Adenosine: A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter.Receptor, Adenosine A2A: A subclass of adenosine A2 receptors found in LEUKOCYTES, the SPLEEN, the THYMUS and a variety of other tissues. It is generally considered to be a receptor for ADENOSINE that couples to the GS, STIMULATORY G-PROTEIN.Receptor, Adenosine A1: A subtype of ADENOSINE RECEPTOR that is found expressed in a variety of tissues including the BRAIN and DORSAL HORN NEURONS. The receptor is generally considered to be coupled to the GI, INHIBITORY G-PROTEIN which causes down regulation of CYCLIC AMP.Adenosine A2 Receptor Antagonists: Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.Purinergic P1 Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.Adenosine Deaminase: An enzyme that catalyzes the hydrolysis of ADENOSINE to INOSINE with the elimination of AMMONIA.Adenosine A1 Receptor Antagonists: Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.Interleukin 1 Receptor Antagonist Protein: A ligand that binds to but fails to activate the INTERLEUKIN 1 RECEPTOR. It plays an inhibitory role in the regulation of INFLAMMATION and FEVER. Several isoforms of the protein exist due to multiple ALTERNATIVE SPLICING of its mRNA.Receptor, Adenosine A3: A subtype of ADENOSINE RECEPTOR that is found expressed in a variety of locations including the BRAIN and endocrine tissues. The receptor is generally considered to be coupled to the GI, INHIBITORY G-PROTEIN which causes down regulation of CYCLIC AMP.Receptor, Adenosine A2B: A subclass of adenosine A2 receptors found in the CECUM, the COLON, the BLADDER, and a variety of other tissues. It is generally considered to be a low affinity receptor for ADENOSINE that couples to the GS, STIMULATORY G-PROTEIN.Neurokinin-1 Receptor Antagonists: Compounds that inhibit or block the activity of NEUROKININ-1 RECEPTORS.Receptors, Adenosine A2: A subclass of ADENOSINE RECEPTORS that are generally considered to be coupled to the GS, STIMULATORY G-PROTEIN which causes up regulation of CYCLIC AMP.Adenosine Kinase: An enzyme that catalyzes the formation of ADP plus AMP from adenosine plus ATP. It can serve as a salvage mechanism for returning adenosine to nucleic acids. EC 2.7.1.20.Receptors, Purinergic P1: A class of cell surface receptors that prefer ADENOSINE to other endogenous PURINES. Purinergic P1 receptors are widespread in the body including the cardiovascular, respiratory, immune, and nervous systems. There are at least two pharmacologically distinguishable types (A1 and A2, or Ri and Ra).Adenosine A2 Receptor Agonists: Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS.Xanthines: Purine bases found in body tissues and fluids and in some plants.Adenosine A1 Receptor Agonists: Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS.Dose-Response Relationship, Drug: The relationship between the dose of an administered drug and the response of the organism to the drug.Rats, Sprague-Dawley: A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.Purinergic P1 Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.Histamine H2 Antagonists: Drugs that selectively bind to but do not activate histamine H2 receptors, thereby blocking the actions of histamine. Their clinically most important action is the inhibition of acid secretion in the treatment of gastrointestinal ulcers. Smooth muscle may also be affected. Some drugs in this class have strong effects in the central nervous system, but these actions are not well understood.Piperidines: A family of hexahydropyridines.Serotonin 5-HT3 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT3 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT3 RECEPTOR AGONISTS.Excitatory Amino Acid Antagonists: Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.Adenosine A3 Receptor Antagonists: Compounds that selectively bind to and block the activation of ADENOSINE A3 RECEPTORS.Dopamine Antagonists: Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME.Angiotensin Receptor Antagonists: Agents that antagonize ANGIOTENSIN RECEPTORS. Many drugs in this class specifically target the ANGIOTENSIN TYPE 1 RECEPTOR.Serotonin 5-HT2 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT2 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT2 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more specific 5-HT2 receptor subtypes.Hormone Antagonists: Chemical substances which inhibit the function of the endocrine glands, the biosynthesis of their secreted hormones, or the action of hormones upon their specific sites.Purinergic P2 Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.Adenosine Monophosphate: Adenine nucleotide containing one phosphate group esterified to the sugar moiety in the 2'-, 3'-, or 5'-position.Rats, Wistar: A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.Adenosine-5'-(N-ethylcarboxamide): A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity.Theophylline: A methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant activities. Theophylline inhibits the 3',5'-CYCLIC NUCLEOTIDE PHOSPHODIESTERASE that degrades CYCLIC AMP thus potentiates the actions of agents that act through ADENYLYL CYCLASES and cyclic AMP.Narcotic Antagonists: Agents inhibiting the effect of narcotics on the central nervous system.Histamine H1 Antagonists: Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.Receptors, Endothelin: Cell surface proteins that bind ENDOTHELINS with high affinity and trigger intracellular changes which influence the behavior of cells.Receptors, Purinergic: Cell surface proteins that bind PURINES with high affinity and trigger intracellular changes which influence the behavior of cells. The best characterized classes of purinergic receptors in mammals are the P1 receptors, which prefer ADENOSINE, and the P2 receptors, which prefer ATP or ADP.Muscarinic Antagonists: Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. Muscarinic antagonists have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system.GABA-A Receptor Antagonists: Drugs that bind to but do not activate GABA-A RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-A RECEPTOR AGONISTS.Phenethylamines: A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)Histamine Antagonists: Drugs that bind to but do not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists. Classical antihistaminics block the histamine H1 receptors only.GABA Antagonists: Drugs that bind to but do not activate GABA RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.Serotonin Antagonists: Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.Leukotriene Antagonists: A class of drugs designed to prevent leukotriene synthesis or activity by blocking binding at the receptor level.Sialoglycoproteins: Glycoproteins which contain sialic acid as one of their carbohydrates. They are often found on or in the cell or tissue membranes and participate in a variety of biological activities.Receptor, Endothelin A: A subtype of endothelin receptor found predominantly in the VASCULAR SMOOTH MUSCLE. It has a high affinity for ENDOTHELIN-1 and ENDOTHELIN-2.Receptors, Serotonin: Cell-surface proteins that bind SEROTONIN and trigger intracellular changes which influence the behavior of cells. Several types of serotonin receptors have been recognized which differ in their pharmacology, molecular biology, and mode of action.Receptors, N-Methyl-D-Aspartate: A class of ionotropic glutamate receptors characterized by affinity for N-methyl-D-aspartate. NMDA receptors have an allosteric binding site for glycine which must be occupied for the channel to open efficiently and a site within the channel itself to which magnesium ions bind in a voltage-dependent manner. The positive voltage dependence of channel conductance and the high permeability of the conducting channel to calcium ions (as well as to monovalent cations) are important in excitotoxicity and neuronal plasticity.Cyclic AMP: An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH.Guinea Pigs: A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.Dizocilpine Maleate: A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.Serotonin 5-HT1 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT1 RECEPTORS, thereby blocking the actions of SEROTONIN 5-HT1 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more of the specific 5-HT1 receptor subtypes.2-Chloroadenosine: 2-Chloroadenosine. A metabolically stable analog of adenosine which acts as an adenosine receptor agonist. The compound has a potent effect on the peripheral and central nervous system.Biphenyl CompoundsRadioligand Assay: Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).Adenosine A3 Receptor Agonists: Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS.Receptors, Interleukin-1: Cell surface receptors that are specific for INTERLEUKIN-1. Included under this heading are signaling receptors, non-signaling receptors and accessory proteins required for receptor signaling. Signaling from interleukin-1 receptors occurs via interaction with SIGNAL TRANSDUCING ADAPTOR PROTEINS such as MYELOID DIFFERENTIATION FACTOR 88.TetrazolesAdrenergic alpha-1 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.Benzazepines: Compounds with BENZENE fused to AZEPINES.Phenylisopropyladenosine: N-Isopropyl-N-phenyl-adenosine. Antilipemic agent. Synonym: TH 162.Cells, Cultured: Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.Nicotinic Antagonists: Drugs that bind to nicotinic cholinergic receptors (RECEPTORS, NICOTINIC) and block the actions of acetylcholine or cholinergic agonists. Nicotinic antagonists block synaptic transmission at autonomic ganglia, the skeletal neuromuscular junction, and at central nervous system nicotinic synapses.Purinergic Antagonists: Drugs that bind to and block the activation of PURINERGIC RECEPTORS.Pyrazoles: Azoles of two nitrogens at the 1,2 positions, next to each other, in contrast with IMIDAZOLES in which they are at the 1,3 positions.Pyridines: Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.Adrenergic alpha-2 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS.Serotonin Receptor Agonists: Endogenous compounds and drugs that bind to and activate SEROTONIN RECEPTORS. Many serotonin receptor agonists are used as ANTIDEPRESSANTS; ANXIOLYTICS; and in the treatment of MIGRAINE DISORDERS.Histamine H3 Antagonists: Drugs that selectively bind to but do not activate HISTAMINE H3 RECEPTORS. They have been used to correct SLEEP WAKE DISORDERS and MEMORY DISORDERS.Sulfonamides: A group of compounds that contain the structure SO2NH2.5'-Nucleotidase: A glycoprotein enzyme present in various organs and in many cells. The enzyme catalyzes the hydrolysis of a 5'-ribonucleotide to a ribonucleoside and orthophosphate in the presence of water. It is cation-dependent and exists in a membrane-bound and soluble form. EC 3.1.3.5.Inosine: A purine nucleoside that has hypoxanthine linked by the N9 nitrogen to the C1 carbon of ribose. It is an intermediate in the degradation of purines and purine nucleosides to uric acid and in pathways of purine salvage. It also occurs in the anticodon of certain transfer RNA molecules. (Dorland, 28th ed)Peptides, Cyclic: Peptides whose amino and carboxy ends are linked together with a peptide bond forming a circular chain. Some of them are ANTI-INFECTIVE AGENTS. Some of them are biosynthesized non-ribosomally (PEPTIDE BIOSYNTHESIS, NON-RIBOSOMAL).Indoles: Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.Serotonin: A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator.Binding, Competitive: The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements.Time Factors: Elements of limited time intervals, contributing to particular results or situations.Purinergic P2X Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P2X RECEPTORS. Included under this heading are antagonists for specific P2X receptor subtypes.Azepines: Seven membered heterocyclic rings containing a NITROGEN atom.Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.Substance P: An eleven-amino acid neurotransmitter that appears in both the central and peripheral nervous systems. It is involved in transmission of PAIN, causes rapid contractions of the gastrointestinal smooth muscle, and modulates inflammatory and immune responses.GABA-B Receptor Antagonists: Drugs that bind to but do not activate GABA-B RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-B RECEPTOR AGONISTS.Theobromine: 3,7-Dimethylxanthine. The principle alkaloid in Theobroma cacao (the cacao bean) and other plants. A xanthine alkaloid that is used as a bronchodilator and as a vasodilator. It has a weaker diuretic activity than THEOPHYLLINE and is also a less powerful stimulant of smooth muscle. It has practically no stimulant effect on the central nervous system. It was formerly used as a diuretic and in the treatment of angina pectoris and hypertension. (From Martindale, The Extra Pharmacopoeia, 30th ed, pp1318-9)Drug Interactions: The action of a drug that may affect the activity, metabolism, or toxicity of another drug.Receptors, Bradykinin: Cell surface receptors that bind BRADYKININ and related KININS with high affinity and trigger intracellular changes which influence the behavior of cells. The identified receptor types (B-1 and B-2, or BK-1 and BK-2) recognize endogenous KALLIDIN; t-kinins; and certain bradykinin fragments as well as bradykinin itself.Endothelin-1: A 21-amino acid peptide produced in a variety of tissues including endothelial and vascular smooth-muscle cells, neurons and astrocytes in the central nervous system, and endometrial cells. It acts as a modulator of vasomotor tone, cell proliferation, and hormone production. (N Eng J Med 1995;333(6):356-63)Calcium: A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.Triazines: Heterocyclic rings containing three nitrogen atoms, commonly in 1,2,4 or 1,3,5 or 2,4,6 formats. Some are used as HERBICIDES.Cimetidine: A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.Receptors, Neurokinin-1: A class of cell surface receptors for TACHYKININS with a preference for SUBSTANCE P. Neurokinin-1 (NK-1) receptors have been cloned and are members of the G protein coupled receptor superfamily. They are found on many cell types including central and peripheral neurons, smooth muscle cells, acinar cells, endothelial cells, fibroblasts, and immune cells.Receptor, Endothelin B: A subtype of endothelin receptor found predominantly in the KIDNEY. It may play a role in reducing systemic ENDOTHELIN levels.TriazolesNeurons: 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.Behavior, Animal: The observable response an animal makes to any situation.Receptors, Dopamine D2: A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D2-class receptor genes contain INTRONS, and the receptors inhibit ADENYLYL CYCLASES.PiperazinesDevazepide: 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.Receptors, Cholecystokinin: Cell surface proteins that bind cholecystokinin (CCK) with high affinity and trigger intracellular changes influencing the behavior of cells. Cholecystokinin receptors are activated by GASTRIN as well as by CCK-4; CCK-8; and CCK-33. Activation of these receptors evokes secretion of AMYLASE by pancreatic acinar cells, acid and PEPSIN by stomach mucosal cells, and contraction of the PYLORUS and GALLBLADDER. The role of the widespread CCK receptors in the central nervous system is not well understood.PyrrolidinesReceptors, Vasopressin: Specific molecular sites or proteins on or in cells to which VASOPRESSINS bind or interact in order to modify the function of the cells. Two types of vasopressin receptor exist, the V1 receptor in the vascular smooth muscle and the V2 receptor in the kidneys. The V1 receptor can be subdivided into V1a and V1b (formerly V3) receptors.Adrenergic alpha-Antagonists: Drugs that bind to but do not activate alpha-adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists. Adrenergic alpha-antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma.Bradykinin: A nonapeptide messenger that is enzymatically produced from KALLIDIN in the blood where it is a potent but short-lived agent of arteriolar dilation and increased capillary permeability. Bradykinin is also released from MAST CELLS during asthma attacks, from gut walls as a gastrointestinal vasodilator, from damaged tissues as a pain signal, and may be a neurotransmitter.Quinoxalines2-Amino-5-phosphonovalerate: The D-enantiomer is a potent and specific antagonist of NMDA glutamate receptors (RECEPTORS, N-METHYL-D-ASPARTATE). The L form is inactive at NMDA receptors but may affect the AP4 (2-amino-4-phosphonobutyrate; APB) excitatory amino acid receptors.Histamine: An amine derived by enzymatic decarboxylation of HISTIDINE. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and also a centrally acting neurotransmitter.Ketanserin: A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients.Receptor, Cannabinoid, CB1: A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.Serotonin 5-HT4 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT4 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN RECEPTOR AGONISTS.Adrenergic Antagonists: Drugs that bind to but do not activate ADRENERGIC RECEPTORS. Adrenergic antagonists block the actions of the endogenous adrenergic transmitters EPINEPHRINE and NOREPINEPHRINE.Disease Models, Animal: Naturally occurring or experimentally induced animal diseases with pathological processes sufficiently similar to those of human diseases. They are used as study models for human diseases.Benzimidazoles: Compounds with a BENZENE fused to IMIDAZOLES.Receptors, Thromboxane: Cell surface proteins that bind THROMBOXANES with high affinity and trigger intracellular changes influencing the behavior of cells. Some thromboxane receptors act via the inositol phosphate and diacylglycerol second messenger systems.Blood Pressure: PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS.Injections, Intraventricular: Injections into the cerebral ventricles.Naltrexone: 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.Synaptic Transmission: The communication from a NEURON to a target (neuron, muscle, or secretory cell) across a SYNAPSE. In chemical synaptic transmission, the presynaptic neuron releases a NEUROTRANSMITTER that diffuses across the synaptic cleft and binds to specific synaptic receptors, activating them. The activated receptors modulate specific ion channels and/or second-messenger systems in the postsynaptic cell. In electrical synaptic transmission, electrical signals are communicated as an ionic current flow across ELECTRICAL SYNAPSES.Receptors, Neurokinin-2: A class of cell surface receptors for tachykinins that prefers neurokinin A; (NKA, substance K, neurokinin alpha, neuromedin L), neuropeptide K; (NPK); or neuropeptide gamma over other tachykinins. Neurokinin-2 (NK-2) receptors have been cloned and are similar to other G-protein coupled receptors.Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.Tubercidin: 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.Famotidine: A competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.Cannabinoid Receptor Antagonists: Compounds that inhibit or block the activity of CANNABINOID RECEPTORS.Bicuculline: An isoquinoline alkaloid obtained from Dicentra cucullaria and other plants. It is a competitive antagonist for GABA-A receptors.Adenosine Triphosphatases: 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.QuinuclidinesAdrenergic beta-2 Receptor Antagonists: Drugs that bind to and block the activation of ADRENERGIC BETA-2 RECEPTORS.Receptors, Purinergic P2: A class of cell surface receptors for PURINES that prefer ATP or ADP over ADENOSINE. P2 purinergic receptors are widespread in the periphery and in the central and peripheral nervous system.BenzodiazepinonesKinetics: The rate dynamics in chemical or physical systems.Signal Transduction: The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.Electric Stimulation: Use of electric potential or currents to elicit biological responses.Angiotensin II: An octapeptide that is a potent but labile vasoconstrictor. It is produced from angiotensin I after the removal of two amino acids at the C-terminal by ANGIOTENSIN CONVERTING ENZYME. The amino acid in position 5 varies in different species. To block VASOCONSTRICTION and HYPERTENSION effect of angiotensin II, patients are often treated with ACE INHIBITORS or with ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKERS.Receptors, Histamine H3: A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H3 receptors were first recognized as inhibitory autoreceptors on histamine-containing nerve terminals and have since been shown to regulate the release of several neurotransmitters in the central and peripheral nervous systems. (From Biochem Soc Trans 1992 Feb;20(1):122-5)Adenine NucleotidesMineralocorticoid Receptor Antagonists: Drugs that bind to and block the activation of MINERALOCORTICOID RECEPTORS by MINERALOCORTICOIDS such as ALDOSTERONE.QuinolinesDogs: 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)Pyrilamine: A histamine H1 antagonist. It has mild hypnotic properties and some local anesthetic action and is used for allergies (including skin eruptions) both parenterally and locally. It is a common ingredient of cold remedies.Receptors, Opioid: Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.Capsaicin: An alkylamide found in CAPSICUM that acts at TRPV CATION CHANNELS.Glutamic Acid: A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.RNA, Messenger: RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.Receptor, Bradykinin B2: 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.Rabbits: The species Oryctolagus cuniculus, in the family Leporidae, order LAGOMORPHA. Rabbits are born in burrows, furless, and with eyes and ears closed. In contrast with HARES, rabbits have 22 chromosome pairs.Enzyme Inhibitors: Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.N-Methylaspartate: An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).Vasodilator Agents: Drugs used to cause dilation of the blood vessels.Endothelins: 21-Amino-acid peptides produced by vascular endothelial cells and functioning as potent vasoconstrictors. The endothelin family consists of three members, ENDOTHELIN-1; ENDOTHELIN-2; and ENDOTHELIN-3. All three peptides contain 21 amino acids, but vary in amino acid composition. The three peptides produce vasoconstrictor and pressor responses in various parts of the body. However, the quantitative profiles of the pharmacological activities are considerably different among the three isopeptides.Receptors, Dopamine D1: A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D1-class receptor genes lack INTRONS, and the receptors stimulate ADENYLYL CYCLASES.Imidazoles: Compounds containing 1,3-diazole, a five membered aromatic ring containing two nitrogen atoms separated by one of the carbons. Chemically reduced ones include IMIDAZOLINES and IMIDAZOLIDINES. Distinguish from 1,2-diazole (PYRAZOLES).Mice, Inbred C57BLPhenylpropionatesAntihypertensive Agents: 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.Dopamine: One of the catecholamine NEUROTRANSMITTERS in the brain. It is derived from TYROSINE and is the precursor to NOREPINEPHRINE and EPINEPHRINE. Dopamine is a major transmitter in the extrapyramidal system of the brain, and important in regulating movement. A family of receptors (RECEPTORS, DOPAMINE) mediate its action.Vasoconstriction: The physiological narrowing of BLOOD VESSELS by contraction of the VASCULAR SMOOTH MUSCLE.Oligopeptides: Peptides composed of between two and twelve amino acids.Muscle, Smooth: Unstriated and unstriped muscle, one of the muscles of the internal organs, blood vessels, hair follicles, etc. Contractile elements are elongated, usually spindle-shaped cells with centrally located nuclei. Smooth muscle fibers are bound together into sheets or bundles by reticular fibers and frequently elastic nets are also abundant. (From Stedman, 25th ed)Interleukin-1: 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.Hippocampus: A curved elevation of GRAY MATTER extending the entire length of the floor of the TEMPORAL HORN of the LATERAL VENTRICLE (see also TEMPORAL LOBE). The hippocampus proper, subiculum, and DENTATE GYRUS constitute the hippocampal formation. Sometimes authors include the ENTORHINAL CORTEX in the hippocampal formation.Receptors, Calcitonin Gene-Related Peptide: 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.Receptors, Opioid, mu: A class of opioid receptors recognized by its pharmacological profile. Mu opioid receptors bind, in decreasing order of affinity, endorphins, dynorphins, met-enkephalin, and leu-enkephalin. They have also been shown to be molecular receptors for morphine.Isoindoles: Benzopyrroles with the nitrogen at the number two carbon, in contrast to INDOLES which have the nitrogen adjacent to the six-membered ring.Receptors, Corticotropin-Releasing Hormone: Cell surface proteins that bind corticotropin-releasing hormone with high affinity and trigger intracellular changes which influence the behavior of cells. The corticotropin releasing-hormone receptors on anterior pituitary cells mediate the stimulation of corticotropin release by hypothalamic corticotropin releasing factor. The physiological consequence of activating corticotropin-releasing hormone receptors on central neurons is not well understood.Norepinephrine: Precursor of epinephrine that is secreted by the adrenal medulla and is a widespread central and autonomic neurotransmitter. Norepinephrine is the principal transmitter of most postganglionic sympathetic fibers and of the diffuse projection system in the brain arising from the locus ceruleus. It is also found in plants and is used pharmacologically as a sympathomimetic.Receptor, Angiotensin, Type 1: An angiotensin receptor subtype that is expressed at high levels in a variety of adult tissues including the CARDIOVASCULAR SYSTEM, the KIDNEY, the ENDOCRINE SYSTEM and the NERVOUS SYSTEM. Activation of the type 1 angiotensin receptor causes VASOCONSTRICTION and sodium retention.Analgesics: Compounds capable of relieving pain without the loss of CONSCIOUSNESS.Receptors, Tachykinin: Cell surface proteins that bind TACHYKININS with high affinity and trigger intracellular changes influencing the behavior of cells. Three classes of tachykinin receptors have been characterized, the NK-1; NK-2; and NK-3; which prefer, respectively, SUBSTANCE P; NEUROKININ A; and NEUROKININ B.Motor Activity: The physical activity of a human or an animal as a behavioral phenomenon.Receptors, G-Protein-Coupled: The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.Suramin: 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.Microdialysis: 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.Receptors, Angiotensin: Cell surface proteins that bind ANGIOTENSINS and trigger intracellular changes influencing the behavior of cells.Receptors, Neurotransmitter: Cell surface receptors that bind signalling molecules released by neurons and convert these signals into intracellular changes influencing the behavior of cells. Neurotransmitter is used here in its most general sense, including not only messengers that act to regulate ion channels, but also those which act on second messenger systems and those which may act at a distance from their release sites. Included are receptors for neuromodulators, neuroregulators, neuromediators, and neurohumors, whether or not located at synapses.Purines: 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.Dipyridamole: 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)Dopamine Agonists: Drugs that bind to and activate dopamine receptors.Calcium Channel Blockers: A class of drugs that act by selective inhibition of calcium influx through cellular membranes.Brain: 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.Ondansetron: 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.Rats, Inbred Strains: 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.Receptors, Opioid, kappa: A class of opioid receptors recognized by its pharmacological profile. Kappa opioid receptors bind dynorphins with a higher affinity than endorphins which are themselves preferred to enkephalins.Vasodilation: The physiological widening of BLOOD VESSELS by relaxing the underlying VASCULAR SMOOTH MUSCLE.Morphine: 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.Naphthalenes: 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.gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.Analysis of Variance: A statistical technique that isolates and assesses the contributions of categorical independent variables to variation in the mean of a continuous dependent variable.Proglumide: 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.Dioxanes: 1,4-Diethylene dioxides. Industrial solvents. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), dioxane itself may "reasonably be anticipated to be a carcinogen." (Merck Index, 11th ed)Receptor, Serotonin, 5-HT2A: A serotonin receptor subtype found widely distributed in peripheral tissues where it mediates the contractile responses of variety of tissues that contain SMOOTH MUSCLE. Selective 5-HT2A receptor antagonists include KETANSERIN. The 5-HT2A subtype is also located in BASAL GANGLIA and CEREBRAL CORTEX of the BRAIN where it mediates the effects of HALLUCINOGENS such as LSD.Cricetinae: A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.Muscle Contraction: A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.Haloperidol: 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)Electrophysiology: The study of the generation and behavior of electrical charges in living organisms particularly the nervous system and the effects of electricity on living organisms.Memantine: AMANTADINE derivative that has some dopaminergic effects. It has been proposed as an antiparkinson agent.Heart Rate: The number of times the HEART VENTRICLES contract per unit of time, usually per minute.Receptors, Histamine H2: 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)Microinjections: The injection of very small amounts of fluid, often with the aid of a microscope and microsyringes.Granisetron: A serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic for cancer chemotherapy patients.Nucleoside Deaminases: Catalyze the hydrolysis of nucleosides with the elimination of ammonia.Patch-Clamp Techniques: An electrophysiologic technique for studying cells, cell membranes, and occasionally isolated organelles. All patch-clamp methods rely on a very high-resistance seal between a micropipette and a membrane; the seal is usually attained by gentle suction. The four most common variants include on-cell patch, inside-out patch, outside-out patch, and whole-cell clamp. Patch-clamp methods are commonly used to voltage clamp, that is control the voltage across the membrane and measure current flow, but current-clamp methods, in which the current is controlled and the voltage is measured, are also used.Purinergic P2Y Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P2Y RECEPTORS. Included under this heading are antagonists for specific P2Y receptor subtypes.
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)
Adenosine A2A receptor
... 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 ...
Adenosine A3 receptor
... 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 ...
CGS-15943
"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 ...
Diprophylline
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. ...
Cartazolate
... 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 ...
Theophylline
... 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 ... asthma infant apnea Blocks the action of adenosine; an inhibitory neurotransmitter that induces sleep, contracts the smooth ...
Adenosine A1 receptor
... an adenosine A1-receptor antagonist,on diuresis and renal function in patients with acute decompensated heart failure and renal ... 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 ...
DMPX
... is a caffeine analog which displays affinity to A2 adenosine receptors, in contrast to the A1 subtype receptors. DMPX had 28× ... a potent and selective in vivo antagonist of adenosine analogs. Life Sci. 1988;43(21):1671-84. PMID 3193854. ...
Thromboregulation
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 ...
Etazolate
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 ...
Prostaglandin DP1 receptor
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: ...
GPCR oligomer
"Stimulation of high-affinity adenosine A2 receptors decreases the affinity of dopamine D2 receptors in rat striatal membranes ... "Structures of the CXCR4 chemokine GPCR with small-molecule and cyclic peptide antagonists". Science. 330 (6007): 1066-71. doi: ... In 1991, the phenomenon of receptor crosstalk was observed between adenosine A2A (A2A) and dopamine D2 receptor (DRD2) thus ... two adenosine A2A receptors and two dopamine D2 receptors). Maggio and co-workers showed in 1993 the ability of the muscarinic ...
Nociceptin receptor
"Modification of nociception and morphine tolerance by the selective opiate receptor-like orphan receptor antagonist (-)-cis-1- ... Fukuda K, Shoda T, Morikawa H, Kato S, Mima H, Mori K (1998). "Activation of phospholipase A2 by the nociceptin receptor ... causing an intracellular decrease in cyclic adenosine monophosphate(cAMP) levels, an important second messenger for many signal ... receptor or kappa-type 3 opioid receptor, is a protein that in humans is encoded by the OPRL1 (opioid receptor-like 1) gene. ...
Multiple electrode aggregometry
The GPIIb/IIIa antagonist blocks the binding of fibrinogen to the GPIIb/IIIa receptors, preventing the formation of platelet- ... Adenosine diphosphate (ADP) is a platelet agonist. When it is added to saline-diluted whole blood in the test cuvette, it ... and PGH2 is then converted to thromboxane A2 (TXA2) by thromboxane synthase. TXA2 increases platelet aggregation, promotes ... Thrombin receptor activating peptide-6 (TRAP-6) activates platelets through the thrombin receptor protease activated receptor-1 ...
5-HT1D receptor
"Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ... mixed 5-HT1B/1D antagonist) LY-310,762 LY-367,642 LY-456,219 LY-456,220 5-HT1 receptor 5-HT receptor GRCh38: Ensembl release 89 ... 5-hydroxytryptamine (serotonin) receptor 1D, also known as HTR1D, is a 5-HT receptor, but also denotes the human gene encoding ... 5HT1D receptor is a G protein linked receptor that activates an intracellular messenger cascade to produce an inhibitory ...
Adenosine
The A1 receptors couple to Gi/o and decreases cAMP levels, while the A2 adenosine receptors couple to Gs, which stimulates ... This is being contended and it is now considered a relative contraindication (however, selective adenosine antagonists are ... In the US, Adenosine is marketed as Adenocard. In India Adenosine is sold as Adenoscan (Cipla) All adenosine receptor subtypes ... Adenosine is believed to be an anti-inflammatory agent at the A2A receptor. Topical treatment of adenosine to foot wounds in ...
PRKCE
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 ...
Proton-pump inhibitor
... called H2-receptor antagonists. PPIs are among the most widely sold drugs in the world, and the first one, omeprazole, is on ... Lucendo AJ, Arias Á, Molina-Infante J (2015). "Efficacy of Proton Pump Inhibitor Drugs for Inducing Clinical and Histological ... 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 ...
Molecular and epigenetic mechanisms of alcoholism
... 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 ...
Arachidonate 5-lipoxygenase
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 ...
12-Hydroxyheptadecatrienoic acid
... 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 ...
Neurotransmitter
... direct-acting Antagonist and indirect-acting Antagonists: Direct-acting antagonist- which takes up space present on receptors ... Rinaman L (February 2011). "Hindbrain noradrenergic A2 neurons: diverse roles in autonomic, endocrine, cognitive, and ... Peptides: somatostatin, substance P, cocaine and amphetamine regulated transcript, opioid peptides Purines: adenosine ... An irreversible antagonist binds so strongly to the receptor as to render the receptor unavailable for binding to the agonist. ...
MicroRNA
Most commonly, enzymes known as adenosine deaminases acting on RNA (ADARs) catalyze adenosine to inosine (A to I) transitions. ... The specific microRNA, miR-506 has been found to work as a tumor antagonist in several studies. In a 2014 study, a significant ... miR-382 is the target for the dopamine receptor D1 (DRD1), and its overexpression results in the upregulation of DRD1 and delta ... December 2003). "High mobility group A2 protein and its derivatives bind a specific region of the promoter of DNA repair gene ...
List of OMIM disorder codes
IGF1R Interleukin 1 receptor antagonist deficiency; 612852; IL1RN Interleukin-2 receptor, alpha chain, deficiency of; 606367; ... IHH Brachydactyly type A2; 112600; BMPR1B Brachydactyly type A2; 112600; GDF5 Brachydactyly type B1; 113000; ROR2 Brachydactyly ... APC Adenosine deaminase deficiency, partial; 102700; ADA Adenosine triphosphate, elevated, of erythrocytes; 102900; PKLR ... associated with acetylcholine receptor deficiency; 608931; MUSK Myasthenic syndrome, congenital, associated with acetylcholine ...
istradefylline | Ligand page | IUPHAR/BPS Guide to PHARMACOLOGY
Characterization of the Potent and Highly Selective A2A Receptor Antagonists Preladenant and SCH 412348 [7-[2-[4-2,4...![Test-retest reproducibility of PET scan with adenosine A2A receptor ligand [C-11]Preladenant in healthy volunteers. -...](data:image/png;base64,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)
Test-retest reproducibility of PET scan with adenosine A2A receptor ligand [C-11]Preladenant in healthy volunteers. -...
Merck to Discontinue Parkinson s Drug Program Targeting the Brain Chemical Adenosine | Parkinson's Disease
3-(2,4,4-trimethylpentan-2-ylamino)propanenitrile 86375-28-2 Chemical Properties Physical Properties
SCH 442416 | A2A Receptor Antagonist | Buy SCH 442416 from Supplier AdooQ®
4-((8-amino-3,6,10,13,16,19-hexaazabicyclo(6.6.6)icosane-1-ylamino)methyl)benzoic acid
Summary Report | CureHunter
ANTAGONIST OF A2B ADENOSINE RECEPTORS FOR ASTHMA | SBIR.gov
Alveolar Epithelial A2B Adenosine Receptors in Pulmonary Protection during Acute Lung Injury | The Journal of Immunology
Abstract 294: The A2b Adenosine Receptor and Newly Identified Opposing Effects of cAMP on Insulin Secretion | Arteriosclerosis,...
Regadenoson Impurity 9 | Anant Pharmaceuticals Pvt. Ltd.
CAS # 3945-69-5, 4-(4,6-Dimethoxy-1,3,5-triazin-2-yl)-4-methyl morpholinium chloride, DMTMM![Methanol,[(4,6-dimethyl-1,3,5-triazin-2-yl)amino]-(9ci) - Alfa Chemistry](data:image/png;base64,iVBORw0KGgoAAAANSUhEUgAAABAAAAAQCAIAAACQkWg2AAAAA3NCSVQICAjb4U/gAAACF0lEQVQokbXSvWsTcRjA8ef3u7fc5a2BDqUWhaJNqpX6nlBfMKV1EfwDFEHo6GQRnCxBcBLEDro5qLi4BCrqICg6SBtEahchuSa5NjHNXZLr5XLpXX5393OIg+3WwWf+fnie4UGUUtjP4H3VAMACQLtjW10nFBSColBvtMUANxCRdKNrOwQAQpKAMDI7tiTy0bDIZDKZh8/eLyy+NS37zPFDM7eetIxuOhlfWFx68PTd66Ucg9HyavHeo+xv1Zg9P44BoKCoAYGTFXXPdoTQ/dtX06l4QdH6AaWUJa5XrjQnxobzpTr16W4A06m4JHKyok6MDf/8VXF6Lq5u6TsOmUyMtDt2vWn+C3yfpm8+fpFdbhnWZGKEuN5GrcUWFA0AKjUdAIqb2p6T7s7NAgClf4N1RcMFRQWAlbUyAMjKLoAR3Lh2jgIFgJW1EkIgKxqWy+pgLPj51Z2gyPfBl1z++vzzmmr0mVxWeY759HJ+aDAib6hsLCpNpxIIoZmpcY5jpk6O+j4FgANDsYGIBADhUODKhaMYo8vJuNMj0NA7lFLTsn3fV6pN4nptc4e4nu2Q5nbH8/xypUGIW9nSez3X6jq4VGnYDsl+XHU9v1rfNtrdNx++64ZV3GzIiqa2zB7xiOd/zeUxRt9+rLNBkWcYfPH0YQajWFSSRP7S2SMhSWAwFng2LAkCz3IMTp4YRRidOnYQ/fdv/QNUegr8Rl0SCgAAAABJRU5ErkJggg==)
Methanol,[(4,6-dimethyl-1,3,5-triazin-2-yl)amino]-(9ci) - Alfa Chemistry
Medicinal chemistry and pharmacology of A2B adenosine receptors | Pubblicazioni Scientifiche Unicam
Welcome to CDC stacks | Regadenoson and adenosine are equivalent vasodilators and are superior than dipyridamole- a study of...
Regadenoson vs. Dipyridamole Hyperemia for Cardiac PET Imaging | Journal Scan - American College of Cardiology
Altered electrical response to caffeine exposure in hypertrophied rat myocardium.![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...](data:image/png;base64,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)
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...
Piperazine, 1-acetyl-4-(4-hydrazino-6-methyl-1,3,5-triazin-2-yl)- | C10H17N7O - PubChem![Microwave Induced Synthesis of 3-Aryl-6-(6-/8-substituted 4-chloroquinoline-3-yl) - s -triazolo [3,4-<em>b]</em> −1,3,4...](data:image/png;base64,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)
Microwave Induced Synthesis of 3-Aryl-6-(6-/8-substituted 4-chloroquinoline-3-yl) - s -triazolo [3,4-<em>b]</em> −1,3,4...
2,6-Bis(5,6-diisopropyl-1,2,4-triazin-3-yl)pyridine: a highly selective N-donor ligand studied by TRLFS, liquid-liquid...
CAS 20125-39-7 N6-(2-Phenylethyl)-adenosine - BOC Sciences![Water-soluble pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidines as human A₃ adenosine receptor antagonists. - PubMed - NCBI](data:image/png;base64,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)
Water-soluble pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidines as human A₃ adenosine receptor antagonists. - PubMed - NCBI
Caffeine exposure leaves bees buzzing | Reuters.com![5,6-Dihydro-[1,2,4]triazolo[1,5-c]quinazolines. Message 1. Features of interactions between [2-(3-aryl-1H-1,2,4-triazole-5-yl...](data:image/png;base64,iVBORw0KGgoAAAANSUhEUgAAABAAAAAQCAYAAAAf8/9hAAAABHNCSVQICAgIfAhkiAAAAzlJREFUOI1d01tMWwUcx/HvOae0wFbsRkOL0tJVboN1mHUSYDJwFx+2CZs3TISZPWzTaFyWMBM1C6uJ0WwqPhgRl2w6HcluGMkSMl1YCW2EIBcFXNfg2pC1ZXSALdCdVjj4MF2q/+ffL/kl/3wE/nfNYBHgILBN0qgstZ+8ihyR/cHhie6Ry/2nHeBPzgtJRZUADqAJUAOoV6fSNNryMBwc9iUGvr7x8VjnQLMDlgCkpPIl4KAgipKxxIQ+PxtJLWHZUsTU2CTxeRnjBpOUt91WtRxPPJE35OvogWXVPzM+BPbmVhay52QjiViC2Mw85rI8WuxvY1ifQzQ0C0DtpweobtpbG5tZ+ICO/mNSMxQJcC4zzyjWn32TrnfOc/39S+RWFOJ3e1i7Lou0NaupP/MGq/SP0Hn0DBvqnsRQbC7LaO+9Ij0Nx4GKmmN1THSPshiOYm+opvSlSsK3gsjR+wx914MciWEsMaHRphEY9mF7rlyMzy2uiMAOgKyCR/G7PUzfChIY8TF9M8B45wC2fWXoTJnkVhay1mpgXVUxYW8IAIPNvEMErADR0Bxag4750Bx+twdRJRH2BMhan4OypGCpLERr0BENzZKRrQNAo021ioAI8Ms5J0+9tYuUdDX35xaJBGbILrXgc90kx24lJVWNHInR1/YTm17Z+uCvK4Io1UAjkBkNzJJYkNl5/EVmfHcZ+76fupYDOE/9wJ6T+7kzeJuud89TdWQ3ueUFAIR+892WaqAE2GwsMZFYjDPZ70WXoyclTY0+P5t73hBZRY8x7QlSvNtOul5LbHaBVfoMxjv6LqtWoFWAQ6UvbxHtDdUA3P39Dj9/eQ2/24O5ogA5EuPXi26mRicB2PhCBeWHdyqD3/S2CgAnoBV4zVxegDpdg9/tQVEUnv/iEH84x3nGUY+ytIzP5SElXY1p8+P8eOLCV3XtrsMqgBU4KkDRZJ+3JhnKxI0xrFuLESURURLJ325DWVZwfd7lHGp3HXlooQeWquGCAHpg07/I5qf+ZNdHDQjCA3P3JkJK72dX2/pOX290gPwfjUkqNwrwOrBNk5FmefbUfuILsj/sDXYPfutsey/210hy/m9gfDT/pquG8AAAAABJRU5ErkJggg==)
5,6-Dihydro-[1,2,4]triazolo[1,5-c]quinazolines. Message 1. Features of interactions between [2-(3-aryl-1H-1,2,4-triazole-5-yl...![TRC | Details of CAS = 1803026-54-1, ChemicalName = (2Z)-1-[5,6-Dihydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazin-7(8H)...](data:image/png;base64,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)
TRC | Details of CAS = 1803026-54-1, ChemicalName = (2Z)-1-[5,6-Dihydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazin-7(8H)...
Adora2a MGI Mouse Gene Detail - MGI:99402 - adenosine A2a receptor
Does a Shortened Hyperemia With Regadenoson Stress Pose a Concern for Quantitative Rb-82 PET Imaging? | JACC: Cardiovascular...
CV Therapeutics and Astellas Announce FDA Approval for Lexiscan(TM) (regadenoson)... ( -First A2A Adenosine Receptor Agoni...)![IUCr) Ethyl 6-methyl-8-phenyl-1,2,4-triazolo[1,5-a]pyridine-7-carboxyl-ate](data:image/png;base64,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)
IUCr) Ethyl 6-methyl-8-phenyl-1,2,4-triazolo[1,5-a]pyridine-7-carboxyl-ate
Adenosine modulates cell growth in human epidermoid carcinoma (A431) cells | 
Unscramble adenosine | Words unscrambled from letters adenosine | Scrabble Word adenosine | Words Made with the Letters...
HIC-Up files for compound 2SA 2-(9-(3,4-dihydroxy-5-phosphonooxymethyl-tetrahydro- furan-2-yl)-9h-purin-6-ylamino)-succinic...
Adenosine Sanolabor - Drugs.com
Studies on enantioselectivity of chiral 4-acetylamino-6-alkyloxy-2-alkylthiopyrimidines acting as antagonists of the human A3...![1,2,4]Triazolo[1,5-a]pyrazine](data:image/png;base64,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)
1,2,4]Triazolo[1,5-a]pyrazine
Gentaur Molecular :BioBasic \ Adenosine \ AD0016
1 | 護心 | 保健品 | 海健藥房
10 Year Old W/ Stretch Marks?? - Mamapedia™![Adenosine A2 Receptor Antagonist Pipeline Insight, 2018 [Report Updated: 14022018] Prices from USD $1250 - BioPortfolio.com](data:image/png;base64,iVBORw0KGgoAAAANSUhEUgAAABAAAAAQCAMAAAAoLQ9TAAAAA3NCSVQICAjb4U/gAAAASFBMVEUrNFpARVsrM1cwLjo4P11KUWgtMU4qKSo2O1YqKTBJTWEsMlOUlqJCSGE7PU8qLUl1eo9/hp1ma342N0BvdYtVWWpfZHmqq7NDqa9CAAAAgUlEQVQYlV3M2w6DQAhFUaiAiMPcdPT//7Q0rUl1vZ1NAsAdPTY4vC5AAR3Wr5eqopsSSFgV2YlUjARKKXEkRDYpIgWkH4YHq3JXxwj5PFNKre6t1db2DDlm6r2Oo++1foLn+D626Qc83vGw5QLMtk3LMl+AbZr/Aef5Hsb2CPwIb7AgB+DUiCyUAAAAAElFTkSuQmCC)
Adenosine A2 Receptor Antagonist Pipeline Insight, 2018 [Report Updated: 14022018] Prices from USD $1250 - BioPortfolio.com
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 ...
https://www.bioportfolio.com/news/article/3573619/Adenosine-A2-Receptor-Antagonist-Pipeline-Insight-2018-Report-Updated-14022018-Prices-from.html
BIIB014 Phase 2a Monotherapy - Full Text View - ClinicalTrials.gov
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 ...
https://clinicaltrials.gov/ct2/show/NCT00451815?term=biogen&spons=biogen&rank=18Using PET Scans to Study Brain Receptor Occupancy of BIIB014 in Healthy Male Volunteers - Full Text View - ClinicalTrials.gov
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 ...
https://clinicaltrials.gov/ct2/show/NCT00531193
Physiological roles of A1 and A2A adenosine receptors in regulating heart rate, body temperature, and locomotion as revealed...
... 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. * ...
https://www.semanticscholar.org/paper/Physiological-roles-of-A1-and-A2A-adenosine-in-body-Yang-Chen/462ed1bcc5b5b1847b0a4a38c0ad02de3c3ee91b
Drug CategoriesBrowse DrugBank Categories - DrugBank
Adenosine A2 Receptor Antagonists. Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.. 4. ... Adenosine A2 Receptor Agonists. Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS.. 4. 3. Details. ... Adenosine A1 Receptor Agonists. Not Available. 1. 0. Details. Adenosine A1 Receptor Antagonists. Compounds that bind to and ... Drugs that inhibit ADENOSINE DEAMINASE activity.. 1. 1. Details. Adenosine Kinase, antagonists & inhibitors. Not Available. 1. ...
https://www.drugbank.ca/categories?page=4Indobufen Sodium | Semantic Scholar
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. ...
https://www.semanticscholar.org/topic/Indobufen-Sodium/5197831Diprophylline - Wikipedia
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. ...
https://en.wikipedia.org/wiki/Diprophylline
Role of Plant Derived Alkaloids and Their Mechanism in Neurodegenerative Disorders
Caffeine portrays its activity as adenosine A2 receptor antagonist which results in enhanced loco motor activity in ... It directs the down-regulation of adenosine A2 receptors to counter the suppressive effect of adenosine on brain dopaminergic ... Rivera-Oliver M, Díaz-Ríos M. Using caffeine and other adenosine receptor antagonists and agonists as therapeutic tools against ... As the Caffeine exerts a potential efficacy to act as antagonist of adenosine receptor, thus it potentially reduces ...
http://www.ijbs.com/v14p0341.htm
Search Articles | University of Toronto Libraries
Adenosine A1 Receptor Antagonists - metabolism , Adenosine A2 Receptor Antagonists - metabolism , Adenosine A2 Receptor ... Receptor, Adenosine A2A - metabolism , Adenosine A2 Receptor Antagonists - pharmacology , Animals , Adenosine A2 Receptor ... Receptor, Adenosine A2A - drug effects , Adenosine A2 Receptor Antagonists - pharmacology , Adenosine A2 Receptor Agonists - ... Receptor heteromer , C-FOS EXPRESSION , Adenosine A2 Receptor Antagonists - pharmacology , Animals , Adenosine A2 Receptor ...
https://query.library.utoronto.ca/index.php/search/q?kw=SubjectTerms:Adenosine%20A2%20Receptor%20Antagonists%20-%20pharmacology
A Category Names List - Drug Information Portal - U.S. National Library of Medicine
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 ...
https://druginfo.nlm.nih.gov/drugportal/drug/categoriesA Category Names List - Drug Information Portal - U.S. National Library of Medicine
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 ...
https://druginfo.nlm.nih.gov/drugportal/jsp/drugportal/drugNamesAndCategories.jsp
Patent US8114147 - Continuous double layered stent for migration resistance - Google Patents
... selective adenosine A1 antagonists, adenosine A2 receptor antagonists (e.g., CGS 21680, regadenoson, UK 432097 or GW 328267), ... beta receptor antagonists (e.g., atenolol, metaprolol and butoxamine), angiotensin-II receptor antagonists (e.g., losartan, ... o) leukotriene receptor antagonists; (p) antagonists of E- and P-selectins;. *(q) inhibitors of VCAM-1 and ICAM-1 interactions; ... receptor antagonists and chimeric fusion proteins, TNF-α pathway agents such as thalidomide and analogs thereof, Thromboxane A2 ...
http://www.google.com/patents/US8114147?dq=7,053,767
KAKEN - Research Projects | Mechanisms of development of ischemic neuronal cell death and protection against ischemic neuronal...
Moreover, CHA, an adenosine A1 receptor antagonist and CGS-21680, an adenosine A2 receptor antagonist, were also effective in ... adenosine / dementia / gerbil / ischemia / neuroprotection / primary culture / adenosine / AMP / ATP / A1 receptor / cortex / ... This selective damage was attenuated by MK-801, a NMDA receptor antagonist and L-NAME, a nitric oxide synthase inhibitor. ... This cell death was attenuated by treatment of MK-801, L-NAME, adenosine, CHA and CGS-21680. CHA reduced hypoxia/hypoglycemia- ...
https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-14572088/
JCI -
The antiinflammatory mechanism of methotrexate. Increased adenosine release at inflamed sites diminishes leukocyte...
... 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. Neither ADA nor DMPX affected leukocyte accumulation in ... Increased adenosine release at inflamed sites diminishes leukocyte accumulation in an in vivo model of inflammation.. B N ... Methotrexate, a folate antagonist, is a potent antiinflammatory agent when used weekly in low concentrations. We examined the ...
https://www.jci.org/articles/view/116884CGS-15943 - Wikipedia
"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 ...
https://en.wikipedia.org/wiki/CGS-15943
Ronald Pearl | Stanford Medicine Profiles
... results consistent with an adenosine A2 receptor. Pretreatment with the adenosine A1 receptor antagonist ... and pretreatment with the adenosine A2 receptor antagonist CGS 15943A increased the ED50 of NECA to 2.7 x 10(-7) mol/L. These ... ADENOSINE PRODUCES PULMONARY VASODILATION IN THE PERFUSED RABBIT LUNG VIA AN ADENOSINE A(2) RECEPTOR ANESTHESIA AND ANALGESIA ... results suggest that adenosine produces pulmonary vasodilation via activation of an adenosine A2 receptor. ...
https://med.stanford.edu/profiles/ronald-pearl![Synthesis, Antibacterial Activity and DFT Calculation of Naphtopyrano, Furo and Pyrazolo [3,2,e] [1,2,4]Triazolo-[1,5-c...](data:image/png;base64,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)
Synthesis, Antibacterial Activity and DFT Calculation of Naphtopyrano, Furo and Pyrazolo [3,2,e] [1,2,4]Triazolo-[1,5-c...
... 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. ...
https://link.springer.com/article/10.1007%2Fs42250-019-00081-yWO2011034768A1 - Integrated stent retrieval loop adapted for snare removal and/or optimized purse stringing
- Google...
... selective adenosine Al antagonists, adenosine A2 receptor antagonists (e.g., CGS 21680, regadenoson, UK 432097 or GW 328267), ... antagonists such as propranolol and α/β-antagonists such as labetalol and carvedilol; (e) endothelin receptor antagonists such ... beta receptor antagonists (e.g., atenolol, metaprolol and butoxamine), angiotensin-II receptor antagonists (e.g., losartan, ... o) leukotriene receptor antagonists; (p) antagonists of E- and P-selectins; (q) inhibitors of VCAM-1 and ICAM-1 interactions; ( ...
https://patents.google.com/patent/WO2011034768A1/en
Patients being sought for clinical trial treating weak respiratory muscles after spinal cord injury
Nantwi KD and Goshgarian HG (2002). Actions of specific adenosine receptor A1 and A2 agonists and antagonists in recovery of ... a general adenosine A1 and A2 receptor antagonist, can activate the latent pathway by acting centrally through antagonism at ... adenosine receptors. 2. The present study was designed to assess the relative contributions of adenosine A1 and A2 receptors in ... To further test the involvement of adenosine receptors, N6 (L-2-phenylisopropyl) adenosine (L-PIA), an analogue of adenosine ...
http://sci.rutgers.edu/forum/showthread.php?38417-Patients-being-sought-for-clinical-trial-treating-weak-respiratory-muscles-after-spinal-cord-injury&s=499442ae1ab1cc6490474666da3282ddDyphylline - DrugBank
Schwabe U, Ukena D, Lohse MJ: Xanthine derivatives as antagonists at A1 and A2 adenosine receptors. Naunyn Schmiedebergs Arch ... Schwabe U, Ukena D, Lohse MJ: Xanthine derivatives as antagonists at A1 and A2 adenosine receptors. Naunyn Schmiedebergs Arch ... Receptor for adenosine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase.. Gene Name. ... Receptor for adenosine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.. Gene Name. ...
https://www.drugbank.ca/drugs/DB00651
neurophysiology - How does caffeine work as an analgesic adjuvant? - Psychology & Neuroscience Stack Exchange
Caffeine is a nonselective antagonist of adenosine A1 and A2 receptors. Adenosine A2a receptors induce intracellular signalling ... disinhibition of inhibitory adenosine actions on central cholinergic nerve terminals, leading to increased acetylcholine ... a blockade of peripheral pro-nociceptive actions of adenosine;. *the activation of the central noradenosine, pain-suppressing ...
https://psychology.stackexchange.com/questions/20758/how-does-caffeine-work-as-an-analgesic-adjuvant
Akamatsu Hiroshi - Inventor Patent Directory, Page 1
That is, it provides a novel condensed imidazole compound which has an adenosine A2 receptor antagonist action, ... ... which is a new type based on an adenosine A2 receptor antagonist action. ... Matsushita Electric, December 22, 2004: EP1488880-A2 (2 worldwide citation) A structure of solder joint structure formed of ...
http://patent.ipexl.com/inventor/akamatsu_hiroshi_1.html
Basal Forebrain Histaminergic Transmission Modulates Electroencephalographic Activity and Emergence from Isoflurane Anesthesia ...
... deprivation on righting reflex in the rat is partially reversed by administration of adenosine A1 and A2 receptor antagonists. ... H1 receptor antagonist triprolidine and H2 receptor antagonist cimetidine had no effect on the breathing rate during isoflurane ... selective H1 receptor antagonist triprolidine (5 μg/1 μl), or selective H2 receptor antagonist cimetidine (25 μg/1 μl) alone 30 ... Antagonists of H1 and H2 receptors were infused directly into the NBM to reveal the specific receptor underlying the ...
http://anesthesiology.pubs.asahq.org/article.aspx?articleid=1932220
Respiratory Pharmacology by Chris Arakawa on Prezi
Nonselective adenosine receptor antagonist (Blocks A1, A2, A3 equally). Mechanism: Nonspecific AChRi -,promotes degrdation of ...
https://prezi.com/h0ofaqeloe0w/respiratory-pharmacology/Molecular probes for adenosine receptors - Patent # 5248770 - PatentGenius
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 ...
http://www.patentgenius.com/patent/5248770.htmlAgonists and antagonistsDrugs that inhibit ADENOSINE DEAMINASEInhibitorsDPCPXSelective antagonistDerivativesInhibitionEffect of adenosineNonselectiveInhibit2018CompoundsHypoxiaNMDACaffeineSubtypeHistamine releaseProtein-coupledMoleculeVascularConcentrationsExertMoietyCardiacIncreasesBlockerAccumulationInvestigationalEstablishBrainHumanPresentReleaseEffective
- Effects of adenosine A2 and A3 receptors agonists and antagonists were also investigated. (ovid.com)
- The binding of agonists and antagonists to a2-adrenergic receptors of human platelets was studied. (uni-wuerzburg.de)
- Stably transfected cell lines bound a variety of adenosine agonists and antagonists with affinities characteristic of a brain adenosine A2a receptor. (garvan.org.au)
- Drugs that inhibit ADENOSINE DEAMINASE activity. (drugbank.ca)
- Adenosine receptor-blocking xanthines as inhibitors of phosphodiesterase isozymes. (semanticscholar.org)
- The effects of adenosine, CPA and ATP were inhibited by DPCPX, a selective adenosine A1 receptor antagonist. (ovid.com)
- CGS-15943 is a drug which acts as a potent and reasonably selective antagonist for the adenosine receptors A1 and A2A, having a Ki of 3.3nM at A2A and 21nM at A1. (wikipedia.org)
- N3,N7-diaminophenothiazinium derivatives as antagonists of α7-nicotinic acetylcholine receptors expressed in Xenopus oocytes. (semanticscholar.org)
- Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype. (semanticscholar.org)
- Both adenosine and xanthine derivatives bind competitively to A-1 and A-2 adenosine receptors. (patentgenius.com)
- Inhibition of rat ventricular automaticity by adenosine. (semanticscholar.org)
- The bronchodilatory action of dyphylline, as with other xanthines, is thought to be mediated through competitive inhibition of phosphodiesterase with a resulting increase in cyclic AMP producing relaxation of bronchial smooth muscle as well as antagonism of adenosine receptors. (drugbank.ca)
- 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)
- Thus, a stimulatory effect of adenosine was seen in the presence ofXAC, whereas an inhibitory effect was unmasked by NBTI. (uni-wuerzburg.de)
- Barbiturates inhibit binding of radioligands to A 1(Ri) adenosine receptors of rat brain membranes. (uni-wuerzburg.de)
- 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)
- Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS. (drugbank.ca)
- Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS. (drugbank.ca)
- Interplay of hypoxia and A2B adenosine receptors in tissue protection. (semanticscholar.org)
- A2B adenosine receptor dampens hypoxia-induced vascular leak. (semanticscholar.org)
- This selective damage was attenuated by MK-801, a NMDA receptor antagonist and L-NAME, a nitric oxide synthase inhibitor. (nii.ac.jp)
- 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)
- 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)
- Second, we investigated the histamine receptor subtype responsible for electroencephalographic activation. (asahq.org)
- 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 actions of adenosine on histamine release of human lung fragments were investigated. (uni-wuerzburg.de)
- 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)
- 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)
- 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)
- These findings suggest an important bimodal role of adenosine in regulating histamine release in the human lung. (uni-wuerzburg.de)
- 5 Histamine acts on G-protein coupled receptors in the brain, with H1 and H2 receptors mainly exciting the postsynaptic membrane and H3 receptors suppressing the presynaptic release of histamine and other neurotransmitters. (asahq.org)
- A cDNA encoding a G protein-coupled receptor of unknown ligand specificity was isolated from a human hippocampal cDNA library by virtue of the high degree of structural homology between members of this receptor family. (garvan.org.au)
- Although CCR7(-/-) naive T cells displayed a small reduction in locomotion, systemic treatment with pertussis toxin reduced naive T lymphocyte speed by 59%, indicating a contribution of Galpha(i)-mediated signaling, but involvement of other G protein-coupled receptors besides CCR7. (ox.ac.uk)
- These data implicate pO(2), tissue architecture, and G-protein coupled receptor signaling in regulation of naive T lymphocyte migration in explanted LNs. (ox.ac.uk)
- The report assesses the active Adenosine A2 Receptor Antagonist pipeline products by developmental stage, product type, molecule type, and administration route. (bioportfolio.com)
- 11C]SCH442416 is a radiolabelled tracer molecule that specifically binds to adenosine A2A sites and will be used to evaluate receptor occupancy. (clinicaltrials.gov)
- 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)
- and (2) a label moiety bonded to said adenosine nucleus. (patentgenius.com)
- Would calcium or potassium channels be responsible for cardiac arrest produced by adenosine and ATP in the right atria of Wistar rats? (ovid.com)
- This study aims to evaluate adenosine and P2 receptors and cellular signalling in cardiac arrest produced by purines in the heart. (ovid.com)
- Cumulative concentration-effect curves of adenosine and CPA resulted in a negative chronotropic effect culminating in cardiac arrest at 1000 μM (adenosine) and 1 μM (CPA). (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)
- 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)
- 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 found that adenosine deaminase abolished 1S,3R-ACPD-stimulated cAMP accumulation whereas the adenosine uptake blocker dipyridamole enhanced this response. (jneurosci.org)
- Increased adenosine release at inflamed sites diminishes leukocyte accumulation in an in vivo model of inflammation. (jci.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)
- 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)
- Tezosentan is an investigational intravenous drug that blocks the endothelin receptors. (stanford.edu)
- To establish the extent to which BIIB014, following 8 to 12 consecutive days of dosing at selected dose levels, occupies the brain's A2A receptors. (clinicaltrials.gov)
- Binding of [3H]KF17837S, a selective adenosine A2 receptor antagonist, to rat brain membranes. (semanticscholar.org)
- The cloned receptor DNA was transfected into human embryonic kidney 293 cells. (garvan.org.au)
- The present invention provides a preventive or therapeutic agent for diabetes mellitus and diabetic complications, which is a new type based on an adenosine A2 receptor antagonist action. (ipexl.com)
- The present application prepares and describes probes radioactive and non-radioactive for more sensitive assay-type quantitative binding measurements of A-1 and A-2 receptors using the functionalized congeners described and claimed in the fourabove-named copending applications. (patentgenius.com)
- Moreover, CHA, an adenosine A1 receptor antagonist and CGS-21680, an adenosine A2 receptor antagonist, were also effective in protection of CA1 pyramidal neurons. (nii.ac.jp)