Adenosine a1 receptor antagonists. Medical search

A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter.

A subclass of adenosine A2 receptors found in LEUKOCYTES, the SPLEEN, the THYMUS and a variety of other tissues. It is generally considered to be a receptor for ADENOSINE that couples to the GS, STIMULATORY G-PROTEIN.

A subtype of ADENOSINE RECEPTOR that is found expressed in a variety of tissues including the BRAIN and DORSAL HORN NEURONS. The receptor is generally considered to be coupled to the GI, INHIBITORY G-PROTEIN which causes down regulation of CYCLIC AMP.

Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.

Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.

An enzyme that catalyzes the hydrolysis of ADENOSINE to INOSINE with the elimination of AMMONIA.

Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.

A ligand that binds to but fails to activate the INTERLEUKIN 1 RECEPTOR. It plays an inhibitory role in the regulation of INFLAMMATION and FEVER. Several isoforms of the protein exist due to multiple ALTERNATIVE SPLICING of its mRNA.

A subtype of ADENOSINE RECEPTOR that is found expressed in a variety of locations including the BRAIN and endocrine tissues. The receptor is generally considered to be coupled to the GI, INHIBITORY G-PROTEIN which causes down regulation of CYCLIC AMP.

A subclass of adenosine A2 receptors found in the CECUM, the COLON, the BLADDER, and a variety of other tissues. It is generally considered to be a low affinity receptor for ADENOSINE that couples to the GS, STIMULATORY G-PROTEIN.

Compounds that inhibit or block the activity of NEUROKININ-1 RECEPTORS.

A subclass of ADENOSINE RECEPTORS that are generally considered to be coupled to the GS, STIMULATORY G-PROTEIN which causes up regulation of CYCLIC AMP.

An enzyme that catalyzes the formation of ADP plus AMP from adenosine plus ATP. It can serve as a salvage mechanism for returning adenosine to nucleic acids. EC 2.7.1.20.

A class of cell surface receptors that prefer ADENOSINE to other endogenous PURINES. Purinergic P1 receptors are widespread in the body including the cardiovascular, respiratory, immune, and nervous systems. There are at least two pharmacologically distinguishable types (A1 and A2, or Ri and Ra).

Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS.

Purine bases found in body tissues and fluids and in some plants.

Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS.

The relationship between the dose of an administered drug and the response of the organism to the drug.

A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.

Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.

Drugs that selectively bind to but do not activate histamine H2 receptors, thereby blocking the actions of histamine. Their clinically most important action is the inhibition of acid secretion in the treatment of gastrointestinal ulcers. Smooth muscle may also be affected. Some drugs in this class have strong effects in the central nervous system, but these actions are not well understood.

A family of hexahydropyridines.

Drugs that bind to but do not activate SEROTONIN 5-HT3 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT3 RECEPTOR AGONISTS.

Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.

Compounds that selectively bind to and block the activation of ADENOSINE A3 RECEPTORS.

Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME.

Agents that antagonize ANGIOTENSIN RECEPTORS. Many drugs in this class specifically target the ANGIOTENSIN TYPE 1 RECEPTOR.

Drugs that bind to but do not activate SEROTONIN 5-HT2 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT2 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more specific 5-HT2 receptor subtypes.

Chemical substances which inhibit the function of the endocrine glands, the biosynthesis of their secreted hormones, or the action of hormones upon their specific sites.

Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.

Adenine nucleotide containing one phosphate group esterified to the sugar moiety in the 2'-, 3'-, or 5'-position.

A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.

A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity.

A methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant activities. Theophylline inhibits the 3',5'-CYCLIC NUCLEOTIDE PHOSPHODIESTERASE that degrades CYCLIC AMP thus potentiates the actions of agents that act through ADENYLYL CYCLASES and cyclic AMP.

Agents inhibiting the effect of narcotics on the central nervous system.

Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.

Cell surface proteins that bind ENDOTHELINS with high affinity and trigger intracellular changes which influence the behavior of cells.

Cell surface proteins that bind PURINES with high affinity and trigger intracellular changes which influence the behavior of cells. The best characterized classes of purinergic receptors in mammals are the P1 receptors, which prefer ADENOSINE, and the P2 receptors, which prefer ATP or ADP.

Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. Muscarinic antagonists have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system.

Drugs that bind to but do not activate GABA-A RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-A RECEPTOR AGONISTS.

A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)

Drugs that bind to but do not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists. Classical antihistaminics block the histamine H1 receptors only.

Drugs that bind to but do not activate GABA RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.

Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.

A class of drugs designed to prevent leukotriene synthesis or activity by blocking binding at the receptor level.

Glycoproteins which contain sialic acid as one of their carbohydrates. They are often found on or in the cell or tissue membranes and participate in a variety of biological activities.

A subtype of endothelin receptor found predominantly in the VASCULAR SMOOTH MUSCLE. It has a high affinity for ENDOTHELIN-1 and ENDOTHELIN-2.

Cell-surface proteins that bind SEROTONIN and trigger intracellular changes which influence the behavior of cells. Several types of serotonin receptors have been recognized which differ in their pharmacology, molecular biology, and mode of action.

A class of ionotropic glutamate receptors characterized by affinity for N-methyl-D-aspartate. NMDA receptors have an allosteric binding site for glycine which must be occupied for the channel to open efficiently and a site within the channel itself to which magnesium ions bind in a voltage-dependent manner. The positive voltage dependence of channel conductance and the high permeability of the conducting channel to calcium ions (as well as to monovalent cations) are important in excitotoxicity and neuronal plasticity.

An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH.

A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.

A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.

Drugs that bind to but do not activate SEROTONIN 5-HT1 RECEPTORS, thereby blocking the actions of SEROTONIN 5-HT1 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more of the specific 5-HT1 receptor subtypes.

2-Chloroadenosine. A metabolically stable analog of adenosine which acts as an adenosine receptor agonist. The compound has a potent effect on the peripheral and central nervous system.

Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).

Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS.

Cell surface receptors that are specific for INTERLEUKIN-1. Included under this heading are signaling receptors, non-signaling receptors and accessory proteins required for receptor signaling. Signaling from interleukin-1 receptors occurs via interaction with SIGNAL TRANSDUCING ADAPTOR PROTEINS such as MYELOID DIFFERENTIATION FACTOR 88.

Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.

Compounds with BENZENE fused to AZEPINES.

N-Isopropyl-N-phenyl-adenosine. Antilipemic agent. Synonym: TH 162.

Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.

Drugs that bind to nicotinic cholinergic receptors (RECEPTORS, NICOTINIC) and block the actions of acetylcholine or cholinergic agonists. Nicotinic antagonists block synaptic transmission at autonomic ganglia, the skeletal neuromuscular junction, and at central nervous system nicotinic synapses.

Drugs that bind to and block the activation of PURINERGIC RECEPTORS.

Azoles of two nitrogens at the 1,2 positions, next to each other, in contrast with IMIDAZOLES in which they are at the 1,3 positions.

Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.

Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS.

Endogenous compounds and drugs that bind to and activate SEROTONIN RECEPTORS. Many serotonin receptor agonists are used as ANTIDEPRESSANTS; ANXIOLYTICS; and in the treatment of MIGRAINE DISORDERS.

Drugs that selectively bind to but do not activate HISTAMINE H3 RECEPTORS. They have been used to correct SLEEP WAKE DISORDERS and MEMORY DISORDERS.

A group of compounds that contain the structure SO2NH2.

A glycoprotein enzyme present in various organs and in many cells. The enzyme catalyzes the hydrolysis of a 5'-ribonucleotide to a ribonucleoside and orthophosphate in the presence of water. It is cation-dependent and exists in a membrane-bound and soluble form. EC 3.1.3.5.

A purine nucleoside that has hypoxanthine linked by the N9 nitrogen to the C1 carbon of ribose. It is an intermediate in the degradation of purines and purine nucleosides to uric acid and in pathways of purine salvage. It also occurs in the anticodon of certain transfer RNA molecules. (Dorland, 28th ed)

Peptides whose amino and carboxy ends are linked together with a peptide bond forming a circular chain. Some of them are ANTI-INFECTIVE AGENTS. Some of them are biosynthesized non-ribosomally (PEPTIDE BIOSYNTHESIS, NON-RIBOSOMAL).

Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.

A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator.

The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements.

Elements of limited time intervals, contributing to particular results or situations.

Compounds that bind to and block the stimulation of PURINERGIC P2X RECEPTORS. Included under this heading are antagonists for specific P2X receptor subtypes.

Seven membered heterocyclic rings containing a NITROGEN atom.

An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.

An eleven-amino acid neurotransmitter that appears in both the central and peripheral nervous systems. It is involved in transmission of PAIN, causes rapid contractions of the gastrointestinal smooth muscle, and modulates inflammatory and immune responses.

Drugs that bind to but do not activate GABA-B RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-B RECEPTOR AGONISTS.

3,7-Dimethylxanthine. The principle alkaloid in Theobroma cacao (the cacao bean) and other plants. A xanthine alkaloid that is used as a bronchodilator and as a vasodilator. It has a weaker diuretic activity than THEOPHYLLINE and is also a less powerful stimulant of smooth muscle. It has practically no stimulant effect on the central nervous system. It was formerly used as a diuretic and in the treatment of angina pectoris and hypertension. (From Martindale, The Extra Pharmacopoeia, 30th ed, pp1318-9)

The action of a drug that may affect the activity, metabolism, or toxicity of another drug.

Cell surface receptors that bind BRADYKININ and related KININS with high affinity and trigger intracellular changes which influence the behavior of cells. The identified receptor types (B-1 and B-2, or BK-1 and BK-2) recognize endogenous KALLIDIN; t-kinins; and certain bradykinin fragments as well as bradykinin itself.

A 21-amino acid peptide produced in a variety of tissues including endothelial and vascular smooth-muscle cells, neurons and astrocytes in the central nervous system, and endometrial cells. It acts as a modulator of vasomotor tone, cell proliferation, and hormone production. (N Eng J Med 1995;333(6):356-63)

A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.

Heterocyclic rings containing three nitrogen atoms, commonly in 1,2,4 or 1,3,5 or 2,4,6 formats. Some are used as HERBICIDES.

A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.

A class of cell surface receptors for TACHYKININS with a preference for SUBSTANCE P. Neurokinin-1 (NK-1) receptors have been cloned and are members of the G protein coupled receptor superfamily. They are found on many cell types including central and peripheral neurons, smooth muscle cells, acinar cells, endothelial cells, fibroblasts, and immune cells.

A subtype of endothelin receptor found predominantly in the KIDNEY. It may play a role in reducing systemic ENDOTHELIN levels.

The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM.

The observable response an animal makes to any situation.

A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D2-class receptor genes contain INTRONS, and the receptors inhibit ADENYLYL CYCLASES.

A derivative of benzodiazepine that acts on the cholecystokinin A (CCKA) receptor to antagonize CCK-8's (SINCALIDE) physiological and behavioral effects, such as pancreatic stimulation and inhibition of feeding.

Cell surface proteins that bind cholecystokinin (CCK) with high affinity and trigger intracellular changes influencing the behavior of cells. Cholecystokinin receptors are activated by GASTRIN as well as by CCK-4; CCK-8; and CCK-33. Activation of these receptors evokes secretion of AMYLASE by pancreatic acinar cells, acid and PEPSIN by stomach mucosal cells, and contraction of the PYLORUS and GALLBLADDER. The role of the widespread CCK receptors in the central nervous system is not well understood.

Specific molecular sites or proteins on or in cells to which VASOPRESSINS bind or interact in order to modify the function of the cells. Two types of vasopressin receptor exist, the V1 receptor in the vascular smooth muscle and the V2 receptor in the kidneys. The V1 receptor can be subdivided into V1a and V1b (formerly V3) receptors.

Drugs that bind to but do not activate alpha-adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists. Adrenergic alpha-antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma.

A nonapeptide messenger that is enzymatically produced from KALLIDIN in the blood where it is a potent but short-lived agent of arteriolar dilation and increased capillary permeability. Bradykinin is also released from MAST CELLS during asthma attacks, from gut walls as a gastrointestinal vasodilator, from damaged tissues as a pain signal, and may be a neurotransmitter.

The D-enantiomer is a potent and specific antagonist of NMDA glutamate receptors (RECEPTORS, N-METHYL-D-ASPARTATE). The L form is inactive at NMDA receptors but may affect the AP4 (2-amino-4-phosphonobutyrate; APB) excitatory amino acid receptors.

An amine derived by enzymatic decarboxylation of HISTIDINE. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and also a centrally acting neurotransmitter.

A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients.

A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.

Drugs that bind to but do not activate SEROTONIN 5-HT4 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN RECEPTOR AGONISTS.

Drugs that bind to but do not activate ADRENERGIC RECEPTORS. Adrenergic antagonists block the actions of the endogenous adrenergic transmitters EPINEPHRINE and NOREPINEPHRINE.

Naturally occurring or experimentally induced animal diseases with pathological processes sufficiently similar to those of human diseases. They are used as study models for human diseases.

Compounds with a BENZENE fused to IMIDAZOLES.

Cell surface proteins that bind THROMBOXANES with high affinity and trigger intracellular changes influencing the behavior of cells. Some thromboxane receptors act via the inositol phosphate and diacylglycerol second messenger systems.

PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS.

Injections into the cerebral ventricles.

Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.

The communication from a NEURON to a target (neuron, muscle, or secretory cell) across a SYNAPSE. In chemical synaptic transmission, the presynaptic neuron releases a NEUROTRANSMITTER that diffuses across the synaptic cleft and binds to specific synaptic receptors, activating them. The activated receptors modulate specific ion channels and/or second-messenger systems in the postsynaptic cell. In electrical synaptic transmission, electrical signals are communicated as an ionic current flow across ELECTRICAL SYNAPSES.

A class of cell surface receptors for tachykinins that prefers neurokinin A; (NKA, substance K, neurokinin alpha, neuromedin L), neuropeptide K; (NPK); or neuropeptide gamma over other tachykinins. Neurokinin-2 (NK-2) receptors have been cloned and are similar to other G-protein coupled receptors.

A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.

An antibiotic purine ribonucleoside that readily substitutes for adenosine in the biological system, but its incorporation into DNA and RNA has an inhibitory effect on the metabolism of these nucleic acids.

A competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.

Compounds that inhibit or block the activity of CANNABINOID RECEPTORS.

An isoquinoline alkaloid obtained from Dicentra cucullaria and other plants. It is a competitive antagonist for GABA-A receptors.

A group of enzymes which catalyze the hydrolysis of ATP. The hydrolysis reaction is usually coupled with another function such as transporting Ca(2+) across a membrane. These enzymes may be dependent on Ca(2+), Mg(2+), anions, H+, or DNA.

Drugs that bind to and block the activation of ADRENERGIC BETA-2 RECEPTORS.

A class of cell surface receptors for PURINES that prefer ATP or ADP over ADENOSINE. P2 purinergic receptors are widespread in the periphery and in the central and peripheral nervous system.

The rate dynamics in chemical or physical systems.

The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.

Use of electric potential or currents to elicit biological responses.

An octapeptide that is a potent but labile vasoconstrictor. It is produced from angiotensin I after the removal of two amino acids at the C-terminal by ANGIOTENSIN CONVERTING ENZYME. The amino acid in position 5 varies in different species. To block VASOCONSTRICTION and HYPERTENSION effect of angiotensin II, patients are often treated with ACE INHIBITORS or with ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKERS.

A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H3 receptors were first recognized as inhibitory autoreceptors on histamine-containing nerve terminals and have since been shown to regulate the release of several neurotransmitters in the central and peripheral nervous systems. (From Biochem Soc Trans 1992 Feb;20(1):122-5)

Drugs that bind to and block the activation of MINERALOCORTICOID RECEPTORS by MINERALOCORTICOIDS such as ALDOSTERONE.

The domestic dog, Canis familiaris, comprising about 400 breeds, of the carnivore family CANIDAE. They are worldwide in distribution and live in association with people. (Walker's Mammals of the World, 5th ed, p1065)

A histamine H1 antagonist. It has mild hypnotic properties and some local anesthetic action and is used for allergies (including skin eruptions) both parenterally and locally. It is a common ingredient of cold remedies.

Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.

An alkylamide found in CAPSICUM that acts at TRPV CATION CHANNELS.

A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.

RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.

A constitutively expressed subtype of bradykinin receptor that may play a role in the acute phase of the inflammatory and pain response. It has high specificity for intact forms of BRADYKININ and KALLIDIN. The receptor is coupled to G-PROTEIN, GQ-G11 ALPHA FAMILY and G-PROTEIN, GI-GO ALPHA FAMILY signaling proteins.

The species Oryctolagus cuniculus, in the family Leporidae, order LAGOMORPHA. Rabbits are born in burrows, furless, and with eyes and ears closed. In contrast with HARES, rabbits have 22 chromosome pairs.

Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.

An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).

Drugs used to cause dilation of the blood vessels.

21-Amino-acid peptides produced by vascular endothelial cells and functioning as potent vasoconstrictors. The endothelin family consists of three members, ENDOTHELIN-1; ENDOTHELIN-2; and ENDOTHELIN-3. All three peptides contain 21 amino acids, but vary in amino acid composition. The three peptides produce vasoconstrictor and pressor responses in various parts of the body. However, the quantitative profiles of the pharmacological activities are considerably different among the three isopeptides.

A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D1-class receptor genes lack INTRONS, and the receptors stimulate ADENYLYL CYCLASES.

Compounds containing 1,3-diazole, a five membered aromatic ring containing two nitrogen atoms separated by one of the carbons. Chemically reduced ones include IMIDAZOLINES and IMIDAZOLIDINES. Distinguish from 1,2-diazole (PYRAZOLES).

Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS.

One of the catecholamine NEUROTRANSMITTERS in the brain. It is derived from TYROSINE and is the precursor to NOREPINEPHRINE and EPINEPHRINE. Dopamine is a major transmitter in the extrapyramidal system of the brain, and important in regulating movement. A family of receptors (RECEPTORS, DOPAMINE) mediate its action.

The physiological narrowing of BLOOD VESSELS by contraction of the VASCULAR SMOOTH MUSCLE.

Peptides composed of between two and twelve amino acids.

Unstriated and unstriped muscle, one of the muscles of the internal organs, blood vessels, hair follicles, etc. Contractile elements are elongated, usually spindle-shaped cells with centrally located nuclei. Smooth muscle fibers are bound together into sheets or bundles by reticular fibers and frequently elastic nets are also abundant. (From Stedman, 25th ed)

A soluble factor produced by MONOCYTES; MACROPHAGES, and other cells which activates T-lymphocytes and potentiates their response to mitogens or antigens. Interleukin-1 is a general term refers to either of the two distinct proteins, INTERLEUKIN-1ALPHA and INTERLEUKIN-1BETA. The biological effects of IL-1 include the ability to replace macrophage requirements for T-cell activation.

A curved elevation of GRAY MATTER extending the entire length of the floor of the TEMPORAL HORN of the LATERAL VENTRICLE (see also TEMPORAL LOBE). The hippocampus proper, subiculum, and DENTATE GYRUS constitute the hippocampal formation. Sometimes authors include the ENTORHINAL CORTEX in the hippocampal formation.

Cell surface proteins that bind CALCITONIN GENE-RELATED PEPTIDE with high affinity and trigger intracellular changes which influence the behavior of cells. CGRP receptors are present in both the CENTRAL NERVOUS SYSTEM and the periphery. They are formed via the heterodimerization of the CALCITONIN RECEPTOR-LIKE PROTEIN and RECEPTOR ACTIVITY-MODIFYING PROTEIN 1.

A class of opioid receptors recognized by its pharmacological profile. Mu opioid receptors bind, in decreasing order of affinity, endorphins, dynorphins, met-enkephalin, and leu-enkephalin. They have also been shown to be molecular receptors for morphine.

Benzopyrroles with the nitrogen at the number two carbon, in contrast to INDOLES which have the nitrogen adjacent to the six-membered ring.

Cell surface proteins that bind corticotropin-releasing hormone with high affinity and trigger intracellular changes which influence the behavior of cells. The corticotropin releasing-hormone receptors on anterior pituitary cells mediate the stimulation of corticotropin release by hypothalamic corticotropin releasing factor. The physiological consequence of activating corticotropin-releasing hormone receptors on central neurons is not well understood.

Precursor of epinephrine that is secreted by the adrenal medulla and is a widespread central and autonomic neurotransmitter. Norepinephrine is the principal transmitter of most postganglionic sympathetic fibers and of the diffuse projection system in the brain arising from the locus ceruleus. It is also found in plants and is used pharmacologically as a sympathomimetic.

An angiotensin receptor subtype that is expressed at high levels in a variety of adult tissues including the CARDIOVASCULAR SYSTEM, the KIDNEY, the ENDOCRINE SYSTEM and the NERVOUS SYSTEM. Activation of the type 1 angiotensin receptor causes VASOCONSTRICTION and sodium retention.

Compounds capable of relieving pain without the loss of CONSCIOUSNESS.

Cell surface proteins that bind TACHYKININS with high affinity and trigger intracellular changes influencing the behavior of cells. Three classes of tachykinin receptors have been characterized, the NK-1; NK-2; and NK-3; which prefer, respectively, SUBSTANCE P; NEUROKININ A; and NEUROKININ B.

The physical activity of a human or an animal as a behavioral phenomenon.

The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.

A polyanionic compound with an unknown mechanism of action. It is used parenterally in the treatment of African trypanosomiasis and it has been used clinically with diethylcarbamazine to kill the adult Onchocerca. (From AMA Drug Evaluations Annual, 1992, p1643) It has also been shown to have potent antineoplastic properties.

A technique for measuring extracellular concentrations of substances in tissues, usually in vivo, by means of a small probe equipped with a semipermeable membrane. Substances may also be introduced into the extracellular space through the membrane.

Cell surface proteins that bind ANGIOTENSINS and trigger intracellular changes influencing the behavior of cells.

Cell surface receptors that bind signalling molecules released by neurons and convert these signals into intracellular changes influencing the behavior of cells. Neurotransmitter is used here in its most general sense, including not only messengers that act to regulate ion channels, but also those which act on second messenger systems and those which may act at a distance from their release sites. Included are receptors for neuromodulators, neuroregulators, neuromediators, and neurohumors, whether or not located at synapses.

A series of heterocyclic compounds that are variously substituted in nature and are known also as purine bases. They include ADENINE and GUANINE, constituents of nucleic acids, as well as many alkaloids such as CAFFEINE and THEOPHYLLINE. Uric acid is the metabolic end product of purine metabolism.

A phosphodiesterase inhibitor that blocks uptake and metabolism of adenosine by erythrocytes and vascular endothelial cells. Dipyridamole also potentiates the antiaggregating action of prostacyclin. (From AMA Drug Evaluations Annual, 1994, p752)

Drugs that bind to and activate dopamine receptors.

A class of drugs that act by selective inhibition of calcium influx through cellular membranes.

The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.

A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties.

Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding.

A class of opioid receptors recognized by its pharmacological profile. Kappa opioid receptors bind dynorphins with a higher affinity than endorphins which are themselves preferred to enkephalins.

The physiological widening of BLOOD VESSELS by relaxing the underlying VASCULAR SMOOTH MUSCLE.

The principal alkaloid in opium and the prototype opiate analgesic and narcotic. Morphine has widespread effects in the central nervous system and on smooth muscle.

Two-ring crystalline hydrocarbons isolated from coal tar. They are used as intermediates in chemical synthesis, as insect repellents, fungicides, lubricants, preservatives, and, formerly, as topical antiseptics.

The most common inhibitory neurotransmitter in the central nervous system.

A statistical technique that isolates and assesses the contributions of categorical independent variables to variation in the mean of a continuous dependent variable.

A drug that exerts an inhibitory effect on gastric secretion and reduces gastrointestinal motility. It is used clinically in the drug therapy of gastrointestinal ulcers.

1,4-Diethylene dioxides. Industrial solvents. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), dioxane itself may "reasonably be anticipated to be a carcinogen." (Merck Index, 11th ed)

A serotonin receptor subtype found widely distributed in peripheral tissues where it mediates the contractile responses of variety of tissues that contain SMOOTH MUSCLE. Selective 5-HT2A receptor antagonists include KETANSERIN. The 5-HT2A subtype is also located in BASAL GANGLIA and CEREBRAL CORTEX of the BRAIN where it mediates the effects of HALLUCINOGENS such as LSD.

A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.

A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.

A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279)

The study of the generation and behavior of electrical charges in living organisms particularly the nervous system and the effects of electricity on living organisms.

AMANTADINE derivative that has some dopaminergic effects. It has been proposed as an antiparkinson agent.

The number of times the HEART VENTRICLES contract per unit of time, usually per minute.

A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H2 receptors act via G-proteins to stimulate ADENYLYL CYCLASES. Among the many responses mediated by these receptors are gastric acid secretion, smooth muscle relaxation, inotropic and chronotropic effects on heart muscle, and inhibition of lymphocyte function. (From Biochem Soc Trans 1992 Feb;20(1):122-5)

The injection of very small amounts of fluid, often with the aid of a microscope and microsyringes.

A serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic for cancer chemotherapy patients.

Catalyze the hydrolysis of nucleosides with the elimination of ammonia.

An electrophysiologic technique for studying cells, cell membranes, and occasionally isolated organelles. All patch-clamp methods rely on a very high-resistance seal between a micropipette and a membrane; the seal is usually attained by gentle suction. The four most common variants include on-cell patch, inside-out patch, outside-out patch, and whole-cell clamp. Patch-clamp methods are commonly used to voltage clamp, that is control the voltage across the membrane and measure current flow, but current-clamp methods, in which the current is controlled and the voltage is measured, are also used.

Compounds that bind to and block the stimulation of PURINERGIC P2Y RECEPTORS. Included under this heading are antagonists for specific P2Y receptor subtypes.

Established cell cultures that have the potential to propagate indefinitely.

Contribution of adenosine to the depression of sympathetically evoked vasoconstriction induced by systemic hypoxia in the rat. (1/174)

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)

Ischaemic tolerance in aged mouse myocardium: the role of adenosine and effects of A1 adenosine receptor overexpression. (2/174)

The genesis of the ischaemia intolerant phenotype in aged myocardium is poorly understood. We tested the hypothesis that impaired adenosine-mediated protection contributes to ischaemic intolerance, and examined whether this is countered by A1 adenosine receptor (A1AR) overexpression. Responses to 20 min ischaemia and 45 min reperfusion were assessed in perfused hearts from young (2-4 months) and moderately aged (16-18 months) mice. Post-ischaemic contractility was impaired by ageing with elevated ventricular diastolic (32 +/- 2 vs. 18 +/- 2 mmHg in young) and reduced developed (37 +/- 3 vs. 83 +/- 6 mmHg in young) pressures. Lactate dehydrogenase (LDH) loss was exaggerated (27 +/- 2 vs. 16 +/- 2 IU g-1 in young) whereas the incidence of tachyarrhythmias was similar in young (15 +/- 1 %) and aged hearts (16 +/- 1 %). Functional analysis confirmed equipotent effects of 50 micro M adenosine at A1 and A2 receptors in young and aged hearts. Nonetheless, while 50 micro M adenosine improved diastolic (5 +/- 1 mmHg) and developed pressures (134 +/- 7 mmHg) and LDH loss (6 +/- 2 IU g-1) in young hearts, it did not alter these variables in the aged group. Adenosine did attenuate arrhythmogenesis for both ages (to ~10 %). In contrast to adenosine, 50 micro M diazoxide reduced ischaemic damage and arrhythmogenesis for both ages. Contractile and anti-necrotic effects of adenosine were limited by 100 micro M 5-hydroxydecanoate (5-HD) and 3 micro M chelerythrine. Anti-arrhythmic effects were limited by 5-HD but not chelerythrine. Non-selective (100 micro M 8-sulfophenyltheophylline) and A1-selective (150 nM 8-cyclopentyl-1,3-dipropylxanthine) adenosine receptor antagonism impaired ischaemic tolerance in young but not aged hearts. Quantitative real-time PCR and radioligand analysis indicated that impaired protection is unrelated to changes in A1AR mRNA transcription, or receptor density (~8 fmol mg-1 protein in both age groups). However, A1AR overexpression improved tolerance for both ages, restoring adenosine-mediated protection. These data reveal impaired protection via exogenous and endogenous adenosine contributes to ischaemic intolerance with ageing. This is independent of A1AR expression, and involves ineffective activation of a 5-HD-/diazoxide-sensitive process. The effects of A1AR overexpression indicate that the age-related failure in signalling can be overcome. (+info)

Alteration of the purinergic modulation of enteric neurotransmission in the mouse ileum during chronic intestinal inflammation. (3/174)

1. The effect of chronic intestinal inflammation on the purinergic modulation of cholinergic neurotransmission was studied in the mouse ileum. Chronic intestinal inflammation was induced by infection of mice with the parasite Schistosoma mansoni during 16 weeks. 2. S. mansoni infection induced a chronic inflammatory response in the small intestine, which was characterised by intestinal granuloma formation, increased intestinal wall thickness, blunted mucosal villi and an enhanced activity of myeloperoxidase. 3. In control ileum and in chronically inflamed ileum, electrical field stimulation (EFS) of longitudinal muscle strips induced frequency-dependent contractions that were abolished by tetrodotoxin (TTX) and atropine. Carbachol induced dose-dependent contractions that were not affected by TTX but abolished by atropine. 4. In control ileum, adenosine and ATP dose-dependently inhibited the contractions to EFS. Theophylline and 8-phenyltheophylline, P(1) and A(1) receptor antagonists respectively, prevented this inhibitory effect of adenosine and ATP. PPADS, DMPX and MRS 1220, antagonists of P(2), A(2) and A(3) receptors, respectively, did not prevent this inhibitory effect of adenosine and ATP. Adenosine and ATP did not affect the contractions to carbachol. 5. The inhibitory effect of adenosine and ATP on contractions to EFS in control ileum was mimicked by the stable adenosine analogue methyladenosine and by the A(1)-receptor agonist N(6)-cyclohexyladenosine, but not by the A3 receptor agonist 2-Cl IB-MECA or by the ATP analogues alphabeta-methylene-ATP and ADPbetaS. The inhibitory effect of adenosine on contractions to EFS was lost after prolonged (90 min) treatment of control ileum with methyladenosine (100 micro M). 6. In chronically inflamed ileum, adenosine, methyladenosine, N(6)-cyclohexyladenosine and ATP all failed to inhibit the cholinergic nerve-mediated contractions to EFS. Also theophylline, 8-phenyltheophylline, PPADS, DMPX and MRS 1220 had no effect on the contractions to EFS and carbachol. The loss of effect of adenosine and ATP was still evident after 52 weeks of infection. 7. These results indicate that in physiological conditions neuronal adenosine A(1) receptors modulate cholinergic nerve activity in the mouse ileum. However, during chronic intestinal inflammation, this purinergic modulation of cholinergic nerve activity is impaired. This suggests that chronic intestinal inflammation leads to a dysfunction of specific neuronal regulatory mechanisms in the enteric nervous system. (+info)

Diadenosine-5-phosphate exerts A1-receptor-mediated proarrhythmic effects in rabbit atrial myocardium. (4/174)

(1) Diadenosine polyphosphates have been described to be present in the myocardium and exert purinergic- and nonreceptor-mediated effects. Since the electrophysiological properties of atrial myocardium are effectively regulated by A(1) receptors, we investigated the effect of diadenosine pentaphosphate (Ap(5)A) in rabbit myocardium. (2) Parameters of supraventricular electrophysiology and atrial vulnerability were measured in Langendorff-perfused rabbit hearts. Muscarinic potassium current (I(K(ACh/Ado))) and ATP-sensitive potassium current (I(K(ATP))) were measured by using the whole-cell voltage clamp method. (3) Ap(5)A prolonged the cycle length of spontaneously beating Langendorff perfused hearts from 225+/-14 (control) to 1823+/-400 ms (Ap(5)A 50 micro M; n=6; P<0.05). This effect was paralleled by higher degree of atrio-ventricular block. Atrial effective refractory period (AERP) in control hearts was 84+/-14 ms (n=6). Ap(5)A>/=1 micro M reduced AERP (100 micro M, 58+/-11 ms; n=6). (4) Extrastimuli delivered to hearts perfused with Ap(5)A- or adenosine (>/= micro M)-induced atrial fibrillation, the incidence of which correlated to the concentration added to the perfusate. The selective A(1)-receptor antagonist CPX (20 micro M) inhibited the Ap(5)A- and adenosine-induced decrease of AERP. Atrial fibrillation was no longer observed in the presence of CPX. (5) The described Ap(5)A-induced effects in the multicellular preparation were enhanced by dipyridamole (10 micro M), which is a cellular adenosine uptake inhibitor. Dipyridamole-induced enhancement was inhibited by CPX. (6) Ap(5)A (+info)

Comparison of effects of MgCl2 and Gpp(NH)p on antagonist and agonist radioligand binding to adenosine A1 receptors. (5/174)

AIM: To investigate modulation of antagonist and agonist binding to adenosine A1 receptors by MgCl2 and 5 -guanylimidodiphosphate (Gpp(NH)p) using rat brain membranes and the A1 antagonist [3H]-8-cyclopentyl-1,3-dipropylxanthine ([3H]DPCPX) and the A1 agonist [3H]-2-chloro-N6-cyclopentyladenosine ([3H]CCPA). METHODS: Parallel saturation and inhibition studies were performed using well-characterised radioligand binding assays and a Brandel Cell Harvester. RESULTS: MgCl2 produced a concentration-dependent decrease (44%), whereas Gpp(NH)p increased [3H]DPCPX binding (19%). In [3H]DPCPX competition studies, agonist affinity was 1.5-14.6-fold higher and 4.6-10-fold lower in the presence of 10 mmol/L MgCl2 and 10 micromol/L Gpp(NH)p respectively; antagonist affinity was unaffected. The decrease in agonist affinity with increasing Gpp(NH)p concentrations was due to a reduction in the proportion of binding to the high affinity receptor state. In contrast to [3H]DPCPX, MgCl2 produced a concentration-dependent increase (72%) and Gpp(NH)p a decrease (85%) in [3H]CCPA binding. Using [3H]CCPA, agonist affinities were 5-17-fold higher than those for [3H]DPCPX, consistent with binding only to the high affinity receptor state. Agonist affinity was 1.3-10.5-fold higher and 2.4-4.7-fold lower on adding MgCl2 or Gpp(NH)p respectively; antagonist affinities were as for [3H]DPCPX. CONCLUSION: The inconsistencies surrounding the effects of MgCl2 and guanine nucleotides on radioligand binding to adenosine A1 receptors were systematically examined. The effects of MgCl2 and Gpp(NH)p on agonist binding to A1 receptors are consistent with their roles in stimulating GTP-hydrolysis at the G-protein alpha-subunit and in blocking formation of the high affinity agonist-receptor-G protein complex. (+info)

An orally active adenosine A1 receptor antagonist, FK838, increases renal excretion and maintains glomerular filtration rate in furosemide-resistant rats. (6/174)

1. Loop and thiazide diuretics are common therapeutic agents for the treatment of sodium retention and oedema. However, resistance to diuretics and decreases in renal function can develop during diuretic therapy. Adenosine causes renal vasoconstriction, sodium reabsorption, and participates in the tubuloglomerular feedback mechanism for the regulation of glomerular filtration rate. 2. We tested the hypothesis that the selective adenosine A(1) receptor antagonist FK838 is orally active and causes diuresis and natriuresis, but maintains glomerular filtration rate in normal rats or in rats with furosemide resistance. 3. In normal male Sprague - Dawley rats, FK838 dose-dependently increased urine flow and sodium and chloride excretion while sparing potassium. In combination with furosemide, FK838 enhanced the diuretic and natriuretic actions of furosemide to the same extent as hydrochlorothiazide and did not increase the potassium loss in normal rats. In furosemide-resistant rats, FK838 increased urine flow and electrolyte excretion to a greater extent than hydrochlorothiazide. In addition, hydrochlorothiazide significantly decreased glomerular filtration rate, whereas FK838 maintained glomerular filtration rate in furosemide-resistant rats. 4. This study shows that the adenosine A(1) receptor antagonist FK838 is orally active and causes potent diuresis and natriuresis and maintains glomerular filtration rate in normal or furosemide-resistant rats. Adenosine A(1) receptor antagonists may be novel therapeutics for the treatment of oedema in normal or otherwise diuretic-resistant patients. (+info)

Brief, repeated, oxygen-glucose deprivation episodes protect neurotransmission from a longer ischemic episode in the in vitro hippocampus: role of adenosine receptors. (7/174)

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)

Involvement of adenosine A1 and A2A receptors in the adenosinergic modulation of the discriminative-stimulus effects of cocaine and methamphetamine in rats. (8/174)

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)

Schwabe U, Ukena D, Lohse MJ (September 1985). "Xanthine derivatives as antagonists at A1 and A2 adenosine receptors". Naunyn- ... v t e (ECHA InfoCard ID from Wikidata, Drugboxes which contain changes to watched fields, Adenosine receptor antagonists, Diols ... It acts as an adenosine receptor antagonist and phosphodiesterase inhibitor. Xanthine "International Non-Proprietary Names. ...

https://en.wikipedia.org/wiki/Diprophylline

It is also an adenosine receptor A1 antagonist. 8-Chlorotheophylline 8-Cyclopentyltheophylline 8-Phenyltheophylline Ortiz MI, ... Adenosine receptor antagonists, Xanthines, Diuretics, All stub articles, Nervous system drug stubs). ... September 1993). "Effect of trifluoromethyl and other substituents on activity of xanthines at adenosine receptors". Journal of ...

https://en.wikipedia.org/wiki/8-Bromotheophylline

... is a drug which acts as a potent and selective antagonist for the adenosine A1 receptor. It has high selectivity for A1 over ... "Potent adenosine receptor antagonists that are selective for the A1 receptor subtype". Molecular Pharmacology. 31 (3): 247-52. ... Chwalczuk K, Rubaj A, Swiader M, Czuczwar SJ (2008). "[Influence of the antagonist of adenosine A1 receptors, 8-cyclopentyl-1 , ... a selective high affinity antagonist radioligand for A1 adenosine receptors". Naunyn-Schmiedeberg's Archives of Pharmacology. ...

https://en.wikipedia.org/wiki/Dipropylcyclopentylxanthine

... activity as antagonists of A1- and A2-adenosine receptors". Biochemical Pharmacology. 37 (4): 655-64. doi:10.1016/0006-2952(88) ... Adenosine receptor antagonists, Amines, Ethyl esters, Carboxylate esters, GABAA receptor positive allosteric modulators, ... 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 ...

https://en.wikipedia.org/wiki/Cartazolate

Popoli P, Reggio R, Pèzzola A, Fuxe K, Ferré S (July 1998). "Adenosine A1 and A2A receptor antagonists stimulate motor activity ... SCH-58261 is a drug which acts as a potent and selective antagonist for the adenosine receptor A2A, with more than 50x ... Kuzmin A, Johansson B, Gimenez L, Ogren SO, Fredholm BB (February 2006). "Combination of adenosine A1 and A2A receptor blocking ... Adenosine receptor antagonists, Experimental drugs, All stub articles, Cardiovascular system drug stubs, Nervous system drug ...

https://en.wikipedia.org/wiki/SCH-58261

Parsons WJ, Ramkumar V, Stiles GL (April 1988). "The new cardiotonic agent sulmazole is an A1 adenosine receptor antagonist and ... Sulmazole inhibits the A1 adenosine receptor and functionally blocks Gi, an inhibitory regulator. Sulmazole is also a ...

https://en.wikipedia.org/wiki/Sulmazole

... (KW-3902) is an experimental diuretic which acts as a selective adenosine A1 receptor antagonist. It was discovered ... an adenosine A1-receptor antagonist, on diuresis and renal function in patients with acute decompensated heart failure and ... dose-finding study of the adenosine A1 receptor antagonist rolofylline in patients with acute heart failure and renal ... Adenosine receptor antagonists, Diuretics, Xanthines, All stub articles, Cardiovascular system drug stubs). ...

https://en.wikipedia.org/wiki/Rolofylline

... is a drug of the xanthine chemical class which acts as a selective adenosine A1 receptor antagonist. Theophylline ... "Effects of A1 adenosine receptor blockade by bamiphylline on ischaemic preconditioning during coronary angioplasty". European ... Adenosine receptor antagonists, Enones, Primary alcohols, Xanthines, All stub articles, Respiratory system drug stubs, ...

https://en.wikipedia.org/wiki/Bamifylline

"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 ... Ki of 3.3nM at A2A and 21nM at A1. It was one of the first adenosine receptor antagonists discovered that is not a xanthine ... Holtzman SG (1991). "CGS 15943, a nonxanthine adenosine receptor antagonist: effects on locomotor activity of nontolerant and ...

https://en.wikipedia.org/wiki/CGS-15943

July 2008). "Brain adenosine A2A receptor occupancy by a novel A1/A2A receptor antagonist, ASP5854, in rhesus monkeys: ... SCH-442,416 is a highly selective adenosine A2a subtype receptor antagonist. It is widely used in its 11C radiolabelled form to ... Adenosine receptor antagonists, All stub articles, Nervous system drug stubs). ... April 2005). "In vivo imaging of adenosine A2A receptors in rat and primate brain using [11C]SCH442416". European Journal of ...

https://en.wikipedia.org/wiki/SCH-442,416

... is a drug which acts as a potent and reasonably selective antagonist for the adenosine receptors A1 and A2A. It has ... "Time and sex-dependent effects of an adenosine A2A/A1 receptor antagonist on motivation to self-administer cocaine in rats". ... Adenosine receptor antagonists, Cyclohexanols, Tertiary alcohols, All stub articles, Nervous system drug stubs). ... Choi MS, Moon SM, Lee SA, Park BR, Kim JS, Kim DK, Kim YH, Kim CS (May 2018). "Adenosine induces intrinsic apoptosis via the ...

https://en.wikipedia.org/wiki/ATL-444

It was found that an adenosine A1-receptor antagonist called KW-3902 was able to improve kidney function in CRS patients. ... Vasopressin antagonists Tolvaptan showed to have no benefit. It is also a very costly drug. Adenosine antagonists Adenosine is ... an adenosine A1-receptor antagonist,on diuresis and renal function in patients with acute decompensated heart failure and renal ... One study showes how ACE inhibitors and angiotensin II receptor antagonists have been found to prevent nephropathy in patients ...

https://en.wikipedia.org/wiki/Cardiorenal_syndrome

... an experimental diuretic which acts as a selective adenosine A1 receptor antagonist This set index page lists chemical ...

https://en.wikipedia.org/wiki/C20H28N4O2

Caffeine acts as an antagonist of adenosine A1 and A2A receptors. Adenosine is a normal neuromodulator that activates adenosine ... A1 receptors are paired with the G-proteins of Gi-1, Gi-2, Gi-3, Go1, and Go2. The g-proteins of A1 receptors continue to ... The actions of A1 and A2A receptors oppose each other but are both inhibited by caffeine due to its function as an antagonist. ... Adenosine acts on A1 receptors to decrease opening of N-type Ca2+ channels in some hippocampal neurons, and therefore decrease ...

https://en.wikipedia.org/wiki/Caffeine-induced_anxiety_disorder

... is a drug derived from the xanthine family which acts as a potent and selective antagonist for the adenosine receptors A1 and ... Adenosine receptor antagonists, Xanthines, All stub articles, Nervous system drug stubs). ... Howell LL, Morse WH, Spealman RD (September 1990). "Respiratory effects of xanthines and adenosine analogs in rhesus monkeys". ... Spealman RD (1988). "Psychomotor stimulant effects of methylxanthines in squirrel monkeys: relation to adenosine antagonism". ...

https://en.wikipedia.org/wiki/8-Phenyltheophylline

He W, Wilder T, Cronstein BN (2013). "Rolofylline, an adenosine A1 receptor antagonist, inhibits osteoclast differentiation as ... The adenosine receptors (or P1 receptors) are a class of purinergic G protein-coupled receptors with adenosine as the ... The adenosine A1 receptor has been found to be ubiquitous throughout the entire body. This receptor has an inhibitory function ... Adenosine receptors play a key role in the homeostasis of bone. The A1 receptor has been shown to stimulate osteoclast ...

https://en.wikipedia.org/wiki/Adenosine_receptor

"Time and sex-dependent effects of an adenosine A2A/A1 receptor antagonist on motivation to self-administer cocaine in rats". ... 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 ...

https://en.wikipedia.org/wiki/Adenosine_A2A_receptor

March 2002). "BG9719 (CVT-124), an A1 adenosine receptor antagonist, protects against the decline in renal function observed ... 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 ... "Adenosine Receptors: A1". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology ...

https://en.wikipedia.org/wiki/Adenosine_A1_receptor

All adenosine receptor subtypes (A1, A2A, A2B, and A3) are G-protein-coupled receptors. The four receptor subtypes are further ... have a purine structure and bind to some of the same receptors as adenosine. Methylxanthines act as competitive antagonists of ... The A1 receptors couple to Gi/o and decreases cAMP levels, while the A2 adenosine receptors couple to Gs, which stimulates ... Cellular signaling by adenosine occurs through four known adenosine receptor subtypes (A1, A2A, A2B, and A3). Extracellular ...

https://en.wikipedia.org/wiki/Adenosine

... is an antagonist of all four adenosine receptor subtypes (A1, A2A, A2B, and A3), although with varying potencies. The ... specifically the A1-D1 receptor heterodimer (this is a receptor complex with 1 adenosine A1 receptor and 1 dopamine D1 receptor ... a receptor complex composed of 1 adenosine A1 receptor and 1 adenosine A2A receptor) in the axon terminal of glutamate neurons ... Adenosine receptor antagonists, Anxiogenics, Bitter compounds, Glycine receptor antagonists, IARC Group 3 carcinogens, Mutagens ...

https://en.wikipedia.org/wiki/Caffeine

Adenosine A1-A2A receptor heteromers: new targets for caffeine in the brain. Frontiers in Bioscience. Volume 13. Pages 2391- ... Adenosine A2A receptor antagonists are a class of drugs that blocks adenosine at the adenosine A2A receptor. Notable adenosine ... adenosine receptor antagonists as potential therapeutics, antagonist for A2A-receptors, adenosine receptor ligands as anti- ... In order to achieve high affinity at adenosine receptors, certain criteria must be fulfilled. Adenosine receptor antagonists, ...

https://en.wikipedia.org/wiki/Adenosine_A2A_receptor_antagonist

May 2022). "A2B adenosine receptor antagonists rescue lymphocyte activity in adenosine-producing patient-derived cancer models ... October 2001). "Differential gene expression of adenosine A1, A2a, A2b, and A3 receptors in the human enteric nervous system". ... The adenosine A2B receptor, also known as ADORA2B, is a G-protein coupled adenosine receptor, and also denotes the human ... "The A2b adenosine receptor mediates cAMP responses to adenosine receptor agonists in human intestinal epithelia". The Journal ...

https://en.wikipedia.org/wiki/Adenosine_A2B_receptor

... is a drug which acts as a potent and selective antagonist for the adenosine receptors, with some selectivity for the A1 ... July 2003). "Involvement of adenosine A1 and A2A receptors in the motor effects of caffeine after its acute and chronic ... Adenosine receptor antagonists, Phosphodiesterase inhibitors, Xanthines, Cyclopentyl compounds, All stub articles, Nervous ... relation to adenosine antagonism". Psychopharmacology. 95 (1): 19-24. doi:10.1007/bf00212759. PMID 3133696. S2CID 11539292. ...

https://en.wikipedia.org/wiki/8-Cyclopentyl-1,3-dimethylxanthine

... is a caffeine analog which displays affinity to A2 adenosine receptors, in contrast to the A1 subtype receptors. DMPX had 28× ... Adenosine receptor antagonists, Anxiogenics, Caffeine, Designer drugs, Vasoconstrictors, Propargyl compounds). ... a potent and selective in vivo antagonist of adenosine analogs". Life Sciences. 43 (21): 1671-84. doi:10.1016/0024-3205(88) ...

https://en.wikipedia.org/wiki/DMPX

... and adenosine A1 receptors. PPADS tetrasodium salt, Santa Cruz Biotechnology Ziganshin, AU (December 1993). "PPADS selectively ... PPADS (pyridoxalphosphate-6-azophenyl-2',4'-disulfonic acid) is a selective purinergic P2X antagonist. It is able to block ... It appears to be relatively selective for P2X receptors, having no appreciable activity at α1 adrenergic, muscarinic M2 and M3 ... Lambrecht, G. (1992). "PPADS, a novel functionally selective antagonist of P2 purinoreceptor mediated responses". European ...

https://en.wikipedia.org/wiki/PPADS

The anti-nociceptive effect of acupuncture may be mediated by the adenosine A1 receptor. A 2014 review in Nature Reviews Cancer ... and that it is possible to inhibit acupuncture's analgesic effects with the opioid antagonist naloxone. Mechanical deformation ... which then triggered nearby A1 receptors. The review found that in those studies, because acupuncture "caused more tissue ... such studies unnecessarily muddled a finding that local inflammation can result in the local release of adenosine with ...

https://en.wikipedia.org/wiki/Acupuncture

GABAA receptor positive allosteric modulators, Adenosine receptor antagonists). ... as an adenosine antagonist of the A1 and A2 subtypes, and as a phosphodiesterase inhibitor selective for the PDE4 isoform. It ... 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 ...

https://en.wikipedia.org/wiki/Etazolate

... histamine H3 receptor, μ opioid receptor, NMDA receptor, and adenosine A1 receptor. D1-D2 receptor complex D1−H3−NMDAR receptor ... No other D1 receptor antagonists have been approved for clinical use. Ecopipam is a selective D1-like receptor antagonist that ... Many typical and atypical antipsychotics are D1 receptor antagonists in addition to D2 receptor antagonists. ... The D1 receptor forms heteromers with the following receptors: dopamine D2 receptor, dopamine D3 receptor, ...

https://en.wikipedia.org/wiki/Dopamine_receptor_D1

... adenosine receptor antagonist, on the negative inotropic action of A(1) adenosine receptor full agonists in isolated guinea pig ... Dhalla AK, Shryock JC, Shreeniwas R, Belardinelli L (2003). "Pharmacology and therapeutic applications of A1 adenosine receptor ... Hormone receptors Neuromodulator receptors Neurotransmitter receptors General anesthetics were once thought to work by ... Upon drug binding, receptors can elicit their normal action (agonist), blocked action (antagonist), or even action opposite to ...

https://en.wikipedia.org/wiki/Pharmacodynamics

... leading to an accumulation of adenosine. On the other hand, the adenosine-receptor antagonist caffeine reverses the anti- ... The other three adenosine receptors are involved in bone formation. In Alzheimer's disease (AD), the expression of A1 and A2A ... In the airways of patients with asthma, the expression of adenosine receptors is upregulated. Adenosine receptors affect ... the expression of adenosine receptors on the neutrophil, and the affinity of these receptors for adenosine. Micromolar ...

https://en.wikipedia.org/wiki/Purinergic_signalling

Receptor. (ligands). P0 (adenine). *Agonists: 8-Aminoadenine. *Adenine. P1. (adenosine). *Agonists: 2-(1-Hexynyl)-N- ... Antagonists: 8-Chlorotheophylline. *8-Phenyl-1,3-dipropylxanthine. *8-Phenyltheophylline. *Acefylline. *Aminophylline ...

https://ml.wikipedia.org/wiki/അഡിനോസിൻ_ഡൈഫോസ്ഫേറ്റ്

Adenosine A1 receptor (en) , Adenosine A2a receptor (en) , Adenosine A2b receptor (en) , Adenosine A2b receptor (en) eta ... hodi-zabaltzaile, Bronkozabaltzaile eta purinergic P1 receptor antagonists (en) Identifikatzaileak. InChlKey. ZFXYFBGIUFBOJW- ...

https://eu.m.wikipedia.org/wiki/Teofilina

... the A1 adenosine receptor, the D2 receptor,[19] the P2 receptor,[20][21] and ryanodine receptors.[22] ... "Synthesis and Structure-Activity Relationships of Suramin-Derived P2Y11 Receptor Antagonists with Nanomolar Potency". J. Med. ... relationships of analogues of NF449 confirm NF449 as the most potent and selective known P2X1 receptor antagonist". Eur. J. Med ... Current status of the nomenclature and properties of P2X receptors and their subunits". Pharmacological Reviews. 53 (1): 107- ...

https://en.wikipedia.org/wiki/Suramin

Adenosine reuptake inhibitor (AdoRI). *Angiotensin II receptor antagonist. *Endothelin receptor antagonist. *NK1 receptor ... GLUA1, GluR1, GluRA, GluR-A, GluR-K1, HBGR1. GLUA2, GluR2, GluRB, GluR-B, GluR-K2, HBGR2. GLUA3, GluR3, GluRC, GluR-C, GluR-K3 ... The α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (also known as AMPA receptor, or quisqualate receptor) is a ... The N-methyl-D-aspartate receptor (NMDA receptor) - a type of ionotropic glutamate receptor - is a ligand-gated ion channel ...

https://en.wikipedia.org/wiki/Ligand-gated_ion_channel

Adenosine modulates the preBötC output via activation of the A1 and A2A receptor subtypes. An adenosine A1 receptor agonist has ... most being selective agonists or antagonists to receptor subtypes on neurons in the vicinity. Since many of these neurons ... Effects of adenosine A1 receptor activation". BMC Neuroscience. 9: 95. doi:10.1186/1471-2202-9-95. PMC 2567986. PMID 18826652. ... Another synthetic drug specific to the adenosine A2A receptor subtype is CGS-21680 that has been shown to cause apneas in 14- ...

https://en.wikipedia.org/wiki/Pre-Bötzinger_complex

... is a drug which acts as a selective antagonist for the adenosine A3 receptor (ki value at human A3 receptor is 0.44 nM ... with high selectivity over the other three adenosine receptor subtypes (ki values at human A1, A2A and A2B receptors are 4.1, ... a novel high-affinity antagonist radioligand for human A(3) adenosine receptors". Bioorg Med Chem Lett. 12 (3): 501-3. doi: ... "Adenosine receptor subtype-selective antagonists in inflammation and hyperalgesia". Naunyn-Schmiedeberg's Archives of ...

https://en.wikipedia.org/wiki/PSB-10

IGF1R Interleukin 1 receptor antagonist deficiency; 612852; IL1RN Interleukin-2 receptor, alpha chain, deficiency of; 606367; ... SIX1 Brachydactyly type A1; 112500; BDA1B Brachydactyly type A1; 112500; IHH Brachydactyly type A2; 112600; BMPR1B ... APC Adenosine deaminase deficiency, partial; 102700; ADA Adenosine triphosphate, elevated, of erythrocytes; 102900; PKLR ... types A1 and B; 174200; GLI3 Polydactyly, preaxial type II; 174500; LMBR1 Polydactyly, preaxial, type IV; 174700; GLI3 ...

https://en.wikipedia.org/wiki/List_of_OMIM_disorder_codes

Caffeine's primary mechanism of action is as an adenosine receptor antagonist in the brain. Ethanol is an adenosine reuptake ... 2010, final ed.: A1. Johnson, Jenna and Kevin Sieff. "Four Loko Ban Fuels Buying Binge." Washington Post 18 Nov. 2010, final ed ... Allen-Gipson DS, Jarrell JC, Bailey KL, Robinson JE, Kharbanda KK, Sisson JH, Wyatt TA (May 2009). "Ethanol blocks adenosine ...

https://en.wikipedia.org/wiki/Caffeinated_alcoholic_drink

... they also express adenosine A1 receptors), while dynorphinergic MSNs connect the striatum with the substantia nigra (pars ... GABA: A recent study on rats that used GABA agonists and antagonists indicated that GABAA receptors in the NAcc shell have ... and express the peptides dynorphin and substance P and dopamine D1 and adenosine A1 but not A2A receptors ... These two ... It has been demonstrated that D1 receptors form the hetero-oligomer with D2 receptors, and that the D1-D2 receptor hetero- ...

https://en.wikipedia.org/wiki/Nucleus_accumbens

Björklund O, Shang M, Tonazzini I, Daré E, Fredholm BB (2008). "Adenosine A1 and A3 receptors protect astrocytes from hypoxic ... H2-receptor antagonists, like cimetidine (Tagamet), inhibit the signaling pathway that leads to activation of the ATPase. This ... eCollection 2015 Gessi S, Merighi S, Stefanelli A, Fazzi D, Varani K, Borea PA (2013). "A(1) and A(3) adenosine receptors ... Memory has been associated with astrocytes and the alpha3 subunit of adenosine receptor found in hydrogen/Sodium-potassium ...

https://en.wikipedia.org/wiki/Hydrogen_potassium_ATPase

... adenosine receptor binding affinity (21 μM for A1, 32 μM for A2A, 4.5 μM for A2B, and >100 for μM for A3) is ... Müller, Christa E.; Jacobson, Kenneth A. (2011), Fredholm, Bertil B. (ed.), "Xanthines as Adenosine Receptor Antagonists", ... "Adenosine receptors: development of selective agonists and antagonists". Progress in Clinical and Biological Research. 230 (1 ... Adenosine receptor antagonists, Animal metabolites, Phosphodiesterase inhibitors, Stimulants, Xanthines). ...

https://en.wikipedia.org/wiki/Paraxanthine

... consist of Isoreceptors D1-D2 D1-D3 D2-D3 D2-D4 D2-D5 Non-isoreceptors D1-adenosine A1 D2-adenosine A2A D2-ghrelin receptor ... Thus, dopamine receptors are common neurologic drug targets; antipsychotics are often dopamine receptor antagonists while ... "Role of iso-receptors in receptor-receptor interactions with a focus on dopamine iso-receptor complexes". Rev Neurosci. 27 (1 ... The D1 and D5 receptors are members of the D1-like family of dopamine receptors, whereas the D2, D3 and D4 receptors are ...

https://en.wikipedia.org/wiki/Dopamine_receptor

April 2011). "Structure of an agonist-bound human A2A adenosine receptor". Science. 332 (6027): 322-7. Bibcode:2011Sci...332.. ... The very large rhodopsin A group has been further subdivided into 19 subgroups (A1-A19). According to the classical A-F system ... and neutral antagonists are ligands that do not affect the equilibrium. It is not yet known how exactly the active and inactive ... transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, and G protein-linked receptors ( ...

https://en.wikipedia.org/wiki/G_protein-coupled_receptor

Reversal of Tau Pathology by an Adenosine A1 Receptor Antagonist. 2018, 2020 ... However, there are exceptions: One is the discovery that certain drugs that bind to a class of adenosine receptors on neurons ( ...

https://curealz.org/research/translational/studies-of-tau/reversal-of-tau-pathology-by-an-adenosine-a1-receptor-antagonist/

Rolofylline, an adenosine A1-receptor antagonist, in acute heart failure. N Engl J Med. 2010 Oct 7. 363(15):1419-28. [QxMD ... The angiotensin receptor neprilysin inhibitor LCZ696 in heart failure with preserved ejection fraction: a phase 2 double-blind ... Effects of beta-adrenergic antagonists in patients with chronic kidney disease: a systematic review and meta-analysis. J Am ... Effects of beta-adrenergic antagonists in patients with chronic kidney disease: a systematic review and meta-analysis. J Am ...

https://www.medscape.com/answers/163062-86251/what-is-the-role-of-serum-electrolyte-values-in-the-diagnosis-of-heart-failure

Time and sex-dependent effects of an adenosine A2A/A1 receptor antagonist on motivation to self-administer cocaine in rats. ... Time and sex-dependent effects of an adenosine A2A/A1 receptor antagonist on motivation to self-administer cocaine in rats. In ... Time and sex-dependent effects of an adenosine A2A/A1 receptor antagonist on motivation to self-administer cocaine in rats. / ... Dive into the research topics of Time and sex-dependent effects of an adenosine A2A/A1 receptor antagonist on motivation to ...

https://scholars.okstate.edu/en/publications/time-and-sex-dependent-effects-of-an-adenosine-a2aa1-receptor-ant

2000) Effects of A1 and A2 adenosine receptor antagonists on the induction and reversal of long-term potentiation in guinea pig ... 1995) Modeling of the pharmacodynamic interaction of an A1 adenosine receptor agonist and antagonist in vivo: N6- ... 1987) 8-Cyclopentyl-1,3-dipropylxanthine (DPCPX)-a selective high affinity antagonist radioligand for A1 adenosine receptors. ... 1997) 8-Cyclopentyltheophylline, an adenosine A1 receptor antagonist, inhibits the reversal of long-term potentiation in ...

https://www.jneurosci.org/content/28/38/9557?ijkey=1f83ebac703def3b2b66023eb84ec9d1e8494726&keytype2=tf_ipsecsha

Reasonably selective antagonists are available for some adenosine receptor subtypes. The receptors for adenine nucleotides, ... Current evidence indicates the existence of four receptors for adenosine: A1, A2A, A2B, and A3. These G protein-coupled ... P2Y-receptor activation stimulates signaling mediated via phospholipase C. There is a paucity of specific antagonists for P2X- ... Despite its structure, uridine triphosphate (UTP) is a potent ligand at several P2Y-receptors. Responses to P2X-receptor ...

http://www2a.cdc.gov/nioshtic-2/BuildQyr.asp?s1=asthma+OR+%27allerg%2A%27+OR+%27immune%2A%27&f1=%2A&Startyear=&Adv=0&terms=1&EndYear=&Limit=10000&sort=&D1=10&PageNo=305&RecNo=3046&View=f&

Rolofylline, an adenosine A1-receptor antagonist, in acute heart failure. N Engl J Med 2010;363:1419-28. The authors apologize ... Rolofylline, an adenosine A1-receptor antagonist, in acute heart failure. N Engl J Med 2010;363:1419-28. The authors apologize ... Rolofylline, an adenosine A1-receptor antagonist, in acute heart failure. N Engl J Med 2010;363:1419-28. The authors apologize ... Rolofylline, an adenosine A1-receptor antagonist, in acute heart failure. N Engl J Med 2010;363:1419-28. The authors apologize ...

https://experts.umn.edu/en/publications/erratum-corrigendum-to-clinical-effectiveness-of-tolvaptan-in-pat

... and the novel adenosine A1 receptor antagonist, SLV320, in experimental models of hypertension and chronic renal failure. The ... The A1 receptor antagonist SLV320 significantly decreased cardiac fibrosis and albuminuria in rats with 5/6 NX. These ... and the adenosin A1 receptor antagonist SLV 320 play important roles in cardio-renal protection in experimental models of ... und der Antagonist des A1 Rezeptors, SLV320, wichtige Rollen in der Kardio- und Nephroprotektion bei experimenteller ...

https://refubium.fu-berlin.de/handle/fub188/9369?locale-attribute=de

A1, A2A, A3, and A2B and, as does adenosine, exerts effects on neurons and glial cells of all brain areas. In consequence, ... caffeine, when acting as an AR antagonist, is doing the opposite of activ … ... Caffeine causes most of its biological effects via antagonizing all types of adenosine receptors (ARs): ... Caffeine causes most of its biological effects via antagonizing all types of adenosine receptors (ARs): A1, A2A, A3, and A2B ...

https://pubmed.ncbi.nlm.nih.gov/20164566/

2-Aryladenine derivatives as a potent scaffold for A1, A3 and dual A1/A3 adenosine receptor antagonists: Synthesis and ...

https://repositorium.sdum.uminho.pt/browse?type=type&value=article

6-diphenylpyrimidines was evaluated as potential dual adenosine A1 and A2A receptor antagonists. The majority of the ... Carbamate substituted 2-amino-4,6-diphenylpyrimidines as adenosine receptor antagonists Robinson, Sarel J.; Petzer, Jacobus P ... Browsing by Subject "Adenosine A1 and A2A receptor". 0-9. A. B. C. D. E. F. G. H. I. J. K. L. M. N. O. P. Q. R. S. T. U. V. W. ...

https://repository.nwu.ac.za/browse?type=subject&value=Adenosine+A1+and+A2A+receptor

Adentri(TM), an A1-adenosine receptor antagonist for the potential treatment of acute and chronic congestive heart failure, is ... Tecadenoson, an A1-adenosine receptor agonist, is being developed for the potential reduction of rapid heart rate during atrial ... CVT-3146, a selective A2A-adenosine receptor agonist, is being developed for potential use as a pharmacologic stress agent in ... approach to develop novel opioid analgesics based upon a new molecular understanding of the function of opioid receptors. ...

https://salesandmarketingnetwork.com/links_bs.html?alpha=A&keyword=Pharma

... lack of effect of adenosine A1 and A2 receptor antagonists. European Journal of Pharmacology. 334: 95-8. PMID 9346333 DOI: ... Relaxation of mouse isolated aorta to adenosine and its analogues does not involve adenosine A1, A2 or A3 receptors European ... Characterization of adenosine receptors mediating the vasodilator effects of adenosine receptor agonists in the ... Post-junctional excitatory adenosine A1 receptors in the rat vas deferens. General Pharmacology. 25: 417-20. PMID 7926584 DOI: ...

https://neurotree.org/neurotree/publications.php?pid=52164

Adenosine A1 Receptor Antagonists - Preferred Concept UI. M0545363. Scope note. Compounds that bind to and block the ... Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.. ... Adenosine A1 Receptor Antagonists [D27.505.519.625.725.400.100.100] Adenosine A1 Receptor Antagonists ... Adenosine A1 Receptor Antagonists [D27.505.696.577.725.400.100.100] Adenosine A1 Receptor Antagonists ...

https://decs.bvsalud.org/en/ths/resource/?id=54164

Effects of the adenosine A1 receptor antagonist rolofylline on renal function in patients with acute heart failure and renal ... placebo-controlled randomized study of the selective adenosine A1 receptor antagonist rolofylline for patients hospitalized ... Adenosine blockers: The adenosine receptor blocker rolofylline was shown in small studies to enhance diuresis and protect renal ... Vasopressin antagonists: Tolvaptan is an oral, selective vasopressin V2-receptor antagonist that acts upon the distal nephron ...

https://file.scirp.org/Html/6-1910139_29039.htm

Adenosine A1 receptor antagonist improves intradialytic hypotension. Kidney Int. 2006;69(5):877-83. Shimizu K et al. Effect of ... Adenosine A1 receptor antagonist, FK352, was associated with improved rates of IDH, similar to anti-diuretic hormone (ADH) that ... Low-dose dopamine acting on the D-1 and D-2 like receptors induces sodium and water excretion, increases renal perfusion and ... Midodrine, an α-1 adrenergic receptor agonist prodrug, given predialysis, improved IDH and increased nadir systolic BP, but had ...

https://www.emjreviews.com/nephrology/article/low-dose-dopamine-in-the-management-of-intradialysis-hypotension-a-retrospective-cohort-study-in-nigeria-j120121/

Interactions Between Adenosine Receptors and Cordycepin (3- Deoxyadenosine) from Cordyceps Militaris: Possible Pharmacological ... regulated the mRNA expression of the A1, A2A, A2B, and A3 adenosine receptors, and that antagonists of A1, A2A, and A3 ... The family of adenosine receptors includes four members: adenosine receptors A1, A2A, A2B, and A3 [7]. Adenosine is a ... Of the four adenosine receptors, the A1 receptor and A2A receptor are both highly expressed throughout the brain, and their ...

https://www.fortunejournals.com/articles/interactions-between-adenosine-receptors-and-cordycepin-339-deoxyadenosine-from-cordyceps-militaris-possible-pharmacological-mecha.html

https://www.staging.medscape.com/answers/163062-86239/what-are-the-clinical-characteristics-of-accaha-stage-d-heart-failure

... CATARZI D.; ... and at cloned human A1 and A3 adenosine receptors. The rationally designed 8-chloro-2-(4-methoxy-phenyl)-1,2,4-triazolo[1,5-a] ... and at cloned human A1 and A3 adenosine receptors. The rationally designed 8-chloro-2-(4-methoxy-phenyl)-1,2,4-triazolo[1,5-a] ... Structure-activity relationships have been explained analyzing the three-dimensional structure of the antagonist-receptor ...

https://arpi.unipi.it/handle/11568/203272

View 4 Non-selective Adenosine Receptor Antagonists Small Molecules and Peptides. Bio-Techne offers high-quality reagents, ... Non-selective Adenosine Receptor Antagonists: Small Molecules and Peptides. 4 results for Non-selective Adenosine Receptor ... Non-selective Adenosine Receptor Antagonists: Small Molecules and Peptides. 4 results for Non-selective Adenosine Receptor ... A1 and A2B antagonist. CNS stimulant. Chemical Name :. 3,7-Dihydro-1,3,7-trimethyl-1H-purine-2,6-dione. ...

https://www.bio-techne.com/t/non-selective-adenosine-receptor-antagonists/small-molecules-peptides

Development and Application of Subtype-Selective Fluorescent Antagonists for the Study of the Human Adenosine A1 Receptor in ... Structure, Dynamics, Receptor Binding, and Antibody Binding of the Fully Glycosylated Full-Length SARS-CoV-2 Spike Protein in a ... 2-Phenyl-1H-pyrrole-3-carboxamide as a New Scaffold for Developing 5-HT6 Receptor Inverse Agonists with Cognition-Enhancing ...

https://axial.acs.org/2021/04/30/browse-the-most-read-articles-of-march-2021/

... nonselective adenosine receptor antagonist, CGS 15943, but not by the selective adenosine A1 receptor antagonist DPCPX (Griebel ... It has also been shown that the selective adenosine A2A receptor antagonist SCH 58261 is at least as potent as the A1 receptor ... In addition to these presynaptically located adenosine A1 receptors, A1 receptors are also present in the substantia nigra and ... Adenosine A1 receptors (in contrast to adenosine A2A receptors) have been shown to influence dopamine release in slices of the ...

https://www.biologyonline.com/articles/actions-caffeine-brain-special

METHODS: In the first trial, various doses of adenosine (an endogenous P1 receptor agonist), and its synthetic antagonist CGS- ... RESULTS: Adenosine did not affect food or fat intake. Food consumption was increased 30 min after injection of CGS-15943. CGS- ... BACKGROUND: Adenosine has many physiological roles in the brain, and in rodents, it changes food intake when applied centrally ... OBJECTIVES: We investigated the effect of central injection of the purine molecule adenosine on both food and fat intakes in ...

https://journals.ut.ac.ir/article_82775.html

It does so by obstructing the adenosine A1 receptors that channel alcoholic effects such as atactic and sleepy behaviors. On ... Caffeine is a non-selective competitive adenosine receptor antagonist, and it releases its psycho-stimulant effects by ... Caffeine is a non-selective adenosine receptor antagonist. During excessive alcohol intake, caffeine counteracts the adverse ... of the alcohol basically by inbiting the production of Adenosine A1 and also the inbition of the adenosine A2A receptors wch ...

https://cheapessaywritingservices.org/there-is-a-perception-that-has-spread-widely-where-people-believe-that-caffeine-antagonizes-the-stimulating-alcohol-effects-both-alcohol-and-caffeine-have-intoxicating-effects/

Adenosine can activate four subtypes of adenosine receptors (A1, A2A, A2B and A3) and has been implicated in diabetic ... The agonist of adenosine receptors ameliorates renal fibrosis, probably via A2A receptors, while the antagonist exacerbates it ... treatment of SHR-STZ rats with a xanthinic antagonist of adenosine receptors decreases adenosine A3 immunoreactivity in SG, PCT ... There is no difference in the immunoreactivity against the adenosine A1 and A2B receptors between the experimental groups. ...

https://pesquisa.bvsalud.org/portal/?lang=pt&q=au:Albino-Teixeira,+Ant%C3%B3nio

Caffeine is an alkaloid, a secondary plant metabolite, that is an antagonist of adenosine receptors: A1 and A2. Caffeine is a ... This said caffeine blocks the effect of adenosine - a neurotransmitter that relaxes the brain and makes you tired as the day ...

https://thewholeportion.com/how-much-caffeine-is-in-a-teabag/

... but not the A1 adenosine receptor agonist, N6-phenyl adenosine (N6-phenyl ADO, 10 microM) markedly increased 125I efflux rate ( ... we show that the new organic antagonist of receptor-mediated Ca2+ entry, SK&F 96365, inhibits the T cell Ca2+ current in a dose ... 2-chloro-adenosine (2-Cl-ADO) > R-phenylisopropyl adenosine (R-PIA). 4. The known potent A2 adenosine receptor (A2AR) agonist, ... Ligation of the extracellular domains of the T-cell receptor activates receptor-associated tyrosine kinases that can ...

https://profiles.stanford.edu/phyllis-gardner

... an adenosine A1-receptor antagonist, but not 3,7-dimethyl-l-propargylxanthine (DMPX 1 mg/kg, ip), an adenosine A2A-receptor ... Protective effect of adenosine in diabetic neuropathic pain is mediated through adenosine A1-receptors. ... Protective effect of adenosine in diabetic neuropathic pain is mediated through adenosine A1-receptors. Indian Journal of ... and the protection produced by adenosine is via stimulation of adenosine A1-receptors. ...

https://imsear.searo.who.int/handle/123456789/145872

The specific A1 adenosine receptor antagonist CPT significantly delayed the suppression of turtle ERG, while the hypoxic shark ... ERG was unaffected by the non-specific adenosine receptor antagonist aminophylline, suggesting adenosinergic involvement in ...

https://research-repository.griffith.edu.au/handle/10072/22112

5-HT through adenosine A1 receptor activity.. AB - The effects of adenosine, adenosine A1 receptor antagonist (DPCPX), or NMDA ... N2 - The effects of adenosine, adenosine A1 receptor antagonist (DPCPX), or NMDA receptor antagonist (APV) on the spontaneous ... abstract = "The effects of adenosine, adenosine A1 receptor antagonist (DPCPX), or NMDA receptor antagonist (APV) on the ... The effects of adenosine, adenosine A1 receptor antagonist (DPCPX), or NMDA receptor antagonist (APV) on the spontaneous ...

https://pure.ewha.ac.kr/en/publications/effect-of-adenosine-on-the-release-of-sup3suph-5-hydroxytryptamin

Ketamine decreases neuronally released glutamate via retrograde stimulation of presynaptic adenosine A1 receptors. Mol. ... receptor antagonist11. However, while some other NMDA receptor antagonists produce rapid antidepressant effects12,13,14, many ... Glutamate N-methyl-D-aspartate receptor antagonists rapidly reverse behavioral and synaptic deficits caused by chronic stress ... Neurogenesis-independent antidepressant-like effects on behavior and stress axis response of a dual orexin receptor antagonist ...

https://www.nature.com/articles/s41467-022-30386-5?trigger_link=dBgLD4ac9MBBrGcEVf3t&error=cookies_not_supported&code=6a8733bf-85e3-4226-94c9-073f7da2cb88

P2Y-receptor activation stimulates signaling mediated via phospholipase C. There is a paucity of specific antagonists for P2X- and P2Y-receptors, and their characteristics have been defined through the use of relative agonist potencies. (cdc.gov)
Here, we summarized the pharmacological basis of adenosine, adenosine receptors, adenosine agonist cordycepin (3'-deoxyadenosine), and Cordyceps product in the brain protection and amelioration of pneumonia to provide useful information to cope with the global pandemic of novel coronavirus (COVID-19). (fortunejournals.com)
Cordyceps and cordycepin products could be used as a potential medicinal adenosine receptor agonist that can play a beneficial role in the amelioration of Covid-19 pneumonia and protection of brain. (fortunejournals.com)
In the first trial, various doses of adenosine (an endogenous P1 receptor agonist), and its synthetic antagonist CGS-15943, were injected intracerebroventricularly (ICV) to the chicks and the cumulative food intake was measured at definite time intervals. (ac.ir)
A1 receptor involvement was assessed using caffeine agonist (CPA) and antagonist (DPCPX). (edu.br)
Both caffeine groups did not show analgesic response induced by CPA when compared to the control group at P14, indicating chronic exposure to caffeine in the aforementioned periods inhibits the antinociceptive effects of the systemic A1 receptor agonist administration. (edu.br)
Functionalized congeners, when a chemically functionalized string is usually integrated at an insensitive site on the pharmacophore, have already been designed from your agonist and antagonist ligands of varied G proteinCcoupled receptors (GPCRs). (thetechnoant.info)

This was mimicked by the selective adenosine A1 receptor antagonist cyclopentyltheophylline. (biologyonline.com)

Caffeine causes most of its biological effects via antagonizing all types of adenosine receptors (ARs): A1, A2A, A3, and A2B and, as does adenosine, exerts effects on neurons and glial cells of all brain areas. (nih.gov)
In consequence, caffeine, when acting as an AR antagonist, is doing the opposite of activation of adenosine receptors due to removal of endogenous adenosinergic tonus. (nih.gov)
Having discussed the molecular and neuronal actions of caffeine, especially as they relate to a primary effect on adenosine receptors, it is important to consider some actions at a more integrated level. (biologyonline.com)
Even though the primary action of caffeine may be to block adenosine receptors this leads to very important secondary effects on many classes of neurotransmitters, including noradrenaline, dopamine, serotonin, acetylcholine, glutamate, and GABA (Daly, 1993). (biologyonline.com)
The interaction between adenosine A2A and dopamine D2 receptors highlighted above could provide a mechanism for several actions of caffeine and some of its metabolites on dopaminergic activity. (biologyonline.com)
Thus, an inhibition of A2A receptors by caffeine would be expected to increase transmission via dopamine at D2 receptors (Ferré et al. (biologyonline.com)
This was interpreted as evidence that caffeine increased the release of DA, which in turn acted on DA receptors to depress firing of the neurons. (biologyonline.com)
Both alcohol and caffeine have intoxicating effects on the adenosine neurotransmission. (cheapessaywritingservices.org)
Caffeine is a non-selective adenosine receptor antagonist. (cheapessaywritingservices.org)
On the other hand, the caffeine arousal effects may be counteracted by the alcohol where it induces production of more Adenosine. (cheapessaywritingservices.org)
The caffeine may be used to treat the withdrawal effects of the alcohol basically by inbiting the production of Adenosine A1 and also the inbition of the adenosine A2A receptors wch contribute to the increasing effects of alcohol. (cheapessaywritingservices.org)
Caffeine is a non-selective competitive adenosine receptor antagonist, and it releases its psycho-stimulant effects by antagonizing the tonic effects of endogenous adenosine on central receptors. (cheapessaywritingservices.org)
The reinforcing effect of the caffeine originates from striatal A1 and A2A receptors. (cheapessaywritingservices.org)
Caffeine is an alkaloid, a secondary plant metabolite, that is an antagonist of adenosine receptors: A1 and A2. (thewholeportion.com)
This said caffeine blocks the effect of adenosine - a neurotransmitter that relaxes the brain and makes you tired as the day goes by making you want to sleep. (thewholeportion.com)
2018). Caffeine is an adenosine receptor antagonist and blocks the detection of pain by blocking adenosine receptors and inhibiting phosphodiesterases (Mantegazza et al. (katedaugherty.com)
2012), the mechanism of caffeine-withdrawal headache is believed to be an "increased functional sensitivity to endogenous adenosine via the upregulation of adenosine receptors. (katedaugherty.com)
Objectives Caffeine is extensively consumed as a psychostimulant drug, acting on A1 and A2A adenosine receptors blockade. (edu.br)
Our goal was to evaluate the effect of chronic caffeine exposure during gestation and breast-feeding in the functionality of adenosine A1 receptors in infant rats at P14. (edu.br)
Conclusions Our results demonstrate that chronic caffeine exposure in gestational and breastfeeding alters A1-mediated analgesic response in rats. (edu.br)
This work, entitled effects of adenosine 2 antagonists, quercetin and caffeine on the alert and vigor, was developed in California in the base 57 patients, who provided moderate (200 mg) doses of caffeine to check its response in different cognitive aspects, such as intellectual performance, reaction and response to fatigue. (huntersmith.com)
Effect neuroprotective mechanism of action of caffeine is the blockade of adenosine receptors type A1 and A2A. (huntersmith.com)

Through the activation of adenosine receptors A1, A2A, A2B and A3, adenosine plays an important role in protecting against acute lung injury and brain injury. (fortunejournals.com)

Despite its structure, uridine triphosphate (UTP) is a potent ligand at several P2Y-receptors. (cdc.gov)
The rationally designed 8-chloro-2-(4-methoxy-phenyl)-1,2,4-triazolo[1,5-a]quinoxalin-4-acetylamine (14) can be considered one of the most potent and hA3 versus hA1 selective AR antagonists reported till now. (unipi.it)
The 1,2,4-Triazolo[4,3-a]pyrazin-3-one as a Versatile Scaffold for the Design of Potent Adenosine Human Receptor Antagonists. (unifi.it)
The 1,2,4-Triazolo[4,3-a]quinoxalin-1-one Moiety as an Attractive Scaffold to Develop New Potent and Selective Human A3 Adenosine Receptor Antagonists: Synthesis, Pharmacological and Ligand-Receptor Modeling Studies. (unifi.it)
1,2,4-Triazolo[4,3-a]quinoxalin-1-one: a versatile tool for the synthesis of potent and selective adenosine receptor antagonists. (unifi.it)
2- Arylpyrazolo[3,4.c]quinolin-4-acylamines as potent and selective human A3 adenosine receptor antagonists. (unifi.it)
2-Arylpyrazolo[4,3-d]pyrimidin-7-amino Derivatives As New Potent and Selective Human A3Adenosine Receptor Antagonists. (unifi.it)

This depotentiation does not require NMDA receptors, group I metabotropic glutamate receptors, or L-type calcium channels, but involves adenosine acting at A 1 receptors. (jneurosci.org)
The effects of adenosine, adenosine A 1 receptor antagonist (DPCPX), or NMDA receptor antagonist (APV) on the spontaneous release of [ 3 H]-5- hydroxytryptamine ([ 3 H]-5-HT) during normoxic/normoglycemic or hypoxic/hypoglycemic period were studied in the rat hippocampal slices. (ewha.ac.kr)
Ketamine is a non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist 11 . (nature.com)
The standard medical treatment for AD includes cholinesterase inhibitors (ChEIs) and a partial N-methyl-D-aspartate (NMDA) antagonist. (medscape.com)

The action of theophylline, a known lipolytic agent (exerting its effects through antagonism of adenosine A1 receptor as well as PDE inhibition) was not potentiated by either fisetin or quercetin. (ironmagazine.com)
It only displays an inhibitory action against PDE2A1 and antagonism at adenosine A(2A) at high concentrations 7 . (drugbank.com)
Increased cardiac sympathetic drive and reduced vagal modulation following endothelin receptor antagonism in healthy conscious rats. (shengsci.com)

The focus of my PhD was the rational (structure-based) design, development and application of novel subtype-selective fluorescent probes to improve the understanding of the molecular pharmacology of the adenosine A1 and A2A receptors in living cells. (nottingham.ac.uk)

Our results reveal that adenosine receptor blockade may mediate both acute increases in the reinforcing effects of cocaine, and longer term inhibitory effects on cocaine reinforcement that differ according to sex. (okstate.edu)
The blockade of adenosine receptors produces increases moderated in the transmission of noradrenergic, dopaminergic, serotonergic and cholinergic neurotransmission systems. (huntersmith.com)
Role of non-selective adenosine receptor blockade and phosphodiesterase inhibition in cisplatin-induced nephrogonadal toxicity in rats. (shengsci.com)
1. The present study evaluated changes in autonomic control of the cardiovascular system in conscious rats following blockade of endothelin (ET) receptors with bosentan. (shengsci.com)

Responses to P2X-receptor stimulation result from activation of nonselective cation channels in the cell membrane. (cdc.gov)
Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS. (bvsalud.org)
These results indicate that adenosine is an effective analgesics in a model of diabetic neuropathy, and the protection produced by adenosine is via stimulation of adenosine A1-receptors. (who.int)
Background - Brief antecedent periods of coronary artery occlusion improve subsequent vessel patency in damaged and stenotic coronary arteries via release of adenosine from ischemic/reperfused myocardium and resultant adenosine receptor stimulation. (cmich.edu)
However, the site of receptor stimulation - circulating blood-borne elements (ie, platelets) versus vessel-wall components of the culprit artery - remains unclear. (cmich.edu)
Conclusions - Brief antecedent coronary artery occlusion enhanced vessel patency in remote, damaged, and stenotic carotid arteries, largely due to adenosine receptor stimulation on circulating elements. (cmich.edu)

Subtype-Selective Fluorescent Ligands as Pharmacological Research Tools for the Human Adenosine A(2A) Receptor JOURNAL OF MEDICINAL CHEMISTRY. (nottingham.ac.uk)
It consists of three components-ligands, including 2-arachidonoylglycerol (2-AG) and arachidonoyl ethanolamide (AEA or anandamide), receptors, such as cannabinoid receptor 1 (CB1) and cannabinoid receptor 2 (CB2), and the metabolizing enzymes-fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL). (encyclopedia.pub)
A2A, and A3 receptor functionalized congeners possess yielded macromolecular conjugates, irreversibly binding AR ligands for receptor inactivation and crosslinking, radioactive probes that make use of prosthetic organizations, immobilized ligands for affinity chromatography, and dual-acting ligands that work as binary medicines. (thetechnoant.info)
Following the successes using the A1 AR, we explored functionalized congeners of ligands from the A2A AR, in cooperation with Gary L. Stiles (Body 4) [54]. (thetechnoant.info)
To explore the relationship between both of these cardioprotective ARs as well as the question which receptor may be the even more essential anti-ischemic receptor, we designed specific binary ligands by tethering functionalized congeners. (thetechnoant.info)

Rolofylline, an adenosine A1-receptor antagonist, in acute heart failure. (umn.edu)
Wells L, Opacka-Juffry J, Fisher D, Ledent C, Hourani S , Kitchen I . In vivo dopaminergic and behavioral responses to acute cocaine are altered in adenosine A(2A) receptor knockout mice. (neurotree.org)
This review discusses the adenosine receptor-mediated pharmacological effects of Cordyceps and cordycepin on acute and chronic pneumonia and the subsequent organ damage. (fortunejournals.com)
Finally, the results of PROTECT (Placebo-controlled randomized study of the selective A1 adenosine receptor antagonist KW-3902 for patients hospitalized with acute HF and volume overload to assess treatment effect on congestion and renal function trial), were presented in the third and final hotline session on Tuesday 1 September. (cardiovascularnews.com)

Treatment of chronic congestive heart failure (HF) has improved substantially during the past decades, with the introduction of modulators of the renin angiotensin aldosterone system (RAAS) such as angiotensin converting enzyme (ACE) inhibitors, angiotensin II receptor blockers (ARBs) and aldosterone antagonists and the introduction of the lifesaving beta-blockers as well as device therapy. (scirp.org)

Al-Hasani R , Foster JD, Metaxas A, Ledent C, Hourani SM , Kitchen I , Chen Y. Increased desensitization of dopamine Dâ‚‚ receptor-mediated response in the ventral tegmental area in the absence of adenosine A(2A) receptors. (neurotree.org)
Adenosine A1 receptors (in contrast to adenosine A2A receptors) have been shown to influence dopamine release in slices of the striatum (Jin et al. (biologyonline.com)
Adenosine A1 agonists, but not adenosine A2A agonists, depressed the dopamine levels (Okada et al. (biologyonline.com)
Interactions with the adenosine A1 receptor, dopamine transporter and dopamine D5 receptor (antagonist activity), serotonin receptors (5-HT1B and 5-HT6 antagonist activity), and the GABA benzodiazepine receptor were demonstrated. (revolutionhealth.org)

Binary medicines with combined selectivity for both A1 and A3 ARs had been produced through the covalent linking of functionalized congeners of adenosine agonists, each which is usually selective for either the A1 or the A3 AR subtype. (thetechnoant.info)

Koetter et al studied the interactions of magnolia and ziziphus extracts with selected central nervous system receptors in a series of assays. (revolutionhealth.org)
MRS 1740 65 and MRS 1741 66, thiourea-linked regioisomers of the binary conjugate, had been highly powerful and selective in radioligand-binding assays for the A1 and A3 ARs (Ki ideals of 0.7C3.5 nM) weighed against the A2A AR. (thetechnoant.info)

These G protein-coupled receptors transduce activation or inhibition of adenylate cyclase and phospholipase C. Reasonably selective antagonists are available for some adenosine receptor subtypes. (cdc.gov)
These results suggest that the flavonoids act synergistically with epinephrine on beta-adrenergic receptor and not through phosphodiesterase inhibition to stimulate adipocyte lipolysis. (ironmagazine.com)
Doxofylline does not demonstrate direct inhibition of any histone deacetylase (HDAC) enzymes or known PDE enzyme isoforms and did not act as an antagonist at A2 or A2 receptors. (drugbank.com)

Jing Du, Weijing Kan, Hongkun Bao, Yue Jia, Jian Yang, Hongxiao Jia, Interactions Between Adenosine Receptors and Cordycepin (3-Deoxyadenosine) from Cordyceps Militaris: Possible Pharmacological Mechanisms for Protection of the Brain and the Amelioration of Covid-19 Pneumonia. (fortunejournals.com)
Conversely, there are many pharmacological effects of alcohol, as its multitude of neurotransmitter receptors that are ghly distributed in the brain. (cheapessaywritingservices.org)

The A1 receptor antagonist SLV320 significantly decreased cardiac fibrosis and albuminuria in rats with 5/6 NX. (fu-berlin.de)
The specific A1 adenosine receptor antagonist CPT significantly delayed the suppression of turtle ERG, while the hypoxic shark ERG was unaffected by the non-specific adenosine receptor antagonist aminophylline, suggesting adenosinergic involvement in turtle but not in shark. (edu.au)
In contrast with other xanthine derivatives, doxofylline does not significantly bind to adenosine alpha-1 or alpha-2 receptors and lacks stimulating effects. (drugbank.com)
One objective was to utilize this ligand device to check the hypothesis that activation of both receptors exerts a cardioprotective impact significantly higher than activation of either receptor independently. (thetechnoant.info)

However, there are exceptions: One is the discovery that certain drugs that bind to a class of adenosine receptors on neurons (ADORA1) can restore memory in transgenic mice that already have become demented. (curealz.org)
This suggests that many of the adenosine A1 receptors in the area of the DA cell bodies are located not on the dopaminergic neurons, but on the terminals of the input neurons. (biologyonline.com)

8-Cyclopentyl-1, 3-dipropylxanthine (DPCPX 1 mg/kg, ip), an adenosine A1-receptor antagonist, but not 3,7-dimethyl-l-propargylxanthine (DMPX 1 mg/kg, ip), an adenosine A2A-receptor antagonist, reversed the protective effect of adenosine. (who.int)
Adenosine A 1 receptor specific antagonist, 8-cyclopentyl-1,3-dipropylxanthine (DPCPX) exacerbate GOD-induced increase of spontaneous release of [ 3 H]-5-HT. (ewha.ac.kr)

Their effects were inhibited by propranolol (a beta-receptor antagonist). (ironmagazine.com)

Effects of purinergic receptor deletion or pharmacologic modulation on pulmonary inflammation in mice. (krakow.pl)

1,2,4-Triazolo[1,5-a]quinoxaline as a versatile tool for the design of selective human A3 adenosine receptor antagonists: synthesis, biological evaluation and molecular modeling studies of 2-(hetero)aryl- and 2-carboxy-substituted derivatives. (unifi.it)

2017). It works to mitigate pain by activating the pain-suppressing noradenosine pathway and acting as a nonselective antagonist of adenosine A1, A2A and A2B receptors which speeds nerve cell communication and results in vasoconstriction (Lipton et al. (katedaugherty.com)

The receptors for adenine nucleotides, such as adenosine triphosphate (ATP), now encompass seven distinct P2X class receptors (P2X1 through P2X7) and ten P2Y subfamily receptors: P2Y1 through P2Y11 (the former P2Y7-receptor is no longer included as a subtype). (cdc.gov)

Georgiou P , Zanos P , Hourani S , Kitchen I , Bailey A. Cocaine abstinence induces emotional impairment and brain region-specific upregulation of the oxytocin receptor binding. (neurotree.org)
Metaxas A, Al-Hasani R , Farshim P, Tubby K, Berwick A, Ledent C, Hourani S , Kitchen I , Bailey A. Genetic deletion of the adenosine A(2A) receptor prevents nicotine-induced upregulation of Î±7, but not Î±4Î²2* nicotinic acetylcholine receptor binding in the brain. (neurotree.org)
Adenosine has many physiological roles in the brain, and in rodents, it changes food intake when applied centrally. (ac.ir)
1995). In these regions of the brain there is a marked discrepancy between the distribution of the receptor and the corresponding mRNA. (biologyonline.com)
Methods and Results - In Protocol 1, anesthetized rabbits received 5 minutes of transient coronary occlusion, 5 minutes of transient bilateral carotid occlusion (purported to cause negligible adenosine release from the brain), or no intervention. (cmich.edu)
Neonatal exposure to a Type-I pyrethroid (bioallethrin) induces dose-response changes in brain muscarinic receptors and behaviour in neonatal and adult mice. (cdc.gov)

Quercetin seems to improve the performance of the receptor that adrenalin attaches itself to. (ironmagazine.com)

1,2,4-Triazolo[1,5-a]quinoxaline derivatives and their simplified analogues as adenosine A3 receptor antagonists. (unifi.it)
Bridged piperidine analogues of a high affinity naphthalene-based P2Y 14 R antagonist. (krakow.pl)

Development and Application of Subtype-Selective Fluorescent Antagonists for the Study of the Human Adenosine A(1) Receptor in Living Cells JOURNAL OF MEDICINAL CHEMISTRY. (nottingham.ac.uk)

Moreover, the protein is synthesised as a precursor which exerts the opposite effect of its mature form through the neurotrophin receptor p75NTR. (sciencegate.app)
Adenosine released during cardiac ischemia exerts a powerful, protective impact in the center via activation of A1 and A3 receptors [42,45,74], which activate different defensive signaling cascades. (thetechnoant.info)

Georgiou P , Zanos P , Garcia-Carmona JA, Hourani S , Kitchen I , Laorden ML, Bailey A. Methamphetamine abstinence induces changes in μ-opioid receptor, oxytocin and CRF systems: Association with an anxiogenic phenotype. (neurotree.org)
Zanos P , Wright SR, Georgiou P , Yoo JH , Ledent C, Hourani SM , Kitchen I , Winsky-Sommerer R , Bailey A. Chronic methamphetamine treatment induces oxytocin receptor up-regulation in the amygdala and hypothalamus via an adenosine A2A receptor-independent mechanism. (neurotree.org)

The role of adenosine A1 receptors of the amygdala on entorhinal cortex kindled seizures was investigated. (celljournal.org)
These results suggest that the amygdala may have a moderate role in seizure propagation from the entorhinal cortex and its adenosine A1 receptor activity has anticovulsant effects on entorhinal cortex kindled seizures. (celljournal.org)
Effect Of Adenosine A1 Recertors Of Amygdala On Entorhinal Cortex Kindled Seizures In Rat', Cell Journal (Yakhteh) , 5(3), pp. 137-143. (celljournal.org)

Thiourea-linked conjugates of the benzimidazole derivative that was a powerful opioid ligand and an AR functionalized congener, either ADAC 20 or XAC 27, destined successfully to both receptors. (thetechnoant.info)
We utilized a book style in which brand-new binary conjugates of adenosine functionalized congeners which were pharmacologically complementary had been synthesized and examined in a book cardiac myocyte style of adenosine-elicited cardioprotection. (thetechnoant.info)

Doxofylline mechanism of action consists of its ability to selectively inhibit phosphodiesterases (PDE III, IV,V) and not the adenosine receptors, A1 and A2. (icepharma.com)

Adenosine (100, 200 and 500 mg/kg, ip) produced significant reversal of responses to thermal and chemical stimuli in diabetic rats. (who.int)

However, the benefits of brief coronary occlusion were abrogated by the A 2 /A 1 antagonist CGS 15943. (cmich.edu)

Structural and molecular insight into piperazine and piperidine derivatives as histamine H 3 and sigma-1 receptor antagonists with promising antinociceptive properties. (krakow.pl)

Additional information about the molecular characteristics of these receptors, their pharmacologic properties, and associated signaling pathways can be found in several recent compendia and reviews. (cdc.gov)
Structure-activity relationships have been explained analyzing the three-dimensional structure of the antagonist-receptor models obtained by molecular docking simulation. (unipi.it)

In experimental animal studies, these compounds have been shown to enhance the activity of gamma-aminobutyric acid (GABA) A receptors and GABA binding, which may help the body cope with the neurologic effects emotions can have on behavior and well-being. (revolutionhealth.org)
CAMP tells the cell that compounds have attached themselves to receptors and that the cell needs to step up its metabolism. (ironmagazine.com)

abstract = "Adenosine is an important neuromodulator, known to interact with both dopaminergic and glutamatergic systems to influence psychostimulant action. (okstate.edu)

Using our recently published hA3 receptor model, to better elucidate our experimental results, we decided to theoretically depict the putative TM binding motif of the herein reported 1,2,4-triazolo[1,5-a]quinoxaline derivatives on human A3 receptor. (unipi.it)

Alcohol potentiates the GABAergic neurotransmission through the facilitation of GABA receptors. (cheapessaywritingservices.org)
Honokiol, administered by intraperitoneal injection in mice, was shown to promote NREM (non-rapid eye movement) sleep by modulating the benzodiazepine site of the GABA (A) receptor. (revolutionhealth.org)
The natural products magnolol and honokiol are positive allosteric modulators of both synaptic and extra-synaptic GABA(A) receptors. (revolutionhealth.org)
Honokiol promotes non-rapid eye movement sleep via the benzodiazepine site of the GABA(A) receptor in mice. (revolutionhealth.org)

1. It is well documented that cisplatin (CDDP) treatment increases the expression of adenosine A(1) receptors in both kidney and testes. (shengsci.com)

In summary, these results demonstrate that the sGC stimulator riociguat, the combined inhibitor of NEP/ECE SLV338, and the adenosin A1 receptor antagonist SLV 320 play important roles in cardio-renal protection in experimental models of hypertension and chronic renal failure. (fu-berlin.de)

We investigated the effect of central injection of the purine molecule adenosine on both food and fat intakes in neonatal chicks. (ac.ir)
IMSEAR at SEARO: Protective effect of adenosine in diabetic neuropathic pain is mediated through adenosine A1-receptors. (who.int)
Balasubramanyan Sridhar, Sharma Shyam S. Protective effect of adenosine in diabetic neuropathic pain is mediated through adenosine A1-receptors. (who.int)
In the present study, the effect of adenosine was investigated in a model of diabetic neuropathic pain. (who.int)
However, the effect of adenosine at these receptors is controversial. (shengsci.com)

Cell signaling throughout the CNS occurs by means of neurotransmitters or ions of various kinds interacting at membrane bound receptors and ion channels that, in turn, send the signal through second messenger systems to different compartments of the cell. (axonmedchem.com)

If platelet adenosine receptors are involved, then the benefits of brief coronary occlusion (1) should be manifested systemically and improve patency at a remote site and (2) should be inhibited by an antagonist of adenosine A 2 receptors, whereas, in contrast, (3) brief vascular occlusion not associated with appreciable adenosine release should be ineffective in improving vessel patency. (cmich.edu)

These results suggest that Adenosine may play a role in the GOD-induced spontaneous release of [ 3 H]-5-HT through adenosine A 1 receptor activity. (ewha.ac.kr)

Zanos P , Georgiou P , Rojo Gonzalez L, Hourani S , Chen Y, Kitchen I , Kieffer BL , Winsky-Sommerer R, Bailey A. Emotional impairment and persistent up-regulation of mGlu5 receptor following morphine abstinence: implications of an mGlu5-MOPr interaction. (neurotree.org)
In fact, the importance for the A3 receptor-ligand interaction of both a strong acidic NH proton donor and a C=O proton acceptor at position-4, able to engage hydrogen-bonding interactions with specific sites on the A3 AR, has been confirmed. (unipi.it)

Anatomy9

Organisms9

Diseases1

Chemicals and Drugs207

Analytical, Diagnostic and Therapeutic Techniques and Equipment11

Psychiatry and Psychology2

Phenomena and Processes16

Disciplines and Occupations1

Health Care1

Contribution of adenosine to the depression of sympathetically evoked vasoconstriction induced by systemic hypoxia in the rat. (1/174)

Ischaemic tolerance in aged mouse myocardium: the role of adenosine and effects of A1 adenosine receptor overexpression. (2/174)

Alteration of the purinergic modulation of enteric neurotransmission in the mouse ileum during chronic intestinal inflammation. (3/174)

Diadenosine-5-phosphate exerts A1-receptor-mediated proarrhythmic effects in rabbit atrial myocardium. (4/174)

Comparison of effects of MgCl2 and Gpp(NH)p on antagonist and agonist radioligand binding to adenosine A1 receptors. (5/174)

An orally active adenosine A1 receptor antagonist, FK838, increases renal excretion and maintains glomerular filtration rate in furosemide-resistant rats. (6/174)

Brief, repeated, oxygen-glucose deprivation episodes protect neurotransmission from a longer ischemic episode in the in vitro hippocampus: role of adenosine receptors. (7/174)

Involvement of adenosine A1 and A2A receptors in the adenosinergic modulation of the discriminative-stimulus effects of cocaine and methamphetamine in rats. (8/174)

Adenosine

Receptor, Adenosine A2A

Receptor, Adenosine A1

Adenosine A2 Receptor Antagonists

Purinergic P1 Receptor Antagonists

Adenosine Deaminase

Adenosine A1 Receptor Antagonists

Interleukin 1 Receptor Antagonist Protein

Receptor, Adenosine A3

Receptor, Adenosine A2B

Neurokinin-1 Receptor Antagonists

Receptors, Adenosine A2

Adenosine Kinase

Receptors, Purinergic P1

Adenosine A2 Receptor Agonists

Xanthines

Adenosine A1 Receptor Agonists

Dose-Response Relationship, Drug

Rats, Sprague-Dawley

Purinergic P1 Receptor Agonists

Histamine H2 Antagonists

Piperidines

Serotonin 5-HT3 Receptor Antagonists

Excitatory Amino Acid Antagonists

Adenosine A3 Receptor Antagonists

Dopamine Antagonists

Angiotensin Receptor Antagonists

Serotonin 5-HT2 Receptor Antagonists

Hormone Antagonists

Purinergic P2 Receptor Antagonists

Adenosine Monophosphate

Rats, Wistar

Adenosine-5'-(N-ethylcarboxamide)

Theophylline

Narcotic Antagonists

Histamine H1 Antagonists

Receptors, Endothelin

Receptors, Purinergic

Muscarinic Antagonists

GABA-A Receptor Antagonists

Phenethylamines

Histamine Antagonists

GABA Antagonists

Serotonin Antagonists

Leukotriene Antagonists

Sialoglycoproteins

Receptor, Endothelin A

Receptors, Serotonin

Receptors, N-Methyl-D-Aspartate

Cyclic AMP

Guinea Pigs

Dizocilpine Maleate

Serotonin 5-HT1 Receptor Antagonists

2-Chloroadenosine

Biphenyl Compounds

Radioligand Assay

Adenosine A3 Receptor Agonists

Receptors, Interleukin-1

Tetrazoles

Adrenergic alpha-1 Receptor Antagonists

Benzazepines

Phenylisopropyladenosine

Cells, Cultured

Nicotinic Antagonists

Purinergic Antagonists

Pyrazoles

Pyridines

Adrenergic alpha-2 Receptor Antagonists

Serotonin Receptor Agonists

Histamine H3 Antagonists

Sulfonamides

5'-Nucleotidase

Inosine

Peptides, Cyclic

Indoles

Serotonin

Binding, Competitive

Time Factors

Purinergic P2X Receptor Antagonists

Azepines