINE and that regulates ion concentrations.
Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.
The attachment of PLATELETS to one another. This clumping together can be induced by a number of agents (e.g., THROMBIN; COLLAGEN) and is part of the mechanism leading to the formation of a THROMBUS.
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.
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.
The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.
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.
A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.
The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.
A calcium-activated enzyme that catalyzes the hydrolysis of ATP to yield AMP and orthophosphate. It can also act on ADP and other nucleoside triphosphates and diphosphates. EC 3.6.1.5.
Adenosine molecules which can be substituted in any position, but are lacking one hydroxyl group in the ribose part of the molecule.
An isoquinoline alkaloid obtained from Dicentra cucullaria and other plants. It is a competitive antagonist for GABA-A receptors.
A competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.
Proteins that bind specific drugs with high affinity and trigger intracellular changes influencing the behavior of cells. Drug receptors are generally thought to be receptors for some endogenous substance not otherwise specified.
A soluble factor produced by MONOCYTES; MACROPHAGES, and other cells which activates T-lymphocytes and potentiates their response to mitogens or antigens. Interleukin-1 is a general term refers to either of the two distinct proteins, INTERLEUKIN-1ALPHA and INTERLEUKIN-1BETA. The biological effects of IL-1 include the ability to replace macrophage requirements for T-cell activation.
Drugs that bind to and block the activation of ADRENERGIC BETA-2 RECEPTORS.
A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs.
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.
Compounds that inhibit or block the activity of CANNABINOID RECEPTORS.
... activity as antagonists of A1- and A2-adenosine receptors". Biochemical Pharmacology. 37 (4): 655-64. doi:10.1016/0006-2952(88) ... Wachtel H (1982). "Characteristic behavioural alterations in rats induced by rolipram and other selective adenosine cyclic 3', ... It is also known to act as an adenosine antagonist at the A1 and A2 subtypes and as a phosphodiesterase inhibitor. Cartazolate ... "Perturbation of benzodiazepine receptor binding by pyrazolopyridines involves picrotoxinin/barbiturate receptor sites". Journal ...
These signaling elements include thromboxane A2, receptor type α, phospholipase Cβ3, and IP3 receptors. Signalization in ... cAMP, cyclic adenosine monophosphate, phosphorylate messengers via protein kinase A (PKA). ... It belongs to the homologous family of glycoprotein IIb-IIa antagonists. Kistrin has an adhesion site that binds to GP IIb-IIIa ... TX2 effects are mediated by G protein-coupled receptors, subtypes TPα and TPβ. Both receptors mediate phospholipase C ...
In order to be able to characterize the function of adenosine A2 receptors, potent and selective A2-receptor antagonists were ... A2A receptors are G-protein coupled receptor (GPCR) that increases cyclic adenosine monophosphate (cAMP). These receptors are ... Adenosine A2A receptor antagonists are a class of drugs that blocks adenosine at the adenosine A2A receptor. Notable adenosine ... adenosine receptor antagonists as potential therapeutics, antagonist for A2A-receptors, adenosine receptor ligands as anti- ...
... receptors that works by activating G-S proteins which in turn raises cellular cAMP levels thereby mobilizing Cyclic adenosine ... Asapiprant (S-555739) and Laropiprant are selective receptor antagonists of DP1 whereas Vidupiprant is a receptor antagonist ... thromboxane A2, with PGD2 being more than 100-fold more potent than PGE2 in binding to and stimulating DP1. (http://www. ... Prostaglandin receptors Prostanoid receptors Prostaglandin DP2 receptor Eicosanoid receptor GRCh38: Ensembl release 89: ...
It acts as a positive allosteric modulator of the GABAA receptor at the barbiturate binding site, as an adenosine antagonist of ... a potent new inhibitor of cyclic 3',5'-nucleotide phosphodiesterases". Biochemical Pharmacology. 21 (18): 2443-50. doi:10.1016/ ... the A1 and A2 subtypes, and as a phosphodiesterase inhibitor selective for the PDE4 isoform. It is currently in clinical trials ... ISBN 3-7643-1837-6. Williams M, Jarvis MF (February 1988). "Adenosine antagonists as potential therapeutic agents". ...
... and reduces inflammation and innate immunity nonselective adenosine receptor antagonist, antagonizing A1, A2, and A3 receptors ... Essayan DM (2001). "Cyclic nucleotide phosphodiesterases". J Allergy Clin Immunol. 108 (5): 671-80. doi:10.1067/mai.2001.119555 ... Daly JW, Jacobson KA, Ukena D (1987). "Adenosine receptors: development of selective agonists and antagonists". Prog Clin Biol ... or rather its adenosine-antagonist behavior). Mandal, Ananya. "Caffeine Pharmacology". Website Medical News. Archived from the ...
Yang Z, Sun W, Hu K (Apr 2012). "Molecular mechanism underlying adenosine receptor-mediated mitochondrial targeting of protein ... Perjés Á, Skoumal R, Tenhunen O, Kónyi A, Simon M, Horváth IG, Kerkelä R, Ruskoaho H, Szokodi I (2014). "Apelin increases ... Lin YH, Swanson ER, Li J, Mkrtschjan MA, Russell B (Oct 2015). "Cyclic mechanical strain of myocytes modifies CapZβ1 post ... Gray MO, Karliner JS, Mochly-Rosen D (Dec 1997). "A selective epsilon-protein kinase C antagonist inhibits protection of ...
Pandey, S.C., Roy, A., Zhang, H. (2003). The decreased phosphorylation of cyclic adenosine monophosphate (cAMP) response ... 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 ... receptors are glutamate receptors particularly important in long-term potentiation in neurons. These receptors have been linked ...
Mello, F. G. (October 1978). "The Ontogeny of Dopamine-Dependent Increase of Adenosine 3',5'-Cyclic Monophosphate in the Chick ... D5 receptors show higher affinity for agonists and lower affinity for antagonists than D1 receptors. Dihydrexidine Rotigotine ... Prado C, Contreras F, González H, Díaz P, Elgueta D, Barrientos M, Herrada AA, Lladser Á, Bernales S, Pacheco R (2012). " ... It belongs to the D1-like receptor family along with the D1 receptor subtype. D5 receptor is a subtype of the dopamine receptor ...
The A1 receptors couple to Gi/o and decreases cAMP levels, while the A2 adenosine receptors couple to Gs, which stimulates ... Its derivatives include the energy carriers adenosine mono-, di-, and triphosphate, also known as AMP/ADP/ATP. Cyclic adenosine ... have a purine structure and bind to some of the same receptors as adenosine. Methylxanthines act as competitive antagonists of ... All adenosine receptor subtypes (A1, A2A, A2B, and A3) are G-protein-coupled receptors. The four receptor subtypes are further ...
... s secrete thromboxane A2, which acts on the platelet's own thromboxane receptors on the platelet surface (hence the so- ... Clopidogrel and related antiplatelet medications also work as purinergic receptor P2Y12 antagonists. Platelet activation begins ... Resting platelets maintain active calcium efflux via a cyclic AMP-activated calcium pump. Intracellular calcium concentration ... "Differential Sensitivity of Various Markers of Platelet Activation with Adenosine Diphosphate". BioNanoScience. 9 (1): 53-58. ...
It promotes vasodilation of smooth muscles by increasing the activity of cyclic adenosine monophosphate (cAMP) to decrease ... It works by binding and activating the prostaglandin E2 receptor which results in the opening and softening of the cervix and ... PGE2 synthesis within the body begins with the activation of arachidonic acid (AA) by the enzyme phospholipase A2. Once ... "A live imaging cell motility screen identifies prostaglandin E2 as a T cell stop signal antagonist". Journal of Immunology. 187 ...
... trienoic acid as a thromboxane A2 receptor antagonist with minimal intrinsic activity". British Journal of Haematology. 101 (1 ... to inhibit platelet aggregation responses to various agents by stimulating platelets to raise their levels of Cyclic adenosine ... BLT1 receptor) and its low affinity BLT2 receptor (Kd=23 nM); both receptors are G protein coupled receptors that, when ligand- ... Hicks, A; Monkarsh, S. P.; Hoffman, A. F.; Goodnow Jr, R (2007). "Leukotriene B4 receptor antagonists as therapeutics for ...
Elias L, Li AP, Longmire J (June 1981). "Cyclic adenosine 3':5'-monophosphate-dependent and -independent protein kinase in ... Alquezar C, Salado IG, de la Encarnación A, Pérez DI, Moreno F, Gil C, de Munain AL, Martínez A, Martín-Requero Á (April 2016 ... and to be antagonists of the Wnt pathway, show structural similarities to benzimidazole-based CK1 inhibitors, among them ... receptors, transport vesicles, components of the cytoskeleton, centrosomes or spindle poles. While the present NLS is not ...
Thromboxane A2 receptor. TP. TXA=PGH2,,PGD2=PGE2=PGF2α=PGI2[14]. contractile. Gq alpha subunit. stimulates PLC & IP3; raises Ca ... production of cyclic AMP [cAMP]);[5] e) G proteins types to which they link and activate, i.e. those containing the Gs alpha ... Prostaglandin receptors or prostanoid receptors represent a sub-class of cell surface membrane receptors that are regarded as ... All of the prostanoid receptors are G protein-coupled receptors belonging to the Subfamily A14 of the rhodopsin-like receptor ...
They are SRIs and litoxetine is also a 5-HT3 receptor antagonist while lubazodone is also a 5-HT2A receptor antagonist. In the ... One such possible mechanism is the increased levels of cyclic adenosine monophosphate (cAMP) as a result of interference with ... PMID 21701626.CS1 maint: multiple names: authors list (link) Romero-Martínez Á, Murciano-Martí S, Moya-Albiol L (May 2019). "Is ... Fluvoxamine is an agonist of the σ1 receptor, while sertraline is an antagonist of the σ1 receptor, and paroxetine does not ...
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 ... cyclic, with epidermolytic hyperkeratosis; 607602; KRT1 Ichthyosis, cyclic, with epidermolytic hyperkeratosis; 607602; KRT10 ...
PDP2 receptor antagonists have been shown to allergic reactions induced in the airways mice and sheep as well as the airways ... G-protein coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger. • chemotaxis. • positive ... thromboxane A2. The cyclopentenone prostaglandins, PGJ2, Δ12-PGJ2, and 15-d-Δ12,14-PGJ2 are spontaneously formed or protein- ... with the C5a receptor, Formyl peptide receptor 1, and Formyl peptide receptor 2 receptors. DP2 has little or no such amino acid ...
... which have high affinity and selectivity for the human adenosine A 2B receptors (hA(2B)-AdoR). Unfortunately, this class of ... Adenosine A2 Receptor Antagonists* * Animals * Binding Sites * Cell Line * Cyclic AMP / analysis ... Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate for chronic inflammatory airway diseases J Med ... which have high affinity and selectivity for the human adenosine A 2B receptors (hA(2B)-AdoR). Unfortunately, this class of ...
Activation of nucleotide receptors with extracellular ATP and nucleotide analogues increased ... Regulation of plasma membrane ion transport by endogenous purinergic receptors was assessed in a distal renal (A6) cell line. ... Neither the change in [Ca2+]i nor the stimulation of cotransport was abolished by the adenosine receptor antagonist 8-{4-[N-(2- ... In contrast to the adenosine A2 receptor agonist 5-N-ethylcarboxamidoadenosine, nucleotide analogues had no discernible effect ...
... activity as antagonists of A1- and A2-adenosine receptors". Biochemical Pharmacology. 37 (4): 655-64. doi:10.1016/0006-2952(88) ... Wachtel H (1982). "Characteristic behavioural alterations in rats induced by rolipram and other selective adenosine cyclic 3, ... It is also known to act as an adenosine antagonist at the A1 and A2 subtypes and as a phosphodiesterase inhibitor. Cartazolate ... "Perturbation of benzodiazepine receptor binding by pyrazolopyridines involves picrotoxinin/barbiturate receptor sites". Journal ...
There are two main classes of adenosine receptor: Al and A2; caffeine and paraxanthine are nonselective antagonists at both, ... Caffeine and Phosphodiesterase Caffeine increases intracellular concentrations of cyclic adenosine mono- phosphate (cAMP) by ... Caffeine and Adenosine Receptors The ability of caffeine to inhibit adenosine receptors appears to be highly important in its ... are in the range associated with adenosine receptor blockade (as quantitated by in vitro receptor binding assays) (Daly, 1993 ...
... and adenosine A2A receptor (A2AR) increases cAMP-dependent protein kinase (PKA) activity in the brain. In Huntingtons disease ... Adenosine A2 Receptor Antagonists * Benzazepines * Dopamine Antagonists * Pyrimidines * Receptor, Adenosine A2A * Receptors, ... Cyclic AMP-Dependent Protein Kinases / metabolism * Disease Models, Animal * Dopamine Antagonists / pharmacology ... Stimulation of dopamine D1 receptor (D1R) and adenosine A2A receptor (A2AR) increases cAMP-dependent protein kinase (PKA) ...
... direct measurements indicate that plasma membrane polypeptide hormone receptors are mobile within the plane of the lipid ... Lohse MJ, Klotz KN, Schwabe U. Mechanism of A2 adenosine receptor activation. I. Blockade of A2 adenosine receptors by ... Mechanism of agonist and antagonist binding to alpha 2 adrenergic receptors: evidence for a precoupled receptor-guanine ... Adv in Cyclic Nucleotide and Prot Phosphor Res 1984; 18: 1-62.Google Scholar ...
These signaling elements include thromboxane A2, receptor type α, phospholipase Cβ3, and IP3 receptors. Signalization in ... cAMP, cyclic adenosine monophosphate, phosphorylate messengers via protein kinase A (PKA). ... It belongs to the homologous family of glycoprotein IIb-IIa antagonists. Kistrin has an adhesion site that binds to GP IIb-IIIa ... TX2 effects are mediated by G protein-coupled receptors, subtypes TPα and TPβ. Both receptors mediate phospholipase C ...
In vitro data indicate that the activation of A2 adenosine receptors increases renin release by the accumulation of cyclic AMP ... during saline infusion and in the presence of the adenosine antagonist theophylline (100 micrograms/100 ml forearm tissue per ... abolished the adenosine-mediated venous angiotensin II increments. Our data indicate that exogenous adenosine can stimulate the ... Adenosine activates a vascular renin-angiotensin system in hypertensive subjects.. S Taddei, A Virdis, S Favilla, A Salvetti ...
Cyclic AMP Medicine & Life Sciences 46% * Adenosine A2 Receptor Antagonists Medicine & Life Sciences 37% ... The action of adenosine was antagonized by an adenosine A2A-receptor (A2AR) antagonist and was mimicked by an A2AR agonist, ... The action of adenosine was antagonized by an adenosine A2A-receptor (A2AR) antagonist and was mimicked by an A2AR agonist, ... The action of adenosine was antagonized by an adenosine A2A-receptor (A2AR) antagonist and was mimicked by an A2AR agonist, ...
Schwabe U, Ukena D, Lohse MJ: Xanthine derivatives as antagonists at A1 and A2 adenosine receptors. Naunyn Schmiedebergs Arch ... a resulting increase in cyclic AMP producing relaxation of bronchial smooth muscle as well as antagonism of adenosine receptors ... Schwabe U, Ukena D, Lohse MJ: Xanthine derivatives as antagonists at A1 and A2 adenosine receptors. Naunyn Schmiedebergs Arch ... Receptor for adenosine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase.. Gene Name. ...
Adenosine Receptor Inhibitors related products. MedChemExpress provides thousands of inhibitors, modulators and agonists with ... Diphylline (Diprophylline) is a potent A1/A2 adenosine receptor antagonist and cyclic nucleotide phosphodiesterase inhibitor. ... Adenosine Receptor Cardiovascular Disease FSCPX is a potent and selective irreversible antagonist of A1 adenosine receptor (A1 ... Diphylline (Diprophylline) is a potent A1/A2 adenosine receptor antagonist and cyclic nucleotide phosphodiesterase inhibitor. ...
... a mechanism different from adenosine diphosphate (ADP) receptor antagonists (1,2). Previous studies have suggested that ... Previous studies reported that elevated cyclic adenosine monophosphate, either by inhibiting ADP-induced inhibition of ... and thromboxane A2 (10,11). A marker of platelet activation, P-selectin is expressed exclusively by platelet activation, ... Furthermore, like ADP-receptor antagonist, cilostazol significantly inhibited platelet aggregation induced by ADP and other ...
... while adenosine A2 receptor activation produces pronociception by increasing cyclic Adenosine Monophosphate (AMP) levels in the ... Caffeine acts as a non-specific adenosine receptor antagonist. When systemic caffeine is administered with systemic ... Experimental evidence Adenosine receptors Fri, 13 Sep 2019 , Neuropathic Pain At peripheral nerve terminals in rodents, ... Adenosine A3 receptor activation produces pain behaviors due to the release of histamine and 5HT from mast cells and ...
Caffeine is a natural alkaloid methylxanthine that acts as a nonselective antagonist of adenosine receptors, with A1 antagonism ... Caffeine also inhibits phosphodiesterase, resulting in increased intracellular cyclic AMP and intracellular calcium levels. ... triggering seizures and A2 antagonism triggering cerebral and coronary vasoconstriction. ... 14][10][4][15] Caffeine also sensitizes dopamine receptors and is a competitive antagonist of benzodiazepine receptors. ...
Adenosine Receptors: Selective agonists and antagonists. In L. Belardinelli and A. Pelleg (Eds.), Adenosine and adenine ... Sattin, A., and Ralf, T. W. (1970). The effect of adenosine and adenine nucleotides on the cyclic adenosine 3,5-phosphate ... and A2-selective adenosine agonists and antagonists: Evidence for synergism and antagonism. Journal of Pharmacology and ... Locomotor Activity Adenosine Receptor Endogenous Adenosine Adenosine Analog Caffeine Treatment These keywords were added by ...
Adenosine A2 Receptor Agonists Adenosine-5-(N-ethylcarboxamide) Purinergic P1 Receptor Antagonists ... nucleotide analogues had no discernible effect on cytosolic adenosine 3′,5′-cyclic monophosphate levels or adenylyl cyclase ... Neither the change in [Ca2+]i nor the stimulation of cotransport was abolished by the adenosine receptor antagonist 8-{4-[N-(2- ... Neither the change in [Ca2+]i nor the stimulation of cotransport was abolished by the adenosine receptor antagonist 8-{4-[N-(2- ...
A2B adenosine receptor (A2B AR) activation induces Gs-dependent cyclic AMP accumulation. However, A2B AR G protein-coupling to ... A2-biosensor-evidence-for-an-allosteric-mechanism-of-action-for-the-a-2b-selective-antagonist-psb-603 ... The adenosine A2B receptor (A2BAR) is the most abundant adenosine receptor (AR) in cardiac fibroblasts and is largely ... Capadenoson, a clinically trialed partial adenosine A1 receptor agonist, can stimulate adenosine A2B receptor biased agonism. ...
Adenosine receptor antagonist. Theophylline antagonizes adenosine receptor A1, A2 strongly, and A3 less potently. It binds to ... which leads to increased tissue cyclic adenine monophosphate (cAMP) and cyclic 3′,5′ guanosine monophosphate concentrations, ... This antagonism of the adenosine receptors, specifically A1 receptors, is responsible for some of the side effects of ... This mechanism is distinct from PDE and adenosine receptor inhibition.[10]. A new study indicates that aminophylline plays an ...
Potent of adenosine A1 receptors and 5-nucleotidase in the brain of adenosine receptor antagonists that are selective for the ... Unlike A1 receptors, A2 adenosine receptors appear to couple to cholera toxin- Neurons were prepared from coronal brain slices ... tion by di usable second messengers that might be produced by activation of this adenosine receptor subtype (e.g. cyclic AMP). ... adenosine receptor: The A3 adenosine receptor. Proc. Natl. Acad.. Chem., 269, 22347 ± 22357.. Sci. U.S.A., 89, 7432 ± 7436.. ...
Adenosine A2 Receptors: 1 study in 1 result : IBA. *Muscarinic M1 Receptor: 1 study in 1 result : IBA ... Interleukin 1 Receptor Antagonist Protein (Anakinra): 1 outcome in 2 results : FDA 2 ... Cyclic AMP Response Element-Binding Protein (Cyclic AMP-Responsive DNA-Binding Protein): 1 study in 1 result : IBA ... Purinergic P1 Receptors (Adenosine Receptor): 4 studies in 23 results : IBA. *Adenosine: 4 studies in 22 results : FDA 19 ...
... administration of adenosine A2 receptor agonists, cell-permeant cyclic AMP analogs, or adenylyl cyclase activators (e.g., ... Alcohol preconditioning experiments with mixed cerebellar cultures using receptor antagonists for NMDA receptors, memantine or ... Adenosine A1 receptor blockade abolished the protection, suggesting a role of adenosine A1 receptor in cardioprotection. In ... Sensors include glutamate receptors (notably the NMDA receptor channel), adenosine receptors, and perhaps others coupled to Gi ...
This effect of (R)-AHPIA is specific for the A2 receptor and can be prevented by the adenosine receptor antagonist theophylline ... Such covalent labelling of the receptor led to a concentration-dependent reduction of cellular cyclic AMP levels. This ... Mechanism of A2 adenosine receptor activation. I. Blockade of A2 adenosine receptors by photoaffinity labeling (1991) ... The binding of agonists and antagonists to a2-adrenergic receptors of human platelets was studied. The receptors showed ...
... blocks the final common pathway of platelet aggregation and thrombus formation by binding to glycoprotein IIb/IIIa receptors on ... Abbreviations: AA, arachidonic acid; COX-2, cyclo-oxygenase-2; cAMP, cyclic adenosine monophosphate; ADP, adenosine diphosphate ... Optimal use of platelet glycoprotein IIb/IIIa receptor antagonists in patients undergoing percutaneous coronary interventions. ... Aspirin, a thromboxane A2 inhibitor, when used alone has limited efficacy in preventing cardiovascular events after coronary ...
... acting on several receptors, including opioids, adenosine A1 and A2, or cholinergic M2, producing changes in K+ channels, ... an antagonist of channels; atropine (1 mg/kg), an antagonist of muscarinic receptors; mecamylamine (2 mg/kg), an antagonist of ... The presence of unsaturation in its cyclic chain structure confers the olefin characteristic for the γ-TPN, which allows easier ... nonselective muscarinic antagonist) and mecamylamine (a α2β3 selective preferential nicotinic receptor antagonist) inhibited ...
More recently, cyclic peptides based on the Arg-Gly-Asp sequence common to many GP IIb/IIIa receptor ligands have been ... prostaglandin endoperoxides and thromboxane A2, cAMP, and cGMP.22 Glycoprotein IIb/IIIa (GP IIb/IIIa) antagonists fall into the ... The second group are agents generated within the platelet that interact with the membrane receptors, for example, adenosine ... GP IIb/IIIa antagonists may be broadly classified as monoclonal antibodies or cyclic peptides. Earlier drugs were intravenously ...
A comparison of A2 adenosine receptor-induced cyclic AMP generation in cerebral cortex and relaxation of pre-contracted aorta. ... 3H]ZM241385-an antagonist radioligand for adenosine A2A receptors in rat brain European Journal of Pharmacology. 411(3), 205- ... Activation of a metabotropic excitatory amino acid receptor potentiates A2b adenosine receptor-stimulated cyclic AMP ... A1 and A2 adenosine receptor modulation of contractility in the cauda epididymis of the guinea-pig. British Journal of ...
Apigenin is a flavonoid and acts as an antagonist at α1β1γ2S receptors and at ρ1 receptors. GABA modulation is a common ... Its principal action is adenosine antagonism, and there are a number of caffeine analogs with variable affinities for A1 and A2 ... It also acts as a cyclic AMP phosphodiesterase inhibitor, perhaps contributing to its alertness and mood elevating effects [3 ... J. W. Daly, I. Hide, C. E. Muller, and M. Shamim, "Caffeine analogs: structure-activity relationships at adenosine receptors," ...
Cangrelor is a new intravenous, reversible P2Y12 receptor antagonist and has a rapid onset of action. It achieves a significant ... It also blocks the uptake of adenosine by the platelets which also increase cyclic AMP.[6] ... This prostaglandin is a precursor of thromboxane A2 and PGI2. Thromboxane A2 works by inducing platelets aggregation and ... These drugs convert to an active drug with the help of hepatic CYP450 system that inhibits the platelet P2Y12 receptor. ...
Clonidine acts on central a2-receptors. Clonidine and w labetalol and carvedilol have a- and b-receptor blocking other a2- ... 9. Adrenal gland 9l Dosage: Adenylate cyclase, see Adenosine monophosphate, cyclic w SVT: 3 mg by rapid iv injection; if ... Celiprolol Methoxamine and phenylephrine are synthetic a1-receptor has b1-receptor antagonist and b2-receptor agonist prop- ... kidney). Stimulates both a- and b-adrenergic receptors; displays a-Adrenergic receptor antagonists (a-Blockers). Usu- ...
Effects of A1 and A2 adenosine receptor antagonists on the induction and reversal of long-term potentiation in guinea pig ... Synaptic potentials in sympathetic ganglia: are they mediated by cyclic nucleotides? Busis, N.A., Weight, F.F., Smith, P.A. ... 3. When the tetanus or LFS was applied to CA1 inputs in the presence of an adenosine A1 receptor antagonist, 8- ... BACKGROUND & AIMS: Adenosine triphosphate (ATP) acting at P2 receptors mediates some fast excitatory postsynaptic potentials ( ...
  • Activation of nucleotide receptors with extracellular ATP and nucleotide analogues increased intracellular calcium concentration ([Ca2+]i) primarily by release of intracellular calcium stores, with relative potency of agonists similar to that seen for stimulation of Na-K-Cl cotransport. (rti.org)
  • We have utilized whole-cell voltage-clamp electrophysiology to examine the modulatory e ects of CADO and other adenosine receptor agonists on voltage-gated calcium channels in dissociated basolateral amygdala neurons. (gotomydoctor.com)
  • 2 CADO, adenosine, and the A1 subtype-selective agonists N6-(L-2-Phenylisopropyl)adenosine (R- PIA) and 2-chloro-N6-cyclopentyladenosine (CCPA) reversibly modulated whole cell Ba2+ currents in a concentration-dependent fashion. (gotomydoctor.com)
  • The binding of agonists and antagonists to a2-adrenergic receptors of human platelets was studied. (uni-wuerzburg.de)
  • Agmon Y, Dinour D, Brezis M (1993) Disparate effects of adenosine A1- and A2-receptor agonists on intrarenal blood flow. (springer.com)
  • In human PRP, naloxone (0.1-0.5 mmol/L) inhibited aggregation stimulated by a variety of agonists (i.e. collagen, adenosine diphosphate (ADP), U46619 and adrenaline). (elsevier.com)
  • 5. It is suggested that the anti platelet effects of naloxone may be caused, at least partly, by the induction of conformational changes in the platelet membrane initially, followed by the inhibition of thromboxane A2 formation and phosphoinositide breakdown of platelets stimulated by agonists. (elsevier.com)
  • Lastly, A3AR is expressed in low levels in normal cells whereas the expression is upregulated in tumour cells, however, agonists to this receptor inhibit tumour proliferation through modulation of Wnt and NF-κB signaling pathways. (eurekaselect.com)
  • Active components of A2AAR antagonists and A3AR agonists have already entered in Phase-I clinical research to prove their safety in human. (eurekaselect.com)
  • Pharmacological agents that act at GPCRs can broadly be categorised into four main classes: agonists, inverse agonists, antagonists and allosteric modulators. (europeanpharmaceuticalreview.com)
  • Although the signal transduction mechanisms associated with adrenergic receptor activation are diverse, studies have identified a relationship between the ocular hypotensive action of adrenergic agonists in their ability to stimulate adenylate cyclase. (arvojournals.org)
  • Classical cannabinoid agonists (structures shown in Table 1 ) bind to and activate cannabinoid receptors 1 and 2 (CB1, CB2) that modulate signal transduction cascades to produce various physiological and pathological outcomes. (frontiersin.org)
  • This invention relates to a method of identifying compounds that are selective partial A 2A -adenosine receptor agonists, preferably with a short duration of action. (justia.com)
  • Other potent and selective agonists for the A 2A adenosine receptor are known. (justia.com)
  • In vitro , D 5 receptors show high constitutive activity that is independent of binding any agonists . (wikidoc.org)
  • Vascular leakage secondary to hypoxia was reversed in part by adenosine receptor agonists or reconstitution with soluble 5′-nucleotidase. (rupress.org)
  • This review provides an overview of the medicinal chemistry and therapeutic potential of various agonists/partial agonists, antagonists and allosteric modulators of A1 AR, with a particular emphasis on their current status and future perspectives in clinical settings. (eurekaselect.com)
  • A1 adenosine receptors, A1 AR agonists, partial agonists, antagonists and allosteric modulators, pharmacology of A1 AR, structure- activity relationships of A1 AR. (eurekaselect.com)
  • A1 adenosine receptor agonists, antagonists, and allosteric modulators. (eurekaselect.com)
  • In contrast to the adenosine A2 receptor agonist 5'-N-ethylcarboxamidoadenosine, nucleotide analogues had no discernible effect on cytosolic adenosine 3',5'-cyclic monophosphate levels or adenylyl cyclase activity. (rti.org)
  • The action of adenosine was antagonized by an adenosine A 2 A-receptor (A2AR) antagonist and was mimicked by an A2AR agonist, suggesting that the stimulation of A2AR may be involved in the actions of adenosine. (elsevier.com)
  • MRE3008F20 is a highly potent and selective antagonist of adenosine A3 receptor (AA3R) , inhibiting agonist-induced cAMP elevation in resting T lymphocytes with an IC 50 of 5 nM. (medchemexpress.com)
  • In order to uncover the estrogen effects on adenosine receptor expression, estrogen-positive MCF-7 cells were used to treat with agonist and antagonist of estrogen and then the mRNA expression of adenosine receptor subtypes were evaluated. (readbyqxmd.com)
  • Estrogen-positive MCF-7 cells were treated with various concentrations of 17β estradiol (E2) as an estrogen agonist, and ICI 182,780 as an estrogen antagonist. (readbyqxmd.com)
  • 1991). However, direct regulation studies outlined below, infusion of the non-selective of postsynaptic processes by amygdala adenosine receptors adenosine receptor agonist 2-chloroadenosine (CADO) has not been examined. (gotomydoctor.com)
  • The receptors showed homogeneaus affinities for antagonists but two affinity states for the agonist (-)-epinephrine, which were modulated by guanine nucleotides. (uni-wuerzburg.de)
  • It is concluded that agonist-specific thennodynamic characteristics of ligand binding to a2-receptors of human platelets can only be investigated by regarding differences between high and low affinity agonist binding. (uni-wuerzburg.de)
  • I am interested in how activation of one of these classes of receptor leads to modification of the response to other receptor classes (cross-talk), as well as how different ligands can provoke different signalling profiles at the same receptor (agonist bias). (nottingham.ac.uk)
  • A stable adenosine A1 and A2 receptor agonist. (curehunter.com)
  • Research evidence supports that the activation of those receptors via specific agonist or antagonist can modulate the proliferation of tumour cells. (eurekaselect.com)
  • 1 2 3 Pharmacologically, epinephrine is a nonselective adrenergic agonist that can activate both α- andβ -adrenergic receptors. (arvojournals.org)
  • In the absence of adenosine A2 receptor blockade, the mGluR agonist, 1-aminocyclopentane-1S,3R-dicarboxylic acid (1S,3R-ACPD) stimulated cAMP accumulation through a pertussis toxin-insensitive mechanism that could be blocked by L-serine-o-phosphate, but not by L(+)-2-amino-3-phosphonopropionic acid. (aspetjournals.org)
  • However, in the presence of the adenosine antagonist, 3-isobutyl-1-methylxanthine, 1S,3R-ACPD had no significant effect on basal cAMP, but it inhibited cAMP formation stimulated by the D1 agonist, SKF 38393. (aspetjournals.org)
  • Platelet activation is subsequently propagated through agonist-receptor interaction, mostly including ADP via P2Y 1 /P2Y 12 , thrombin via protease-activated receptor 1(PAR1) and PAR4, and thromboxane via the thromboxane receptor (TP). (omicsonline.org)
  • For example, MRE-0470 (Medco) is an adenosine A 2A receptor agonist that is a potent and selective derivative of adenosine. (justia.com)
  • WRC-0470 (Medco) is an adenosine A 2A agonist used as an adjuvant in imaging. (justia.com)
  • Activator of protein kinase A (cyclic AMP agonist). (biolog.de)
  • Ticlopidine hydrochloride is an adenosine diphosphate (ADP) receptor inhibitor against platelet aggregation with IC50 of ~2 μM. (medchemexpress.com)
  • The second group are agents generated within the platelet that interact with the membrane receptors, for example, adenosine diphosphate (ADP), prostaglandin D2, prostaglandin E2, and serotonin. (americorpshealth.biz)
  • They release thromboxane A2 and adenosine diphosphate (ADP) that amplifies and propagates the process by stimulating surrounding platelets. (medicosnotes.com)
  • Compounds 1 - 5 inhibited the platelet aggregation induced by adenosine diphosphate and/or arachidonic acid, with inhibition rates of 18.0%-61.1% and 65.9%-87.3%, respectively. (mdpi.com)
  • Compounds 1 and 5 were the most active compounds, inhibiting adenosine-diphosphate-induced platelet aggregation by 57.2% and 61.1%, respectively. (mdpi.com)
  • The present study evaluated the effect of T. sarmentosa on adenosine diphosphate-induced platelet aggregation. (ijpsonline.com)
  • Our results showed that aqueous stem extract of T. sarmentosa inhibited adenosine diphosphate-induced platelet aggregation. (ijpsonline.com)
  • In addition, we found components in T. sarmentosa, including caffeic acid, rosmarinic acid, salvianolic acid, play important roles in mediating adenosine diphosphate-induced platelet aggregation suppression. (ijpsonline.com)
  • The stem extract of T. sarmentosa inhibited the adenosine diphosphate receptor P2Y 12 -mediated cyclic AMP production. (ijpsonline.com)
  • Furthermore, treatment of platelets with T. sarmentosa , or the components in stem extract of T. sarmentosa , suppressed adenosine diphosphate-induced release of thromboxane A2 and arachidonic acid and surface PAC-1 expression. (ijpsonline.com)
  • Caffeine also inhibits phosphodiesterase, resulting in increased intracellular cyclic AMP and intracellular calcium levels. (statpearls.com)
  • Elevation of intracellular cyclic AMP levels leads to diverse cellular responses dependent on the cell type. (nottingham.ac.uk)
  • While the alkylxanthine PTX could act as an inhibitor of phosphodiesterases, it is also likely that PTX interferes with the specific ADO receptors thereby increasing intracellular cyclic adenosine monophosphate (cAMP). (springer.com)
  • The adenosine triggers the immunosuppressive signaling via intracellular cyclic AMP-elevating A2A adenosine receptors (A2AR) on antitumor T cells. (aacrjournals.org)
  • Elevation of intracellular cyclic AMP promotes myometrial relaxation, and thus quiescence, via effects on multiple intracellular targets including calcium channels, potassium channels and myosin light chain kinase. (springer.com)
  • In fact, adenosine receptor activation can subtypes of P1 receptors can be distinguished from one even prevent the acquisition of amygdala kindling (Abdul- another by receptor pharmacology or by examination of the signal transduction pathways to which the individual receptors couple. (gotomydoctor.com)
  • For example, the A1 adenosine receptor *Author for correspondence at: Department of Medical subtype is classically associated with the inhibition of Pharmacology and Toxicology, The Texas A&M Univ. (gotomydoctor.com)
  • My central area of research concerns the pharmacology and biochemistry of G protein-coupled receptors (in particular, cannabinoid, adenosine and glutamate) in the CNS and peripheral tissues. (nottingham.ac.uk)
  • Borea PA, Gessi S, Merighi S, Vincenzi F, Varani K. Pharmacology of adenosine receptors: the state of the art. (eurekaselect.com)
  • Theobromine is a methylxanthine found in cacao beans which can inhibit adenosine receptor A1 ( AR1 ) signaling. (medchemexpress.com)
  • anxiety have implicated the basolateral complex (BLA), as Previous work has demonstrated that adenosine receptors being centrally important in both the acquisition and may act presynaptically in the amygdala to inhibit both expression of fear/apprehension-related behaviours (re- excitatory and inhibitory transmission (Heinbockel & viewed in Davis, 1992). (gotomydoctor.com)
  • Barbiturates inhibit binding of radioligands to A 1(Ri) adenosine receptors of rat brain membranes. (uni-wuerzburg.de)
  • The nucleoside adenosine (ADO) has been shown to inhibit several leukocyte functions, such as the production of superoxide anions, degranulation, adherence, and cell-mediated cytotoxicity, and can enhance the chemotactic response of polymorphonuclear leukocytes (PMNL). (springer.com)
  • We now show that MSCs can, dependent on their tissue origin, inhibit platelet activation involving adenosine converted from adenosine monophosphate by CD73 ectonucleotidase activity. (biomedcentral.com)
  • Once the receptor becomes occupied, the alpha subunit exchanges GDP for GTP, becomes activated, and dissociates from the receptor and can stimulate or inhibit many intracellular activities such as phosphorylation and channel conductance. (ubc.ca)
  • Drugs that inhibit ADENOSINE DEAMINASE activity. (nih.gov)
  • Dopamine is a light-adaptive signal in the retina, causing uncoupling of photoreceptors via D4 receptors (D4R), which inhibit adenylyl cyclase (AC) and reduce PKA activity. (jneurosci.org)
  • The use of tocolytic drugs, including those that operate through cyclic AMP such as beta-mimetics, to inhibit uterine contractility in preterm labour is controversial because there is no evidence that currently available drugs improve long term neonatal outcome. (springer.com)
  • After the secretion, 5-HT increases the effects of prothrombotic agents by its binding with 5-HT2 receptors Thromboregulation is also in charge of regulating the process of clot elimination, called primary hemostasis inhibition. (wikipedia.org)
  • The bronchodilatory action of dyphylline, as with other xanthines, is thought to be mediated through competitive inhibition of phosphodiesterase with a resulting increase in cyclic AMP producing relaxation of bronchial smooth muscle as well as antagonism of adenosine receptors. (drugbank.ca)
  • Theophylline causes non-selective inhibition of type III and type IV isoenzymes of phosphodiesterase, which leads to increased tissue cyclic adenine monophosphate (cAMP) and cyclic 3′,5′ guanosine monophosphate concentrations, resulting in smooth muscle relaxation in lungs and pulmonary vessels, diuresis, CNS and cardiac stimulation. (statpearls.com)
  • This mechanism is distinct from PDE and adenosine receptor inhibition. (statpearls.com)
  • CADO inhibition of barium currents was also sensitive to the A1 antagonist 1,3-dipropyl-8-cyclopentylxanthine (DPCPX). (gotomydoctor.com)
  • 5 Using Ca2+ channel subtype-selective antagonists, CADO inhibition appeared to target multiple channel subtypes, with the inhibition of o-conotoxin GVIA-sensitive calcium channels being more prominent. (gotomydoctor.com)
  • 6 Our results indicate that the anti-convulsant e ects CADO in the basolateral amygdala may be mediated, in part, by the A1 receptor-dependent inhibition of voltage gated calcium channels. (gotomydoctor.com)
  • Studies of proposed analgesic-like activity mechanisms have been conducted with some monoterpenes, acting on several receptors, including opioids, adenosine A1 and A2, or cholinergic M2, producing changes in K+ channels, inhibition of peripheral mediators, and nitric oxide synthesis modulation, among others mechanisms [ 4 - 11 ]. (hindawi.com)
  • Bailey MA (2004) Inhibition of bicarbonate reabsorption in the rat proximal tubule by activation of luminal P2Y1 receptors. (springer.com)
  • This latter possibility was supported by the findings that the specific ADO receptor antagonist BW A1433U was able to block PTX in restoring the chemotactic response of human PMNL after inhibition by tumor necrosis factor a (TNF-a) [12]. (springer.com)
  • In addition, the effect of the ADO receptor antagonist 8-phenyltheophylline (8-PT) was compared with the ADO- and PTX-mediated inhibition. (springer.com)
  • Nielson CP, Crowley JJ, Morgan ME, Vestal RE (1988) Polymorphonuclear leukocyte inhibition by therapeutic concentrations of theophylline is mediated by cyclic-3', 5'-adenosine monophosphate. (springer.com)
  • Smellie FW, Davis CW, Daly JW, Wells JN (1979) Alkylxanthines: inhibition of adenosine-elicited accumulation of cyclicAMP in brain slices and of brain phosphodiesterase activity. (springer.com)
  • Sullivan GW, Linden J, Hewlett EL, Carper HT, Hylton JB, Mandell GL (1990) Adenosine and related compounds conteract tumor necrosis factor-α inhibition of neutrophil migration: implication of a novel cAMP-independent action on the cell surface. (springer.com)
  • Prasugrel is a prodrug from the same family as clopidogrel, with more efficient platelet inhibition, a thienopyridine that inhibits the ADP receptors on the platelets, hence preventing them from aggregating and causing blood clots. (medicosnotes.com)
  • Thus, 1S,3R-ACPD was determined to activate distinct mGluRs in the striatum that mediate either inhibition or activation of cAMP accumulation, with the latter effect being dependent on the activation of adenosine A2 receptors. (aspetjournals.org)
  • We propose that tumor protection is to a large extent due to ( a ) inhibition of antitumor T cells by hypoxia-driven accumulation of extracellular adenosine in local tumor microenvironment and due to ( b ) T regulatory cell-produced extracellular adenosine. (aacrjournals.org)
  • The promising strategy may be in combining the anti-hypoxia-adenosinergic treatment that prevents inhibition of antitumor T cells by tumor-produced and T regulatory cell-produced adenosine with targeting of other negative regulators, such as CTL antigen-4 blockade. (aacrjournals.org)
  • Schema of the hypoxia-adenosinergic suppression of antitumor T-cell response ( A ) and suggested therapeutic approach to remove hypoxia/adenosine-mediated T-cell inhibition using antagonists of A2A and A2B adenosine receptors ( B ). (aacrjournals.org)
  • Thromboxane A2 (TX2) has a positive feedback in platelet activation. (wikipedia.org)
  • It is produced by the oxygenation of arachidonic acid by two enzymes: cycloxygenase and thromboxane A2 synthase. (wikipedia.org)
  • These signaling elements include thromboxane A2, receptor type α, phospholipase Cβ3, and IP3 receptors. (wikipedia.org)
  • This kinase inhibits Gαq-phospholipase C-inositol 1,4,5-triphosphate signaling and the mobilization of calcium inside the cell for thromboxane A2. (wikipedia.org)
  • This prostaglandin is a precursor of thromboxane A2 and PGI2. (statpearls.com)
  • Thromboxane A2 works by inducing platelets aggregation and vasoconstriction, and COX-1 inhibits its production while PGI2 works by inhibiting platelets aggregation and induces vasodilation and inhibited by COX-2. (statpearls.com)
  • Effect of serotonin and thromboxane A2 on endothelial cell proliferation: effect of specific receptor antagonists. (rushf.org)
  • Carvedilol may be avoided in elimination in thromboxane a2. (dc3.edu)
  • ASA, if given at low doses,specifically inhibits plateletsynthesis of thromboxane A2 and this will leads to antithrombotic effect. (medicosnotes.com)
  • TxA2, thromboxane A2. (wordpress.com)
  • A 70-year-old woman who have to prove at least 12 1175 leukotriene receptor blockers and thromboxane a2. (apariscommechezsoi.com)
  • As shown in the figure, aspirin inhibits platelet cyclooxygenase, a key enzyme in thromboxane A2 (TXA2) generation. (pharmacologycorner.com)
  • Thromboxane A2 triggers reactions that lead to platelet activation and aggregation, aspirin acts as a potent antiplatelet agent by inhibiting generation of this mediator. (pharmacologycorner.com)
  • It is also known to act as an adenosine antagonist at the A1 and A2 subtypes and as a phosphodiesterase inhibitor. (wikipedia.org)
  • TX2 effects are mediated by G protein-coupled receptors, subtypes TPα and TPβ. (wikipedia.org)
  • Estrogen stimulates adenosine receptor expression subtypes in human breast cancer MCF-7 cell line. (readbyqxmd.com)
  • The activity of adenosine exclusively depends upon the interaction with four subtypes of heterodimeric G-protein-coupled adenosine receptors (AR), A1, A2A, A2B, and A3-ARs on the cell surface. (eurekaselect.com)
  • Adenosine exerts its biological effects by interacting with a family of adenosine receptors characterized as subtypes A 1 , A 2A , A 2B , and A 3 . (justia.com)
  • These adverse effects of adenosine are due to the activation of other adenosine receptor subtypes in addition to A 2A , which mediates the vasodilatory effects of adenosine. (justia.com)
  • Caffeine is a natural alkaloid methylxanthine that acts as a nonselective antagonist of adenosine receptors, with A1 antagonism triggering seizures and A2 antagonism triggering cerebral and coronary vasoconstriction. (statpearls.com)
  • Central effects of adenosine analogs on loco-motor activity in mice and antagonism of caffeine. (springer.com)
  • [6] [7] This antagonism of the adenosine receptors, specifically A1 receptors, is responsible for some of the side effects of theophylline like seizures and cardiac arrhythmias. (statpearls.com)
  • Its principal action is adenosine antagonism, and there are a number of caffeine analogs with variable affinities for A1 and A2 receptors [ 2 ]. (hindawi.com)
  • The main mechanism of action of theophylline is that of adenosine receptor antagonism . (chemeurope.com)
  • In preclinical studies, antagonism of the A2A receptor resulted in increases in dopamine levels, which gave rise to the reversal of motor deficits. (newdrugapprovals.org)
  • These findings suggest an important bimodal role of adenosine in regulating histamine release in the human lung. (uni-wuerzburg.de)
  • In this article, we will describe the role of adenosine signaling in regulating tumor immunity, highlighting potential therapeutic targets in the pathway. (biomedcentral.com)
  • This study evaluated the role of adenosine receptor activation in epinephrine-induced changes in ocular function. (arvojournals.org)
  • In addition, compound 62 showed high functional potency in inhibiting the accumulation of cyclic adenosine monophosphate induced by 5'- N-ethylcarboxamidoadenosine in HEK-A(2B)-AdoR and NIH3T3 cells with K(B) values of 6 and 2 nM, respectively. (nih.gov)
  • In vitro data indicate that the activation of A2 adenosine receptors increases renin release by the accumulation of cyclic AMP. (ahajournals.org)
  • van Calker D, Müller M, Hamprecht B. Adenosine regulates via two different types of receptors, the accumulation of cyclic AMP in cultured brain cells. (eurekaselect.com)
  • ADP-dependent aggregation is mediated by two receptors: the purinergic P2Y1, coupled to Gαq, mediates the shape in the structure of platelets and triggers the aggregation process. (wikipedia.org)
  • Eptifibatide is an intravenous antiplatelet agent that blocks the final common pathway of platelet aggregation and thrombus formation by binding to glycoprotein IIb/IIIa receptors on the surface of platelets. (dovepress.com)
  • Glycoprotein platelets inhibitors work by inhibiting glycoprotein IIb/IIIa (GpIIb-IIIa) receptors on platelets, thus decrease platelet aggregation and most commonly used in an acute form of ACS. (statpearls.com)
  • This enzyme is responsible for degradation of AMP to 5' AMP which increases intra-platelet cyclic AMP accumulation and inhibits platelets aggregation. (statpearls.com)
  • It also blocks the uptake of adenosine by the platelets which also increase cyclic AMP. (statpearls.com)
  • 2. Naloxone (0.1-0.5 mmol/L) did not significantly affect cyclic adenosine monophosphate and cGMP levels in human washed platelets, whereas naloxone (0.5 mmol/L) significantly inhibited thromboxane B 2 formation stimulated by collagen (5 μg/mL) in human washed platelets. (elsevier.com)
  • Platelet membrane GPIIb-IIa receptors constitute the final common pathway of platelet aggregation, the integrin GPIIb/IIIa antagonists prevent cross-linking of platelets. (pharmacologycorner.com)
  • Stimulation of dopamine D1 receptor (D1R) and adenosine A2A receptor (A2AR) increases cAMP-dependent protein kinase (PKA) activity in the brain. (nih.gov)
  • However, exploitation of the 3D structures of GPCRs is now preferable due to the elucidation of the structure of rhodopsin17, followed by those of the beta118, beta219, adrenergic, adenosine A2A20, dopamine D321, CXCR4 chemokine22, histamine H1 receptors23 and recently sphingosine 1-phosphate receptor24 and the M2 muscarinic acetylcholine receptor25. (europeanpharmaceuticalreview.com)
  • Intracellular fragments of the natriuretic peptide receptor-C (NPR-C) attenuate dopamine efflux. (umn.edu)
  • Regulation of striatal cyclic-3',5'-adenosine monophosphate accumulation and GABA release by glutamate metabotropic and dopamine D1 receptors. (aspetjournals.org)
  • In this study, the regulation of striatal cyclic-3',5'-adenosine monophosphate (cAMP) formation and GABA release by dopamine D1 and metabotropic glutamate receptors (mGluR) was studied in brain slices. (aspetjournals.org)
  • The selective expression of high levels of Golf in dopamine-rich forebrain areas suggest that it may couple DI dopamine receptors to adenylyl cyclase. (ubc.ca)
  • Dopamine receptor D 5 , also known as D1BR , is a protein that in humans is encoded by the DRD5 gene . (wikidoc.org)
  • D 5 receptor is a subtype of the dopamine receptor that has a 10-fold higher affinity for dopamine than the D 1 subtype. (wikidoc.org)
  • D 1 receptors were shown to stimulate monophasic dose-dependent accumulation of cAMP in response to dopamine , and the D 5 receptors were able to stimulate biphasic accumulation of cAMP under the same conditions, suggesting that D 5 receptors may use a different system of secondary messengers than D 1 receptors. (wikidoc.org)
  • D 5 receptor is expressed more widely in the CNS than its close structural homolog dopamine receptor D1 . (wikidoc.org)
  • [11] Dopamine receptor D 5 is exclusively expressed by large aspiny neurons in neostriatum of primates, which are typically cholinergic interneurons . (wikidoc.org)
  • Polymorphisms in the DRD5 gene, which encodes dopamine receptor D 5 , have been suggested to play a role in the initiation of smoking. (wikidoc.org)
  • We conclude that adenosine and dopamine coregulate photoreceptor coupling through opposite action on the PKA pathway and Cx36 phosphorylation. (jneurosci.org)
  • The A2A receptor modulates the production of dopamine, glutamine and serotonin in several brain regions. (newdrugapprovals.org)
  • Clopidogrel is a thienopyridine ADP-receptor antagonist which irreversibly binds to the P2Y12 receptor.An ADP receptor antagonist that competitively inhibits ADP from binding to platelet receptors, preventing ADP-mediated up-regulation of glycoprotein (GP) IIb/IIIa receptor, again blocking amplification of platelet aggregation. (medicosnotes.com)
  • These data demonstrate the aqueous stem extract of T. sarmentosa significantly suppressed platelet aggregation through P2Y 1 and P2Y 12 receptor signal pathways. (ijpsonline.com)
  • The platelet GP IIb/IIIa receptor inhibitors, by blocking the final common pathway of platelet aggregation, have become a breakthrough in the management of acute coronary syndromes. (opencardiovascularmedicinejournal.com)
  • Activation of A2AR is known to increase cyclic adenosine monophosphate (cAMP) levels and to activate protein kinase A (PKA). (elsevier.com)
  • Theophylline pretreatment blunted adenosine-mediated forearm blood flow increments and angiotensin II release. (ahajournals.org)
  • Theophylline is a nonselective phosphodiesterase (PDE) inhibitor , adenosine receptor blocker, and histone deacetylase (HDAC) activator. (medchemexpress.com)
  • Caffeine and theophylline as adenosine receptor antagonists in humans. (springer.com)
  • Caffeine and theophylline analogues: Correlation of behavioral effects with activity as adenosine receptor antagonists and as phosphodiesterase inhibitors. (springer.com)
  • Theophylline antagonizes adenosine receptor A1, A2 strongly, and A3 less potently. (statpearls.com)
  • Theophylline also increases calcium uptake through the adenosine-mediated calcium channels in the diaphragm leading to increased contraction and reversal of diaphragm fatigue. (statpearls.com)
  • Theophylline is a non-specific adenosine antagonist, antagonizing A1, A2, and A3 receptors almost equally, which explains many of its cardiac effects and some of its anti-asthmatic effects. (chemeurope.com)
  • FSCPX could modifie the effect of NBTI, a nucleoside transport inhibitor , by reducing the interstitial adenosine level in the guinea pig atrium. (medchemexpress.com)
  • On the other hand, in the presence of the nucleoside transport inhibitor S-(p-nitrobenzyl)-6-thioninosine (NBTI), adenosine caused a reduction in stimulated histamine release. (uni-wuerzburg.de)
  • Effects of adenosine on tubular transport are most pronounced in the proximal tubule where the nucleoside stimulates NaCl reabsorption in the subnormal concentration range while inhibiting transport at elevated levels. (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)
  • In this regard, the level of nucleoside adenosine is increased in individuals with obesity. (elsevier.es)
  • Adenosine is a ubiquitous signaling nucleoside molecule, released from different cells within the body to act on vasculature and immunoescape. (eurekaselect.com)
  • Adenosine, a naturally occurring nucleoside, also is useful as a vasodilator. (justia.com)
  • Adenosine is a purine nucleoside, responsible for the regulation of a wide range of physiological and pathophysiological conditions by binding with four G-protein-coupled receptors (GPCRs), namely A1, A2A, A2B and A3 adenosine receptors (ARs). (eurekaselect.com)
  • Drug classes include: ADP antagonists (Thienopyridines), COX-1 inhibitors (the only member of this class is aspirin), phosphodiestherase inhibitors and GPIIb/IIIa antagonists. (pharmacologycorner.com)
  • The peptide derivatives, eptifibatide and tirofiban are more selective towards the GPIIb/IIIa receptor and have a shorter effect than abciximab. (pharmacologycorner.com)
  • The most serious adverse effects of GPIIB-IIIa antagonists include major bleeding, intracerebral hemorrhage and thrombocytopenia. (pharmacologycorner.com)
  • The current antiplatelet drugs used in daily clinical practice include COX-1 inhibitor aspirin, ADP P2Y12 receptor antagonist clopidogrel, and the GPIIb-IIIa antagonists (abciximab, eptifibatide and tirofiban). (omicsonline.org)
  • To address possible mechanisms for stimulation of Na-K-Cl cotransport by the nucleotide receptor, I-125 efflux and patch-clamp studies were used to measure chloride secretion. (rti.org)
  • This study demonstrates that nucleotide receptors in this model of renal epithelium initiate distinct regulation of Na-K-Cl cotransport. (rti.org)
  • Nucleotide receptors may effect their responses through primary activation of membrane chloride channels. (rti.org)
  • Diphylline (Diprophylline) is a potent A1/A2 adenosine receptor antagonist and cyclic nucleotide phosphodiesterase inhibitor . (medchemexpress.com)
  • Dipyridamole has antiplatelet and vasodilating properties and inhibits platelet cyclic nucleotide phosphodiesterase. (statpearls.com)
  • Considerably higher resistance against cyclic nucleotide phosphodiesterases compared to dibutyryl- or 8-Br-cAMP (Cat. (biolog.de)
  • The generation of extracellular adenosine involves phosphohydrolysis of adenine nucleotide intermediates, and is regulated by the terminal enzymatic step catalyzed by ecto-5′-nucleotidase (CD73). (rupress.org)
  • Previous studies indicated that extracellular nucleotide metabolites, predominantly adenosine, may trigger an endogenous protective mechanism during hypoxia and ischemia ( 12 - 15 ). (rupress.org)
  • However the identification of PRKA substrates in human myometrium is a challenging area of research and more information is required before the mechanism of cyclic nucleotide-induced relaxation is understood. (springer.com)
  • Rabbits were pretreated topically with the moderately selective adenosine A 1 antagonist 8-(p-sulfophenyl)theophyline (8-SPT) or the adenosine A 2 antagonist 3,7-dimethyl-l-propargylxanthine (DMPX). (arvojournals.org)
  • SYN-115, a potent and selective adenosine A2A receptor antagonist, is in phase III clinical trials at Biotie Therapeutics for the treatment of Parkinson's disease, as an adjunjunctive therapy with levodopa. (newdrugapprovals.org)
  • [2] The D 5 subtype is a G-protein coupled receptor , which promotes synthesis of cAMP by adenylyl cyclase via activation of Gα s/olf family of G proteins . (wikidoc.org)
  • Neither the change in [Ca2+]i nor the stimulation of cotransport was abolished by the adenosine receptor antagonist 8-{4-[N-(2-aminoethyl)carbamoylmethoxy]-phenyl}-1,3-dipropylxanthine (XAC). (rti.org)
  • Both receptors mediate phospholipase C stimulation causing an increase of intracellular levels of inositol 1,4,5-triphosphate and diacylglycerol. (wikipedia.org)
  • Because in human forearm vessels beta-adrenergic receptor stimulation causes the local release of renin and angiotensin II through the increase of cyclic AMP, we evaluated in six essential hypertensive subjects whether adenosine can release vascular angiotensin II. (ahajournals.org)
  • Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS. (nih.gov)
  • Glutamate receptors have a large extracellular N-terminus (often likened to a clam) which binds the orthosteric (endogenous) ligand. (europeanpharmaceuticalreview.com)
  • NMDA (N-methyl- D- aspartate) receptor is an ionotropic (Excitatory) glutamate receptor. (blogspot.com)
  • Glutamate receptor antagonists have been shown to ameliorate injury in animal models of focal and global ischemia, Finally glutamate receptors antagonists attenuate injury of cultured neurons when the neurons are exposed to oxygen deprivation. (blogspot.com)
  • The NMDA receptor is the most widely studied glutamate receptor. (blogspot.com)
  • The channel gated by this receptor allows entry of sodium, potassium and calcium, and calcium accumulation via this channel is felt to be responsible for the neuro toxicity of glutamate. (blogspot.com)
  • We further display an increased discharge of glutamate in the vertebral dorsal horn, which blockade of NMDA and non-NMDA glutamate receptors a week after muscles insult [23,24]. (antibodyassay.com)
  • We further hypothesized that activation of PKC in the spinal-cord produces mechanised hyperalgesia through activation of NMDA and non-NMDA glutamate receptors. (antibodyassay.com)
  • Beach RE, Good DW (1992) Effects of adenosine on ion transport in rat medullary thick ascending limb. (springer.com)
  • The local origin of angiotensin II was further confirmed in another group of six hypertensive subjects in whom the angiotensin converting enzyme inhibitor captopril, locally infused at the rate of 2.5 micrograms/100 ml forearm tissue per minute for 15 minutes, abolished the adenosine-mediated venous angiotensin II increments. (ahajournals.org)
  • N-[(4-Aminophenyl)methyl] adenosine is a adenosine receptor inhibitor , with Ki of 29 nM for Rat ecto-5′-Nucleotidase. (medchemexpress.com)
  • 5-Iodotubercidin (NSC 113939), an ATP mimetic, is a potent adenosine kinase inhibitor with an IC 50 of 26 nM. (medchemexpress.com)
  • The binding of the potent adenosine uptake inhibitor [3H]nitrobenzylthioinosine ([3H]NBI) to brain membrane fractions was investigated. (meta.org)
  • abstract = "Adenosine inhibited interleukin (IL)-18 production in lipopolysaccharide (LPS)-stimulated monocytes. (elsevier.com)
  • Jans DA, Peters R, Fahrenholz F. Lateral mobility of the phospholipase-C-activating vasopressin V,-type receptor in A7r5 smooth muscle cells: a comparison with the adenylate cyclase-coupled V2-receptor. (springer.com)
  • It is suggested that these G protein-coupled receptors redundantly activate phospholipase C in basolateral amygdala . (wikidoc.org)
  • The group IIA secretory phospholipase A2 (sPLA2-IIA) continues to be studied extensively due to its involvement in inflammatory processes. (stemcellethics.net)
  • These drugs convert to an active drug with the help of hepatic CYP450 system that inhibits the platelet P2Y12 receptor. (statpearls.com)
  • Cangrelor is a new intravenous, reversible P2Y12 receptor antagonist and has a rapid onset of action. (statpearls.com)
  • It will irreversibly binds to the P2Y12 receptor. (medicosnotes.com)
  • Calcium mobilization by muscarinic receptors in human astrocytoma cells: measurements with quin 2. (nih.gov)
  • Cyclic AMP is a diffusible intracellular second messenger, which influences many physiological events, by transducing hormone and small molecule effects into activation of protein kinases, modulating calcium transport and regulating gene activation. (springer.com)
  • ANP activates guanylyl cyclase that converts guanosine triphosphate into cyclic guanosine monophosphate (cGMP). (bvsalud.org)
  • In this review, we will examine the rationale for therapeutic blockade of this pathway, provide an overview of preclinical data, briefly describe ongoing clinical work, and assess potential future applications targeting the adenosine pathway in cancer immunotherapy. (biomedcentral.com)
  • We found that CRE-mediated gene expression induced by ethanol occurs in two phases: an early phase (4 h), in which adenosine receptor blockade prevents ethanol-induced gene expression, and a later phase (14 h), which is not blocked by an adenosine receptor antagonist. (aspetjournals.org)
  • Adenosine -2'-monophosphate is further metabolized to extracellular adenosine (a mechanism called the extracellular 2',3'-cAMP- adenosine pathway). (medchemexpress.com)
  • Extracellular adenosine has been widely implicated in adaptive responses to hypoxia. (rupress.org)
  • Guided by previous work indicating that hypoxia-induced vascular leakage is, at least in part, controlled by adenosine, we generated mice with a targeted disruption of the third coding exon of Cd73 to test the hypothesis that CD73-generated extracellular adenosine functions in an innate protective pathway for hypoxia-induced vascular leakage. (rupress.org)
  • We also determined whether ethanol-induced increases in gene expression are mediated by ethanol-induced increases in extracellular adenosine. (aspetjournals.org)
  • GPCRs respond to various ligands extracellularly, such as amines, peptides, hydrophobic effectors, hormones, small proteins and volatiles, which allows the receptors to activate the G-proteins intracellularly. (europeanpharmaceuticalreview.com)
  • We hypothesized that the GLP-1R could activate PI 3-kinase and promote β-cell proliferation through transactivation of the epidermal growth factor (EGF) receptor (EGFR), an event possibly linked to GPCRs via activation of c-Src and the production of putative endogenous EGF-like ligands. (diabetesjournals.org)
  • GLP-1 interaction with its specific high-affinity receptor (GLP-1R), a member of the G protein-coupled receptor (GPCR) superfamily, increases cAMP levels in several β-cell models to activate the protein kinase A signal transduction system ( 4 , 17 , 18 ). (diabetesjournals.org)
  • Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS. (nih.gov)
  • Surface-localized CD73 converts AMP into adenosine, which in turn can activate transmembrane adenosine receptors or can be internalized through dipyridamole-sensitive carriers ( 14 ). (rupress.org)
  • The OT released by volume expansion also acts on its tubular receptors to activate nitric oxide synthase. (bvsalud.org)
  • 1) Adenosine 5 - Triphosphate Depletion (ATP). (blogspot.com)
  • Tyrosine kinase and GTP-binding protein activating receptors appear to be essentially different in terms of their lateral mobility properties, and it seems plausible to relate these differences to their distinct signal transduction mechanisms. (springer.com)
  • 1-8 As discussed in chapter 4, lateral movement of hormone-occupied tyrosine kinase receptors is required to effect receptor dimerization which triggers the association of a variety of cytosolic signaling molecules in order to effect signal transduction. (springer.com)
  • The mobile receptor hypothesis revisited: a mechanistic role for hormone receptor lateral mobility in signal transduction. (springer.com)
  • Jans DA, Pavo I. A mechanistic role for polypeptide hormone receptor lateral mobility in signal transduction. (springer.com)
  • Schlessinger J. Signal transduction by allosteric receptor oligomerization. (springer.com)
  • Ullrich A, Schlessinger J. Signal transduction by receptors with tyrosine kinase activity. (springer.com)
  • Adenosine Receptors: Structure, Distribution, and Signal Transduction. (eurekaselect.com)
  • Tolkovsky AM, Levitzki A. Mode of coupling between the (3-adrenergic receptor and adenylate cyclase in turkey erythrocytes. (springer.com)
  • Hanski E, Rimon G, Levitzki A. Adenylate cyclase activation by the 3-adrenergic receptor as a diffusion controlled process. (springer.com)
  • Brum PC, Rolim NP, Bacurau AV, Medeiros A.. Neurohumoral activation in heart failure: the role of adrenergic receptors. (rushf.org)
  • It has been shown that M 1 -Muscarinic receptors cooperate with D 5 receptors and beta-2 adrenergic receptors to consolidate cued fear memory. (wikidoc.org)
  • Regulation of plasma membrane ion transport by endogenous purinergic receptors was assessed in a distal renal (A6) cell line. (rti.org)
  • Barrett RJ, Droppleman DA (1993) Interactions of adenosine A1 receptor-mediated renal vasoconstriction with endogenous nitric oxide and ANG II. (springer.com)
  • This rise in endogenous levels of adenosine then leads to the activation of ocular adenosine receptors and is in part responsible for the ocular hypotensive action of epinephrine. (arvojournals.org)
  • The actions of cannabinoids are also regulated by the endocannabinoid system (ECS) which includes enzymes involved in synthesis, uptake and degradation of endogenous cannabinoid ligands, and the CB1 and CB2 receptors. (frontiersin.org)
  • Adenosine activates a vascular renin-angiotensin system in hypertensive subjects. (ahajournals.org)
  • However, the exact mechanism by which the GLP-1 receptor (GLP-1R), a member of the G protein-coupled receptor (GPCR) superfamily, activates the PI 3-kinase signaling pathway to promote β-cell growth remains unknown. (diabetesjournals.org)
  • Activation of cAMP (cyclic adenosine monophosphate) spinally activates intracellular pathways that leads to sensitization of vertebral neurons and mechanised hyperalgesia. (antibodyassay.com)
  • In line with these findings, chronic (but not acute) combined treatment with D1R plus A2AR antagonists (SCH23390 and SCH58261, respectively) normalizes PKA activity in the hippocampus, facilitates long-term potentiation in behaving R6/1 mice, and ameliorates cognitive dysfunction. (nih.gov)
  • By contrast, chronic treatment with either D1R or A2AR antagonist alone does not modify PKA activity or improve cognitive dysfunction in R6/1 mice. (nih.gov)
  • Hyperactivation of both D1R and A2AR occurs in HD striatum and chronic treatment with D1R plus A2AR antagonists normalizes striatal PKA activity but it does not affect motor dysfunction in R6/1 mice. (nih.gov)
  • Essentially, novel compound demonstrated remarkable potential as A2AR antagonist in the therapy of PD. (curehunter.com)
  • Complete rejection or tumor growth retardation was observed when A2AR has been genetically eliminated or antagonized with synthetic drug or with natural A2AR antagonist 1,3,7-trimethylxanthine (caffeine). (aacrjournals.org)
  • Both D4R and A2a receptor (A2aR) mRNAs were present in photoreceptors, inner nuclear layer neurons, and ganglion cells in C57BL/6 mouse retina, and showed cyclic expression with partially overlapping rhythms. (jneurosci.org)
  • It belongs to the homologous family of glycoprotein IIb-IIa antagonists. (wikipedia.org)
  • Aspirin, the thienopyridine derivatives ticlopidine and clopidogrel, and a number of platelet glycoprotein (GP) IIb/IIIa receptor antagonists have been demonstrated to be efficacious in preventing and/or treating thrombotic vascular disease. (wordpress.com)
  • Strategies for preventing ischemic complications during percutaneous coronary interventions (PCI) in the setting of acute myocardial infarction (AMI) have focused on the platelet surface-membrane glycoprotein (GP) IIb/IIIa receptor. (opencardiovascularmedicinejournal.com)
  • These compounds, which have a high affinity for the A 2A receptor, and, consequently, a long duration of action, which is undesirable in imaging. (justia.com)
  • Preferred compounds would be selective for the A 2A adenosine receptor and have a short duration of action (although longer acting than compounds such as adenosine), thus obviating the need for multiple dosing. (justia.com)
  • Furthermore, natriuresis is rapidly induced by the action of ANP on its tubular guanylyl cyclase receptors, resulting in the production of cGMP that closes Na+ channels. (bvsalud.org)
  • In this review we propose that adenosine could be a key element in the development of new strategies for limit lipoinflammation and regulate metabolic homeostasis through modulation of adipocyte-macrophage dialog. (elsevier.es)
  • Biochemical and pharmacological role of A1 adenosine receptors and their modulation as novel therapeutic strategy In: ed Protein Reviews. (eurekaselect.com)
  • We hypothesized that adenosine, with its extracellular levels increasing in darkness, may serve as a dark signal to coregulate photoreceptor coupling through modulation of gap junction phosphorylation. (jneurosci.org)
  • PKC is normally involved with many areas of mobile sensitization, including modulation of route conductivity by phosphorylation, elevated trafficking of receptors towards the cell membrane, and discharge of excitatory neurotransmitters [4-9]. (antibodyassay.com)
  • Due to caffeine's ability to affect a variety of different receptors, the side effects of caffeine overdose can be profound. (statpearls.com)
  • Cross-tolerance studies between caffeine and (−)-N6- (phenylisopropyl)adenosine (PIA) in mice. (springer.com)
  • Caffeine-induced anxiogenesis: The role of the adenosine, benzodiazepine and noradrenergic receptors. (springer.com)
  • Caffeine-induced increase in adenosine deaminase activity in mammalian lymphoid organs. (springer.com)
  • Caffeine withdrawal affects central adenosine receptors but not benzodiazepine receptors. (springer.com)
  • Caffeine enhances acetylcholine release in the hippocampus in vivo by a selective interaction with adenosine A, receptors. (springer.com)
  • 1997). This anticonvulsant activity of CADO highly integrative role in the sense/memory-response is dose-dependent and blocked by ca eine, suggesting that pathway and is believed to occupy a pivotal position in activation of adenosine heptahelical receptors in the the regulation of fear and anxiety. (gotomydoctor.com)
  • We have shown in the NG108-15 neuroblastoma × glioma hybrid cell line that ethanol increases cellular cAMP levels via activation of adenosine A 2 receptors, leading to phosphorylation of the cAMP response element-binding protein (CREB). (aspetjournals.org)
  • an active role for receptor immobilization in down-regulation? (springer.com)
  • Heterologous up-regulation of Ni-coupled receptors in cultured neural hybrid cells by a transferable factor, whose expression is inhibited in a cyclic AMP-dependent, cell-specific manner. (nih.gov)
  • Adenosine-dependent regulation of renal function in healthy and diseased kidney is mediated by activation of the four types of P1 purinergic adenosine receptors (A 1 AR, A 2A AR, A 2B AR, A 3 AR). (springer.com)
  • 4. Trachte, G.J. , Neuronal Regulation and Function of Natriuretic Peptide Receptor C. Peptides 26: 1060-1067, 2005. (umn.edu)
  • Both protein kinase C (PKC) and A (PKA) are involved in regulation of γ-aminobutyric acid type A (GABA A ) receptors through phosphorylation. (frontiersin.org)
  • D 5 receptors are expressed in kidneys and are involved in regulation of sodium excretion. (wikidoc.org)
  • An additional focus of my research has been an investigation of enzymes (particularly those involved in turnover of endocannabinoids, hydrogen sulphide and cyclic nucleotides), as convergence points for signalling cross-talk, as well as quantifying enzyme activities ex vivo , for example, in pathological conditions or following drug exposure. (nottingham.ac.uk)
  • Dipyridamole act by inhibiting the activity of adenosine deaminase and phosphodiesterase, this will result in accumulation of adenosine, adenine nucleotides, and cyclic adenosine monophosphate. (medicosnotes.com)
  • It inhibits adenosine uptake and cyclic GMP phosphodiesterase activity, this decreases platelet aggregability. (pharmacologycorner.com)
  • The adenylate cyclase-coupled vasopressin V2-receptor is highly laterally mobile in membranes of LLC-PK, renal epithelial cells at physiological temperature. (springer.com)
  • The presence of unsaturation in its cyclic chain structure confers the olefin characteristic for the γ -TPN, which allows easier absorption through biological membranes, due to the lipossolubility [ 15 ]. (hindawi.com)
  • Here, we investigated the role of the A2B adenosine receptor (A2BAR) and its associated signaling pathways in governing the proliferation and viability of breast cancer cell line derived CSCs. (readbyqxmd.com)
  • Purinergic receptors are implicated in the pathogenesis of gastrointestinal disorders and are being explored as potential therapeutic targets. (readbyqxmd.com)
  • Aki Y, Tomohiro A, Nishiyama A et al (1997) Effects of KW-3902, a selective and potent adenosine A1 receptor antagonist, on renal hemodynamics and urine formation in anesthetized dogs. (springer.com)
  • Tolkovsky A, Braun S, Levitzki A. Kinetics of interaction between 3-receptors, GTP-proteins and the catalytic subunit of turkey erythrocyte adenylate cyclase. (springer.com)
  • Behavioral interaction of adenosine and methylxanthines on central purinergic systems. (springer.com)
  • A potential physiological role for the interaction between the D1 and adenosine-dependent stimulatory metabotropic receptor was sought by examining this interaction on striatal GABA release. (aspetjournals.org)
  • However, it has become clear that not all effects of cannabinoid drugs are attributable to their interaction with CB1 and CB2 receptors. (frontiersin.org)
  • Thus, a stimulatory effect of adenosine was seen in the presence ofXAC, whereas an inhibitory effect was unmasked by NBTI. (uni-wuerzburg.de)
  • Babich V, Vadnagara K, Di Sole F (2015) Dual effect of adenosine a1 receptor activation on renal O2 consumption. (springer.com)
  • Thiel M, Bardenheuer H (1989) Effect of adenosine on oxygen free radical production in human polymorphonuclear leukocytes. (springer.com)
  • Our data indicate that exogenous adenosine can stimulate the production of angiotensin II in the forearm vessels of hypertensive patients. (ahajournals.org)
  • 1987). Unlike A1 receptors, A2 adenosine receptors appear to couple to cholera toxin- Neurons were prepared from coronal brain slices of juvenile sensitive G proteins and can stimulate cyclic AMP male rats (*P17 ± P28) as previously described (McCool & accumulation. (gotomydoctor.com)
  • The slight stimulatory effect of NBTI alone demonstrates that trapping intracellularly formed adenosine inside mast cells leads to sufficient concentrations of adenosine to stimulate histamine release. (uni-wuerzburg.de)
  • cAMP, cyclic adenosine monophosphate, phosphorylate messengers via protein kinase A (PKA). (wikipedia.org)
  • Schlessinger J. The epidermal growth factor receptor as a multifunctional allosteric protein. (springer.com)
  • To explore the impact of electroacupuncture (EA) on the protein expression of adenosine receptors in the heart of the rats with myocardial ischemia (MI). (readbyqxmd.com)
  • Experimental studies with experimental rodent models and cultures (cardiac myocytes, endothelial cells) indicate that moderate alcohol exposure can promote anti-inflammatory processes involving adenosine receptors, protein kinase C (PKC), nitric oxide synthase, heat shock proteins, and others which could underlie cardioprotection. (pubmedcentralcanada.ca)
  • G protein-coupled receptor list: recommendations for new pairings with cognate ligands. (nottingham.ac.uk)
  • G-protein coupled receptors (GPCRs) are a diverse super-family of proteins located within the plasma membrane of eukaryotic cells which have a common architecture consisting of seven-transmembrane (7-TM) segments, connected by extracellular (ECL) and intracellular (ICL) loops. (europeanpharmaceuticalreview.com)
  • To achieve this, we probed the role of increased leptin action as a result of insulin therapy, determined the function of insulin-like growth factor binding protein-2 (IGFBP2) in the glucose lowering actions of leptin, investigated the necessity of insulin for leptin treatment and glucagon suppression therapy, and explored the potential of glucagon suppression therapy via glucagon receptor (Gcgr) small interfering ribonucleic acid (siRNA) delivered by lipid nanoparticle (LNP) technology. (ubc.ca)
  • Activation of D 5 receptors is shown to promote expression of brain-derived neurotrophic factor and increase phosphorylation of protein kinase B in rat and mice prefrontal cortex neurons. (wikidoc.org)
  • D 5 receptor has a long C-terminus of 93 amino acids , accounting for 26% of the entire protein. (wikidoc.org)
  • Adenosine signaling has emerged as a key metabolic pathway that regulates tumor immunity. (biomedcentral.com)
  • As we saw in the previous chapter, direct measurements indicate that plasma membrane polypeptide hormone receptors are mobile within the plane of the lipid bilayer. (springer.com)
  • Ammonium chloride affects receptor number and lateral mobility of the vasopressin V2-type receptor in the plasma membrane of LLC-PK, renal epithelial cells: role of the cytoskeleton. (springer.com)
  • The first group are agents generated outside the platelet that interact with platelet membrane receptors, for example, catecholamines, collagen, thrombin, and prostacyclin. (americorpshealth.biz)
  • Many of the receptors have accessory proteins which either facilitate trafficking to the plasma membrane or influence the specificity of the ligand 8 . (europeanpharmaceuticalreview.com)
  • Each of the symbol cD leukotriene receptor causing membrane by atheroma. (apariscommechezsoi.com)
  • [12] Within a cell, D 5 receptors are found on the membrane of soma and proximal dendrites . (wikidoc.org)