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.
Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.
Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.
An enzyme that catalyzes the hydrolysis of ADENOSINE to INOSINE with the elimination of AMMONIA.
Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.
A ligand that binds to but fails to activate the INTERLEUKIN 1 RECEPTOR. It plays an inhibitory role in the regulation of INFLAMMATION and FEVER. Several isoforms of the protein exist due to multiple ALTERNATIVE SPLICING of its mRNA.
A 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.
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.
Compounds that inhibit or block the activity of NEUROKININ-1 RECEPTORS.
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.
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 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.
The relationship between the dose of an administered drug and the response of the organism to the drug.
A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.
Compounds that bind to and stimulate PURINERGIC P1 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.
A family of hexahydropyridines.
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.
Compounds that selectively bind to and block the activation of ADENOSINE A3 RECEPTORS.
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.
Agents that antagonize ANGIOTENSIN RECEPTORS. Many drugs in this class specifically target the ANGIOTENSIN TYPE 1 RECEPTOR.
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.
Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.
Adenine nucleotide containing one phosphate group esterified to the sugar moiety in the 2'-, 3'-, or 5'-position.
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 stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity.
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.
Agents inhibiting the effect of narcotics on the central nervous system.
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.
Cell surface proteins that bind ENDOTHELINS with high affinity and trigger intracellular changes which influence the behavior of cells.
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.
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.
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 compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)
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 RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.
Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.
A class of drugs designed to prevent leukotriene synthesis or activity by blocking binding at the receptor level.
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.
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.
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.
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.
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.
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.
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.
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 selectively bind to and activate ADENOSINE A3 RECEPTORS.
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.
Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.
Compounds with BENZENE fused to AZEPINES.
N-Isopropyl-N-phenyl-adenosine. Antilipemic agent. Synonym: TH 162.
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.
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 PURINERGIC RECEPTORS.
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.
Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.
Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS.
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.
Drugs that selectively bind to but do not activate HISTAMINE H3 RECEPTORS. They have been used to correct SLEEP WAKE DISORDERS and MEMORY DISORDERS.
A group of compounds that contain the structure SO2NH2.
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.
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)
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).
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.
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.
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.
Elements of limited time intervals, contributing to particular results or situations.
Compounds that bind to and block the stimulation of PURINERGIC P2X RECEPTORS. Included under this heading are antagonists for specific P2X receptor subtypes.
Seven membered heterocyclic rings containing a NITROGEN atom.
An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.
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.
Drugs that bind to but do not activate GABA-B RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-B RECEPTOR AGONISTS.
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)
The action of a drug that may affect the activity, metabolism, or toxicity of another drug.
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.
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)
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.
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.
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.
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.
A subtype of endothelin receptor found predominantly in the KIDNEY. It may play a role in reducing systemic ENDOTHELIN levels.
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.
The observable response an animal makes to any situation.
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 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.
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.
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 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.
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.
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.
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.
A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.
Drugs that bind to but do not activate SEROTONIN 5-HT4 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN RECEPTOR AGONISTS.
Drugs that bind to but do not activate ADRENERGIC RECEPTORS. Adrenergic antagonists block the actions of the endogenous adrenergic transmitters EPINEPHRINE and NOREPINEPHRINE.
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.
Compounds with a BENZENE fused to IMIDAZOLES.
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.
PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS.
Injections into the cerebral ventricles.
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 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.
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.
A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.
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.
A competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.
Compounds that inhibit or block the activity of CANNABINOID RECEPTORS.
An isoquinoline alkaloid obtained from Dicentra cucullaria and other plants. It is a competitive antagonist for GABA-A receptors.
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.
Drugs that bind to and block the activation of ADRENERGIC BETA-2 RECEPTORS.
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 rate dynamics in chemical or physical systems.
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.
Use of electric potential or currents to elicit biological responses.
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.
A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H3 receptors were first recognized as inhibitory autoreceptors on histamine-containing nerve terminals and have since been shown to regulate the release of several neurotransmitters in the central and peripheral nervous systems. (From Biochem Soc Trans 1992 Feb;20(1):122-5)
Drugs that bind to and block the activation of MINERALOCORTICOID RECEPTORS by MINERALOCORTICOIDS such as ALDOSTERONE.
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 histamine H1 antagonist. It has mild hypnotic properties and some local anesthetic action and is used for allergies (including skin eruptions) both parenterally and locally. It is a common ingredient of cold remedies.
Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.
An alkylamide found in CAPSICUM that acts at TRPV CATION CHANNELS.
A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.
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.
A constitutively expressed subtype of bradykinin receptor that may play a role in the acute phase of the inflammatory and pain response. It has high specificity for intact forms of BRADYKININ and KALLIDIN. The receptor is coupled to G-PROTEIN, GQ-G11 ALPHA FAMILY and G-PROTEIN, GI-GO ALPHA FAMILY signaling proteins.
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.
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).
Drugs used to cause dilation of the blood vessels.
21-Amino-acid peptides produced by vascular endothelial cells and functioning as potent vasoconstrictors. The endothelin family consists of three members, ENDOTHELIN-1; ENDOTHELIN-2; and ENDOTHELIN-3. All three peptides contain 21 amino acids, but vary in amino acid composition. The three peptides produce vasoconstrictor and pressor responses in various parts of the body. However, the quantitative profiles of the pharmacological activities are considerably different among the three isopeptides.
A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D1-class receptor genes lack INTRONS, and the receptors stimulate ADENYLYL CYCLASES.
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).
Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS.
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.
The physiological narrowing of BLOOD VESSELS by contraction of the VASCULAR SMOOTH MUSCLE.
Peptides composed of between two and twelve amino acids.
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)
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.
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.
Cell surface proteins that bind CALCITONIN GENE-RELATED PEPTIDE with high affinity and trigger intracellular changes which influence the behavior of cells. CGRP receptors are present in both the CENTRAL NERVOUS SYSTEM and the periphery. They are formed via the heterodimerization of the CALCITONIN RECEPTOR-LIKE PROTEIN and RECEPTOR ACTIVITY-MODIFYING PROTEIN 1.
A class of opioid receptors recognized by its pharmacological profile. Mu opioid receptors bind, in decreasing order of affinity, endorphins, dynorphins, met-enkephalin, and leu-enkephalin. They have also been shown to be molecular receptors for morphine.
Benzopyrroles with the nitrogen at the number two carbon, in contrast to INDOLES which have the nitrogen adjacent to the six-membered ring.
Cell surface proteins that bind corticotropin-releasing hormone with high affinity and trigger intracellular changes which influence the behavior of cells. The corticotropin releasing-hormone receptors on anterior pituitary cells mediate the stimulation of corticotropin release by hypothalamic corticotropin releasing factor. The physiological consequence of activating corticotropin-releasing hormone receptors on central neurons is not well understood.
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.
An angiotensin receptor subtype that is expressed at high levels in a variety of adult tissues including the CARDIOVASCULAR SYSTEM, the KIDNEY, the ENDOCRINE SYSTEM and the NERVOUS SYSTEM. Activation of the type 1 angiotensin receptor causes VASOCONSTRICTION and sodium retention.
Compounds capable of relieving pain without the loss of CONSCIOUSNESS.
Cell surface proteins that bind TACHYKININS with high affinity and trigger intracellular changes influencing the behavior of cells. Three classes of tachykinin receptors have been characterized, the NK-1; NK-2; and NK-3; which prefer, respectively, SUBSTANCE P; NEUROKININ A; and NEUROKININ B.
The physical activity of a human or an animal as a behavioral phenomenon.
The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.
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.
A technique for measuring extracellular concentrations of substances in tissues, usually in vivo, by means of a small probe equipped with a semipermeable membrane. Substances may also be introduced into the extracellular space through the membrane.
Cell surface proteins that bind ANGIOTENSINS and trigger intracellular changes influencing the behavior of cells.
Cell surface receptors that bind signalling molecules released by neurons and convert these signals into intracellular changes influencing the behavior of cells. Neurotransmitter is used here in its most general sense, including not only messengers that act to regulate ion channels, but also those which act on second messenger systems and those which may act at a distance from their release sites. Included are receptors for neuromodulators, neuroregulators, neuromediators, and neurohumors, whether or not located at synapses.
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.
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)
Drugs that bind to and activate dopamine receptors.
A class of drugs that act by selective inhibition of calcium influx through cellular membranes.
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.
A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties.
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 class of opioid receptors recognized by its pharmacological profile. Kappa opioid receptors bind dynorphins with a higher affinity than endorphins which are themselves preferred to enkephalins.
The physiological widening of BLOOD VESSELS by relaxing the underlying VASCULAR SMOOTH MUSCLE.
The principal alkaloid in opium and the prototype opiate analgesic and narcotic. Morphine has widespread effects in the central nervous system and on smooth muscle.
Two-ring crystalline hydrocarbons isolated from coal tar. They are used as intermediates in chemical synthesis, as insect repellents, fungicides, lubricants, preservatives, and, formerly, as topical antiseptics.
The most common inhibitory neurotransmitter in the central nervous system.
A statistical technique that isolates and assesses the contributions of categorical independent variables to variation in the mean of a continuous dependent variable.
A drug that exerts an inhibitory effect on gastric secretion and reduces gastrointestinal motility. It is used clinically in the drug therapy of gastrointestinal ulcers.
1,4-Diethylene dioxides. Industrial solvents. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), dioxane itself may "reasonably be anticipated to be a carcinogen." (Merck Index, 11th ed)
A serotonin receptor subtype found widely distributed in peripheral tissues where it mediates the contractile responses of variety of tissues that contain SMOOTH MUSCLE. Selective 5-HT2A receptor antagonists include KETANSERIN. The 5-HT2A subtype is also located in BASAL GANGLIA and CEREBRAL CORTEX of the BRAIN where it mediates the effects of HALLUCINOGENS such as LSD.
A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.
A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279)
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.
AMANTADINE derivative that has some dopaminergic effects. It has been proposed as an antiparkinson agent.
The number of times the HEART VENTRICLES contract per unit of time, usually per minute.
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)
The injection of very small amounts of fluid, often with the aid of a microscope and microsyringes.
A serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic for cancer chemotherapy patients.
Catalyze the hydrolysis of nucleosides with the elimination of ammonia.
An electrophysiologic technique for studying cells, cell membranes, and occasionally isolated organelles. All patch-clamp methods rely on a very high-resistance seal between a micropipette and a membrane; the seal is usually attained by gentle suction. The four most common variants include on-cell patch, inside-out patch, outside-out patch, and whole-cell clamp. Patch-clamp methods are commonly used to voltage clamp, that is control the voltage across the membrane and measure current flow, but current-clamp methods, in which the current is controlled and the voltage is measured, are also used.
Compounds that bind to and block the stimulation of PURINERGIC P2Y RECEPTORS. Included under this heading are antagonists for specific P2Y receptor subtypes.
Established cell cultures that have the potential to propagate indefinitely.

Contribution of adenosine to the depression of sympathetically evoked vasoconstriction induced by systemic hypoxia in the rat. (1/257)

Previous studies have shown that systemic hypoxia evokes vasodilatation in skeletal muscle that is mediated mainly by adenosine acting on A1 receptors, and that the vasoconstrictor effects of sympathetic nerve activity are depressed during hypoxia. The aim of the present study was to investigate the role of adenosine in this depression. In anaesthetised rats, increases in femoral vascular resistance (FVR) evoked by stimulation of the lumbar sympathetic chain with bursts of impulses at 40 or 20 Hz were greater than those evoked by continuous stimulation at 2 Hz with the same number of impulses (120) over 1 min. All of these responses were substantially reduced by infusion of adenosine or by graded systemic hypoxia (breathing 12, 10 or 8 % O2), increases in FVR evoked by continuous stimulation at 2 Hz being most vulnerable. Blockade of A1 receptors ameliorated the depression caused by adenosine infusion of the increase in FVR evoked by 2 Hz only and did not ameliorate the depression caused by 8 % O2 of increases in FVR evoked by any pattern of sympathetic stimulation. A2A receptor blockade accentuated hypoxia-induced depression of the increase in FVR evoked by burst stimulation at 40 Hz, but had no other effect. Neither A1 nor A2A receptor blockade affected the depression caused by hypoxia (8 % O2) of the FVR increase evoked by noradrenaline infusion. These results indicate that endogenously released adenosine is not responsible for the depression of sympathetically evoked muscle vasoconstriction caused by systemic hypoxia; adenosine may exert a presynaptic facilitatory influence on the vasoconstrictor responses evoked by bursts at high frequency.  (+info)

Neuroprotection by caffeine and adenosine A2A receptor blockade of beta-amyloid neurotoxicity. (2/257)

Adenosine is a neuromodulator in the nervous system and it has recently been observed that pharmacological blockade or gene disruption of adenosine A(2A) receptors confers neuroprotection under different neurotoxic situations in the brain. We now observed that coapplication of either caffeine (1-25 micro M) or the selective A(2A) receptor antagonist, 4-(2-[7-amino-2(2-furyl)(1,2,4)triazolo (2,3-a)(1,3,5)triazin-5-ylamino]ethyl)phenol (ZM 241385, 50 nM), but not the A receptor antagonist, 8-cyclopentyltheophylline (200 nM), prevented the neuronal cell death caused by exposure of rat cultured cerebellar granule neurons to fragment 25-35 of beta-amyloid protein (25 micro M for 48 h), that by itself caused a near three-fold increase of propidium iodide-labeled cells. This constitutes the first in vitro evidence to suggest that adenosine A(2A) receptors may be the molecular target responsible for the observed beneficial effects of caffeine consumption in the development of Alzheimer's disease.  (+info)

Synergistic effect of SCH 58261, an adenosine A2A receptor antagonist, and L-DOPA on the reserpine-induced muscle rigidity in rats. (3/257)

The aim of the present study was to find out whether a blockade of adenosine A2A receptors by the selective antagonist, SCH 58261, potentiates the attenuating effect of L-DOPA, the well-known antiparkinsonian drug, on parkinsonian-like muscle rigidity in rats. Muscle tone was examined using a combined mechano- and electromyographic method, which simultaneously measured muscle resistance of a rat hindfoot to passive extension and flexion in the ankle joint and the electromyographic (EMG) activity of the antagonistic muscles of that joint: gastrocnemius and tibialis anterior. Muscle rigidity was produced by reserpine (5 mg/kg ip) injected in combination with alpha-methyl-p-tyrosine (alpha-MT, 250 mg/kg ip). L-DOPA (25 mg/kg ip) or SCH 58261 (0.1 mg/kg ip) administered separately, slightly influenced the reserpine + alpha-MT-induced muscle rigidity. However, only ankle joint extension was affected significantly while the effect on flexion of the rat hindfoot was not significant. Neither L-DOPA nor SCH 58261 given separately modified the reserpine-enhanced tonic or reflex EMG activities in both muscles examined. However, when L-DOPA (25 mg/kg) was given together with SCH 58261 (0.1 mg/kg), a clear synergistic effect was seen on both examined movements and muscles. The present results show that the blockade of adenosine A2A receptors potentiates the antiparkinsonian effect of L-DOPA. Since such an effect was seen in different animal models of Parkinson's disease (PD), it seems that co-administration of SCH 58261 may allow for the lowering of the doses of L-DOPA in clinical practice, which indicates a potential therapeutic value of this compound in the treatment of PD.  (+info)

Brief, repeated, oxygen-glucose deprivation episodes protect neurotransmission from a longer ischemic episode in the in vitro hippocampus: role of adenosine receptors. (4/257)

1. Ischemic preconditioning in the brain consists of reducing the sensitivity of neuronal tissue to further, more severe, ischemic insults. We recorded field epsps (fepsps) extracellularly from hippocampal slices to develop a model of in vitro ischemic preconditioning and to evaluate the role of A1, A2A and A3 adenosine receptors in this phenomenon. 2. The application of an ischemic insult, obtained by glucose and oxygen deprivation for 7 min, produced an irreversible depression of synaptic transmission. Ischemic preconditioning was induced by four ischemic insults (2 min each) separated by 13 min of normoxic conditions. After 30 min, an ischemic insult of 7 min was applied. This protocol substantially protected the tissue from the irreversible depression of synaptic activity. 3. The selective adenosine A1 receptor antagonist, 8-cyclopentyl-1,3-dipropylxanthine (DPCPX, 100 nm), completely prevented the protective effect of preconditioning. The selective adenosine A2A receptor antagonist 4-(2-[7-amino-2-(2-furyl)[1,2,4]triazolo[2,3-a][1,3,5]triazin-5-ylamino]ethyl)phe nol (ZM 241385, 100 nm) did not modify the magnitude of fepsp recovery compared to control slices. The selective A3 adenosine receptor antagonists, 3-propyl-6-ethyl-5[ethyl(thio)carbonyl]-2-phenyl-4-propyl-3-pyridinecarboxylate (MRS 1523, 100 nm) significantly improved the recovery of fepsps after 7 min of ischemia. 4. Our results show that in vitro ischemic preconditioning allows CA1 hippocampal neurons to become resistant to prolonged exposure to ischemia. Adenosine, by stimulating A1 receptors, plays a crucial role in eliciting the cell mechanisms underlying preconditioning; A2A receptors are not involved in this phenomenon, whereas A3 receptor activation is harmful to ischemic preconditioning.  (+info)

Adenosine-induced IL-6 expression in pituitary folliculostellate cells is mediated via A2b adenosine receptors coupled to PKC and p38 MAPK. (5/257)

Activation of adenosine receptors in folliculostellate (FS) cells of the pituitary gland leads to the secretion of IL-6 and vascular endothelial growth factor (VEGF). We investigated the action of adenosine A2 receptor agonists on IL-6 and VEGF secretion in two murine FS cell lines (TtT/GF and Tpit/F1), and demonstrated a rank order of potency, 5'-N-ethylcarboxamidoadenosine (NECA)>2-p-(2-carboxyethyl)phenethylamino-5'-N-ethylcarboxamidoadenosine>adenosin e, suggesting mediation via the A2b receptor. NECA-mediated IL-6 release was inhibited by the PLC inhibitor 1-[6-((17beta-3-methoxyestra-1,3,5(10)-tiene-17-yl)amino)hexyl]-1H-pyrrole-2,5-di one, the PI3 kinase inhibitor wortmannin and the PKC inhibitors bisindolylmaleimide 1 and bisindolymaleimide X1 HCl (Ro-32-0432). NECA-mediated IL-6 release was attenuated (<50%) by the extracellular signal-regulated kinase MAPK inhibitor 2'-amino-3'-methoxyflavone, and completely (>95%) inhibited by the p38 MAPK inhibitor 4-(4-fluorophenyl)-2-(4-methylsulphinylphenyl)-5-(4-pyridyl)1H-imidazole. NECA stimulates p38 MAPK phosphorylation that is inhibited by Ro-32-0432 but not by wortmannin. Dexamethasone inhibits NECA-stimulated IL-6 and VEGF secretion. These findings indicate that adenosine can stimulate IL-6 secretion in FS cells via the A2b receptor coupled principally to PLC/PKC and p38 MAPK; such an action may be important in the modulation of inflammatory response processes in the pituitary gland.  (+info)

Possible targeting of G protein coupled receptors to manipulate inflammation in vivo using synthetic and natural ligands. (6/257)

Cyclic AMP elevating Gs protein coupled receptors were considered for a long time to be immunosuppressive. One of these receptors, adenosine A(2A) receptor, was implicated in a physiological mechanism that down regulates inflammation and protects tissues from excessive immune mediated damage. Targeting of these receptors by selective agonists may lead to better protocols of anti-inflammatory treatments. At the same time inhibiting the Gs protein coupled mediated signalling with antagonists could be explored in studies of approaches to enhance inflammation and tissue damage. Enhancement of targeted tissue damage is highly desirable when it is cancerous tissue, while enhancement of inflammatory events might be desirable in the development of new vaccine adjuvants.  (+info)

Involvement of adenosine A1 and A2A receptors in the adenosinergic modulation of the discriminative-stimulus effects of cocaine and methamphetamine in rats. (7/257)

Adenosine, by acting on adenosine A1 and A2A receptors, is known to antagonistically modulate dopaminergic neurotransmission. We have recently reported that nonselective adenosine receptor antagonists (caffeine and 3,7-dimethyl-1-propargylxanthine) can partially substitute for the discriminative-stimulus effects of methamphetamine. In the present study, by using more selective compounds, we investigated the involvement of A1 and A2A receptors in the adenosinergic modulation of the discriminative-stimulus effects of both cocaine and methamphetamine. The effects of the A1 receptor agonist N6-cyclopentyladenosine (CPA; 0.01-0.1 mg/kg) and antagonist 8-cyclopentyl-1,3-dimethylxanthine (CPT; 1.3-23.7 mg/kg) and the A2A receptor agonist 2-p-(2-carboxyethyl)phenethylamino-5'-N-ethylcarboxamidoadenosine hydrochloride (CGS 21680; 0.03-0.18 mg/kg) and antagonist 3-(3-hydroxypropyl)-8-(3-methoxystyryl)-7-methyl-1-propargylxanthin phosphate disodium salt (MSX-3; 1-56 mg/kg) were evaluated in rats trained to discriminate either 1 mg/kg methamphetamine or 10 mg/kg cocaine from saline under a fixed-ratio 10 schedule of food presentation. The A1 and A2A receptor antagonists (CPT and MSX-3) both produced high levels of drug-lever selection when substituted for either methamphetamine or cocaine and significantly shifted dose-response curves of both psychostimulants to the left. Unexpectedly, the A2A receptor agonist CGS 21680 also produced drug-appropriate responding (although at lower levels) when substituted for the cocaine-training stimulus, and both CGS 21680 and the A1 receptor agonist CPA significantly shifted the cocaine dose-response curve to the left. In contrast, both agonists did not produce significant levels of drug-lever selection when substituted for the methamphetamine-training stimulus and failed to shift the methamphetamine dose-response curve. Therefore, adenosine A1 and A2A receptors appear to play important but differential roles in the modulation of the discriminative-stimulus effects of methamphetamine and cocaine.  (+info)

Antinociceptive effects of novel A2B adenosine receptor antagonists. (8/257)

Caffeine, an adenosine A1, A2A, and A2B receptor antagonist, is frequently used as an adjuvant analgesic in combination with nonsteroidal anti-inflammatory drugs or opioids. In this study, we have examined the effects of novel specific adenosine receptor antagonists in an acute animal model of nociception. Several A2B-selective compounds showed antinociceptive effects in the hot-plate test. In contrast, A1- and A2A-selective compounds did not alter pain thresholds, and an A3 adenosine receptor antagonist produced thermal hyperalgesia. Evaluation of psychostimulant effects of these compounds in the open field showed only small effects of some antagonists at high doses. Coadministration of low, subeffective doses of A2B-selective antagonists with a low dose of morphine enhanced the efficacy of morphine. Our results indicate that analgesic effects of caffeine are mediated, at least in part, by A2B adenosine receptors.  (+info)

The IUPHAR/BPS Guide to Pharmacology. istradefylline ligand page. Quantitative data and detailed annnotation of the targets of licensed and experimental drugs.
In 6-OHDA-lesioned rats, repeated administration produces behavioral sensitization, manifested as a marked increase in l-Dopa-induced contralateral rotations across days of treatment (Henry et al., 1998). Behavioral sensitization has been suggested to predict the development of dyskinesias after chronic treatment with l-Dopa (Tronci et al., 2007). Here, we found that l-Dopa produced behavioral sensitization after only 4 days of treatment in 6-OHDA-lesioned rats. However, when l-Dopa was delivered concurrently with preladenant, the rats displayed no behavioral sensitization for as long as 23 days of treatment. The blockade of behavioral sensitization by preladenant in this model suggests that this agent may not only have antiparkinsonian effects on its own but also may reduce dyskinesias when used in combination with l-Dopa.. Aside from the motor symptoms that characterize PD, there are a collection of nonmotor symptoms that are not treated by current pharmacotherapies. One of the most severe is ...
How and where to buy Nourianz/Nouriast: You can order Nourianz/Nouriast from TheSocialMedwork if the drug has not been approved or is not available in your country.
Major surface area glycoprotein (Msg) one of the most abundant cell surface area protein of in 3 species of cant be cultured promoter activity was measured in luciferase being a reporter gene. different types with infecting human beings infecting rats and infecting mice (7-9). Main surface area glycoprotein (Msg) may be the most abundant proteins in the cell surface area of gene is certainly expressed within an specific cell and that expressed gene is situated downstream of an area termed the upstream conserved series (UCS) (17-21). Although appearance of Msg gene variations continues to be well studied small Istradefylline is known about how exactly expression is governed. In and since intergenic locations are often ~300 to 500 bp lengthy (unpublished observations). This shows that this area may be essential in regulating appearance perhaps through promoter components (22). Although cannot presently end up being cultured for suffered periods advancement of vectors you can use to transfect ...
Test-retest reproducibility study of [C-11]Preladenant. Assessment of stability and variation of the PET measures in healthy volunteers.
Discouraging news this week for the Parkinson s community, as drug giant Merck announced that they will discontinue their program developing a novel therapy for PD called preladenant.
3-(2,4,4-trimethylpentan-2-ylamino)propanenitrile chemical properties, What are the chemical properties of 3-(2,4,4-trimethylpentan-2-ylamino)propanenitrile 86375-28-2, What are the physical properties of 3-(2,4,4-trimethylpentan-2-ylamino)propanenitrile ect.
Structure, properties, spectra, suppliers and links for: N-[3-(2,1,3-Benzothiadiazol-5-ylamino)-2-quinoxalinyl]-4-methylbenzenesulfonamide.
Disclosed are processes for the synthesis of novel compounds that are A.sub.2B adenosine receptor antagonists, having the structure of Formula I or Formula II: ##STR00001## by cyclizing a compound of the formula (3): ##STR00002##
Prostaglandins (PGs) are essential the different parts of inflammatory discomfort as indicated with the efficiency of cyclooxygenase 1/2 (COX1/2) inhibitors. reducing the synthesis and/or discharge of vasoactive realtors. Synthesis and features of arachidonic acidity and its own metabolites Arachidonic acidity (AA) and its own metabolites get excited about a Istradefylline number of important cardiovascular features. In this specific article, we address the adverse cardiovascular results that arise due to stop of PG mediated modulation of nociceptive ion stations. AA is normally created from membrane phospholipids by phospholipase A2 (PLA2), a calcium-dependent enzyme, which is normally turned on by proinflammatory realtors and shear tension exerted over the vessel wall structure. Activation of phospholipase C (PLC) hydrolyzes phosphatidyl inositol 4, 5 bisphosphate (PIP2) to inositol 1, 4, 5 trisphosphate (IP3) and diacyl glycerol (DAG). DAG activates proteins kinase C (PKC) and DAG lipase, ...
Learn about regadenoson: What is it used for, what you need to know before taking, important warnings and safety info, how to take, side effects and more...
SCH 442416 is a selective adenosine A2A receptor antagonist; binds to human and rat A2A receptors with high affinity (Ki values are 0.048 and 0.5 nM respectively). Displays > 23000-fold selectivity for hA2A over hA1 in vitro with minimal affinity for h
4-((8-amino-3,6,10,13,16,19-hexaazabicyclo(6.6.6)icosane-1-ylamino)methyl)benzoic acid: a bifunctional chelating agent; structure in first source
DESCRIPTION: (Adapted from the Investigators Abstract): Adenosine administered as an aerosol to asthmatics causes bronchoconstriction, while in non-asthmatics adenosine causes bronchodilation. This occurs because the activation of A2B adenosine receptors on sensitized mast cells triggers degranulation, releasing histamine, leukotrienes, and other allergic mediators. A2B adenosine receptors are blocked by theophylline, a xanthine that is effective in treating asthma. However, theophylline is a non-selective antagonist of all four adenosine receptor subtypes and produces side effects due primarily to A1 receptor blockade, including insomnia and diuresis. The incidence of asthma is increasing and current treatment options are limited. New drugs that are potent and selective antagonists of A2B adenosine receptors have great potential for the treatment of asthma and other allergic diseases. Adenosine Therapeutics, LLC owns the first potent and selective A2B antagonists. The purpose of this phase I ...
ALI is one of the leading causes of morbidity and mortality of critical illness with extremely limited therapeutic options. In the present study, we pursued the hypothesis that tissue-specific adenosine signaling events through the A2B adenosine receptor contribute to lung protection and can thus be targeted for ALI treatment. To make progress on this front, we performed a head-to-head comparison of mice with genetic deletion of Adora2b in the myeloid lineage, vascular endothelial cells, or alveolar epithelial cells. Interestingly, we only observed a phenotype in mice with tissue-specific Adora2b deletion in alveolar epithelial cells, closely resembling the observed detrimental effects of global Adora2b deletion during ALI. Interestingly, the injurious effects of our two-hit model where an inflammatory event (i.t. LPS treatment) is followed by injurious mechanical ventilation seem to be supra-additive compared with the effects of injurious ventilation or LPS i.t. alone. Based on these findings ...
The proinflammatory cytokine macrophage migration inhibitory factor (MIF) has been proven to become cardioprotective in a variety of pathological conditions. the result which was avoided by MIF knockout. Furthermore, our data exhibited that degrees of MIF, AMPK activation and autophagy were elevated in individual faltering hearts concurrently. These data reveal that endogenous MIF regulates the mTOR signaling Istradefylline to activate autophagy to protect cardiac geometry and drive back hypertrophic replies. model. To combine the helpful aftereffect of autophagy in phenylephrine-induced hypertrophic response, autophagy was inhibited using 3-methyl adenine (3-MA). Our outcomes uncovered that autophagy inhibition with 3-MA markedly marketed phenylephrine-induced upsurge in the cell surface area compared with cells treated with phenylephrine alone. Furthermore, the beneficial effect of MIF reconstitution against exacerbation in phenylephrine-induced hypertrophic response was nullified by autophagy ...
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The present invention provides compounds and pharmaceutical compositions that are substituted pyridyl-linked-xantbines of formula I which are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.
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The adenosinergic pathway plays a critical role in cancer development and progression, as well as in drug resistance to chemotherapy and/or targeted-therapy. The goal of this PhD thesis was to investigate and fully ...
A review. The low affinity A2B adenosine receptor, like any other adenosine receptor subtype, belongs to the super-family of seven transmembrane domain G protein-coupled receptors (7TMs GPCR) and is classified by the GPCR database in the family of rhodopsin like receptors (Class A of GPCR). It has been cloned from various species, including rat and human, and its sequences are highly similar across species, ranging from 85% identity between human and mouse and 95% identity between rat and mouse. The A2B receptors show a ubiquitous distribution, the highest levels are present in cecum, colon and bladder, followed by blood vessels, lung, eye and mast cells. Through A2B receptors adenosine seems to cause mast cells degranulation, vasodilation, cardiac fibroblast proliferation, inhibition of Tumor Necrosis Factor (TNF-α), increased synthesis of interleukin-6 (IL-6), stimulation of Cl- secretion in intestinal epithelia and hepatic glucose prodn. Hence, A2B adenosine receptor agonists could be useful ...
Regadenoson produced higher stress MBF than dipyridamole and adenosine (3.58 ± 0.58 vs. 2.81 ± 0.67 vs. 2.78 ± 0.61 ml/min/g, p = 0.0009 and p = 0.0008 respectively). Regadenoson had a much higher heart rate response than adenosine and dipyridamole respectively (95 ± 11 vs. 76 ± 13 vs. 86 ± 12 beats/ minute) When stress MBF was adjusted for heart rate, there were no differences between regadenoson and adenosine (37.8 ± 6 vs. 36.6 ± 4 μl/sec/g, p = NS), but differences between regadenoson and dipyridamole persisted (37.8 ± 6 vs. 32.6 ± 5 μl/sec/g, p = 0.03). The unadjusted MPR was higher with regadenoson (3.11 ± 0.63) when compared with adenosine (2.7 ± 0.61, p = 0.02) and when compared with dipyridamole (2.61 ± 0.57, p = 0.04). Similar to stress MBF, these differences in MPR between regadenoson and adenosine were abolished when adjusted for heart rate (2.04 ± 0.34 vs. 2.12 ± 0.27, p = NS), but persisted between regadenoson and dipyridamole (2.04 ± 0.34 vs. 1.77 ± 0.33, p = ...
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This trial will investigate the effects of single doses of preladenant and placebo on the dyskinesia and antiparkinsonian actions of a levodopa infusion.
The development, maintenance and repair of the skeletal system are dependent on the differentiation of both chondrocytes and osteoblasts from their common progenitor, the mesenchymal stem cell (MSC). The A2B adenosine receptor (A2BAR) is a G-protein-coupled receptor that signals by increasing cAMP and/or activating phospholipase C signaling. Considering the published roles of cAMP on MSC differentiation, and our finding that the expression of the A2BAR is induced following injury, we hypothesized that ablation or activation of the A2BAR impacts the differentiation of osteoblasts and chondrocytes and that this would manifest as changes in skeletal development and bone fracture repair. Activation of the A2BAR increased the differentiation of bone marrow-derived MSCs to osteoblasts by increasing mRNA expression of the transcription factors runt-related transcription factor 2 (Runx2) and Sp7 transcription factor (Osterix), which are essential for osteoblast differentiation. To examine the effect of ...
TY - JOUR. T1 - Attenuation of chronic pulmonary inflammation in A2B adenosine receptor knockout mice. AU - Zaynagetdinov, Rinat. AU - Ryzhov, Sergey. AU - Goldstein, Anna E.. AU - Yin, Huiyong. AU - Novitskiy, Sergey V.. AU - Goleniewska, Kasia. AU - Polosukhin, Vasiliy V.. AU - Newcomb, Dawn C.. AU - Mitchell, Daphne. AU - Morschl, Eva. AU - Zhou, Yang. AU - Blackburn, Michael R.. AU - Peebles, R. Stokes. AU - Biaggioni, Italo. AU - Feoktistov, Igor. PY - 2010/5/1. Y1 - 2010/5/1. N2 - Pharmacologic evidence suggests that activation of A2B adenosine receptors results in proinflammatory effects relevant to the progression of asthma, a chronic lung disease associated with elevated interstitial adenosine concentrations in the lung. This concept has been challenged by the finding that genetic removal of A2B receptors leads to exaggerated responses in models of acute inflammation. Therefore, the goal of our study was to determine the effects of A2B receptor gene ablation in the context of ...
Information for 5,8-Dimethoxy-[1,2,4]triazolo[1,5-c]pyrimidin-2-amine 219715-62-5 including 5,8-Dimethoxy-[1,2,4]triazolo[1,5-c]pyrimidin-2-amine CAS NO 219715-62-5, 5,8-Dimethoxy-[1,2,4]triazolo[1,5-c]pyrimidin-2-amine Suppliers, 5,8-Dimethoxy-[1,2,4]triazolo[1,5-c]pyrimidin-2-amine Manufacturers, related products of 5,8-Dimethoxy-[1,2,4]triazolo[1,5-c]pyrimidin-2-amine.
This work done by an eminent group in the area raises concerns over the use of regadenoson for clinical stress testing, whether done by PET or SPECT. Invasive and pharmacologic studies had previously demonstrated peak regadenoson effect at approximately 1-2 minutes after injection, consistent with the findings of the present study. Stress labs which are not already following a 1- to 2-minute delay may wish to consider introducing one.. There are several reasons to view these results with caution, however. First, many prior studies had compared regadenoson to other vasodilators using a variety of techniques including PET, SPECT, and invasive methods. In general, no significant differences or only minimal differences, below the level of clinical relevance, were observed. The reasons for the discrepancies are unclear.. One longstanding concern with regards to regadenoson has been the use of a single fixed dose without weight adjustment, as is usually done for other vasodilators. The investigators ...
Approximately 250 patients who are referred for a nuclear stress testing of the heart with regadenoson (Lexiscan®) will be recruited to participate in the study. Following regadenoson (administered as part of a stress routine test protocol) participants will receive either aminophylline (75 mg - intravenously) or a matching inactive placebo (sterile salt water) injection. Participants will be surveyed for gastrointestinal symptoms and other side effects related to regadenoson. The frequency and severity of such side effects will be compared between the two study groups (aminophylline vs. placebo ...
You are looking for 2,6-di-tert-butyl-4-(4,6-bis(octylthio)-1,3,5-triazin-2-ylamino)phenol from Kuo Ching Chemical Co., LTD ? ...
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Regadenoson is an A2A adenosine receptor agonist that causes coronary vasodilation and used for myocardial perfusion imagining. Manufactured by Astellas and FDA approved April 10, 2008.
We investigated the electrophysiological effects of cardiac hypertrophy induced by different experimental models. Comparison of the action potentials of hypertrophied and control rat hearts reveals a pronounced prolongation of the action potential fo
Page contains details about film of 3,9-di(9H-carbazol-9-yl)benzo-[d]benzo[4,5]imidazo[2,1-b]thiazole doped with 10-(4-(4,6-diphenyl-1,3,5-triazin-2-yl)phenyl)-9,9-diphenyl-9,10-dihydroacridine . It has composition images, properties, Characterization methods, synthesis, applications and reference articles : nano.nature.com
Microwave Induced Synthesis of 3-Aryl-6-(6-/8-substituted 4-chloroquinoline-3-yl) - s -triazolo [3,4-|em|b]|/em| −1,3,4-thiadiazoles | Ren-Zhong Qiao; Xta-Ptag Hui; Peng-Fei Xu; Zi-Yi Zhang; Dong-Liang Cheng | download | BookSC. Download books for free. Find books
This patent search tool allows you not only to search the PCT database of about 2 million International Applications but also the worldwide patent collections. This search facility features: flexible search syntax; automatic word stemming and relevance ranking; as well as graphical results.
IL-2Rα Antagonist - CAS 1217448-66-2 - Calbiochem The IL-2Rα Antagonist, also referenced under CAS 1217448-66-2, controls the biological activity of IL-2Rα. - Find MSDS or SDS, a COA, data sheets and more information.
Corresponding Author: Anaclet Ngezahayo Department of Cell Physiology and Biophysics, Institute of Cell Biology and Biophysics, Leibniz University Hannover, Herrenhäuser Straße 2, Hannover, 30419 (Germany ...
A Quinolino novel series[3,2-f] [1,2,4] The [3,4-b] Triazolo [1,3,4] The Thiadiazepine (7a-i) derivatives incorporated with 3-(5-i) (benzofuran-2-yl) -1-phenyl-1H-3-yl pyrazol) Moiety was synthesised by a 5-(5-(benzofuran-2-yl)-1-phenyl-1H-pyrazol-3-yl)) one-point cyclo-condensation reaction. -4-amino-4H-1,2,4-triazole-3-thiol (4) in the presence of K2CO3 in DMF with 2-chloro-quinoline-3-carbaldehyde derivatives (6a-i). Characterization of 3-(5-(benzofuran-2-yl)-1-phenyl-1H-pyrazol-3-yl)-substituted quinolino [3,2-f] newly synthesised compounds [1,2,4] triazolo[3,4-b] triazolo Elemental analysis and spectral studies such as FT-IR, 1H NMR and 13C NMR, further assisted by Mass Spectra, have been performed with[1,3,4]thiadiazepines. Both synthesised compounds were tested in vitro against the pathogenic microorganism bacterial strains, S. aureus E.coli, P.vulgaris, S.typhi at different concentrations for their antimicrobial activities. In comparison with Chloramphenicol, the bioassay outcome ...
Read about the chemical and physical properties of 2-(4-Chloro-benzylsulfanyl)-5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidine. Get 2-(4-Chloro-benzylsulfanyl)-5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidine molecular formula, CAS number, boiling point, melting point, applications, synonyms and more here.
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2,6-Bis(5,6-diisopropyl-1,2,4-triazin-3-yl)pyridine: a highly selective N-donor ligand studied by TRLFS, liquid-liquid extraction and molecular ...
6-(2-hydroxy-1-naphthyl)-3-thioxo-3,4-dihydro-1,2,4-triazin-5(2H)-one - chemical structural formula, chemical names, chemical properties, synthesis references
Boc Sciences offers cas 20125-39-7 N6-(2-Phenylethyl)-adenosine in bulk,please inquire us to get a quote for 20125-39-7 N6-(2-Phenylethyl)-adenosine.
10. Akbarzadeh T, Noushini S, Taban S, Mahdavi M, Khoshneviszadeh M, Saeedi M, Emami S, Eghtedari M, Sarrafi Y, Khoshneviszadeh M, Safavi M, Divsalar K, Moshafi MH, Asadipour A, Sabourian R, Edraki N, Firouzi O, Miri R, Shafiee A, Foroumadi A. 2015 Synthesis and cytotoxic activity of novel poly-substituted imidazo[2,1-[Formula: see text]][1,2,4]triazin-6-amines. Mol Divers. 2015;19(2):273-81 ...
Schwabe, U; Ukena, D; Lohse, MJ (September 1985). "Xanthine Derivatives as Antagonists at A1 and A2 Adenosine Receptors". ... It acts as an adenosine receptor antagonist and phosphodiesterase inhibitor. Xanthine "International Non-Proprietary Names. ...
... activity as antagonists of A1- and A2-adenosine receptors". Biochemical Pharmacology. 37 (4): 655-64. doi:10.1016/0006-2952(88) ... 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 ... O'Brien, Robert (1986). Receptor binding in drug research. New York: Dekker. p. 519. ISBN 0-8247-7548-1. US Patent 3966746 ...
"Comparison of the behavioural effects of an adenosine A1/A2-receptor antagonist, CGS 15943A, and an A1-selective antagonist, ... CGS-15943 is a drug which acts as a potent and reasonably selective antagonist for the adenosine receptors A1 and A2A, having a ... It was one of the first adenosine receptor antagonists discovered that is not a xanthine derivative, instead being a ... Holtzman SG (1991). "CGS 15943, a nonxanthine adenosine receptor antagonist: effects on locomotor activity of nontolerant and ...
... and reduces inflammation and innate immunity nonselective adenosine receptor antagonist, antagonizing A1, A2, and A3 receptors ... 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 ... asthma infant apnea Blocks the action of adenosine; an inhibitory neurotransmitter that induces sleep, contracts the smooth ...
... a potent and selective adenosine A2 receptor antagonist". European Journal of Pharmacology. 267 (3): 335-41. doi:10.1016/0922- ... Older research on adenosine receptor function, and non-selective adenosine receptor antagonists such as aminophylline, focused ... As a result, Adenosine receptor A2A decreases activity in the Dopamine D2 receptors. The adenosine A2A receptor has also been ... "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ...
In order to be able to characterize the function of adenosine A2 receptors, potent and selective A2-receptor antagonists were ... 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- ... In order to achieve high affinity at adenosine receptors, certain criteria must be fulfilled. Adenosine receptor antagonists, ...
... an adenosine A1-receptor antagonist, on diuresis and renal function in patients with acute decompensated heart failure and ... Caffeine may reduce cerebral blood flow in premature infants, it is presumed by blocking vascular A2 ARs. Thus, it may prove ... The adenosine A1 receptor is one member of the adenosine receptor group of G protein-coupled receptors with adenosine as ... The adenosine A1 receptor has been found to be ubiquitous throughout the entire body. Activation of the adenosine A1 receptor ...
... is a caffeine analog which displays affinity to A2 adenosine receptors, in contrast to the A1 subtype receptors. DMPX had 28× ... a potent and selective in vivo antagonist of adenosine analogs". Life Sciences. 43 (21): 1671-84. doi:10.1016/0024-3205(88) ...
These signaling elements include thromboxane A2, receptor type α, phospholipase Cβ3, and IP3 receptors. Signalization in ... It belongs to the homologous family of glycoprotein IIb-IIa antagonists. Kistrin has an adhesion site that binds to GP IIb-IIIa ... cAMP, cyclic adenosine monophosphate, phosphorylate messengers via protein kinase A (PKA). ... TX2 effects are mediated by G protein-coupled receptors, subtypes TPα and TPβ. Both receptors mediate phospholipase C ...
... a potent and selective adenosine A2 receptor antagonist.". Eur. J. Pharmacol. 267 (3): 335-41. PMID 8088373. doi:10.1016/0922- ... 1992). "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor.". Genomics ... "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics 11 (1): ... 1994). "Identification of adenosine A2 receptor-cAMP system in human aortic endothelial cells.". Biochem. Biophys. Res. Commun. ...
It acts as a positive allosteric modulator of the GABAA receptor at the barbiturate binding site, as an adenosine antagonist of ... 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". ... Zezula J, Slany A, Sieghart W (April 1996). "Interaction of allosteric ligands with GABAA receptors containing one, two, or ...
Asapiprant (S-555739) and Laropiprant are selective receptor antagonists of DP1 whereas Vidupiprant is a receptor antagonist ... the DP1-dependent stimulation of adenosine formation and subsequent simulation of the Adenosine A2A receptor by adenosine. In ... 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: ...
... a novel specific adenosine A(3) receptor antagonist with adenosine A(3) receptor agonists both in vitro and in vivo". Eur. J. ... 1997). "Adenosine inhibits neutrophil degranulation in activated human whole blood: involvement of adenosine A2 and A3 ... a novel ligand that demonstrates both adenosine A(2A) receptor agonist and adenosine A(3) receptor antagonist activity". ... is an adenosine receptor, but also denotes the human gene encoding it. Adenosine A3 receptors are G protein-coupled receptors ...
1992). "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor.". Genomics ... GR-127,935 (mešoviti 5-HT1B/1D antagonist). *LY-310,762. *LY-367,642 ... 5-HT1D receptor (5-hidroksitriptaminski (serotoninski) receptor 1D, HTR1D) je 5-HT receptor. On je kodiran istoimenim genom.[1] ... Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A • ...
... a novel ligand that demonstrates both adenosine A(2A) receptor agonist and adenosine A(3) receptor antagonist activity". ... 1997). „Adenosine inhibits neutrophil degranulation in activated human whole blood: involvement of adenosine A2 and A3 ... Adenosine Receptors: A3". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology ... Docking studies of agonists and antagonists suggest an activation pathway of the A3 adenosine receptor". Journal of Molecular ...
"Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ... mixed 5-HT1B/1D antagonist) LY-310,762 LY-367,642 LY-456,219 LY-456,220 5-HT1 receptor 5-HT receptor GRCh38: Ensembl release 89 ... 5-hydroxytryptamine (serotonin) receptor 1D, also known as HTR1D, is a 5-HT receptor, but also denotes the human gene encoding ... 5HT1D receptor is a G protein linked receptor that activates an intracellular messenger cascade to produce an inhibitory ...
The A1 receptors couple to Gi/o and decreases cAMP levels, while the A2 adenosine receptors couple to Gs, which stimulates ... 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 ... Adenosine is believed to be an anti-inflammatory agent at the A2A receptor. Topical treatment of adenosine to foot wounds in ...
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 ... Gray MO, Karliner JS, Mochly-Rosen D (Dec 1997). "A selective epsilon-protein kinase C antagonist inhibits protection of ... Yang Z, Sun W, Hu K (Apr 2012). "Molecular mechanism underlying adenosine receptor-mediated mitochondrial targeting of protein ...
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). " ... Mello, F. G. (October 1978). "The Ontogeny of Dopamine-Dependent Increase of Adenosine 3',5'-Cyclic Monophosphate in the Chick ... It belongs to the D1-like receptor family along with the D1 receptor subtype. D5 receptor is a subtype of the dopamine receptor ...
... the H2-receptor antagonists. PPIs are among the most widely sold medications in the world. The class of proton-pump inhibitor ... Lucendo AJ, Arias Á, Molina-Infante J (January 2016). "Efficacy of Proton Pump Inhibitor Drugs for Inducing Clinical and ... Proton pump inhibitors act by irreversibly blocking the hydrogen/potassium adenosine triphosphatase enzyme system (the H+/K+ ... H2-receptor antagonists and prokinetics for gastro-oesophageal reflux disease-like symptoms and endoscopy negative reflux ...
... glutamate receptor antagonist on ethanol consumption by genetic drinking rats. Alcohol, 40, 494-497. Hodge, C.W., Miles, M.F., ... Katsura, M., Shibasaki, M., Hayashida, S., Torigoe, F., Tsujimura, A., Ohkuma, S. (2006) Increase in expression of a1 and a2/d1 ... Pandey, S.C., Roy, A., Zhang, H. (2003). The decreased phosphorylation of cyclic adenosine monophosphate (cAMP) response ... receptors are glutamate receptors particularly important in long-term potentiation in neurons. These receptors have been linked ...
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 ... It promotes vasodilation of smooth muscles by increasing the activity of cyclic adenosine monophosphate (cAMP) to decrease ... "A live imaging cell motility screen identifies prostaglandin E2 as a T cell stop signal antagonist". Journal of Immunology. 187 ...
... 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 ... "Differential Sensitivity of Various Markers of Platelet Activation with Adenosine Diphosphate". BioNanoScience. 9 (1): 53-58. ... These receptors trigger intraplatelet signaling, which converts GPIIb/IIIa receptors to their active form to initiate ...
Montelukast, Zafirlukast, and Pranlukast are receptor antagonists for the Cysteinyl leukotriene receptor 1 which contributes to ... The cytosolic PLA2 set (i.e. cPLA2s) of PLA2 enzymes (cPLA2; see Phospholipase A2#Cytosolic phospholipases A2) in particular ... may serve as a mobile lid over ALOX5's substrate-binding site An Adenosine triphosphate (ATP) binding site; ATP is crucial for ... as well as of LTC4 and LTD4 receptor antagonists have proven inferior to corticosteroids as single drug therapy for persistent ...
Antagonists[edit]. Main article: Receptor antagonist. An antagonist is a chemical that acts within the body to reduce the ... Adenosine. Ado. Adenosine receptors. -. Small: Purine. Adenosine triphosphate. ATP. P2Y receptors. P2X receptors. ... "Hindbrain noradrenergic A2 neurons: diverse roles in autonomic, endocrine, cognitive, and behavioral functions". American ... NMDA receptors, kainate receptors, AMPARs. Small: Amino acids. Gamma-aminobutyric acid. GABA. GABAB receptors. GABAA receptors ...
... 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 ...
Thromboxane A2 receptor. TP. TXA=PGH2,,PGD2=PGE2=PGF2α=PGI2[14]. contractile. Gq alpha subunit. stimulates PLC & IP3; raises Ca ... 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 ... There are 9 established prostanoid receptors. The following table gives these receptors: a) full name; b) shortened names; c) ...
... drugs which are selective receptor antagonists of CysLTR1 but not CysLTR2.[20][21][22][23] Models of allergic reactions in ... TP (TXA2). *Agonists: Carbocyclic thromboxane A2. *I-BOP. *Thromboxane A2 ... leukotriene receptor activity. • cysteinyl leukotriene receptor activity. • galanin receptor activity. Cellular component. • ... "Leukotriene Receptors: CysLT2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ...
PDP2 receptor antagonists have been shown to allergic reactions induced in the airways mice and sheep as well as the airways ... 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 ... prostaglandin D receptor activity. • G-protein coupled receptor activity. • prostaglandin J receptor activity. • prostaglandin ...
Receptor antagonists. *ERA (Atrasentan). *Retinoid X receptor (Bexarotene). *Sex steroid (Testolactone). Other/ungrouped. * ... Adenosine deaminase inhibitor (Pentostatin). *Halogenated/ribonucleotide reductase inhibitors (Cladribine. *Clofarabine. * ...
Montelukast, Zafirlukast, and Pranlukast are receptor antagonists for the Cysteinyl leukotriene receptor 1 which contributes to ... The cytosolic PLA2 set (i.e. cPLA2s) of PLA2 enzymes (cPLA2; see Phospholipase A2#Cytosolic phospholipases A2) in particular ... An Adenosine triphosphate (ATP) binding site; ATP is crucial for ALOX5's metabolic activity ... as well as of LTC4 and LTD4 receptor antagonists have proven inferior to corticosteroids as single drug therapy for persistent ...
"Prostanoid Receptors: EP3". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ... Antagonists: RO1138452. TP (TXA2). *Agonists: Carbocyclic thromboxane A2. *I-BOP ... prostaglandin receptor activity. • signal transducer activity. • prostaglandin E receptor activity. • protein binding. ... Prostaglandin E2 receptor 4 (EP4). അവലംബം[തിരുത്തുക]. *↑ 1.0 1.1 1.2 GRCh38: Ensembl release 89: ENSG00000050628 - Ensembl, May ...
血栓素合成酶抑制劑(英語:Thromboxane synthase inhibitors)(雙嘧達莫、吡考他胺(英語:Picotamide)) · 受體拮抗劑(英語:Thromboxane receptor antagonist)(Terutroban( ... ADP受體/P2Y12(英語:P2Y12)抑制劑(英語:Adenosine diphosphate receptor inhibitor)類 ... 阿司匹林低劑量服用時能阻止血小板中血栓素A2的合成,這會在受影響的血小板的
... called H2-receptor antagonists. PPIs are among the most widely sold drugs in the world, and the first one, omeprazole, is on ... Proton pump inhibitors act by irreversibly blocking the hydrogen/potassium adenosine triphosphatase enzyme system (the H+/K+ ... Lucendo AJ, Arias Á, Molina-Infante J (2015). "Efficacy of Proton Pump Inhibitor Drugs for Inducing Clinical and Histological ... H2-receptor antagonists and prokinetics for gastro-oesophageal reflux disease-like symptoms and endoscopy negative reflux ...
It binds in a reversible fashion to the adenosine triphosphate (ATP) binding site of the receptor.[28] For the signal to be ... Ephrins (A1, A2, A3, A4, A5, B1, B2, B3). *Erythropoietin (see here instead) ... It is a receptor tyrosine kinase inhibitor, which acts on the epidermal growth factor receptor (EGFR). ... Antagonists: ANA-12. *Cyclotraxin B. *Gossypetin (3,5,7,8,3',4'-HHF) ...
Adenosine reuptake inhibitor (AdoRI). *Angiotensin II receptor antagonist. *Endothelin receptor antagonist. *NK1 receptor ... Newton, David; Alasdair Thorpe; Chris Otter (2004). Revise A2 Chemistry. Heinemann Educational Publishers. p. 1. ISBN 0-435- ... Major receptor types studied in pharmacology include G protein coupled receptors, ligand gated ion channels and receptor ... Systems, receptors and ligands[edit]. This section needs expansion. You can help by adding to it. (July 2019) ...
Sunitinib, an inhibitor of the receptors for FGF, PDGF and VEGF is also based on early studies on TKIs aiming at VEGF receptors ... TKIs operate by four different mechanisms: they can compete with adenosine triphosphate (ATP), the phosphorylating entity, the ... Ephrins (A1, A2, A3, A4, A5, B1, B2, B3). *Erythropoietin (see here instead) ... Antagonists: ANA-12. *Cyclotraxin B. *Gossypetin (3,5,7,8,3',4'-HHF) ...
Most commonly, enzymes known as adenosine deaminases acting on RNA (ADARs) catalyze adenosine to inosine (A to I) transitions. ... miR-382 is the target for the dopamine receptor D1 (DRD1), and its overexpression results in the upregulation of DRD1 and delta ... The specific microRNA, miR-506 has been found to work as a tumor antagonist in several studies. A significant number of ... "High mobility group A2 protein and its derivatives bind a specific region of the promoter of DNA repair gene ERCC1 and modulate ...
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 ... associated with acetylcholine receptor deficiency; 608931; MUSK Myasthenic syndrome, congenital, associated with acetylcholine ...
... direct-acting Antagonist and indirect-acting Antagonists: Direct-acting antagonist- which takes up space present on receptors ... adenosine triphosphate (ATP), adenosine Others: acetylcholine (ACh), anandamide, etc. In addition, over 50 neuroactive peptides ... Rinaman L (February 2011). "Hindbrain noradrenergic A2 neurons: diverse roles in autonomic, endocrine, cognitive, and ... An irreversible antagonist binds so strongly to the receptor as to render the receptor unavailable for binding to the agonist. ...
They are SRIs and litoxetine is also a 5-HT3 receptor antagonist while lubazodone is also a 5-HT2A receptor antagonist. In the ... PMID 21701626.CS1 maint: multiple names: authors list (link) Romero-Martínez Á, Murciano-Martí S, Moya-Albiol L (May 2019). "Is ... One such possible mechanism is the increased levels of cyclic adenosine monophosphate (cAMP) as a result of interference with ... Fluvoxamine is an agonist of the σ1 receptor, while sertraline is an antagonist of the σ1 receptor, and paroxetine does not ...
Adenosine A2 Receptor Antagonist Pipeline Insight, 2018 report by DelveInsight offers comprehensive insights of the pipeline ... Pipeline Therapeutics assessment of products for Adenosine A2 Receptor Antagonist The report assesses the active Adenosine A2 ... Adenosine A2 Receptor Antagonist Pipeline Insight, 2018 [Report Updated: 14022018] Prices from USD $1250. 02:34 EDT 21 Mar 2018 ... Features the Adenosine A2 Receptor Antagonist pipeline across the complete product development cycle including all clinical and ...
Effect of A2 Adenosine Receptor Antagonists on Adoptively Transferred Antitumor CD8+ T Cells.. The A2 receptors antagonists ... Effect of A2 Adenosine Receptor Antagonist on Endogenously Developed Antitumor CD8+ T Cells.. The antagonists significantly ... A2 adenosine receptor antagonists also improved the antitumor activity of effector CD8+ T cells specific for the poorly ... T cells and A2 receptor antagonists. (c) ZM241,385, an antagonist of A2AR and A2BR, enhances CD8+ T cell-mediated antitumor ...
Adenosine A2 Receptor Antagonists. Purinergic P1 Receptor Antagonists. Purinergic Antagonists. Purinergic Agents. ... Participation in a previous adenosine A2A trial.. *Participation in any other investigational drug study within 1 month prior ...
Adenosine A2 Receptor Antagonists. Purinergic P1 Receptor Antagonists. Purinergic Antagonists. To Top ... An Open-Label, Positron Emission Tomography Study to Assess Adenosine A2A Brain Receptor Occupancy of BIIB014 at Multiple Dose ... occupies the brains A2A receptors. Receptor occupancy will be assessed by PET scanning using a radiolabelled tracer. ... Using PET Scans to Study Brain Receptor Occupancy of BIIB014 in Healthy Male Volunteers. The safety and scientific validity of ...
Schwabe, U; Ukena, D; Lohse, MJ (September 1985). "Xanthine Derivatives as Antagonists at A1 and A2 Adenosine Receptors". ... It acts as an adenosine receptor antagonist and phosphodiesterase inhibitor. Xanthine "International Non-Proprietary Names. ...
... and D2 receptors interact to regulate effort-related decision making, which may have implications for the treatment of ... Adenosine A1 Receptor Antagonists * Adenosine A2 Receptor Antagonists * Dopamine Antagonists * MSX 3 compound ... Co-administration of the adenosine A(2A) receptor antagonist MSX-3 (0.75, 1.5, and 3.0 mg/kg i.p.), but not the A(1) antagonist ... The adenosine A2A antagonist MSX-3 reverses the effects of the dopamine antagonist haloperidol on effort-related decision ...
... receptor antagonist alternatives to the clinical candidate 8-(3-oxa-tricyclo[3.2.1.0(2,4)]oct-6-yl)-1,3-dipropyl-3,7-dihydro- ... During the search for second-generation adenosine A(1) ... Adenosine A1 Receptor Antagonists* * Adenosine A2 Receptor ... Norbornyllactone-substituted xanthines as adenosine A(1) receptor antagonists Bioorg Med Chem. 2006 Jun 1;14(11):3654-61. doi: ... During the search for second-generation adenosine A(1) receptor antagonist alternatives to the clinical candidate 8-(3-oxa- ...
0 (Adenosine A2 Receptor Antagonists); 0 (Antiparkinson Agents); 0 (Dopamine Agonists); 0 (Indoles); 0 (Purines); 0 (Receptor, ... 0 (Adenosine A2 Receptor Antagonists); 0 (Antiparkinson Agents); 0 (Dopamine Agonists); 0 (Indoles); 0 (Purines); 030PYR8953 ( ... The adenosine A2A receptor antagonist, istradefylline enhances the anti-parkinsonian activity of low doses of dopamine agonists ... The adenosine A2A receptor antagonist, istradefylline improves motor function in patients with advanced Parkinsons disease (PD ...
Adenosine A2A Receptor Agonists (0) see Adenosine A2 Receptor Agonists. Adenosine A2A Receptor Antagonists (0) see Adenosine A2 ... Adenosine A2B Receptor Agonists (0) see Adenosine A2 Receptor Agonists. Adenosine A2B Receptor Antagonists (0) see Adenosine A2 ... Adenosine A2 Receptor Antagonists (8) • Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS. ... Adenosine A2 Receptor Agonists (4) • Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS. MeSH ...
Nonselective adenosine receptor antagonist (Blocks A1, A2, A3 equally). Mechanism: Nonspecific AChRi -,promotes degrdation of ...
... activity as antagonists of A1- and A2-adenosine receptors". Biochemical Pharmacology. 37 (4): 655-64. doi:10.1016/0006-2952(88) ... 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 ... OBrien, Robert (1986). Receptor binding in drug research. New York: Dekker. p. 519. ISBN 0-8247-7548-1. US Patent 3966746 ...
1994) CGS 15943, an adenosine A2 receptor antagonist, reduces cerebral ischaemic injury in the Mongolian gerbil. Life Sci 55: ... Almost all A2A adenosine receptor agonists and antagonists also have some effects on A1 or A3 receptors (Jacobson et al., 1992 ... 1992) Molecular cloning of the rat A2 adenosine receptor: selective coexpression with D2 dopamine receptors in rat striatum. ... 1994) In vivo and ex vivo effects of adenosine A1 and A2 receptor agonists on platelet aggregation in the rabbit. Eur J ...
... were studied in awake mice lacking one or both of the adenosine A(1) or A(2A) receptors (A(1)R or A(2A)R, respectively) using ... indicating effects of endogenous adenosine. The A(2A)R plays an important role in the modulation of O(2)C and LA by acute and ... Modulation of paracetamol antinociception by caffeine and by selective adenosine A2 receptor antagonists in mice.. *Lisa ... Selective Deletion of the A1 Adenosine Receptor Abolishes Heart-Rate Slowing Effects of Intravascular Adenosine In Vivo. * ...
There are two main classes of adenosine receptor: Al and A2; caffeine and paraxanthine are nonselective antagonists at both, ... 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 ... This ability results from the competitive binding of caffeine and paraxanthir e to adenosine receptors and is of importance in ...
These probes bind to A.sub.2 and A.sub.3 adenosine receptors and aid in quantifying and characterizing the receptors. The ... This application discloses probes for adenosine receptors which are functionalized congeners of the following compound: ##STR1# ... which are antagonists for A-1 and A-2 receptors, these probes are prepared by reacting a fluorescent dye marker, or electron ... Both adenosine and xanthine derivatives bind competitively to A-1 and A-2 adenosine receptors.. UTILITY STATEMENT. The present ...
Additionally, adenosine receptor antagonists blocked mGluR-mediated increases in cAMP accumulation with potencies that were ... highly correlated with their potencies at A2 adenosine receptors. Furthermore, we performed a series of studies that suggest ... We found that adenosine deaminase abolished 1S,3R-ACPD-stimulated cAMP accumulation whereas the adenosine uptake blocker ... Metabotropic glutamate receptors (mGluRs) are coupled to effector systems through GTP-binding proteins (G-proteins) and appear ...
A2 ( straium) Adenosine receptors ... Caffeine is an Antagonist of A1 (cerebral cortex & hippocampus ... 5/12/09 Introduction f Adenosine receptor 1??? Contradictary evidence  activiation of A1 inhibit acetylcholine release  Ach ... As daily caffeine use increases the number of free receptors decreases and the ...
... an adenosine A1 receptor antagonist. Effects of adenosine A2 and A3 receptors agonists and antagonists were also investigated. ... a selective adenosine A1 receptor antagonist. The selective adenosine A2 and A3 receptors antagonists did not alter the ... Adenosine and ATP exert a negative chronotropic effect in the heart. This study aims to evaluate adenosine and P2 receptors and ... Adenosine A1 receptor activation by adenosine and ATP produces cardiac arrest in the right atrium of Wistar rats predominantly ...
... including an A2 receptor antagonist caffeine; (6) better tumor rejection observed in A2 receptor antagonist-treated mice is at ... solid tumors are surrounded by extracellular adenosine; (3) A2 adenosine receptors are capable of inhibiting anti-tumor T cells ... The treatment with antagonists of A2 receptors significantly delayed the onset of rapid growth of CL8-1 melanoma, even if ... As it was shown, the dramatic inhibition of tumor neovascularization can be achieved by A2 receptor antagonists [1]. These data ...
Chlorofuryl-triazolo-quinazolinamine (CGS-15943; 1 micromol/L), an adenosine A1 and A2 receptor antagonist, and ... and mice treated with adenosine A2A receptor antagonist [11].. *RESULTS: Adenosine A2A receptor occupancy promoted collagen ... a selective adenosine A2A receptor agonist, affected nucleoside release [22].. *The selective adenosine A2A receptor antagonist ... Adenosine A2A receptor antagonists as new agents for the treatment of Parkinsons disease. Richardson, P.J., Kase, H., Jenner, ...
This study explored whether selective pharmacological antagonism of the adenosine A1 receptor subtype synergizes with ESS, ... and systemic effects of the synergistic application of A1 antagonists and spinal stimulation in intact and injured spinal cord. ... We hypothesized that selective pharmacological antagonism of A1 receptors during ESS would produce facilitatory effects in ... We hypothesized that selective pharmacological antagonism of A1 receptors during ESS would produce facilitatory effects in ...
... based on experiments involving application of an A2-type adenosine receptor ligand, 5′-N-ethylcarboxamidoadenosine and A2bAR ... antagonists in control and A2bAR KO cells and mice, it was concluded that this receptor can also exert influences via ... Although adenosine activates multiple receptor subtypes (A1, A2a, A2b, and A3 receptors), the adenylyl cyclase stimulatory A2a ... adenosine receptors (A2aARs) are regarded mainly as cardioprotective receptors (1). In general, the A2-type receptors have been ...
Preladenant (SCH 420814) is a novel adenosine A-2 receptor antagonist being evaluated for the treatment of Parkinsons disease ... MK-4305 is a novel orexin receptor antagonist being evaluated in Phase III studies for the treatment of insomnia. Phase IIb ... Vorapaxar (SCH 530348) is an investigational protease activated receptor-1 (PAR-1) antagonist for the treatment of thrombosis. ... Tags: Acute Coronary Syndrome, Adenosine, Allergen, Anacetrapib, Antibodies, Antibody, Asenapine, Asthma, Atherosclerosis, ...
Binding of [3H]KF17837S, a selective adenosine A2 receptor antagonist, to rat brain membranes. ... The adenosine antagonist 9-chloro-2-(2-furanyl)[1,2,4]triazolo[1,5-c]quinazolin-5-amine (CGS15943) binds to human A3 receptors ... Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype. ... N3,N7-diaminophenothiazinium derivatives as antagonists of α7-nicotinic acetylcholine receptors expressed in Xenopus oocytes. ...
A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity. ... 01/01/1993 - "The A1 adenosine antagonist 8-phenyltheophylline (8-PT) potentiated catalepsy induced by NECA, R-PIA and CHA. ". ... Subscribe to New Research on Adenosine-5-(N-ethylcarboxamide) A stable adenosine A1 and A2 receptor agonist. Experimentally, ... 05/01/1998 - "The effect of serotonergic agents was studied on the adenosine A2 receptor agonist NECA-induced catalepsy in mice ...
... lines bound a variety of adenosine agonists and antagonists with affinities characteristic of a brain adenosine A2a receptor. ... lines bound a variety of adenosine agonists and antagonists with affinities characteristic of a brain adenosine A2a receptor. ... The cloned receptor DNA was transfected into human embryonic kidney 293 cells. Stably transfected cell ... The cloned receptor DNA was transfected into human embryonic kidney 293 cells. Stably transfected cell ...
Preladenant (SCH 420814) is a novel adenosine A-2 receptor antagonist being evaluated for the treatment of Parkinsons disease ... MK-4305 is a novel orexin receptor antagonist being evaluated in Phase III studies for the treatment of insomnia. Phase IIb ... Vorapaxar (SCH 530348) is an investigational protease activated receptor-1 (PAR-1) antagonist for the treatment of thrombosis. ... Dalotuzumab (MK-0646) is an antibody targeting the insulin-like growth factor receptor-1 (IGF-1r). Interim analysis of the ...
Adenosine A2 Receptor Antagonists Concept Adenosine A2 Receptor Agonists Concept Receptors, Adenosine A2 ... studies on selective adenosine A2A receptor antagonists. Academic Article Adenosine A2A antagonists as neurotherapeutics: ... Targeting adenosine A2A receptors in Parkinsons disease. Academic Article Adenosine A2A receptors and metabotropic glutamate 5 ... receptor antagonists in Parkinsons disease. Academic Article Mice heterozygous for both A1 and A(2A) adenosine receptor genes ...
Adenosine A2 Receptor Agonists. 1. 2017. 30. 0.050. Why? Purinergic P2X Receptor Antagonists. 1. 2017. 32. 0.050. Why? ... Nuclear Receptor Subfamily 1, Group F, Member 3. 1. 2012. 106. 0.130. Why? ... NK Cell Lectin-Like Receptor Subfamily B. 1. 2014. 71. 0.160. Why? ...
... new potent adenosine A2 receptor antagonists. Eur J Med Chem 28(7-8):569-576. https://doi.org/10.1016/0223-5234(93)90087-U ... and biodistribution of a new potent and selective ligand for in vivo imaging of the adenosine A2A receptor system using ... pyrimidines as inhibitors of receptor tyrosine kinases (RTK). Helv Chim Acta 87(4):956-975. https://doi.org/10.1002/hlca. ...
  • Effects of adenosine A2 and A3 receptors agonists and antagonists were also investigated. (ovid.com)
  • Stably transfected cell lines bound a variety of adenosine agonists and antagonists with affinities characteristic of a brain adenosine A2a receptor. (garvan.org.au)
  • The binding of agonists and antagonists to a2-adrenergic receptors of human platelets was studied. (uni-wuerzburg.de)
  • Evidence for the involvement of A1 (inhibitory) and A2 (stimulatory) adenosine receptors in regulating cell growth of these tumor cells was obtained through plating efficiency studies based on the relative potency of adenosine agonists and antagonists. (nus.edu.sg)
  • The distinction between receptor-binding sites for agonists and antagonists underpins the pharmacological differences between these two classes of ligands. (pianolarge.cf)
  • The use of antagonists, including caffeine, or targeting the A2 receptors by siRNA pretreatment of T cells improved the inhibition of tumor growth, destruction of metastases, and prevention of neovascularization by antitumor T cells. (pnas.org)
  • We propose to target the hypoxia→adenosine→A2AR pathway as a cancer immunotherapy strategy to prevent the inhibition of antitumor T cells in the tumor microenvironment. (pnas.org)
  • Inhibition of rat ventricular automaticity by adenosine. (semanticscholar.org)
  • This may be now possible because of the recent demonstration that genetic deletion of immunosuppressive A2A and A2B adenosine receptors (A2AR and A2BR) or their pharmacological inactivation can prevent the inhibition of anti-tumor T cells by the hypoxic tumor microenvironment and as a result facilitate full tumor rejection [Ohta A, Gorelik E, Prasad SJ et al (2006) Proc Natl Acad Sci USA 103(35):13132-3137]. (pubmedcentralcanada.ca)
  • Monoamine oxidase B inhibition and neuroprotection: studies on selective adenosine A2A receptor antagonists. (harvard.edu)
  • Accordingly, the tissue hypoxia caused by limited blood supply may lead to an increase of local adenosine levels, probably because of insufficient ATP production and the inhibition of adenosine-metabolizing enzyme ( 14 , 15 , 16 ). (jimmunol.org)
  • 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)
  • Inhibition of adenylate cyclase by (R)-PIA was attenuated by the A1 receptor antagonist XAC and following inactivation of Gi with pertussis toxin (100 ng/ml). (aspetjournals.org)
  • Doxofylline does not demonstrate direct inhibition of any histone deacetylase (HDAC) enzymes or known PDE enzyme isoforms and did not act as an antagonist at A2 or A2 receptors. (drugbank.ca)
  • Thromboxane A2 receptor antagonism and synthase inhibition in essential hypertension. (ahajournals.org)
  • AZD4635 is in Phase 1 clinical trial with AstraZeneca, to block the adenosine A 2A receptor and immune checkpoint inhibition via PDL1, CTLA4 and enhance the activity of CD73 inhibition. (guidetopharmacology.org)
  • This mechanism is distinct from PDE and adenosine receptor inhibition. (statpearls.com)
  • Bailey MA (2004) Inhibition of bicarbonate reabsorption in the rat proximal tubule by activation of luminal P2Y1 receptors. (springer.com)
  • CONCLUSION: Adenosine A2AR antagonists improve 6-OHDA-motor deficit and this effect seems to be mediated by the inhibition of A2A presynaptic receptors in substantia nigra pars compacta. (bvsalud.org)
  • In A431 cells adenosine evoked a biphasic response in which a low concentration (~10 μM) produced inhibition of colony formation but at higher concentrations (up to 100 μM) this inhibition was progressively reversed. (nus.edu.sg)
  • Receptor knockouts or pharmacological inhibition in the adenosine, PG/lipoxygenase, lysophosphatidylcholine, and sphingosine-1-phosphate pathways did not individually alter naive T cell migration. (ox.ac.uk)
  • This PET study was conducted to investigate the receptor occupancy of 11 C-SCH442416 in the human brain and to determine plasma concentrations and dose of preladenant which result in inhibition of 11 C-SCH442416 binding to adenosine 2A receptors. (openmedscience.com)
  • Antagonist inhibition curves were steep and best described by a one-site binding model. (kzeng.info)
  • The mechanisms of the cardiovascular effects of caffeine include the blocking of adenosine receptors and the inhibition of phosphodiesterases. (kzeng.info)
  • abstract = "Adenosine inhibited interleukin (IL)-18 production in lipopolysaccharide (LPS)-stimulated monocytes. (elsevier.com)
  • Physiological roles of A1 and A2A adenosine receptors in regulating heart rate, body temperature, and locomotion as revealed using knockout mice and caffeine. (semanticscholar.org)
  • Heart rate (HR), body temperature (Temp), locomotor activity (LA), and oxygen consumption (O(2)C) were studied in awake mice lacking one or both of the adenosine A(1) or A(2A) receptors (A(1)R or A(2A)R, respectively) using telemetry and respirometry, before and after caffeine administration. (semanticscholar.org)
  • Caffeine reduces hypnotic effects of alcohol through adenosine A2A receptor blockade. (semanticscholar.org)
  • Modulation of paracetamol antinociception by caffeine and by selective adenosine A2 receptor antagonists in mice. (semanticscholar.org)
  • Neuroprotection by caffeine and more specific A2A receptor antagonists in animal models of Parkinson's disease. (harvard.edu)
  • Mice heterozygous for both A1 and A(2A) adenosine receptor genes show similarities to mice given long-term caffeine. (harvard.edu)
  • Pathophysiological roles for purines: adenosine, caffeine and urate. (harvard.edu)
  • E)-8-(3-Chlorostyryl)-1,3,7-trimethylxanthine, a caffeine derivative acting both as antagonist of adenosine A2A receptors and as inhibitor of MAO-B. (harvard.edu)
  • Neuroprotection by caffeine in the MPTP model of parkinson's disease and its dependence on adenosine A2A receptors. (harvard.edu)
  • Effects of caffeine could be mediated by its action on several different targets such as cAMP phosphodiesterase, phosphatidylinositol-3 kinase, and adenosine receptors ( 1 , 2 ). (jimmunol.org)
  • The behavioral activation by caffeine is largely accounted for by the antagonism of tonic activation of the A2A adenosine receptor (A2AR) 3 in the brain ( 1 ). (jimmunol.org)
  • Role of adenosine receptors in caffeine tolerance. (aspetjournals.org)
  • Caffeine is a competitive antagonist at adenosine receptors. (aspetjournals.org)
  • Receptor up-regulation during chronic drug treatment has been proposed to be the mechanism of tolerance to the behavioral stimulant effects of caffeine. (aspetjournals.org)
  • Thus, the adenosine-antagonist activity of caffeine was undiminished in tolerant rats. (aspetjournals.org)
  • The effects of chronic caffeine administration on parameters of adenosine receptor binding and function were measured in cerebral cortex. (aspetjournals.org)
  • There were no differences between brain tissue from control and caffeine-treated rats in number and affinity of adenosine binding sites or in receptor-mediated increases (A2 adenosine receptor) and decreases (A1 adenosine receptor) in cAMP accumulation. (aspetjournals.org)
  • Experimental evidence and theoretical considerations indicate that up-regulation of adenosine receptors is not the mechanism of tolerance to caffeine-induced stimulation of locomotor activity. (aspetjournals.org)
  • Now, a team of researchers from the University of South Carolina has hypothesized that the blockade of adenosine receptors by caffeine may be the most likely mechanism of CNS stimulation and delayed fatigue. (innovations-report.com)
  • The researchers' hypothesis is the foundation of a new study to determine the effects of intracerebroventricular injection of caffeine and the adenosine A1 and A2 receptor agonist 5'-N-ethylcarboxamidoadenosine (NECA) on treadmill run time to fatigue in rats. (innovations-report.com)
  • NECA was chosen for the study because caffeine is a nonselective adenosine receptor antagonist, and it is not known which of the four subtypes of adenosine receptors may be involved in an effect of caffeine on fatigue. (innovations-report.com)
  • Consumption of caffeine, a non-selective adenosine A 2A receptor (A 2A R) antagonist, reduces the risk of developing Alzheimer's disease (AD) and mitigates both amyloid and Tau lesions in transgenic mouse models of the disease. (frontiersin.org)
  • Reduced appetite for caffeine in adenosine A(2A) receptor knockout mice. (ac.be)
  • Caffeine is a nonselective antagonist of adenosine A1 and A2 receptors. (stackexchange.com)
  • Adenosine A2a receptors induce intracellular signalling events that cause an upregulation of the COX-2 gene and the release of PGE2 in rat microglia, which is antagonized by caffeine. (stackexchange.com)
  • However, adenosine continues to be released even with caffeine in your bloodstream. (kzeng.info)
  • It promotes wakefulness by blocking adenosine A 2A receptors (A 2A Rs) in the brain, but the specific neurons on which caffeine acts to produce arousal have not been identified. (kzeng.info)
  • We propose, therefore, that up-regulation of adenosine receptors may underlie the development of tolerance to the CNS effects of caffeine. (kzeng.info)
  • In early pathological stages of HD and even in symptomatic patients with a grade of 0 on Vonsattelâ s neuropathological severity in HD scale, both D 2 R and A 2A R are significantly and differentially downregulated when compared with D 1 R. 6 These data suggest a selective functional alteration in â ¦ Caffeine hijacks the receptors, artificially controlling your energy levels. (kzeng.info)
  • Tolerance occurs as caffeine binds the adenosine receptors in the body, leading to an antagonizing effect and as adenosine is needed, the brain dumps greater and greater amounts of adenosine into circulation, as well as increases cell receptor number (increasing chances of binding adenosine), so there is an increased need to increase the population of caffeine molecules, and so on and so forth. (kzeng.info)
  • C57BL/6J and DBA/2J mice were used to determine if possible differences in the behavioral response to caffeine might be related to differences in A1 adenosine receptors. (kzeng.info)
  • Thus, although using the hypoxia→adenosine→A2AR pathway inhibitors may improve antitumor immunity, the recruitment of this pathway by selective drugs is expected to attenuate the autoimmune tissue damage. (pnas.org)
  • Adenosine receptor-blocking xanthines as inhibitors of phosphodiesterase isozymes. (semanticscholar.org)
  • Alkaloids constitute positive roles in ameliorating pathophysiology of these illnesses by functioning as muscarinic and adenosine receptors agonists, anti-oxidant, anti-amyloid and MAO inhibitors, acetylcholinestrase and butyrylcholinesterase inhibitor, inhibitor of α-synuclein aggregation, dopaminergic and nicotine agonist, and NMDA antagonist. (ijbs.com)
  • From previous researches, crystallography for fragment-based screening has been successfully used to discover inhibitors, especially some difficult targets such as b-secretase[5], as well as inhibitors of a wide range of other enzymes: hPNMT, Phosphodiesterase 4A, Hsp90, Bromodomain, Adenosine A2 receptor, etc. (wordpress.com)
  • Antagonists/enzyme inhibitors were applied prior to U46619 addition. (nottingham.ac.uk)
  • Anticoagulants can be further divided into direct factor Xa inhibitors, vitamin K antagonists, direct thrombin inhibitors, and heparin. (teletype.in)
  • Anti-platelet agents (such as aspirin, ADP receptor antagonists, and GPIIb/IIIa antagonists), phosphodiesterase inhibitors and anti-coagulants are major part of the current treatment towards treating ischemic diseases. (eurekaselect.com)
  • 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)
  • This study investigated the involvement of 5-HT1 and 5-HT2 receptors in the antidepressant-like effect of adenosine in the mouse forced swimming test (FST). (unboundmedicine.com)
  • Taken together, the results indicate that the antidepressant-like effect of adenosine in the FST appears to be mediated, at least in part, by an interaction with 5-HT1A receptors. (unboundmedicine.com)
  • TY - JOUR T1 - Involvement of 5-HT1A receptors in the antidepressant-like effect of adenosine in the mouse forced swimming test. (unboundmedicine.com)
  • The present work used a T-maze choice procedure to assess the effects of adenosine A(2A) and A(1) antagonism. (nih.gov)
  • Right atria of adult Wistar rats were used to evaluate the effects of adenosine, ATP and CPA (an adenosine A1 receptor agonist), in the presence and absence of DPCPX, an adenosine A1 receptor antagonist. (ovid.com)
  • The effects of adenosine, CPA and ATP were inhibited by DPCPX, a selective adenosine A1 receptor antagonist. (ovid.com)
  • The cardiovascular protective effects of adenosine have been described in recent years. (pnas.org)
  • 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)
  • Agmon Y, Dinour D, Brezis M (1993) Disparate effects of adenosine A1- and A2-receptor agonists on intrarenal blood flow. (springer.com)
  • Beach RE, Good DW (1992) Effects of adenosine on ion transport in rat medullary thick ascending limb. (springer.com)
  • It acts as an adenosine receptor antagonist and phosphodiesterase inhibitor. (wikipedia.org)
  • It is also known to act as an adenosine antagonist at the A1 and A2 subtypes and as a phosphodiesterase inhibitor. (wikipedia.org)
  • Doxofylline is an antagonist of adenosine A1 receptor which also inhibits phosphodiesterase IV . (medchemexpress.com)
  • Theophylline is a nonselective phosphodiesterase (PDE) inhibitor , adenosine receptor blocker, and histone deacetylase (HDAC) activator. (medchemexpress.com)
  • Diphylline (Diprophylline) is a potent A1/A2 adenosine receptor antagonist and cyclic nucleotide phosphodiesterase inhibitor . (medchemexpress.com)
  • Furthermore, previous studies suggest that glutamate increases cAMP accumulation by a mechanism that is dependent upon the presence of endogenous adenosine. (jneurosci.org)
  • Therefore, we tested the hypothesis that 1S,3R- ACPD-stimulated increases in cAMP accumulation in rat hippocampal slices are dependent upon the presence of endogenous adenosine and are mediated by an mGluR that potentiates cAMP responses to other agonists. (jneurosci.org)
  • Furthermore, we performed a series of studies that suggest that 1S,3R- ACPD activates an mGluR subtype that potentiates responses to agonists of other receptors that are coupled to adenylate cyclase and that 1S,3R- ACPD-stimulated increases in cAMP accumulation in hippocampal slices are mediated by potentiation of the cAMP response to low levels of endogenous adenosine that are continuously present extracellularly. (jneurosci.org)
  • We demonstrated that ESS combined with the blockage of A1 receptors increased the magnitude of the endogenous modulation and postponed the decay of responses that occur during ESS alone. (frontiersin.org)
  • The mechanism of physiologically relevant increases in the levels of endogenous adenosine to enable the adenosine-mediated down-regulation of inflammation in hypoxic areas of inflamed tissues is supported by observations of the obstruction of blood perfusion in inflamed tissue ( 13 ). (jimmunol.org)
  • Regulation of plasma membrane ion transport by endogenous purinergic receptors was assessed in a distal renal (A6) cell line. (rti.org)
  • These results indicate that adenosine is endogenous neuroprotection substance against ischemic neuronal cell death. (nii.ac.jp)
  • Previous studies indicated that extracellular nucleotide metabolites, predominantly adenosine, may trigger an endogenous protective mechanism during hypoxia and ischemia ( 12 - 15 ). (rupress.org)
  • In control animals, endogenous adenosine reduces vascular resistance of the efferent arteriole via adenosine A 2 -receptors resulting in reduced filtration fraction. (diva-portal.org)
  • Barrett RJ, Droppleman DA (1993) Interactions of adenosine A1 receptor-mediated renal vasoconstriction with endogenous nitric oxide and ANG II. (springer.com)
  • Adenosine A1 receptor (ADORA1, also known as A1AR) is one of four subtypes of adenosine receptors that belong to a superfamily of protein G-coupled receptors. (ptglab.com)
  • There are at least two subtypes of adenosine receptors in the heart: A1 and A2. (justia.com)
  • Responses of platelets to a thromboxane A2 mimetic and to adenosine diphosphate were studied turbidometrically. (ahajournals.org)
  • Ryanodine reduced calcium activity in the boutons, whereas the ATP antagonist adenosine-5′-O-(α, β- methylene diphosphate) reduced calcium activity in both the boutons and vascular tone. (arvojournals.org)
  • adenosine-5′-diphosphate (ADP), uridine-5′-triphosphate (UTP) and MRS2768, a selective P2Y2 agonist, were applied cumulatively, while adenosine-5′-triphosphate (ATP) and αβ-methylene-ATP (αβ-meATP) response curves were generated from single concentrations per tissue segment. (nottingham.ac.uk)
  • Various new anti-platelet drugs include adenosine diphosphate receptor (ADP) antagonists, thromboxane A2 receptor antagonists, and protease-activated receptors (PAR-1) antagonists. (teletype.in)
  • Various platelet agonists like adenosine diphosphate (ADP), thrombin and thromboxane A2 (TXA2) activate platelets by acting via their respective surface receptors, which couple to one or more distinct G-proteins belonging to either the Gi, Gq, G12/13 or Gs families. (eurekaselect.com)
  • The effects on blood pressure were analyzed through the pressor test with handgrip, and platelet aggregation was analyzed using adenosine diphosphate, collagen, and adrenaline. (bvsalud.org)
  • Ticlopidine hydrochloride is an adenosine diphosphate (ADP) receptor inhibitor against platelet aggregation with IC50 of ~2 μM. (medchemexpress.com)
  • The A2A adenosine receptor (A2AR) has been shown to be a critical and nonredundant negative regulator of immune cells in protecting normal tissues from inflammatory damage. (pnas.org)
  • We hypothesized that cancerous tissues are protected from antitumor T cells because of immunosuppressive signaling via T cell A2A adenosine receptor (A2AR) ( 15 - 17 ) activated by extracellular adenosine produced from hypoxic tumor ( Fig. 1 a ). (pnas.org)
  • Indeed, hypoxic cancerous tissues may be protected by the same hypoxia→adenosine→A2AR pathway that was recently shown to be critical and nonredundant in preventing excessive damage of normal tissues by overactive immune cells in vivo ( 18 ). (pnas.org)
  • a ) It is assumed that adenosine and A2AR, which inhibit overactive immune cells to protect normal tissues ( 18 ), may protect malignant tissues from antitumor T cells. (pnas.org)
  • Essentially, novel compound demonstrated remarkable potential as A2AR antagonist in the therapy of PD. (curehunter.com)
  • The genetic elimination of A2A adenosine receptors (A2AR) was shown to disengage the critical immunosuppressive mechanism and cause the dramatic exacerbation of acute inflammatory tissue damage by T cells and myeloid cells. (jimmunol.org)
  • A2AR is a G s protein-coupled receptor, and ligand binding to A2AR increases intracellular cAMP. (jimmunol.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)
  • Activation of A2AR is known to increase cyclic adenosine monophosphate (cAMP) levels and to activate protein kinase A (PKA). (elsevier.com)
  • Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS. (nih.gov)
  • These studies support the future investigation of the optimal dosage, methods of delivery, and systemic effects of the synergistic application of A1 antagonists and spinal stimulation in the intact and injured spinal cord. (frontiersin.org)
  • Adenosine A2A receptors in neuroadaptation to repeated dopaminergic stimulation: implications for the treatment of dyskinesias in Parkinson's disease. (harvard.edu)
  • Adenosine A2A receptor stimulation potentiates nitric oxide release by activated microglia. (harvard.edu)
  • 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)
  • 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)
  • 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)
  • Theophylline-induced respiratory recovery following cervical spinal cord hemisection is augmented by serotonin 2 receptor stimulation. (rutgers.edu)
  • The present study was designed to specifically determine if concurrent stimulation of 5-HT2 receptors may enhance motor recovery induced by theophylline alone. (rutgers.edu)
  • 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)
  • The vessels were mounted in a confocal myograph for simultaneous recordings of tone and calcium activity in cells of the vascular wall during stimulation with ATP and adenosine, with and without modifiers of these compounds. (arvojournals.org)
  • Stimulation of the A1 adenosine receptor induces two distinct physiological responses. (justia.com)
  • Stimulation of the adenosine A1 receptor accordingly shortens the duration and decreases the amplitude of the action potential of AV nodal cells and subsequently prolongs the refractory period of the cells. (justia.com)
  • This selective damage was attenuated by MK-801, a NMDA receptor antagonist and L-NAME, a nitric oxide synthase inhibitor. (nii.ac.jp)
  • Genetic deletion of the adenosine A(2A) receptor in mice reduces the changes in spinal cord NMDA receptor binding and glucose uptake caused by a nociceptive stimulus. (ac.be)
  • This was accompanied by increased NMDA receptor gating, dependent on mGluR5 and linked to enhanced Ca 2+ influx. (nature.com)
  • The activation of N -methyl- d -aspartate (NMDA) receptors plays a pivotal role, because it can induce either long-term potentiation (LTP) or long-term depression (LTD), depending on the extent of the resultant intracellular [Ca 2+ ] rise in the dendritic spines and the downstream activation of specific intracellular cascades [ 3 ]. (nature.com)
  • Reduced response to the formalin test and lowered spinal NMDA glutamate receptor binding in adenosine A2A receptor knockout mice. (ac.be)
  • NMDA antagonists. (chmpsy.com)
  • This study reports the effects of glutamyl cysteine synthetase [GCS], as an A2A receptor agonist, and succinylcholine [SCH], as an A2A receptor antagonist, on Sprague Dawley rats, both in the presence and absence of MDMA. (bvsalud.org)
  • It is well established that some areas of solid tumors often have transient or chronic hypoxia ( 19 , 20 ), which is conducive to extracellular adenosine accumulation ( 21 ). (pnas.org)
  • First, adenosine levels markedly increase in response to cerebral ischemia and hypoxia as ATP breakdown dramatically increases the formation of adenosine. (jneurosci.org)
  • Interplay of hypoxia and A2B adenosine receptors in tissue protection. (semanticscholar.org)
  • A2B adenosine receptor dampens hypoxia-induced vascular leak. (semanticscholar.org)
  • 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)
  • Vascular leakage secondary to hypoxia was reversed in part by adenosine receptor agonists or reconstitution with soluble 5′-nucleotidase. (rupress.org)
  • Adenosine is produced in response to trauma, ischemia, and hypoxia and plays an important role in preventing excessive tissue damage. (ptglab.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)
  • This study explored whether selective pharmacological antagonism of the adenosine A1 receptor subtype synergizes with ESS, thereby increasing motor response. (frontiersin.org)
  • Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype. (semanticscholar.org)
  • Second, we investigated the histamine receptor subtype responsible for electroencephalographic activation. (asahq.org)
  • We recently reported the cloning of a cDNA (designated RFL9) that encodes a novel A2-adenosine receptor subtype. (pianolarge.cf)
  • For instance, adenosine inhibits the proliferation of murine VSMC via activation of the A2bAR ( 4 ). (pnas.org)
  • Their theory is based on the fact that adenosine is produced within the body and inhibits neuronal excitability and synapse transmission. (innovations-report.com)
  • Adenosine also inhibits the release of most brain excitatory neurotransmitters, particularly dopamine (DA), and may reduce DA synthesis. (innovations-report.com)
  • Thus, in patients with essential hypertension, acute administration of ridogrel reduces renal and extrarenal thromboxane A2 biosynthesis, increases renal and extrarenal prostacyclin biosynthesis, inhibits thromboxane receptor-activated platelet aggregation, but has no effect on systemic arterial pressure. (ahajournals.org)
  • From these data it is concluded that adenosine exerts two opposing effects on histamine release in the human lung which neutralize each other: it inhibits release via a si te antagonized by XAC, which presumably represents an A2 adenosine receptor, and it stimulates release via a mechanism that is blocked by NBTI, suggesting that adenosine needs to reach the interior of cells to exert this effect. (uni-wuerzburg.de)
  • Adenosine -2'-monophosphate inhibits LPS-induced TNF-α and CXCL10 production via A 2A receptor activation. (medchemexpress.com)
  • Adenosine 5'-succinate is a chemically AMP-related compound and potently inhibits Denatonium benzoate/taste receptor activation of transducin. (medchemexpress.com)
  • 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)
  • Blockade of A 2A receptors on both of these GABAergic neuronal pathways reduces indirect striato-pallidal output neuron activity, thereby compensating for the overactivity of these cells due to dopamine deficiency in PD [ 9 ]. (openmedscience.com)
  • To overcome these pharmacological limitations, we explored the consequences of deleting the A 2A adenosine receptor on brain damage after transient focal ischemia. (jneurosci.org)
  • Together with complimentary pharmacological studies, these data suggest that A 2A receptors play a prominent role in the development of ischemic injury within brain and demonstrate the potential for anatomical and functional neuroprotection against stroke by A 2A receptor antagonists. (jneurosci.org)
  • We hypothesized that selective pharmacological antagonism of A1 receptors during ESS would produce facilitatory effects in spinal sensorimotor networks detected as an increased amplitude of spinally-evoked motor potentials and sustained duration of ESS induced activity. (frontiersin.org)
  • Genetic and pharmacological inactivation of the adenosine A2A receptor attenuates 3-nitropropionic acid-induced striatal damage. (harvard.edu)
  • Genetic and pharmacological inactivation of adenosine A2A receptor reveals an Egr-2-mediated transcriptional regulatory network in the mouse striatum. (harvard.edu)
  • Conditional neural knockout of the adenosine A(2A) receptor and pharmacological A(2A) antagonism reduce pilocarpine-induced tremulous jaw movements: studies with a mouse model of parkinsonian tremor. (harvard.edu)
  • Biochemical and pharmacological role of A1 adenosine receptors and their modulation as novel therapeutic strategy In: ed Protein Reviews. (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)
  • Borea PA, Gessi S, Merighi S, Vincenzi F, Varani K. Pharmacology of adenosine receptors: the state of the art. (eurekaselect.com)
  • Short-term effects of ridogrel, a combined thromboxane synthase inhibitor and receptor antagonist, were investigated in 16 patients with uncomplicated essential hypertension. (ahajournals.org)
  • 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)
  • 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)
  • The pre-treatment of mice with DPCPX (2mg/kg, i.p., a selective adenosine A1 receptor antagonist) or ZM241385 (1mg/kg, i.p., a selective adenosine A2A receptor antagonist) did not prevent the effect of fluoxetine (32 mg/kg, i.p., a preferential serotonin reuptake inhibitor) in the FST. (unboundmedicine.com)
  • Endothelium removal and DUP 697, a cyclooxygenase-2 inhibitor, had no significant effect on contraction to ATP but attenuated that to UTP, indicating actions at distinct receptors. (nottingham.ac.uk)
  • N-[(4-Aminophenyl)methyl] adenosine is a adenosine receptor inhibitor , with Ki of 29 nM for Rat ecto-5′-Nucleotidase. (medchemexpress.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)
  • 5-Iodotubercidin (NSC 113939), an ATP mimetic, is a potent adenosine kinase inhibitor with an IC 50 of 26 nM. (medchemexpress.com)
  • The volume of cerebral infarction, as well as the associated neurological deficit induced by transient filament occlusion of the middle cerebral artery, were significantly attenuated in A 2A receptor knock-out mice. (jneurosci.org)
  • This neuroprotective phenotype of A 2A receptor-deficient mice was observed in different genetic backgrounds, confirming A 2A receptor disruption as its cause. (jneurosci.org)
  • To examine the functional significance of this receptor expression, we applied a femoral artery injury model to A2bAR knockout (KO) mice and showed that the A2bAR prevents vascular lesion formation in an injury model that resembles human restenosis after angioplasty. (pnas.org)
  • Forebrain adenosine A2A receptors contribute to L-3,4-dihydroxyphenylalanine-induced dyskinesia in hemiparkinsonian mice. (harvard.edu)
  • In the present study, we have evaluated the effect of a 6-month treatment of APPsw/PS1dE9 mice with the potent and selective A 2A R antagonist MSX-3 from 3 to 9-10 months of age. (frontiersin.org)
  • Measurements were performed in isoflurane-anesthetized normoglycemic and alloxan-diabetic C57BL/6 mice during baseline and after acute administration of 3,7-dimethyl-1-propargylxanthine (DMPX), a selective A2 receptor antagonist. (diva-portal.org)
  • In conclusion, adenosine acting on A2 receptors mediates an efferent arteriolar dilatation which reduces filtration fraction (FF) and maintains GFR within normal range in normoglycemic mice. (diva-portal.org)
  • Behavioural and biochemical responses to morphine associated with its motivational properties are altered in adenosine A(2A) receptor knockout mice. (ac.be)
  • Characterization of [3H]ZM 241385 binding in wild-type and adenosine A2A receptor knockout mice. (ac.be)
  • Changes in spinal delta and kappa opioid systems in mice deficient in the A2A receptor gene. (ac.be)
  • Adenosine (general agonist), NECA (A2Aand A2B receptor agonist) and CGS-21380(A2Aselective agonist), were used in absence and presence of A2A receptors- selective antagonist, ZM-243185, in naive and morphine-dependent rats. (phypha.ir)
  • 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)
  • Cerebral morphology, as well as vascular and physiological measures (before, during, and after ischemia) did not differ between A 2A receptor knock-out and wild-type littermates. (jneurosci.org)
  • The A2b adenosine receptor (A2bAR) is highly abundant in bone marrow macrophages and vascular smooth muscle cells (VSMC). (pnas.org)
  • Indirect evidence suggests that the adenylyl cyclase stimulatory A2b adenosine receptors (A2bARs) also affect vascular function ( 4 - 6 ). (pnas.org)
  • In the current study we examined the role of vascular and bone marrow adenosine receptors in vascular response to injury using a model that mimics human restenosis after angioplasty. (pnas.org)
  • Moreover, this results rise the possibility that adenosine becomes a drug for the dementia induced by vascular damage. (nii.ac.jp)
  • In addition, adenosine can directly regulate vascular tone by acting on A1 and A2 receptors expressed in afferent and efferent arterioles. (diva-portal.org)
  • Adenosine activates a vascular renin-angiotensin system in hypertensive subjects. (ahajournals.org)
  • The contractions to ATP and αβ-meATP were attributed to actions at P2X1 receptors on the vascular smooth muscle, whereas it was shown for the first time that UTP induced an endothelium-dependent vasoconstriction which may involve P2Y2 and/or P2Y4 receptors. (nottingham.ac.uk)
  • Drugs that inhibit ADENOSINE DEAMINASE activity. (nih.gov)
  • We found that adenosine deaminase abolished 1S,3R-ACPD-stimulated cAMP accumulation whereas the adenosine uptake blocker dipyridamole enhanced this response. (jneurosci.org)
  • The methotrexate-mediated reduction in leukocyte accumulation was partially reversed by injection of adenosine deaminase (ADA) into the air pouch, completely reversed by a specific adenosine A2 receptor antagonist, 3,7-dimethyl-1-propargylxanthine (DMPX), but not affected by an adenosine A1 receptor antagonist, 8-cyclopentyl-dipropylxanthine. (jci.org)
  • Inactivation of neuronal forebrain A receptors protects dopaminergic neurons in a mouse model of Parkinson's disease. (harvard.edu)
  • 8,9 The γ-aminobutyric acid-mediated anesthetic agents that act on γ-aminobutyric acid receptor type A may decrease TMN neuronal firing and histamine release, thus reducing histamine's excitation of the cortical activation circuitry. (asahq.org)
  • The purine nucleotide adenosine is a ubiquitous modulator of neuronal function in the central and peripheral nervous systems. (openmedscience.com)
  • Methotrexate, a folate antagonist, is a potent antiinflammatory agent when used weekly in low concentrations. (jci.org)
  • Pharmacologically relevant doses of methotrexate increased splenocyte AICAR content, raised adenosine concentrations in exudates from carrageenan-inflamed air pouches, and markedly inhibited leukocyte accumulation in inflamed air pouches. (jci.org)
  • It only displays an inhibitory action against PDE2A1 and antagonism at adenosine A(2A) at high concentrations [A31642]. (drugbank.ca)
  • 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)
  • When both A1 and A2 receptors were blocked, colony formation or growth was not inhibited at low concentrations of adenosine but was inhibited at high adenosine concentrations. (nus.edu.sg)
  • The E max model that predicted plasma concentrations corresponding to 50%, 80%, and 90% receptor occupancy was validated. (openmedscience.com)
  • Under normal physiological conditions, adenosine is present in sufficient concentrations to activate A 1 and A 2a receptors. (kzeng.info)
  • Role of adenosine A2A receptors in parkinsonian motor impairment and l-DOPA-induced motor complications. (harvard.edu)
  • These findings suggest an important bimodal role of adenosine in regulating histamine release in the human lung. (uni-wuerzburg.de)
  • PURPOSE: To investigate the role of adenosine A2A receptors on 6-OHDA-induced motor disorder in rat. (bvsalud.org)
  • The role of adenosine A2 receptors in regulation of pial vessels blood flow in anesthetized morphine dependent rats. (phypha.ir)
  • Hoseini M, Hajizadeh S, Fathollahi Y, Golmohammadi M, Erfani B, Heidarian Pour A. The role of adenosine A2 receptors in regulation of pial vessels blood flow in anesthetized morphine dependent rats. (phypha.ir)
  • In addition, platelets with the Q43P β1-tubulin variant had reduced adenosine triphosphate (ATP) secretion, thrombin receptor activating peptide (TRAP)-induced aggregation and collagen adhesion. (bloodjournal.org)
  • The retinal blood flow is regulated by the tone of resistance arterioles, which is influenced by purinergic compounds such as adenosine and adenosine 5′-triphosphate (ATP) released from the retinal tissue. (arvojournals.org)
  • 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)
  • 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)
  • In vitro data indicate that the activation of A2 adenosine receptors increases renin release by the accumulation of cyclic AMP. (ahajournals.org)
  • Additionally, adenosine receptor antagonists blocked mGluR-mediated increases in cAMP accumulation with potencies that were highly correlated with their potencies at A2 adenosine receptors. (jneurosci.org)
  • We examined the hypothesis that the antiphlogistic effects of methotrexate result from its capacity to promote intracellular accumulation of 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR) that, under conditions of cell injury, increases local adenosine release. (jci.org)
  • In addition, adenosine has been shown to reduce arousal, induce sleep, and suppress spontaneous activity, which are all behaviors associated with increases in 5-HT. (innovations-report.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)
  • The dominant effect of an elevation of plasma adenosine in the renal vasculature is an A 2A AR- and A 2B AR-mediated vasodilatation that increases global as well as medullary renal blood flow and is in part endothelium-dependent. (springer.com)
  • Metabotropic glutamate receptors (mGluRs) are coupled to effector systems through GTP-binding proteins (G-proteins) and appear to mediate slow synaptic responses in the CNS. (jneurosci.org)
  • Adenosine A2A receptors and metabotropic glutamate 5 receptors are co-localized and functionally interact in the hippocampus: a possible key mechanism in the modulation of N-methyl-D-aspartate effects. (harvard.edu)
  • Although adenosine activates multiple receptor subtypes (A1, A2a, A2b, and A3 receptors), the adenylyl cyclase stimulatory A2a adenosine receptors (A2aARs) are regarded mainly as cardioprotective receptors ( 1 ). (pnas.org)
  • 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)
  • Adenosine A2 Receptor Antagonist Pipeline Insight, 2018 report by DelveInsight offers comprehensive insights of the pipeline under development therapeutics scenario and growth prospects across Adenosine A2 Receptor Antagonist development. (bioportfolio.com)
  • Binding of [3H]KF17837S, a selective adenosine A2 receptor antagonist, to rat brain membranes. (semanticscholar.org)
  • The adenylate cyclase-coupled vasopressin V2-receptor is highly laterally mobile in membranes of LLC-PK, renal epithelial cells at physiological temperature. (springer.com)
  • Adenosine receptors of the A1 and A2 subtypes were characterized in membranes from DDT1 MF-2 smooth muscle cells. (aspetjournals.org)
  • Adenosine receptor agonists [(R)-PIA, NECA, and (S)-PIA] inhibited isoproterenol-stimulated adenylate cyclase activity in DDT1 MF-2 cell membranes with IC50 values of 62, 538, and 750 nM, respectively. (aspetjournals.org)
  • Barbiturates inhibit binding of radioligands to A 1(Ri) adenosine receptors of rat brain membranes. (uni-wuerzburg.de)
  • Striatal D/sub 1/ receptors and their activity were characterized by (/sup 3/H)SCH23390 binding parameters and D/sub 1/ receptor-stimulated adenylate cyclase activity in striatal membranes. (kzeng.info)
  • The actions of adenosine on histamine release of human lung fragments were investigated. (uni-wuerzburg.de)
  • 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)
  • [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)
  • Extracellular adenosine critically modulates ischemic brain injury, at least in part through activation of the A 1 adenosine receptor. (jneurosci.org)
  • 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)
  • Adenosine -2'-monophosphate is further metabolized to extracellular adenosine (a mechanism called the extracellular 2',3'-cAMP- adenosine pathway). (medchemexpress.com)
  • These cells possess a high density of A1 adenosine receptors (Bmax = 0.8-0.9 pmol/mg of protein), as measured by both agonist and antagonist radioligands. (aspetjournals.org)
  • Adenosine regulates GFR through tubuloglomerular feedback mechanism acting on adenosine A1 receptor. (diva-portal.org)
  • Here, we show in rat that purinergic signaling, possibly through P2Y 2/4 receptors, in the retrotrapezoid nucleus (RTN) maintains arteriole tone during high CO 2 /H + and disruption of this mechanism decreases the CO 2 ventilatory response. (elifesciences.org)
  • The main mechanism of action of theophylline is that of adenosine receptor antagonism . (chemeurope.com)
  • Compound 4g is a potent, efficient, selective, and orally active 1,2,4-triazine derivative ligand identified by Heptares using structure-based drug design approaches to discover antagonists of the adenosine A2 A receptor. (guidetopharmacology.org)
  • 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)
  • Introduction:Adenosine as a potent vasodilator has physiological role in regulation of regional cerebral blood flow (rCBF). (phypha.ir)
  • FSCPX is a potent and selective irreversible antagonist of A 1 adenosine receptor (A 1 AR) , with low nanomolar potency for binding to the A 1 AR. (medchemexpress.com)
  • Both adenosine and xanthine derivatives bind competitively to A-1 and A-2 adenosine receptors. (patentgenius.com)
  • In contrast with other xanthine derivatives, doxofylline does not significantly bind to adenosine alpha-1 or alpha-2 receptors and lacks stimulating effects. (drugbank.ca)
  • 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)
  • In this study we developed a refined pharmacophore model for antagonists of the human adenosine A1 receptor, based on features of known pyrimidine and purine derivatives. (nih.gov)
  • Baranowski RL, Westenfelder C (1994) Estimation of renal interstitial adenosine and purine metabolites by microdialysis. (springer.com)
  • Theophylline** Theophylline is an adenosine receptor antagonist. (rutgers.edu)
  • Decreased affinity for adenosine receptors may account for the better safety profile of doxofylline compared to theophylline 7 . (drugbank.ca)
  • Theophylline pretreatment blunted adenosine-mediated forearm blood flow increments and angiotensin II release. (ahajournals.org)
  • Theophylline antagonizes adenosine receptor A1, A2 strongly, and A3 less potently. (statpearls.com)
  • Vasopressin V2-receptor mobile fraction and ligand-dependent adenylate cyclase-activity are directly correlated in LLC-PK, renal epithelial cells. (springer.com)
  • Finally, adenosine receptor agonists stimulated adenylate cyclase activity by approximately 2-3 fold with the following potency series: PAPA-APEC greater than or equal to NECA greater than (R)-PIA, indicative of their interaction at A2 receptors. (aspetjournals.org)
  • Would calcium or potassium channels be responsible for cardiac arrest produced by adenosine and ATP in the right atria of Wistar rats? (ovid.com)
  • 4-Aminopyridine, a blocker of potassium channels at 10 mM, prevented the cardiac arrest produced by adenosine and ATP, while BayK 8644, activator of calcium channels, did not prevent cardiac arrest. (ovid.com)
  • These structures showed calcium activity when the vessel was relaxed with ATP but not when it was relaxed with adenosine. (arvojournals.org)
  • These results are consistent with theoretical arguments that changes in receptor density should not affect the potency of a competitive antagonist. (aspetjournals.org)
  • 5-n-ethylcarboxamidadenosine, 2-chloro-adenosine and R-phenylisopropyl adenosine also blocked tumor necrosis factor release in a potency suggestive of A2 receptor activity. (duke.edu)
  • Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS. (nih.gov)
  • that the claimed compounds would have an A1-adenosine receptor antagonistic activity. (epo.org)
  • Compounds which are able to block adenosine receptors are commonly found in tea, chocolate, and coffee. (kzeng.info)
  • Adenosine mediates many physiological functions via activation of extracellular receptors. (nus.edu.sg)
  • 11C]SCH442416 is a radiolabelled tracer molecule that specifically binds to adenosine A2A sites and will be used to evaluate receptor occupancy. (clinicaltrials.gov)
  • It binds to adenosine A2B receptors to prevent bronchoconstriction by inhibiting the release of mediators like histamine and leukotrienes from mast cells. (statpearls.com)
  • N3,N7-diaminophenothiazinium derivatives as antagonists of α7-nicotinic acetylcholine receptors expressed in Xenopus oocytes. (semanticscholar.org)
  • Targeting adenosine A2A receptors in Parkinson's disease. (harvard.edu)
  • Dual-target-directed drugs that block monoamine oxidase B and adenosine A(2A) receptors for Parkinson's disease. (harvard.edu)
  • Therapeutic potential of adenosine A(2A) receptor antagonists in Parkinson's disease. (harvard.edu)
  • Adenosine A2A receptor antagonists for Parkinson's disease: rationale, therapeutic potential and clinical experience. (harvard.edu)
  • Adenosine A2A receptor gene disruption protects in an a-synuclein model of Parkinson's disease. (harvard.edu)
  • A2A antagonist prevents dopamine agonist-induced motor complications in animal models of Parkinson's disease. (harvard.edu)
  • 1000-fold versus A 1 , A 2B , and A 3 receptors) A 2A receptor antagonist being investigated for the management of movement disorders, including idiopathic Parkinson's disease. (openmedscience.com)
  • The binding characteristics of B2 to rat striatum adenosine A2A receptor was studied by radioligand 3H-MSX-2 binding assay. (bvsalud.org)
  • Within the striatum A 2A receptors are predominantly localized to the GABAergic striatopallidal enkephalin-expressing neurons, where they are co-localized with dopamine D 2 receptors, and to intrastriatal GABAergic recurrent collaterals [ 7 , 8 ]. (openmedscience.com)
  • Competition studies revealed that the binding of (3H)CGS 15943 was consistent with the labeling of brain adenosine A1 receptors. (kzeng.info)
  • Adenosine A1 receptor activation by adenosine and ATP produces cardiac arrest in the right atrium of Wistar rats predominantly through activation of potassium channels. (ovid.com)
  • Results: Adenosine, NECA and CGS-21680 increased pial vessels blood flow in naive and dependent rats dose dependently. (phypha.ir)
  • Responses of pial vessels to adenosine (10-4, 10-5, 10-6 M) and NECA (10-4, 10-5, 10-6 M) were increased significantly in morphine- dependent rats in comparison to naive rats. (phypha.ir)
  • Conclusion:Based on these results it could be concluded that the role of A2B receptors in regulation of rCBF in morphine-dependent rats is more effective than A2A receptors. (phypha.ir)
  • Adenosine receptors also play a major role in several inflammation-associated processes by inhibiting immune activation and preventing excessive tissue damage. (pnas.org)
  • Nucleotide receptors may effect their responses through primary activation of membrane chloride channels. (rti.org)
  • Hanski E, Rimon G, Levitzki A. Adenylate cyclase activation by the 3-adrenergic receptor as a diffusion controlled process. (springer.com)
  • Given that adenosine receptor activation (via adenosine liberated from CD73) elevates intracellular cAMP, and that elevated cAMP in endothelia promotes barrier function ( 2 , 20 ), we considered the possibility that endothelial CD73 functions to regulate permeability. (rupress.org)
  • Adenosine has been suggested to play a role in asthma, possibly via activation of A(2B) adenosine receptors on mast cells and other pulmonary cells. (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)
  • Moreover, adenosine protects against renal ischemic reperfusion injury by the anti-inflammatory effect of enhancing the activity of regulatory T cell and by attenuating the inflammatory injury produced by neutrophils via A 2 AR activation. (springer.com)
  • Al-Mashhadi RH, Skott O, Vanhoutte PM et al (2009) Activation of A(2) adenosine receptors dilates cortical efferent arterioles in mouse. (springer.com)
  • Awad AS, Huang L, Ye H et al (2006) Adenosine A2A receptor activation attenuates inflammation and injury in diabetic nephropathy. (springer.com)
  • This study investigates the involvement of adenosine A2 receptors in regulation of renal blood flow (RBF) and GFR in control and diabetic kidneys. (diva-portal.org)
  • The modulation of cell growth by adenosine was found to be receptor-mediated. (nus.edu.sg)
  • This study demonstrates that nucleotide receptors in this model of renal epithelium initiate distinct regulation of Na-K-Cl cotransport. (rti.org)
  • 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)
  • A vasopressin antagonist that binds to the V2-receptor of LLC-PK, renal epithelial cells is highly laterally mobile but does not effect ligand-induced receptor immobilization. (springer.com)
  • Renal and systemic thromboxane A2 and prostacyclin biosynthesis were investigated by measuring urinary excretion of thromboxane B2, 6-oxo-prostaglandin F1 alpha, and their respective 2,3-dinor metabolites using gas chromatography/mass spectrometry. (ahajournals.org)
  • Experimental evidence supports the notion that adenosine protects against ischemia-induced acute kidney injury by directly acting on renal endothelial and tubular A 1 AR. (springer.com)
  • Beach RE, Watts BA 3rd, Good DW et al (1991) Effects of graded oxygen tension on adenosine release by renal medullary and thick ascending limb suspensions. (springer.com)
  • The receptors showed homogeneaus affinities for antagonists but two affinity states for the agonist (-)-epinephrine, which were modulated by guanine nucleotides. (uni-wuerzburg.de)
  • A number of G-protein-linked receptors that are not directly coupled to adenylate cyclase increase cAMP accumulation by potentiating cAMP responses to other agonists. (jneurosci.org)
  • Increased adenosine release at inflamed sites diminishes leukocyte accumulation in an in vivo model of inflammation. (jci.org)