Adenosine a1 receptor agonists. 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 bind to and stimulate PURINERGIC P1 RECEPTORS.

Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS.

Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS.

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.

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

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.

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).

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.

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

Compounds that bind to and block the stimulation of ADENOSINE A1 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 bind to and activate dopamine receptors.

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

Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT1 RECEPTORS. Included under this heading are agonists for one or more of the specific 5-HT1 receptor subtypes.

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

Drugs that selectively bind to and activate ADENOSINE A3 RECEPTORS.

Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT2 RECEPTORS. Included under this heading are agonists for one or more of the specific 5-HT2 receptor subtypes.

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

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

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

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

Endogenous compounds and drugs that bind to and activate GAMMA-AMINOBUTYRIC ACID receptors (RECEPTORS, GABA).

Endogenous compounds and drugs that bind to and activate GABA-A RECEPTORS.

Endogenous compounds and drugs that bind to and activate GABA-B RECEPTORS.

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.

Compounds that bind to and stimulate PURINERGIC P2 RECEPTORS.

Compounds that interact with and stimulate the activity of CANNABINOID RECEPTORS.

Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT4 RECEPTORS.

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.

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

Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS.

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

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.

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

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.

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.

Drugs that bind to and activate histamine receptors. Although they have been suggested for a variety of clinical applications histamine agonists have so far been more widely used in research than therapeutically.

Drugs that bind to and activate muscarinic cholinergic receptors (RECEPTORS, MUSCARINIC). Muscarinic agonists are most commonly used when it is desirable to increase smooth muscle tone, especially in the GI tract, urinary bladder and the eye. They may also be used to reduce heart rate.

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 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.

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.

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

A selective D1 dopamine receptor agonist used primarily as a research tool.

Drugs that bind to and activate adrenergic receptors.

A GAMMA-AMINOBUTYRIC ACID derivative that is a specific agonist of GABA-B RECEPTORS. It is used in the treatment of MUSCLE SPASTICITY, especially that due to SPINAL CORD INJURIES. Its therapeutic effects result from actions at spinal and supraspinal sites, generally the reduction of excitatory transmission.

Compounds that bind to and activate ADRENERGIC BETA-3 RECEPTORS.

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

A dopamine D2/D3 receptor agonist.

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

Drugs that bind to and activate nicotinic cholinergic receptors (RECEPTORS, NICOTINIC). Nicotinic agonists act at postganglionic nicotinic receptors, at neuroeffector junctions in the peripheral nervous system, and at nicotinic receptors in the central nervous system. Agents that function as neuromuscular depolarizing blocking agents are included here because they activate nicotinic receptors, although they are used clinically to block nicotinic transmission.

A class of opioid receptors recognized by its pharmacological profile. Delta opioid receptors bind endorphins and enkephalins with approximately equal affinity and have less affinity for dynorphins.

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.

Drugs that bind to and activate excitatory amino acid receptors.

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

A 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)

A family of hexahydropyridines.

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.

Drugs that selectively bind to and activate beta-adrenergic receptors.

Compounds with BENZENE fused to AZEPINES.

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

A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.

An enkephalin analog that selectively binds to the MU OPIOID RECEPTOR. It is used as a model for drug permeability experiments.

Drugs that selectively bind to and activate alpha adrenergic receptors.

Compounds having the cannabinoid structure. They were originally extracted from Cannabis sativa L. The most pharmacologically active constituents are TETRAHYDROCANNABINOL; CANNABINOL; and CANNABIDIOL.

Compounds that bind to and activate ADRENERGIC ALPHA-1 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.

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.

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)

A neurotoxic isoxazole isolated from species of AMANITA. It is obtained by decarboxylation of IBOTENIC ACID. Muscimol is a potent agonist of GABA-A RECEPTORS and is used mainly as an experimental tool in animal and tissue studies.

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.

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 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.

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.

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.

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.

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.

Drugs that bind to and activate cholinergic receptors.

Compounds that bind to and stimulate PURINERGIC P2Y RECEPTORS. Included under this heading are agonists for specific P2Y receptor subtypes.

The rate dynamics in chemical or physical systems.

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.

A disulfide opioid pentapeptide that selectively binds to the DELTA OPIOID RECEPTOR. It possesses antinociceptive activity.

Isopropyl analog of EPINEPHRINE; beta-sympathomimetic that acts on the heart, bronchi, skeletal muscle, alimentary tract, etc. It is used mainly as bronchodilator and heart stimulant.

Cell surface receptors that bind glucagon with high affinity and trigger intracellular changes which influence the behavior of cells. Activation of glucagon receptors causes a variety of effects; the best understood is the initiation of a complex enzymatic cascade in the liver which ultimately increases the availability of glucose to body organs.

OXAZINES with a fused BENZENE ring.

Compounds that bind to and stimulate PURINERGIC P2X RECEPTORS. Included under this heading are agonists for specific P2X receptor subtypes.

A subclass of cannabinoid receptor found primarily on immune cells where it may play a role modulating release of CYTOKINES.

An enzyme of the lyase class that catalyzes the formation of CYCLIC AMP and pyrophosphate from ATP. EC 4.6.1.1.

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

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.

Poisonous animal secretions forming fluid mixtures of many different enzymes, toxins, and other substances. These substances are produced in specialized glands and secreted through specialized delivery systems (nematocysts, spines, fangs, etc.) for disabling prey or predator.

Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT3 RECEPTORS.

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

A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)

The observable response an animal makes to any situation.

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

Compounds that bind to and activate PURINERGIC RECEPTORS.

Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.

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

A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use.

A serotonin agonist that acts selectively at 5HT1 receptors. It is used in the treatment of MIGRAINE DISORDERS.

Partially saturated 1,2,3,4-tetrahydronaphthalene compounds.

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.

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.

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.

A subtype of dopamine D2 receptors that are highly expressed in the LIMBIC SYSTEM of the brain.

A series of structurally-related alkaloids that contain the ergoline backbone structure.

One of the three major families of endogenous opioid peptides. The enkephalins are pentapeptides that are widespread in the central and peripheral nervous systems and in the adrenal medulla.

A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.

Histamine substituted in any position with one or more methyl groups. Many of these are agonists for the H1, H2, or both histamine receptors.

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

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

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

A serotonin receptor subtype found at high levels in the BASAL GANGLIA and the frontal cortex. It plays a role as a terminal autoreceptor that regulates the rate of SEROTONIN release from nerve endings. This serotonin receptor subtype is closely related to and has similar drug binding properties as the 5-HT1D RECEPTOR. It is particularly sensitive to the agonist SUMATRIPTAN and may be involved in mediating the drug's antimigraine effect.

Catalyze the hydrolysis of nucleosides with the elimination of ammonia.

Established cell cultures that have the potential to propagate indefinitely.

A subtype of G-protein-coupled SEROTONIN receptors that preferentially couple to GS STIMULATORY G-PROTEINS resulting in increased intracellular CYCLIC AMP. Several isoforms of the receptor exist due to ALTERNATIVE SPLICING of its mRNA.

A subset of GABA RECEPTORS that signal through their interaction with HETEROTRIMERIC G-PROTEINS.

Drugs used to cause dilation of the blood vessels.

Compounds based on benzeneacetamide, that are similar in structure to ACETANILIDES.

A class of cell surface receptors recognized by its pharmacological profile. Sigma receptors were originally considered to be opioid receptors because they bind certain synthetic opioids. However they also interact with a variety of other psychoactive drugs, and their endogenous ligand is not known (although they can react to certain endogenous steroids). Sigma receptors are found in the immune, endocrine, and nervous systems, and in some peripheral tissues.

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

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

Cell surface receptors which bind prostaglandins with a high affinity and trigger intracellular changes which influence the behavior of cells. Prostaglandin E receptors prefer prostaglandin E2 to other endogenous prostaglandins. They are subdivided into EP1, EP2, and EP3 types based on their effects and their pharmacology.

CELL LINE derived from the ovary of the Chinese hamster, Cricetulus griseus (CRICETULUS). The species is a favorite for cytogenetic studies because of its small chromosome number. The cell line has provided model systems for the study of genetic alterations in cultured mammalian cells.

A serotonin receptor subtype found distributed through the CENTRAL NERVOUS SYSTEM where they are involved in neuroendocrine regulation of ACTH secretion. The fact that this serotonin receptor subtype is particularly sensitive to SEROTONIN RECEPTOR AGONISTS such as BUSPIRONE suggests its role in the modulation of ANXIETY and DEPRESSION.

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.

Cell surface proteins that bind glutamate and act through G-proteins to influence second messenger systems. Several types of metabotropic glutamate receptors have been cloned. They differ in pharmacology, distribution, and mechanisms of action.

A ribonucleoside antibiotic synergist and adenosine deaminase inhibitor isolated from Nocardia interforma and Streptomyces kaniharaensis. It is proposed as an antineoplastic synergist and immunosuppressant.

Cell-surface proteins that bind histamine and trigger intracellular changes influencing the behavior of cells. Histamine receptors are widespread in the central nervous system and in peripheral tissues. Three types have been recognized and designated H1, H2, and H3. They differ in pharmacology, distribution, and mode of action.

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.

Cell-surface proteins that bind dopamine with high affinity and trigger intracellular changes influencing the behavior of cells.

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

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)

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 imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.

Proteins that bind specific drugs with high affinity and trigger intracellular changes influencing the behavior of cells. Drug receptors are generally thought to be receptors for some endogenous substance not otherwise specified.

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.

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)

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 class of saturated compounds consisting of two rings only, having two or more atoms in common, containing at least one hetero atom, and that take the name of an open chain hydrocarbon containing the same total number of atoms. (From Riguady et al., Nomenclature of Organic Chemistry, 1979, p31)

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

A highly potent and specific histamine H2 receptor agonist. It has been used diagnostically as a gastric secretion indicator.

A serotonin receptor subtype found primarily in the CENTRAL NERVOUS SYSTEM and the CHOROID PLEXUS. This receptor subtype is believed to mediate the anorectic action of SEROTONIN, while selective antagonists of the 5-HT2C receptor appear to induce ANXIETY. Several isoforms of this receptor subtype exist, due to adenine deaminase editing of the receptor mRNA.

The most common inhibitory neurotransmitter in the central nervous system.

Any drugs that are used for their effects on dopamine receptors, on the life cycle of dopamine, or on the survival of dopaminergic neurons.

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.

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.

Guanosine 5'-(trihydrogen diphosphate), monoanhydride with phosphorothioic acid. A stable GTP analog which enjoys a variety of physiological actions such as stimulation of guanine nucleotide-binding proteins, phosphoinositide hydrolysis, cyclic AMP accumulation, and activation of specific proto-oncogenes.

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)

Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.

A dopamine D1 receptor agonist that is used as an antihypertensive agent. It lowers blood pressure through arteriolar vasodilation.

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

Uridine 5'-(tetrahydrogen triphosphate). A uracil nucleotide containing three phosphate groups esterified to the sugar moiety.

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.

The voltage differences across a membrane. For cellular membranes they are computed by subtracting the voltage measured outside the membrane from the voltage measured inside the membrane. They result from differences of inside versus outside concentration of potassium, sodium, chloride, and other ions across cells' or ORGANELLES membranes. For excitable cells, the resting membrane potentials range between -30 and -100 millivolts. Physical, chemical, or electrical stimuli can make a membrane potential more negative (hyperpolarization), or less negative (depolarization).

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

Analogs or derivatives of AMPHETAMINE. Many are sympathomimetics and central nervous system stimulators causing excitation, vasopressin, bronchodilation, and to varying degrees, anorexia, analepsis, nasal decongestion, and some smooth muscle relaxation.

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.

Regulatory proteins that act as molecular switches. They control a wide range of biological processes including: receptor signaling, intracellular signal transduction pathways, and protein synthesis. Their activity is regulated by factors that control their ability to bind to and hydrolyze GTP to GDP. EC 3.6.1.-.

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

A potent inhibitor of ADENOSINE DEAMINASE. The drug induces APOPTOSIS of LYMPHOCYTES, and is used in the treatment of many lymphoproliferative malignancies, particularly HAIRY CELL LEUKEMIA. It is also synergistic with some other antineoplastic agents and has immunosuppressive activity.

One of two major pharmacologically defined classes of adrenergic receptors. The beta adrenergic receptors play an important role in regulating CARDIAC MUSCLE contraction, SMOOTH MUSCLE relaxation, and GLYCOGENOLYSIS.

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)

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

A group of enzymes that are dependent on CYCLIC AMP and catalyze the phosphorylation of SERINE or THREONINE residues on proteins. Included under this category are two cyclic-AMP-dependent protein kinase subtypes, each of which is defined by its subunit composition.

A purine base and a fundamental unit of ADENINE NUCLEOTIDES.

One of the two major classes of cholinergic receptors. Muscarinic receptors were originally defined by their preference for MUSCARINE over NICOTINE. There are several subtypes (usually M1, M2, M3....) that are characterized by their cellular actions, pharmacology, and molecular biology.

Striped GRAY MATTER and WHITE MATTER consisting of the NEOSTRIATUM and paleostriatum (GLOBUS PALLIDUS). It is located in front of and lateral to the THALAMUS in each cerebral hemisphere. The gray substance is made up of the CAUDATE NUCLEUS and the lentiform nucleus (the latter consisting of the GLOBUS PALLIDUS and PUTAMEN). The WHITE MATTER is the INTERNAL CAPSULE.

Sulfhydryl analog of INOSINE that inhibits nucleoside transport across erythrocyte plasma membranes, and has immunosuppressive properties. It has been used similarly to MERCAPTOPURINE in the treatment of leukemia. (From Martindale, The Extra Pharmacopoeia, 30th ed, p503)

5'-Adenylic acid, monoanhydride with sulfuric acid. The initial compound formed by the action of ATP sulfurylase on sulfate ions after sulfate uptake. Synonyms: adenosine sulfatophosphate; APS.

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

The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.

A 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.

One of the virulence factors produced by BORDETELLA PERTUSSIS. It is a multimeric protein composed of five subunits S1 - S5. S1 contains mono ADPribose transferase activity.

A subclass of alpha-adrenergic receptors found on both presynaptic and postsynaptic membranes where they signal through Gi-Go G-PROTEINS. While postsynaptic alpha-2 receptors play a traditional role in mediating the effects of ADRENERGIC AGONISTS, the subset of alpha-2 receptors found on presynaptic membranes signal the feedback inhibition of NEUROTRANSMITTER release.

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

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.

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.

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.

An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent.

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

Nucleotides in which the base moiety is substituted with one or more sulfur atoms.

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

A psychoactive compound extracted from the resin of Cannabis sativa (marihuana, hashish). The isomer delta-9-tetrahydrocannabinol (THC) is considered the most active form, producing characteristic mood and perceptual changes associated with this compound.

Cell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and contain an integral membrane chloride channel. Each receptor is assembled as a pentamer from a pool of at least 19 different possible subunits. The receptors belong to a superfamily that share a common CYSTEINE loop.

Monohydroxy derivatives of cyclohexanes that contain the general formula R-C6H11O. They have a camphorlike odor and are used in making soaps, insecticides, germicides, dry cleaning, and plasticizers.

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

A subclass of G-protein coupled SEROTONIN receptors that couple preferentially to GI-GO G-PROTEINS resulting in decreased intracellular CYCLIC AMP levels.

Compounds based on a partially saturated iminoethanophenanthrene, which can be described as ethylimino-bridged benzo-decahydronaphthalenes. They include some of the OPIOIDS found in PAPAVER that are used as ANALGESICS.

Alteration of the purinergic modulation of enteric neurotransmission in the mouse ileum during chronic intestinal inflammation. (1/122)

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)

Comparison of effects of MgCl2 and Gpp(NH)p on antagonist and agonist radioligand binding to adenosine A1 receptors. (2/122)

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)

Involvement of adenosine A1 and A2A receptors in the adenosinergic modulation of the discriminative-stimulus effects of cocaine and methamphetamine in rats. (3/122)

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)

Adenosine A1 receptor agonists block the neuropathological changes in rat retrosplenial cortex after administration of the NMDA receptor antagonist dizocilpine. (4/122)

Noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist dizocilpine ((+)-MK-801) is known to induce neurotoxicity in rat retrosplenial cortex after systemic administration. The present study was undertaken to examine the effects of adenosine A(1) receptor agonists on the neurotoxicity in rat retrosplenial cortex after administration of dizocilpine. Pretreatment with adenosine A(1) receptor agonists, 2-chloro-N(6)-cyclopentyladenosine (CCPA) (0.1, 0.3, 1, or 3 mg/kg, intraperitoneally (i.p.)), or N(6)-cyclopentyladenosine (CPA) (1, 3, or 10 mg/kg, i.p.), attenuated neurotoxicity by dizocilpine (0.5 mg/kg, i.p), in a dose-dependent manner. Coadministration with adenosine A(1) receptor antagonist, 1,3-dipropyl-8-cyclopentylxanthine (DPCPX; 3 mg/kg, i.p.) significantly blocked the protective effects of CCPA for dizocilpine-induced neurotoxicity. Furthermore, pretreatment with CCPA (3 mg/kg) attenuated significantly the dizocilpine-induced expression of HSP-70 protein, which is known as a sensitive marker of reversible neuronal damage, and coadministration with DPCPX (3 mg/kg) blocked the inhibitory effects of CCPA for marked expression of HSP-70 protein by administration of dizocilpine. Moreover, pretreatment with CCPA (3 mg/kg, i.p.) significantly suppressed the increase of extracellular acetylcholine (ACh) levels in the retrosplenial cortex by administration of dizocilpine (0.5 mg/kg). In contrast, local perfusion of CCPA (1 microM) into the retrosplenial cortex via the dialysis probe did not alter the ACh levels by administration of dizocilpine (0.5 mg/kg), suggesting that the locus of action of CCPA is not in the retrosplenial cortex. These findings suggest that adenosine A(1) receptors agonists could protect against neuropathological changes in rat retrosplenial cortex after administration of the NMDA receptor antagonist dizocilpine. (+info)

Allosteric enhancers of A1 adenosine receptors increase receptor-G protein coupling and counteract Guanine nucleotide effects on agonist binding. (5/122)

Endogenous ligands of G protein-coupled receptors bind to orthosteric sites that are topologically distinct from allosteric sites. Certain aminothiophenes such as (2-amino-4,5-dimethyl-3-thienyl)-[3-(trifluromethyl)-phenyl]-methanone (PD81,723) and 2-amino-4,5,6,7-tetrahydro-benzo[b]thiophen-3-yl)-biphenyl-4-yl-methanone (ATL525) are positive allosteric regulators, or enhancers, of the human A1 adenosine receptor (A1AR). In equilibrium binding assays, 125I-N6-aminobenzyladenosine (125I-ABA) binds to two affinity states of A1AR with KD-high (0.33 microM) and KD-low ( approximately 10 nM). Enhancers have little effect on KD-high but convert all A1AR binding sites to the high-affinity state. Enhancers decrease the potency of guanosine 5'-O-(3-thio)triphosphate (GTPgammaS) as an inhibitor of agonist binding by 100-fold and increase agonist-stimulated guanine nucleotide exchange. The association of 125I-ABA to high-affinity receptors on Chinese hamster ovary (CHO)-hA1 membranes does not follow theoretical single-site association kinetics but is approximated by a bi-exponential equation with t1/2 values of 1.85 and 12.8 min. Allosteric enhancers selectively increase the number of slow binding sites, possibly by stabilizing newly formed receptor-G protein complexes. A new rapid assay method scores enhancer activity on a scale from 0 to 100 based on their ability to prevent the rapid dissociation of 125I-ABA from A1AR in response to GTPgammaS. Compared with PD81,723, ATL525 (100 microM) scores higher (27 versus 79) and has less antagonist activity. ATL525 functionally enhances A1 signaling to inhibit cAMP accumulation in CHO-hA1 cells. These data suggest that simultaneously binding orthosteric and allosteric enhancer ligands convert the A1AR from partly to fully coupled to G proteins and prevents rapid uncoupling upon binding of GTPgammaS. (+info)

Role of direct RhoA-phospholipase D1 interaction in mediating adenosine-induced protection from cardiac ischemia. (6/122)

Activation of adenosine A1 or A3 receptors protects heart cells from ischemia-induced injury. The A3 receptor signals via RhoA and phospholipase D (PLD) to induce cardioprotection. The objective of the study was to investigate how RhoA activates PLD to achieve the anti-ischemic effect of adenosine A3 receptors. In an established cardiac myocyte model of preconditioning using the cultured chick embryo heart cells, overexpression of the RhoA-noninteracting PLD1 mutant I870R selectively blocked the A3 agonist (Cl-IBMECA, 10 nM)-induced cardioprotection. I870R caused a significantly higher percentage of cardiac cells killed in A3 agonist-treated than in A1 agonist (CCPA, 10 nM)-treated myocytes (ANOVA and posttest comparison, P<0.01). Consistent with its inhibitory effect on the PLD activity, I870R attenuated the Cl-IBMECA-mediated PLD activation. Cl-IBMECA caused a 41 +/- 15% increase in PLD activity in mock-transfected myocytes (P<0.01, paired t test) while having only a slight stimulatory effect on the PLD activity in I870R-transfected cells. To further test the anti-ischemic role of a direct RhoA-PLD1 interaction, atrial cardiac myocytes were rendered null for native adenosine receptors by treatment with irreversible A1 antagonist m-DITC-XAC and were selectively transfected with the human adenosine A1 or A3 receptor cDNA individually or they were cotransfected with cDNAs encoding either receptor plus I870R. I870R preferentially inhibited the human A3 receptor-mediated protection from ischemia. The RhoA-noninteracting PLD1 mutant caused a significantly higher percentage of cardiac cells killed in myocytes cotransfected with the human A3 receptor than in those cells expressing the human A1 receptor (ANOVA and posttest comparison, P<0.01). The present data provided the first demonstration of a novel physiological role for the direct RhoA-PLD1 interaction, that of potent protection from cardiac ischemia. The study further supported the concept that a divergent signaling mechanism mediates the anti-ischemic effect of adenosine A1 and A3 receptors. (+info)

A1 and A2A adenosine receptor modulation of alpha 1-adrenoceptor-mediated contractility in human cultured prostatic stromal cells. (7/122)

1. This study investigated the possibility that adenosine receptors modulate the alpha(1)-adrenoceptor-mediated contractility of human cultured prostatic stromal cells (HCPSC). 2. The nonselective adenosine receptor agonist, 5'-N-ethylcarboxamido-adenosine (NECA; 10 nm-10 microm), and the A(1) adenosine receptor selective agonist, cyclopentyladenosine (CPA; 10 nm-10 microm), elicited significant contractions in HCPSC, with maximum contractile responses of 18+/-3% and 17+/-2% reduction in initial cell length, respectively. 3. In the presence of a threshold concentration of phenylephrine (PE) (100 nm), CPA (1 nm-10 microm) caused contractions, with an EC(50) of 124+/-12 nm and maximum contractile response of 37+/-4%. The A(1) adenosine receptor-selective antagonist 8-cyclopentyl-1,3-dipropylxanthine (DPCPX 100 nm) blocked this effect. In the presence of DPCPX (100 nm), NECA (1 nm-10 microm) inhibited contractions elicited by a submaximal concentration of PE (10 microm), with an IC(50) of 48+/-2 nm. The A(2A) adenosine receptor-selective antagonist 4-(2-[7-amino-2-[furyl][1,2,4]triazolo[2,3-alpha][1,3,5,]triazin-5-yl amino]ethyl)phenol (Zm241385 100 nm) blocked this effect. 4. In BCECF-AM (10 microm)-loaded cells, both CPA (100 pM-1 microm) and NECA (100 pm-10 microm) elicited concentration-dependent decreases in intracellular pH (pH(i)), with EC(50) values of 3.1+/-0.3 and 6.0+/-0.3 nm, respectively. The response to NECA was blocked by Zm241385 (100 nm; apparent pK(B) of 9.4+/-0.4), but not by DPCPX (100 nm). The maximum response to CPA was blocked by DPCPX (100 nm), and unaffected by Zm241385 (100 nm). 5. NECA (10 nm-10 microm) alone did not increase [(3)H]-cAMP in HCPSC. In the presence of DPCPX (100 nm), NECA (10 nm-10 microm) caused a concentration dependent increase in [(3)H]-cAMP, with an EC(50) of 1.2+/-0.1 microm. This response was inhibited by Zm241385 (100 nm). CPA (10 nm-10 microm) had no effect on cAMP, in the presence or absence of forskolin (1 microm). 6. These findings are consistent with a role for adenosine receptors in the modulation of adrenoceptor-mediated contractility in human prostate-derived cells. (+info)

A1 adenosine receptor upregulation and activation attenuates neuroinflammation and demyelination in a model of multiple sclerosis. (8/122)

The neuromodulator adenosine regulates immune activation and neuronal survival through specific G-protein-coupled receptors expressed on macrophages and neurons, including the A1 adenosine receptor (A1AR). Here we show that A1AR null (A1AR-/-) mice developed a severe progressive-relapsing form of experimental allergic encephalomyelitis (EAE) compared with their wild-type (A1AR+/+) littermates. Worsened demyelination, axonal injury, and enhanced activation of microglia/macrophages were observed in A1AR-/- animals. In addition, spinal cords from A1AR-/- mice demonstrated increased proinflammatory gene expression during EAE, whereas anti-inflammatory genes were suppressed compared with A1AR+/+ animals. Macrophages from A1AR-/- animals exhibited increased expression of the proinflammatory genes, interleukin-1beta, and matrix metalloproteinase-12 on immune activation when matched with A1AR+/+ control cells. A1AR-/- macrophage-derived soluble factors caused significant oligodendrocyte cytotoxicity compared with wild-type controls. The A1AR was downregulated in microglia in A1AR+/+ mice during EAE accompanied by neuroinflammation, which recapitulated findings in multiple sclerosis (MS) patients. Caffeine treatment augmented A1AR expression on microglia, with ensuing reduction of EAE severity, which was further enhanced by concomitant treatment with the A1AR agonist, adenosine amine congener. Thus, modulation of neuroinflammation by the A1AR represents a novel mechanism that provides new therapeutic opportunities for MS and other demyelinating diseases. (+info)

1) They share similarities with humans: Many animal species share similar biological and physiological characteristics with humans, making them useful for studying human diseases. For example, mice and rats are often used to study diseases such as diabetes, heart disease, and cancer because they have similar metabolic and cardiovascular systems to humans.

2) They can be genetically manipulated: Animal disease models can be genetically engineered to develop specific diseases or to model human genetic disorders. This allows researchers to study the progression of the disease and test potential treatments in a controlled environment.

3) They can be used to test drugs and therapies: Before new drugs or therapies are tested in humans, they are often first tested in animal models of disease. This allows researchers to assess the safety and efficacy of the treatment before moving on to human clinical trials.

4) They can provide insights into disease mechanisms: Studying disease models in animals can provide valuable insights into the underlying mechanisms of a particular disease. This information can then be used to develop new treatments or improve existing ones.

5) Reduces the need for human testing: Using animal disease models reduces the need for human testing, which can be time-consuming, expensive, and ethically challenging. However, it is important to note that animal models are not perfect substitutes for human subjects, and results obtained from animal studies may not always translate to humans.

6) They can be used to study infectious diseases: Animal disease models can be used to study infectious diseases such as HIV, TB, and malaria. These models allow researchers to understand how the disease is transmitted, how it progresses, and how it responds to treatment.

7) They can be used to study complex diseases: Animal disease models can be used to study complex diseases such as cancer, diabetes, and heart disease. These models allow researchers to understand the underlying mechanisms of the disease and test potential treatments.

8) They are cost-effective: Animal disease models are often less expensive than human clinical trials, making them a cost-effective way to conduct research.

9) They can be used to study drug delivery: Animal disease models can be used to study drug delivery and pharmacokinetics, which is important for developing new drugs and drug delivery systems.

10) They can be used to study aging: Animal disease models can be used to study the aging process and age-related diseases such as Alzheimer's and Parkinson's. This allows researchers to understand how aging contributes to disease and develop potential treatments.

There are several different types of pain, including:

1. Acute pain: This type of pain is sudden and severe, and it usually lasts for a short period of time. It can be caused by injuries, surgery, or other forms of tissue damage.
2. Chronic pain: This type of pain persists over a long period of time, often lasting more than 3 months. It can be caused by conditions such as arthritis, fibromyalgia, or nerve damage.
3. Neuropathic pain: This type of pain results from damage to the nervous system, and it can be characterized by burning, shooting, or stabbing sensations.
4. Visceral pain: This type of pain originates in the internal organs, and it can be difficult to localize.
5. Psychogenic pain: This type of pain is caused by psychological factors such as stress, anxiety, or depression.

The medical field uses a range of methods to assess and manage pain, including:

1. Pain rating scales: These are numerical scales that patients use to rate the intensity of their pain.
2. Pain diaries: These are records that patients keep to track their pain over time.
3. Clinical interviews: Healthcare providers use these to gather information about the patient's pain experience and other relevant symptoms.
4. Physical examination: This can help healthcare providers identify any underlying causes of pain, such as injuries or inflammation.
5. Imaging studies: These can be used to visualize the body and identify any structural abnormalities that may be contributing to the patient's pain.
6. Medications: There are a wide range of medications available to treat pain, including analgesics, nonsteroidal anti-inflammatory drugs (NSAIDs), and muscle relaxants.
7. Alternative therapies: These can include acupuncture, massage, and physical therapy.
8. Interventional procedures: These are minimally invasive procedures that can be used to treat pain, such as nerve blocks and spinal cord stimulation.

It is important for healthcare providers to approach pain management with a multi-modal approach, using a combination of these methods to address the physical, emotional, and social aspects of pain. By doing so, they can help improve the patient's quality of life and reduce their suffering.

It is important to note that catalepsy is not the same as catatonia, which is a more specific condition characterized by a wide range of symptoms, including immobility, mutism, negativism, and emotional dysregulation. However, catalepsy and catatonia do share some similarities, and the terms are often used interchangeably in clinical practice.

The exact cause of catalepsy is not fully understood, but it is thought to be related to dysfunction in certain areas of the brain, such as the neocortex and basal ganglia. In some cases, catalepsy may be a side effect of medication or drug intoxication.

Treatment for catalepsy typically focuses on addressing the underlying cause, such as managing seizures or withdrawing from drugs. In some cases, medications such as benzodiazepines or antipsychotics may be used to help manage symptoms. Other approaches, such as physical therapy and behavioral interventions, may also be helpful in improving mobility and function.

Hyperalgesia is often seen in people with chronic pain conditions, such as fibromyalgia, and it can also be a side effect of certain medications or medical procedures. Treatment options for hyperalgesia depend on the underlying cause of the condition, but may include pain management techniques, physical therapy, and medication adjustments.

In clinical settings, hyperalgesia is often assessed using a pinprick test or other pain tolerance tests to determine the patient's sensitivity to different types of stimuli. The goal of treatment is to reduce the patient's pain and improve their quality of life.

In some cases, hyperemia can be a sign of a more serious underlying condition that requires medical attention. For example, if hyperemia is caused by an inflammatory or infectious process, it may lead to tissue damage or organ dysfunction if left untreated.

Hyperemia can occur in various parts of the body, including the skin, muscles, organs, and other tissues. It is often diagnosed through physical examination and imaging tests such as ultrasound, computed tomography (CT), or magnetic resonance imaging (MRI). Treatment for hyperemia depends on its underlying cause, and may include antibiotics, anti-inflammatory medications, or surgery.

In the context of dermatology, hyperemia is often used to describe a condition called erythema, which is characterized by redness and swelling of the skin due to increased blood flow. Erythema can be caused by various factors, such as sun exposure, allergic reactions, or skin infections. Treatment for erythema may include topical medications, oral medications, or other therapies depending on its underlying cause.

There are several key features of inflammation:

1. Increased blood flow: Blood vessels in the affected area dilate, allowing more blood to flow into the tissue and bringing with it immune cells, nutrients, and other signaling molecules.
2. Leukocyte migration: White blood cells, such as neutrophils and monocytes, migrate towards the site of inflammation in response to chemical signals.
3. Release of mediators: Inflammatory mediators, such as cytokines and chemokines, are released by immune cells and other cells in the affected tissue. These molecules help to coordinate the immune response and attract more immune cells to the site of inflammation.
4. Activation of immune cells: Immune cells, such as macrophages and T cells, become activated and start to phagocytose (engulf) pathogens or damaged tissue.
5. Increased heat production: Inflammation can cause an increase in metabolic activity in the affected tissue, leading to increased heat production.
6. Redness and swelling: Increased blood flow and leakiness of blood vessels can cause redness and swelling in the affected area.
7. Pain: Inflammation can cause pain through the activation of nociceptors (pain-sensing neurons) and the release of pro-inflammatory mediators.

Inflammation can be acute or chronic. Acute inflammation is a short-term response to injury or infection, which helps to resolve the issue quickly. Chronic inflammation is a long-term response that can cause ongoing damage and diseases such as arthritis, asthma, and cancer.

There are several types of inflammation, including:

1. Acute inflammation: A short-term response to injury or infection.
2. Chronic inflammation: A long-term response that can cause ongoing damage and diseases.
3. Autoimmune inflammation: An inappropriate immune response against the body's own tissues.
4. Allergic inflammation: An immune response to a harmless substance, such as pollen or dust mites.
5. Parasitic inflammation: An immune response to parasites, such as worms or fungi.
6. Bacterial inflammation: An immune response to bacteria.
7. Viral inflammation: An immune response to viruses.
8. Fungal inflammation: An immune response to fungi.

There are several ways to reduce inflammation, including:

1. Medications such as nonsteroidal anti-inflammatory drugs (NSAIDs), corticosteroids, and disease-modifying anti-rheumatic drugs (DMARDs).
2. Lifestyle changes, such as a healthy diet, regular exercise, stress management, and getting enough sleep.
3. Alternative therapies, such as acupuncture, herbal supplements, and mind-body practices.
4. Addressing underlying conditions, such as hormonal imbalances, gut health issues, and chronic infections.
5. Using anti-inflammatory compounds found in certain foods, such as omega-3 fatty acids, turmeric, and ginger.

It's important to note that chronic inflammation can lead to a range of health problems, including:

1. Arthritis
2. Diabetes
3. Heart disease
4. Cancer
5. Alzheimer's disease
6. Parkinson's disease
7. Autoimmune disorders, such as lupus and rheumatoid arthritis.

Therefore, it's important to manage inflammation effectively to prevent these complications and improve overall health and well-being.

Hypothermia can be mild, moderate, or severe. Mild hypothermia is characterized by shivering and a body temperature of 95 to 97 degrees Fahrenheit (32 to 36.1 degrees Celsius). Moderate hypothermia has a body temperature of 82 to 94 degrees Fahrenheit (28 to 34 degrees Celsius), and the person may appear lethargic, drowsy, or confused. Severe hypothermia is characterized by a body temperature below 82 degrees Fahrenheit (28 degrees Celsius) and can lead to coma and even death if not treated promptly.

Treatment for hypothermia typically involves warming the person up slowly, using blankets or heating pads, and providing warm fluids to drink. In severe cases, medical professionals may use a specialized warm water bath or apply warm packs to specific areas of the body.

Preventing hypothermia is important, especially in cold weather conditions. This can be done by dressing appropriately for the weather, staying dry and avoiding wet clothing, eating regularly to maintain energy levels, and seeking shelter if you become stranded or lost. It's also essential to recognize the signs of hypothermia early on so that treatment can begin promptly.

There are different types of anoxia, including:

1. Cerebral anoxia: This occurs when the brain does not receive enough oxygen, leading to cognitive impairment, confusion, and loss of consciousness.
2. Pulmonary anoxia: This occurs when the lungs do not receive enough oxygen, leading to shortness of breath, coughing, and chest pain.
3. Cardiac anoxia: This occurs when the heart does not receive enough oxygen, leading to cardiac arrest and potentially death.
4. Global anoxia: This is a complete lack of oxygen to the entire body, leading to widespread tissue damage and death.

Treatment for anoxia depends on the underlying cause and the severity of the condition. In some cases, hospitalization may be necessary to provide oxygen therapy, pain management, and other supportive care. In severe cases, anoxia can lead to long-term disability or death.

Prevention of anoxia is important, and this includes managing underlying medical conditions such as heart disease, diabetes, and respiratory problems. It also involves avoiding activities that can lead to oxygen deprivation, such as scuba diving or high-altitude climbing, without proper training and equipment.

In summary, anoxia is a serious medical condition that occurs when there is a lack of oxygen in the body or specific tissues or organs. It can cause cell death and tissue damage, leading to serious health complications and even death if left untreated. Early diagnosis and treatment are crucial to prevent long-term disability or death.

* Anxiety
* Depression
* Fatigue
* Insomnia
* Muscle and bone pain
* Nausea and vomiting
* Seizures (in severe cases)
* Sweating
* Tremors

The specific symptoms of substance withdrawal syndrome can vary depending on the substance being withdrawn from, but some common symptoms include:

* Alcohol: tremors, anxiety, insomnia, nausea and vomiting, headaches, and seizures
* Opioids: withdrawal symptoms can include anxiety, muscle aches, sweating, nausea and vomiting, diarrhea, and depression
* Benzodiazepines: withdrawal symptoms can include anxiety, insomnia, tremors, and seizures

The diagnosis of substance withdrawal syndrome is typically made based on the patient's history of substance use and the presence of withdrawal symptoms. A healthcare provider may also order laboratory tests to rule out other conditions that may be causing the symptoms. Treatment for substance withdrawal syndrome usually involves supportive care, such as rest, hydration, and pain management, as well as medication to manage withdrawal symptoms. In some cases, medical professionals may also recommend a gradual tapering of the substance over a period of time to minimize withdrawal symptoms.

It is important for individuals who are experiencing withdrawal symptoms to seek medical attention as soon as possible, as untreated withdrawal can lead to serious complications, such as seizures and dehydration. With appropriate treatment, most individuals with substance withdrawal syndrome can recover fully and successfully overcome their addiction.

Dyskinesias can be caused by a variety of drugs, including:

1. Antipsychotic medications: These drugs are commonly used to treat conditions such as schizophrenia and bipolar disorder.
2. Antidepressant medications: Certain antidepressants, such as selective serotonin reuptake inhibitors (SSRIs), can cause dyskinesias.
3. Anti-anxiety medications: Benzodiazepines can cause dyskinesias, especially at high doses or with long-term use.
4. Opioids: These drugs can cause dyskinesias as a side effect, particularly when taken in high doses or for prolonged periods.
5. Antihistamines: Some antihistamines can cause dyskinesias, especially in older adults.
6. Anticonvulsants: Certain anticonvulsant medications, such as valproate and carbamazepine, can cause dyskinesias.
7. Corticosteroids: Long-term use of corticosteroids can lead to dyskinesias, especially in the face and limbs.

The symptoms of drug-induced dyskinesias can vary depending on the type of medication being taken and the individual's response to it. Common symptoms include:

1. Involuntary movements of the face, arms, legs, or trunk
2. Jerky or twitching movements
3. Tremors or shaking
4. Slow, rigid movements
5. Lack of coordination and balance
6. Difficulty with speech and swallowing
7. Fatigue and weakness

If you are experiencing dyskinesias as a result of medication, it is important to speak with your healthcare provider. They may be able to adjust your medication regimen or recommend alternative treatments to help manage the symptoms. In some cases, discontinuing the medication that is causing the dyskinesias may be necessary. Additionally, your healthcare provider may recommend other therapies, such as physical therapy or speech therapy, to help improve your mobility and communication skills.

MRI can occur in various cardiovascular conditions, such as myocardial infarction (heart attack), cardiac arrest, and cardiac surgery. The severity of MRI can range from mild to severe, depending on the extent and duration of the ischemic event.

The pathophysiology of MRI involves a complex interplay of various cellular and molecular mechanisms. During ischemia, the heart muscle cells undergo changes in energy metabolism, electrolyte balance, and cell membrane function. When blood flow is restored, these changes can lead to an influx of calcium ions into the cells, activation of enzymes, and production of reactive oxygen species (ROS), which can damage the cells and their membranes.

The clinical presentation of MRI can vary depending on the severity of the injury. Some patients may experience chest pain, shortness of breath, and fatigue. Others may have more severe symptoms, such as cardiogenic shock or ventricular arrhythmias. The diagnosis of MRI is based on a combination of clinical findings, electrocardiography (ECG), echocardiography, and cardiac biomarkers.

The treatment of MRI is focused on addressing the underlying cause of the injury and managing its symptoms. For example, in patients with myocardial infarction, thrombolysis or percutaneous coronary intervention may be used to restore blood flow to the affected area. In patients with cardiac arrest, cardiopulmonary resuscitation (CPR) and other life-saving interventions may be necessary.

Prevention of MRI is crucial in reducing its incidence and severity. This involves aggressive risk factor management, such as controlling hypertension, diabetes, and dyslipidemia, as well as smoking cessation and stress reduction. Additionally, patients with a history of MI should adhere to their medication regimen, which may include beta blockers, ACE inhibitors or ARBs, statins, and aspirin.

In conclusion, myocardial injury with ST-segment elevation (MRI) is a life-threatening condition that requires prompt recognition and treatment. While the clinical presentation can vary depending on the severity of the injury, early diagnosis and management are crucial in reducing morbidity and mortality. Prevention through aggressive risk factor management and adherence to medication regimens is also essential in preventing MRI.

Myocardial ischemia can be caused by a variety of factors, including coronary artery disease, high blood pressure, diabetes, and smoking. It can also be triggered by physical exertion or stress.

There are several types of myocardial ischemia, including:

1. Stable angina: This is the most common type of myocardial ischemia, and it is characterized by a predictable pattern of chest pain that occurs during physical activity or emotional stress.
2. Unstable angina: This is a more severe type of myocardial ischemia that can occur without any identifiable trigger, and can be accompanied by other symptoms such as shortness of breath or vomiting.
3. Acute coronary syndrome (ACS): This is a condition that includes both stable angina and unstable angina, and it is characterized by a sudden reduction in blood flow to the heart muscle.
4. Heart attack (myocardial infarction): This is a type of myocardial ischemia that occurs when the blood flow to the heart muscle is completely blocked, resulting in damage or death of the cardiac tissue.

Myocardial ischemia can be diagnosed through a variety of tests, including electrocardiograms (ECGs), stress tests, and imaging studies such as echocardiography or cardiac magnetic resonance imaging (MRI). Treatment options for myocardial ischemia include medications such as nitrates, beta blockers, and calcium channel blockers, as well as lifestyle changes such as quitting smoking, losing weight, and exercising regularly. In severe cases, surgical procedures such as coronary artery bypass grafting or angioplasty may be necessary.

There are many different types of seizures, each with its own unique set of symptoms. Some common types of seizures include:

1. Generalized seizures: These seizures affect both sides of the brain and can cause a range of symptoms, including convulsions, loss of consciousness, and muscle stiffness.
2. Focal seizures: These seizures affect only one part of the brain and can cause more specific symptoms, such as weakness or numbness in a limb, or changes in sensation or vision.
3. Tonic-clonic seizures: These seizures are also known as grand mal seizures and can cause convulsions, loss of consciousness, and muscle stiffness.
4. Absence seizures: These seizures are also known as petit mal seizures and can cause a brief loss of consciousness or staring spell.
5. Myoclonic seizures: These seizures can cause sudden, brief muscle jerks or twitches.
6. Atonic seizures: These seizures can cause a sudden loss of muscle tone, which can lead to falls or drops.
7. Lennox-Gastaut syndrome: This is a rare and severe form of epilepsy that can cause multiple types of seizures, including tonic, atonic, and myoclonic seizures.

Seizures can be diagnosed through a combination of medical history, physical examination, and diagnostic tests such as electroencephalography (EEG) or imaging studies. Treatment for seizures usually involves anticonvulsant medications, but in some cases, surgery or other interventions may be necessary.

Overall, seizures are a complex and multifaceted symptom that can have a significant impact on an individual's quality of life. It is important to seek medical attention if you or someone you know is experiencing seizures, as early diagnosis and treatment can help to improve outcomes and reduce the risk of complications.

Hyperkinesis can manifest in different ways, including:

1. Excessive movement or restlessness: This can include fidgeting, pacing, or other forms of constant motion.
2. Involuntary movements: These can include tremors, tics, or other sudden, uncontrolled movements.
3. Overactive behavior: This can include rapid speaking, excessive talking, or other behaviors that are not typical for the individual.
4. Difficulty sitting still or remaining quiet: This can be due to an inability to focus or a sense of inner restlessness or agitation.
5. Increased energy levels: This can result in excessive physical activity, such as running, jumping, or other forms of high-energy behavior.

Hyperkinesis can have a significant impact on daily life, making it difficult to focus, complete tasks, and maintain relationships. It is important to seek medical attention if symptoms persist or worsen over time, as hyperkinesis can be a sign of an underlying neurological or psychiatric condition that requires treatment.

Reperfusion injury can cause inflammation, cell death, and impaired function in the affected tissue or organ. The severity of reperfusion injury can vary depending on the duration and severity of the initial ischemic event, as well as the promptness and effectiveness of treatment to restore blood flow.

Reperfusion injury can be a complicating factor in various medical conditions, including:

1. Myocardial infarction (heart attack): Reperfusion injury can occur when blood flow is restored to the heart muscle after a heart attack, leading to inflammation and cell death.
2. Stroke: Reperfusion injury can occur when blood flow is restored to the brain after an ischemic stroke, leading to inflammation and damage to brain tissue.
3. Organ transplantation: Reperfusion injury can occur when a transplanted organ is subjected to ischemia during harvesting or preservation, and then reperfused with blood.
4. Peripheral arterial disease: Reperfusion injury can occur when blood flow is restored to a previously occluded peripheral artery, leading to inflammation and damage to the affected tissue.

Treatment of reperfusion injury often involves medications to reduce inflammation and oxidative stress, as well as supportive care to manage symptoms and prevent further complications. In some cases, experimental therapies such as stem cell transplantation or gene therapy may be used to promote tissue repair and regeneration.

Body weight is an important health indicator, as it can affect an individual's risk for certain medical conditions, such as obesity, diabetes, and cardiovascular disease. Maintaining a healthy body weight is essential for overall health and well-being, and there are many ways to do so, including a balanced diet, regular exercise, and other lifestyle changes.

There are several ways to measure body weight, including:

1. Scale: This is the most common method of measuring body weight, and it involves standing on a scale that displays the individual's weight in kg or lb.
2. Body fat calipers: These are used to measure body fat percentage by pinching the skin at specific points on the body.
3. Skinfold measurements: This method involves measuring the thickness of the skin folds at specific points on the body to estimate body fat percentage.
4. Bioelectrical impedance analysis (BIA): This is a non-invasive method that uses electrical impulses to measure body fat percentage.
5. Dual-energy X-ray absorptiometry (DXA): This is a more accurate method of measuring body composition, including bone density and body fat percentage.

It's important to note that body weight can fluctuate throughout the day due to factors such as water retention, so it's best to measure body weight at the same time each day for the most accurate results. Additionally, it's important to use a reliable scale or measuring tool to ensure accurate measurements.

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

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https://en.wikipedia.org/wiki/N6-Cyclopentyladenosine

"Repeated treatment with adenosine A1 receptor agonist and antagonist modifies the anticonvulsant properties of CPPene". ... 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. ... It has been used to study the function of the adenosine A1 receptor in animals, which has been found to be involved in several ...

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

Tecadenoson is an effective A1 adenosine agonist, as is selodenoson. The A1, together with A2A receptors of endogenous ... 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

2-Chloro-N6-cyclopentyladenosine (CCPA) is a specific receptor agonist for the Adenosine A1 receptor. It is similar to N6- ... a high affinity agonist radioligand for A1 adenosine receptors". Naunyn-Schmiedeberg's Archives of Pharmacology. 340: 679-683. ... Adenosine receptor agonists, Cyclopentanes, All stub articles, Nervous system drug stubs). ...

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... which has been shown to be an inverse agonist for adenosine A1 receptor sites. Hydrophilic extractions of the herb commonly ... Identification of isovaltrate as an inverse agonist at A1 receptors". Biochemical Pharmacology. 73 (2): 248-58. doi:10.1016/j. ... Valerenic acid in valerian stimulates GABA(A) and serotonin receptors as a positive allosteric modulator and partial agonist, ... Holzl J, Godau P (1989). "Receptor binding studies with Valeriana officinalis on the benzodiazepine receptor". Planta Medica. ...

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Activation of the adenosine A1 receptor by an agonist causes binding of Gi1/2/3 or Go protein. Binding of Gi1/2/3 causes an ... The adenosine A1 receptor is one member of the adenosine receptor group of G protein-coupled receptors with adenosine as ... A1 receptors are also present in smooth muscle throughout the vascular system. The adenosine A1 receptor has been found to be ... July 2022). "Selective activation of Gαob by an adenosine A1 receptor agonist elicits analgesia without cardiorespiratory ...

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Adenosine modulates the preBötC output via activation of the A1 and A2A receptor subtypes. An adenosine A1 receptor agonist has ... 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- ... Since many of these neurons express GABA, glutamate, serotonin and adenosine receptors, chemicals custom tailored to bind at ...

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

There are four well-known adenosine receptors found in the body, A1, A2A, A2B, and A3. The endogenous agonist for these ... Adenosine is a normal neuromodulator that activates adenosine g-protein coupled receptors. The actions of A1 and A2A receptors ... 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 ... 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

"Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ... adenosine (YT-146), a selective adenosine A2 receptor agonist, involve the opening of glibenclamide-sensitive K+ channels". ... 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

... with high selectivity over the other three adenosine receptor subtypes (ki values at human A1, A2A and A2B receptors are 4.1, ... structure-activity relationships and characterization of potent and selective inverse agonists at Human A3 adenosine receptors ... PSB-10 is a drug which acts as a selective antagonist for the adenosine A3 receptor (ki value at human A3 receptor is 0.44 nM ... Bilkei-Gorzo A, Abo-Salem OM, Hayallah AM, Michel K, Müller CE, Zimmer A (March 2008). "Adenosine receptor subtype-selective ...

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

... histamine H3 receptor, μ opioid receptor, NMDA receptor, and adenosine A1 receptor. D1-D2 receptor complex D1−H3−NMDAR receptor ... D1-NMDAR receptor complex D1-A1 receptor complex Several CryoEM structures of agonists bound to the dopamine D1 receptor ... All of these drugs are preferentially D2-like receptor agonists. Fenoldopam is a selective D1 receptor partial agonist that ... The D1 receptor forms heteromers with the following receptors: dopamine D2 receptor, dopamine D3 receptor, ...

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

... which triggers intracellular signal transduction via both adenosine A1 receptors and two sub-types of adenosine A2 receptors ( ... Moreover, minoxidil contains a nitric oxide moiety and may act as a nitric oxide agonist. This may cause follicles in the ... The expression of SUR2B in dermal papilla cells might play a role in the production of adenosine. Minoxidil induces cell growth ... Minoxidil is an adenosine 5'-triphosphate-sensitive potassium channel opener, causing hyperpolarization of cell membranes. ...

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

"The A2b adenosine receptor mediates cAMP responses to adenosine receptor agonists in human intestinal epithelia". The Journal ... 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 ... alkyl-2-alkynyl derivatives of adenosine as potent and selective agonists at the human adenosine A(3) receptor and a starting ...

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

... 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 ... receptor reserve is an integrative measure of the response-inducing capacity of an agonist (in some receptor models it is ... Hormone receptors Neuromodulator receptors Neurotransmitter receptors General anesthetics were once thought to work by ...

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

... adenosine A1, AMPA, mGluR2/3, mGlu5, and OX2 receptors. In the rat cerebellum, the protein has also been found in the Golgi ... The 5-HT2A receptor is known primarily to couple to the Gαq signal transduction pathway. Upon receptor stimulation with agonist ... OSU-6162 acts as a partial agonist at both 5-HT2A and dopamine D2 receptors Quipazine, 5-HT2A agonist but also potent 5-HT3 ... The 5-HT2A receptor is a subtype of the 5-HT2 receptor that belongs to the serotonin receptor family and is a G protein-coupled ...

https://en.wikipedia.org/wiki/5-HT2A_receptor

"Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ... This is a valuable guide to design potential 5HT1D receptor agonists. When sumatriptan binds there is major conformational ... 5-hydroxytryptamine (serotonin) receptor 1D, also known as HTR1D, is a 5-HT receptor, but also denotes the human gene encoding ... Goadsby, P.J., Serotonin 5-HT1B/1D receptor agonists in migraine - Comparative pharmacology and its therapeutic implications. ...

https://en.wikipedia.org/wiki/5-HT1D_receptor

... a novel specific adenosine A(3) receptor antagonist with adenosine A(3) receptor agonists both in vitro and in vivo". Eur. J. ... 1999). "Cardiac myocytes rendered ischemia resistant by expressing the human adenosine A1 or A3 receptor". FASEB J. 12 (15): ... a novel ligand that demonstrates both adenosine A(2A) receptor agonist and adenosine A(3) receptor antagonist activity". ... is an adenosine receptor, but also denotes the human gene encoding it. Adenosine A3 receptors are G protein-coupled receptors ...

https://en.wikipedia.org/wiki/Adenosine_A3_receptor

ATP targets P2X receptors, P2Y, and A1 receptors. ATP has several functions as a gliotransmitter, including insertion of AMPA ... Other less common gliotransmitters include: homocysteic acid, an endogenous N-methyl-(D)-aspartic acid receptor (NMDAR) agonist ... activity is controlled in the retina by the molecule's ability to hyperpolarize the neuron by converting from ATP to adenosine ... Its main target receptors include Kainate receptors, metabotropic glutamate receptors (mGluRs), and especially N-methyl D- ...

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

... consist of Isoreceptors D1-D2 D1-D3 D2-D3 D2-D4 D2-D5 Non-isoreceptors D1-adenosine A1 D2-adenosine A2A D2-ghrelin receptor ... unless blocked by a receptor antagonist or a synthetic partial agonist. D3 is encoded by the Dopamine receptor D3 gene (DRD3). ... "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

Structure of the adenosine A1 receptor reveals the basis for subtype selectivity. Cell 168: 867-877. Bradley, S.J., Bourgognon ... Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist. Proc. ... Structure of the adenosine-bound human A1 receptor-Gi complex. Nature 558: 559-563. Harvey Motulsky, Arthur Christopoulos. ... Positive allosteric mechanisms of adenosine A1 receptor-mediated analgesia. Nature 597: 571-576. Josephs, T.M., Belousoff, M.J ...

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

... specifically the A1-D1 receptor heterodimer (this is a receptor complex with 1 adenosine A1 receptor and 1 dopamine D1 receptor ... "Allosteric interactions between agonists and antagonists within the adenosine A2A receptor-dopamine D2 receptor heterotetramer ... a receptor complex composed of 1 adenosine A1 receptor and 1 adenosine A2A receptor) in the axon terminal of glutamate neurons ... this is a receptor complex with 2 adenosine A2A receptors and 2 dopamine D2 receptors). The A2A-D2 receptor heterotetramer has ...

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

It is believed it acts as an adenosine A2A receptor neutral antagonist or as an inverse agonist. Caffeine's A2A receptor ... 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- ...

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

... adenosine receptor binding affinity (21 μM for A1, 32 μM for A2A, 4.5 μM for A2B, and >100 for μM for A3) is ... "Adenosine receptors: development of selective agonists and antagonists". Progress in Clinical and Biological Research. 230 (1 ... Müller, Christa E.; Jacobson, Kenneth A. (2011), Fredholm, Bertil B. (ed.), "Xanthines as Adenosine Receptor Antagonists", ... Studies indicate that, similar to caffeine, simultaneous antagonism of adenosine receptors is responsible for paraxanthine's ...

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

... muscarinic acetylcholine receptor M4, and adenosine receptor A1. The direct pathway has been proposed to facilitate motor ... This model of direct D1, and indirect D2 pathways explain why selective agonists of each receptor are not rewarding, as ... This pathway consists of MSNs that express dopamine receptor D2, muscarinic acetylcholine receptor M1, and adenosine receptor ... "Adenosine-cannabinoid receptor interactions. Implications for striatal function". British Journal of Pharmacology. 160 (3): 443 ...

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

The other three adenosine receptors are involved in bone formation. In Alzheimer's disease (AD), the expression of A1 and A2A ... Cerqueira MD (July 2004). "The future of pharmacologic stress: selective A2A adenosine receptor agonists". The American Journal ... 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

"Control of Cannabinoid CB1 Receptor Function on Glutamate Axon Terminals by Endogenous Adenosine Acting at A1 Receptors". ... Ma, D.; Rajakumaraswamy, N.; Maze, M. (2004). "2-Adrenoceptor agonists: Shedding light on neuroprotection?". British Medical ... "Regulation of Hippocampal Cannabinoid CB1 Receptor Actions by Adenosine A1 Receptors and Chronic Caffeine Administration: ... v t e v t e (CS1: long volume value, Receptors, Cell signaling, All stub articles, Receptor stubs, Molecular and cellular ...

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

... cannabinoid receptor 1 and CB1-OX1 receptor heterodimers, adenosine A1 receptors, muscarinic M3 receptors, serotonin 5-HT1A ... Orexin receptor agonists). ... Orexin receptor subtypes readily formed homo- and hetero(di) ... Liu ZW, Gao XB (January 2007). "Adenosine inhibits activity of hypocretin/orexin neurons by the A1 receptor in the lateral ... CB1 receptors formed homodimers, and they also heterodimerized with both orexin receptors. ... In conclusion, orexin receptors ...

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

... and hydroxycarboxylic acid receptor 3 (HCA3), which are highly expressed in body fat. HCA2 and HCA3 inhibit cyclic adenosine ... GABAA receptor positive allosteric modulators, GPER agonists, Hypolipidemic agents, 3-Pyridyl compounds, Multiple Chemboxes). ... Niacin increases apolipoprotein A1 levels by inhibiting the breakdown of this protein, which is a component of HDL-C. It also ... reduced synthesis of neuro-protective brain-derived neurotrophic factor or its receptor tropomyosin receptor kinase B; or E) ...

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

... receptors are glutamate receptors particularly important in long-term potentiation in neurons. These receptors have been linked ... Funk, C.K. and Koob, G.F. (2007). A CRF2 agonist administered into the central nucleus of the amygdala decreases ethanol self- ... Katsura, M., Shibasaki, M., Hayashida, S., Torigoe, F., Tsujimura, A., Ohkuma, S. (2006) Increase in expression of a1 and a2/d1 ... Pandey, S.C., Roy, A., Zhang, H. (2003). The decreased phosphorylation of cyclic adenosine monophosphate (cAMP) response ...

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

... they also express adenosine A1 receptors), while dynorphinergic MSNs connect the striatum with the substantia nigra (pars ... Microinjections of μ-opioid agonists, δ-opioid agonists or κ-opioid agonists in the rostrodorsal quadrant of the medial shell ... 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

p. A1. Shingo Kajimura (27 August 2009). "Initiation of myoblast/brown fat switch through a PRDM16-C/EBP-β transcriptional ... The mitochondria in a eukaryotic cell utilize fuels to produce adenosine triphosphate (ATP). This process involves storing ... Pharmacological approaches using β3-adrenoceptor agonists have been shown to enhance glucose metabolic activity of brown ... "Quantitative assessment of brown adipose tissue metabolic activity and volume using 18F-FDG PET/CT and β3-adrenergic receptor ...

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

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 ... transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, and G protein-linked receptors ( ... January 2011). "The structural basis for agonist and partial agonist action on a β(1)-adrenergic receptor". Nature. 469 (7329 ...

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

IP3 receptor and ryanodine receptor and this has recently been borne out by the molecular identification of the NAADP receptor ... As noted above, this usually entails collapsing the H+ gradient with either V-ATPase inhibitors (e.g. Bafilomycin A1) or ... Like its mechanistic cousins, IP3 and cyclic adenosine diphosphoribose (Cyclic ADP-ribose), NAADP binds to and opens Ca2+ ... Cancela, Jose Manuel; Churchill, Grant C.; Galione, Antony (1999). "Coordination of agonist-induced Ca2+-signalling patterns by ...

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

Within the cell, bafilomycin A1 specifically interacts with the proton pump V-ATPase. This large protein depends on Adenosine ... its acidification of endosomes is critical in receptor endocytosis as low pH tends to drive ligand release as well as receptor ... The lipophilic agent xylometazoline, an alpha-adrenoreceptor agonist, displayed an increased effect when administered after ... When one of these drugs is co-applied to cells with bafilomycin A1, the action of bafilomycin A1 prevents the acidification of ...

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

... receptor (A,sub,1,/sub,R) is implicated in pain, sleep, substance use disorders, and neurodegenerative diseases, and is an ... Representative adenosine receptor (radio)ligands and affinities at human adenosine receptors. A). Adenosine antagonist ligands ... Representative adenosine receptor (radio)ligands and affinities at human adenosine receptors. A). Adenosine antagonist… ... Use of 11C-MPDX and PET to study adenosine A1 receptor occupancy by nonradioactive agonists and antagonists. Paul S, Khanapur S ...

https://www.ncbi.nlm.nih.gov/pubmed/30359014

Regulated hypothermia in mouse is caused by AMP, adenosine A1 and A3 receptor agonists via three distinct mechanisms. Thursday ... However, AMP-induced torpor was intact in mice lacking any one of the adenosine receptors (A1AR, A2AAR, A2BAR, or A3AR). Our ... Adenosine is thought to act through A1AR in the nucleus of the solitary tract or pre-optic area to elicit hypothermia in ... Adenosine and AMP have been implicated in triggering the torpor response seen in small mammals during hibernation or fasting. ...

https://researchfestival.nih.gov/2016/posters/regulated-hypothermia-mouse-caused-amp-adenosine-a1-and-a3-receptor

Receptor, Adenosine A1/agonists. Adenosine A1 Receptor Agonists. Receptor, Adenosine A1/antagonists & inhibitors ...

https://www.nlm.nih.gov/pubs/techbull/nd10/nd10_entry_combo_table.html

T1 - New fluorescent adenosine A1-receptor agonists that allow quantification of ligand-receptor interactions in microdomains ... title = "New fluorescent adenosine A1-receptor agonists that allow quantification of ligand-receptor interactions in ... New fluorescent adenosine A1-receptor agonists that allow quantification of ligand-receptor interactions in microdomains of ... New fluorescent adenosine A1-receptor agonists that allow quantification of ligand-receptor interactions in microdomains of ...

https://research.nottingham.edu.cn/en/publications/new-fluorescent-adenosine-asub1sub-receptor-agonists-that-allow-q

The effect of GR190178, a selective low-efficacy adenosine A1 receptor agonist, on the treatment of neuropathic hyperalgesia in ... The effect of GR190178, a selective low-efficacy adenosine A1 receptor agonist, on the treatment of neuropathic hyperalgesia in ...

https://www.cmd.ox.ac.uk/publications/37780?f34b9846-03f8-11ee-9c14-0a3af28e70c2

... and examined the potential of the three compounds as PET ligands for CNS adenosine A1 receptors. The three compounds had hig … ... Discovery of Highly Potent Adenosine A1 Receptor Agonists: Targeting Positron Emission Tomography Probes. Guo M, Bakhoda A, Gao ... Evaluation of carbon-11 labeled KF15372 and its ethyl and methyl derivatives as a potential CNS adenosine A1 receptor ligand J ... Evaluation of carbon-11 labeled KF15372 and its ethyl and methyl derivatives as a potential CNS adenosine A1 receptor ligand J ...

https://pubmed.ncbi.nlm.nih.gov/9080475

NIDDK releases highly selective A1 adenosine receptor (AR) agonist ... NIDDK announces the availability of a highly selective A1 adenosine receptor (AR) agonist. This receptor is neuroprotective in ... Adenosine receptor agonists, partial agonists, and antagonists (U.S. Patent Number 13/479,973). ... Adenosine receptor agonists, partial agonists, and antagonists (U.S. Patent Number 13/479,973) ...

https://www.niddk.nih.gov/research-funding/technology-advancement-transfer/research-materials-licensing/adenosine-receptor-agonists

4. AMP is an adenosine A1 receptor agonist.. Rittiner JE; Korboukh I; Hull-Ryde EA; Jin J; Janzen WP; Frye SV; Zylka MJ. J Biol ... 7. Rolofylline, an adenosine A1 receptor antagonist, inhibits osteoclast differentiation as an inverse agonist.. He W; Wilder T ... Endogenous activation of adenosine A1 receptors, but not P2X receptors, during high-frequency synaptic transmission at the ... Presynaptic A1 inhibitory/A2A facilitatory adenosine receptor activation balance depends on motor nerve stimulation paradigm at ...

https://pubmedhh.nlm.nih.gov/biomarkers/search.php?id=34905223&mod=related&page=1&outid=&proj=

Antagonist of adenosine A1 receptors and dopamine D1 receptors eliminated rapid tolerance development as does ketamine, a ... The GABA B receptor agonist, baclofen blocked tolerance while two specific GABA B receptor antagonists facilitated tolerance ... Furthermore, the GABA B receptor agonist reversed the action of the receptor antagonists. ... A signal transduction cascade involving the glutamate receptor delta2 protein, the Ephrin B3 ligand, the NMDA receptor, the ...

https://grants.nih.gov/grants/guide/rfa-files/RFA-AA-08-010.html

Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS.. Terms. Adenosine A1 Receptor Agonists Preferred Term Term UI ... Adenosine A1 Receptor Agonists [D27.505.519.625.725.200.100.100] * Adenosine A2 Receptor Agonists [D27.505.519.625.725.200. ... Adenosine A1 Receptor Agonists [D27.505.696.577.725.200.100.100] * Adenosine A2 Receptor Agonists [D27.505.696.577.725.200. ... Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS.. Registry Number. 0. Previous Indexing. Receptor, Adenosine A1/ ...

https://meshb.nlm.nih.gov/record/ui?ui=D058907

MeSH Terms: Adenosine A1 Receptor Agonists/pharmacology; Adenosine A1 Receptor Agonists/therapeutic use; Adenosine/analogs & ... we pharmacologically preconditioned male and female hearts with the adenosine A1 receptor agonist N6-cyclohexyl adenosine (CHA ... Title: Adenosine A1 receptor activation increases myocardial protein S-nitrosothiols and elicits protection from ischemia- ... Receptor, Adenosine A1/metabolism*; Recovery of Function/drug effects; Reperfusion Injury/drug therapy; Reperfusion Injury/ ...

https://tools.niehs.nih.gov/portfolio/index.cfm?do=portfolio.publicationDetail&id=3278433

Adenosine and its analogues potently suppress nociception in preclinical models by activating A1 and/or A3 adenosine receptors( ... or direct blockade of CGRP or its receptor. Lasmiditan is a highly selective 5-HT receptor agonist and, unlike the triptans, is ... Normally, opioids function in a receptor-dependent manner. They bind to opioid receptors, activate or inhibit receptor ... Alleviating pain with delta opioid receptor agonists: evidence from experimental models. The use of opioids for the relief of ...

https://www.iasp-pain.org/pow-issue/2020-03-14/

... and that this decline may be caused by a decrease in coupling between adenosine A1 receptors (AdoA1R) and guanine nucleotide- ... Previously published reports from this laboratory have shown that the antiadrenergic effect of adenosine A1 agonists declines ... Adrenergic and Adenosine A,sub,1,/sub, Receptor Function in the Heart Are Attenuated by Dietary Restriction DP - 1998 Apr 01 TA ... In AL rats, inhibition of ISO-stimulated adenylyl cyclase by the AdoA1R agonist, N6-p-sulfophenyladenosine (SPA) decreased with ...

https://jpet.aspetjournals.org/highwire/citation/36396/medlars

CGS 15943 was consistent with the labeling of brain adenosine A1 receptors. Adenosine agonists inhibited 1 nM [3H]CGS 15943 ... In contrast, adenosine A1 agonist competition curves were shallow, as indicated by Hill coefficients less than unity. Computer ... to multiple affinity states of the adenosine A1 receptor in the rat cortex.. M F Jarvis, M Williams, U H Do and M A Sills ... to multiple affinity states of the adenosine A1 receptor in the rat cortex.. M F Jarvis, M Williams, U H Do and M A Sills ...

https://molpharm.aspetjournals.org/content/39/1/49

13151 Adenosine A1 receptor agonist 25406 Adenosine A1 receptor antagonist 8460 Adenosine A2 receptor agonist 16326 Adenosine ... 35017 Adenosine A2a receptor agonist 24353 Adenosine A2a receptor antagonist 9116 Adenosine A3 receptor agonist 130827 ... 13123 Adenosine deaminase inhibitor 50463 Adenosine kinase inhibitor 8501 Adenosine receptor agonist 21556 Adenosine receptor ... 81942 GABA A receptor agonist 77515 GABA A receptor antagonist 98060 GABA B receptor agonist 64771 GABA B receptor antagonist ...

https://cactus.nci.nih.gov/ncidb2.2/PASS_Predictions.txt

Adenosine A1 Receptor Agonists - Preferred Concept UI. M0545333. Scope note. Compounds that bind to and stimulate ADENOSINE A1 ... Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS.. Allowable Qualifiers:. AD administration & dosage. AE adverse ... Adenosine A1 Receptor Agonists [D27.505.519.625.725.200.100.100] Adenosine A1 Receptor Agonists ... Adenosine A1 Receptor Agonists [D27.505.696.577.725.200.100.100] Adenosine A1 Receptor Agonists ...

https://decs.bvsalud.org/en/ths/resource/?id=54156&filter=ths_regid&q=D058907

https://meshb-prev.nlm.nih.gov/record/ui?ui=D058907

... and systemic application of an A2 receptor agonist has been shown to suppress breathing by a GABAergic-dependent mechanism ( ... suggesting blockade of A1 receptors did not reveal roles for A2 or A3 receptors that were otherwise masked by A1 receptor ... Sichardt K, Nieber K (2007) Adenosine A(1) receptor: functional receptor-receptor interactions in the brain. Purinergic Signal ... Adenosine A1 receptors are Gi/Go-coupled and in other brain regions are known to inhibit neural activity by presynaptic and ...

https://www.eneuro.org/content/5/6/eneuro.0404-18.2018

The Histamine H4 Receptor Participates in the Anti-Neuropathic Effect of the Adenosine A3 Receptor Agonist IB-MECA: Role of CD4 ... Receptor A1 de Adenosina/genética , Receptor A2A de Adenosina/genética , Receptor A2B de Adenosina/genética , Receptor A3 de ... Receptor A1 de Adenosina/metabolismo , Receptor A2A de Adenosina/metabolismo , Receptor A2B de Adenosina/metabolismo , Receptor ... The A1, A2A, A2B and A3 adenosine receptors serve to regulate immune function. Despite characterization of the adenosine ...

https://pesquisa.bvsalud.org/controlecancer/?lang=pt&q=mh:Receptor+A3+de+Adenosina/gen%C3%A9tica

cAMPNOMAD Adenosine A1 Receptor Cell Line 9.995,00€. cAMPNOMAD Cells are cell lines stably co-expressing tag-free GPCRs and ... When an agonist binds to M5 Receptor, the Gq/G11 protein is activated which, in turn, triggers a cellular response mediated by ... Each vial of cAMPNOMAD Adenosine A1 Receptor Cell Line contains HEK293 cells stably expressing the following constructs:. * ... cAMPNOMAD Adenosine A3 Receptor Cell Line 9.995,00€. cAMPNOMAD Cells are cell lines stably co-expressing tag-free GPCRs and ...

https://innoprot.com/product-tag/gpcr/

... more important than A1 AR because A2B AR inhibition by MRS1754 completely reversed the effect of the adenosine receptor agonist ... Using intravital microscopy we investigated the effects of the adenosine receptor (AR) agonist NECA (5′-N-ethyl carboxamide ... Keywords: Adenosine, adenosine receptor, intestine, microcirculation, intravital microscopy, ischemia, reperfusion, leukocyte ... Adenosine receptor activation improves microcirculation in experimental intestinal ischemia/reperfusion Authors: Zhou, Juan , ...

https://content.iospress.com/journals/clinical-hemorheology-and-microcirculation/59/3

... a specific adenosine A1 receptor agonist, in a similar manner. To examine adenosine receptor subtype involved in inhibition of ... Glutamate release evoked by the TRPV-1 receptor agonist, capsaicin, was measured. Adenosine with or without adenosine A1 and A2 ... the mechanisms by which A1adenosine receptor agonists cause pain relief are incompletely understood. A1adenosine receptor ... Yamamoto S, Nakanishi O, Matsui T, Shinohara N, Kinoshita H, Lambert C, Ishikawa T: Intrathecal adenosine A1 receptor agonist ...

https://pubs.asahq.org/anesthesiology/article/103/5/1060/6886/Adenosine-Reduces-Glutamate-Release-in-Rat-Spinal

... adenosine A1 receptor agonist, selective and high-affinity * GC17408 (±)-AC 7954 hydrochloride urotensin-II (UT) receptor ... GC11577 α-Methyl-5-hydroxytryptamine maleate 5-HT2B receptor agonist * GC31237 α1 adrenoceptor-MO-1 α1 adrenoceptor-MO-1, S 거울상 ... GC17301 (+)-SK&F 10047 hydrochloride prototypical σ1 receptor agonist * GC10675 (+,-)-Octopamine HCl 노르아드레날린과 구조적으로 관련된 생체 ... GA20063 (D-Ala²)-Gastric Inhibitory Polypeptide (human) GIP receptor agonist. * GA20084 (Deamino-Cys¹,β-cyclohexyl-Ala⁴,Arg⁸)- ...

https://www.glpbio.com/kr/research-area/gpcr-g-protein.html

The application of adenosine A1 receptor agonists in regard to cerebral disorders is hampered by serious cardiovascular side ... The objective of this study was to characterize the effects of the adenosine A1 receptor agonist N6-cyclopentyladenosine (CPA) ... Therapeutic efficacy of the adenosine A1 receptor agonist N6-cyclopentyladenosine (CPA) against organophosphate intoxication ... Low efficacy adenosine A1 agonists inhibit striatal acetylcholine release in rats improving central selectivity of action ...

https://repository.tno.nl/islandora/search/subject%3A%22Corpus%255C%2BStriatum%22

A Selective A Adenosine Receptor Agonist, Reduces Myocardial Infarct Size in a Rat Ischemia/Reperfusion Model ... An adenosine A1 receptor agonist, R(-)-N-(2-phenylisopropyl)-adenosine (PIA), but not adenosine itself, acts as a therapeutic ... 2] demonstrated that stimulation of adenosine receptors with an adenosine A1 receptor agonist, R(-)-N-(2-phenylisopropyl)- ... 12] administered adenosine A1/A2 receptor agonist AMP 579 before ischemia (bolus loading dose i.v. followed by continuous i.v. ...

https://opencardiovascularmedicinejournal.com/VOLUME/3/PAGE/166/

Objectives: Adenosine and adenosine A1 receptor agonists exert protective effects against reperfusion injury in different ... The aim of the present study was to examine the effects of adenosine A1 /A2 receptor activation on reperfusion-induced small ... Conclusion: We offer additional evidence that activation of A1 /A2 adenosine receptors provides partial protection against ... non-selective A1 /A2 agonist, 0.1 mg/kg, i.v.)-treated I/R, and theophylline (non-selective A1 /A2 antagonist, 20 mg/kg, i.v.)- ...

https://acikarsiv.beun.edu.tr/?p=1&dil=0&q=&fq%5B%5D=Koleksiyon_strs:758&fq%5B%5D=Koleksiyon_strs:6&fq%5B%5D=Koleksiyon_strs%3A%22759%22

We recently found an A1 adenosine receptor agonist that has antiseizure effects in mice without some of the side effects ... A3 adenosine receptor agonists at low concentrations and P2Y6 receptor agonists have antiapoptotic effects. Furthermore, P2Y6 ... The determination of the X-ray crystallographic structures of the P2Y1 receptor and an agonist bound A2A adenosine receptor by ... in combination with receptor mutagenesis. The neoceptor concept has so far been applied to A1, A2A and A3 adenosine receptors. ...

https://irp.nih.gov/pi/kenneth-jacobson

Selective A3 Adenosine Receptor Agonists for the Treatment of Chronic Neuropathic Pain and Other Conditions *Read more about ... This technology relates to a group of compounds that display high affinity and specificity for the A1 adenosine receptor ... Adenosine modulates many physiological processes by activating specific adenosine receptors. These adenosine receptors play a ... This technology includes the creation and use of A3 adenosine receptor (A3AR)-selective agonists for treating chemotherapy- ...

https://www.techtransfer.nih.gov/taxonomy/term/265?page=25

1997 Persistent activation by and receptor reserve for an irreversible A1-adenosine receptor agonist in DDT1 MF-2 cells and in ... ethane appears to be an uncompetitive inverse agonist for the thyrotropin receptor.. ≫ ...

https://allie.dbcls.jp/short/exact/Any/DDT.html

The uptake of each compound was decreased by carrier KF15372, but not by an A2A antagonist, indicating the selective affinity for the A1 receptors. (nih.gov)
Synthesis and preliminary evaluation of [11C]KF15372, a selective adenosine A1 antagonist. (nih.gov)
2. The role of CGRP receptor antagonist (CGRP8-37) and Endomorphin-1 combination therapy on neuropathic pain alleviation and expression of Sigma-1 receptors and antioxidants in rats. (nih.gov)
Characterization of the binding of a novel nonxanthine adenosine antagonist radioligand, [3H]CGS 15943, to multiple affinity states of the adenosine A1 receptor in the rat cortex. (aspetjournals.org)
The triazoloquinazoline CGS 15943 is the first reported nonxanthine adenosine antagonist that has high affinity for brain adenosine receptors. (aspetjournals.org)
Agonist competition curves generated in the presence of 1 mM GTP resulted in a rightward shift and steepening of the inhibition-concentration curves, whereas antagonist binding was not altered in the presence of GTP. (aspetjournals.org)
Next, using a newly developed coculture system of isolated myenteric neurons and mucosal-type bone-marrow-derived mast cells (mBMMCs) with a calcium imaging system, we demonstrated that the stimulation of isolated myenteric neurons by veratridine caused the activation of mBMMCs, which was suppressed by the adenosine A3 receptor antagonist MRE 3008F20. (bvsalud.org)
14)Characterization of peptide 20-30 of follicle stimulating hormone receptor as an antagonist of receptor activity: significance of charged residues. (edu.in)
Blockade of capsaicin-evoked glutamate release by adenosine was reversed similarly in synaptosomes from normal and spinal nerve-ligated animals by an A1 adenosine receptor antagonist DPCPX (8-cyclopentyl-1,3-dipropylxanthine) but not by an A2 adenosine receptor antagonist DMPX (3'7-dimethyl-1-proparaglyxanthine). (asahq.org)
GC62708 σ1 Receptor antagonist-1 σ1 수용체 길항제-1은 매우 강력하고 선택적인 시그마 1 수용체 길항제입니다(pKi=10.28). (glpbio.com)
GC41668 (±)-Clopidogrel (hydrochloride) Clopidogrel is an antithrombic compound whose active metabolite is a selective, irreversible antagonist of the platelet purinergic P2Y12 receptor (IC50 = 100 nM). (glpbio.com)
N-ethylcarboxamidoadenosine (NECA) (non-selective A1 /A2 agonist, 0.1 mg/kg, i.v.)-treated I/R, and theophylline (non-selective A1 /A2 antagonist, 20 mg/kg, i.v.)-treated I/R groups. (beun.edu.tr)
A 2a receptor antagonist), or dimethyl sulfoxide (DMSO) administrations. (ijp-online.com)

The potency order for adenosine antagonists was CGS 15943 (IC50 = 5 nM) greater than 8-phenyltheophylline greater than 1,3-dipropyl-8-(4-amino-2-chloro)phenylxanthine greater than 1,3-diethyl-8-phenylxanthine greater than theophylline = caffeine (IC50 greater than 10,000 nM). (aspetjournals.org)
This work may also have clinical relevance since A1 receptor antagonists like caffeine are used to treat respiratory problems in premature infancy. (eneuro.org)
Adenosine with or without adenosine A1 and A2 receptor antagonists was applied to determine the efficacy and mechanism of adenosine to reduce capsaicin-evoked glutamate release. (asahq.org)
6-9 Peripheral noxious stimulation increases the release of glutamate from the rat dorsal spinal cord in vivo , 10 whereas pharmacologic and electrophysiologic studies indicate that glutamate receptor antagonists produce antinociceptive effects in rodents and humans. (asahq.org)
Our overall goals are to design, chemically synthesize, and characterize pharmacologically new agonists and antagonists for the four subtypes of adenosine receptors (ARs) and eight subtypes of P2Y receptors and to explore their potential for treating human disease conditions. (nih.gov)
I am a medicinal chemist with interests in the structure and pharmacology of receptors and in developing drugs that act as agonists or antagonists of G protein-coupled receptors (GPCRs). (nih.gov)
Recent accomplishments include the design and synthesis of the highly potent and selective A3 adenosine receptor agonists and antagonists, using a combination of library screening and optimization of known adenosine receptor ligands. (nih.gov)
We have synthesized the first P2Y1 receptor-selective antagonists through functionalization of adenine nucleotides. (nih.gov)
The antagonists were optimized with the aid of receptor homology modeling. (nih.gov)

To address the emerging need for fluorescently labeled ligands to support these technologies, we have developed a series of red-emitting agonists for the human adenosine A 1 -receptor that, collectively, are N 6 -aminoalkyl derivatives of adenosine or adenosine 5′-N-ethyl carboxamide. (nottingham.edu.cn)
These results show that three compounds have potential as PET ligands for CNS adenosine A1 receptors. (nih.gov)
The opioid system of mu, delta and kappa receptors (MOR, DOR, KOR) and their peptide ligands (β-endorphin, enkephalin, dynorphin) have complex and partially opposing effects on amygdala function. (iasp-pain.org)
26)New ligands for melanocortin receptors. (edu.in)
Novel ligands (small molecules) for these receptors are developed using classical synthetic approaches and also by semirational methods based on molecular modeling and template design. (nih.gov)
I am interested in how activation of one of these classes of receptor leads to modification of the response to other receptor classes (cross-talk), as well as how different ligands can provoke different signalling profiles at the same receptor (agonist bias). (nottingham.ac.uk)
Cannabinoid receptors and their ligands: beyond CB₁ and CB₂. (nottingham.ac.uk)
G protein-coupled receptor list: recommendations for new pairings with cognate ligands. (nottingham.ac.uk)

We report the presence of functional high-affinity IgE receptors (FcÎµRIs) in enteric neurons. (bvsalud.org)
Fluorescence Correlation Spectroscopy (FCS) studies with a fluorescent agonist (ABEA-X-BY630) demonstrated that both wild-type and mutant receptors bind agonist with high affinity but in subsequent downstream signaling assays the R108A mutation abolished agonist-mediated inhibition of cAMP production and ERK phosphorylation. (bvsalud.org)
This technology relates to a group of compounds that display high affinity and specificity for the A1 adenosine receptor subtype. (nih.gov)

The effect of GR190178, a selective low-efficacy adenosine A1 receptor agonist, on the treatment of neuropathic hyperalgesia in the rat. (ox.ac.uk)
14. Activation of spinal and supraspinal cannabinoid-1 receptors leads to antinociception in a rat model of neuropathic spinal cord injury pain. (nih.gov)
Treatment of chronic neuropathic pain: purine receptor modulation. (iasp-pain.org)
A3 adenosine receptor (A3AR) agonists have emerged as potent relievers of neuropathic pain by a T cell-mediated production of IL-10. (bvsalud.org)
4,5 The primary aim of the current study was to determine whether adenosine-mediated inhibition of spinal glutamate release was increased in an animal model of neuropathic pain, potentially providing an explanation for this selective effect of intrathecal adenosine in hypersensitive states. (asahq.org)
We recently published in collaboration with Daniela Salvemini of St. Louis University the protective effect of A3 agonists in animal models of neuropathic pain. (nih.gov)
We have discovered highly specific A3 agonists that reduce neuropathic pain in the mouse and rat and prevent its development. (nih.gov)
This technology includes the creation and use of A3 adenosine receptor (A3AR)-selective agonists for treating chemotherapy-induced peripheral neuropathy, chronic neuropathic pain, rheumatoid arthritis, psoriasis, and other conditions. (nih.gov)

The complex binding interactions found with adenosine agonists indicate that [3H]CGS 15943 labels both high and low affinity components of the adenosine A1 receptor in the rat cortex. (aspetjournals.org)
Additionally, the present data also provide some evidence that [3H]CGS 15943 may also recognize an additional low affinity binding component, which may represent a putative low affinity A2b receptor in this tissue. (aspetjournals.org)
The binding affinity of D1 receptors is 10 to 100-fold lower than D2 receptors. (brainmatrix.com)
The difference in affinity takes on significance as different temporal patterns of release and relative extracellular concentration of dopamine engage differently with D1 or D2 receptors. (brainmatrix.com)
[6] With their lower-affinity, D1 receptors are considered to activate in response to phasic dopamine signals in the micromolar range, whereas higher-affinity, D2 receptors respond to nanomolar, tonic levels. (brainmatrix.com)

15)Cross-Linking of a DOPA-Containing Peptide Ligand into its G Protein-Coupled Receptor. (edu.in)
Dopamine receptors belong to the 7 transmembrane, G protein-coupled receptor family (GPCRs). (brainmatrix.com)
The receptors belong to and are structurally homologous to the G-protein coupled receptor (GPCR) superfamily, and contain the requisite seven-transmembrane domains. (brainmatrix.com)

Fluorescence spectroscopy is becoming a valuable addition to the array of techniques available for scrutinizing ligand-receptor interactions in biological systems. (nottingham.edu.cn)
Visualization and confirmation of ligand-receptor interactions at the cell membrane were accomplished using confocal microscopy, and their suitability for use in FCS was demonstrated by quantification of agonist binding in small areas of cell membrane. (nottingham.edu.cn)
Advanced microscopy techniques have shown that these receptors can be localized to discrete microdomains and reorganization upon ligand activation is crucial in orchestrating their signaling. (bvsalud.org)
Receptors are computer-modeled by homology to GPCRs of known structure, and the models for ligand recognition are tested and refined using site-directed mutagenesis of the receptor proteins. (nih.gov)

The goal of this study was to characterize effects of adenosine on chemosensitive RTN neurons and identify intrinsic and synaptic mechanisms underlying this response. (eneuro.org)
The aim of the present study was to examine the effects of adenosine A1 /A2 receptor activation on reperfusion-induced small intestinal injury in rat. (beun.edu.tr)

PMID- 214398 TI - Characterization of an adenosine triphosphatase of the avian myeloblastosis virus and the virus-infected myeloblast. (nih.gov)

The objective of the present study was to characterize the effects of the full agonist N6-cyclopentyladenosine (CPA) and its. (tno.nl)
The objective of this study was to characterize the effects of the adenosine A1 receptor agonist N6-cyclopentyladenosine (CPA) and its low efficacy derivatives 2′-deoxy-CPA (2DCPA), 3′-deoxy-CPA (3DCPA), 8-ethylamino-CPA (8ECPA) and 8-butylamino-CPA (8BCPA) on the release of acetylcholine (ACh) using intrastriatal microdialysis. (tno.nl)

A3 receptors for adenosine are found in most cells and endogenous activation of the A3 receptors can result in apoptosis, thereby relieving the inflammation or targeting a tumor. (nih.gov)
Adenosine is an endogenous nucleoside that shows its well-known cardiovascular effects by A 1 , A 2a , and A 2b receptors. (ijp-online.com)
Some studies have shown that adenosine A 1 receptor stimulation and/or endogenous adenosine may have a role in amitriptyline-a tricyclic antidepressant (TCA)-induced cardiovascular toxicity such as hypotension, QRS, and QT prolongation. (ijp-online.com)
Therefore, aim of this study is to clarify the role of adenosine receptors and/or endogenous adenosine in the mechanism of the cardiovascular toxic effects induced by citalopram overdose in rats. (ijp-online.com)
The indole moiety is related to the neurotransmitter serotonin which is widely implicated for brain function and cognition as the endogenous receptor agonist. (frontiersin.org)

NIDDK announces the availability of a highly selective A1 adenosine receptor (AR) agonist. (nih.gov)

However, AMP-induced torpor was intact in mice lacking any one of the adenosine receptors (A1AR, A2AAR, A2BAR, or A3AR). (nih.gov)
Our lab has characterized a third mechanism to achieve hypothermia through A3AR mast cell degranulation and central histamine H1 receptors. (nih.gov)
We found that putative A1AR agonists at commonly used doses are non-selective and work via both A1AR and A3AR to cause hypothermia. (nih.gov)
Finally, we show the torpor response after a 24 hour fast occurs in mice lacking A1AR, A3AR, or both, demonstrating that these receptors are not required for this effect. (nih.gov)
In the mouse model of Chronic Constriction Injury (CCI), the acute intraperitoneal co-administration of the A3AR agonist IB-MECA (0.5 mg/kg) and the H4R agonist VUF 8430 (10 mg/kg), were additive in counteracting mechano-allodynia increasing IL-10 plasma levels. (bvsalud.org)

Four different adenosine receptor subtypes have been defined. (asahq.org)
There are five receptor subtypes, D1-D5, distinguished by the different second messengers they couple to. (brainmatrix.com)
D1 and D5 form the stimulatory D1-like dopamine receptor family, and D2, D3, and D4 receptor subtypes the inhibitory D2-like family of receptors. (brainmatrix.com)
This has recently been called into question under models of normal physiological conditions, taking into account the kinetics of and relative abundance of the two, and showing both receptor subtypes respond equally to either phasic or tonic scenarios owing fundamentally to their slower unbinding of dopamine. (brainmatrix.com)

In AL rats, inhibition of ISO-stimulated adenylyl cyclase by the AdoA1R agonist, N6-p-sulfophenyladenosine (SPA) decreased with age. (aspetjournals.org)
Here, the authors test whether increased inhibition by adenosine of glutamate release from afferents after injury accounts for this difference. (asahq.org)
Capsaicin-evoked glutamate release, as well as its inhibition by adenosine, did not differ between synaptosomes prepared from tissue ipsilateral and contralateral to spinal nerve ligation. (asahq.org)
[11] It was observed that the negative inotropic and chronotropic effects induced by citalopram can be explained by the inhibition of re-uptake of adenosine or the activation of adenosine A 1 receptors. (ijp-online.com)

Recent evidence suggests adenosine inhibits RTN chemoreception in vivo by activation of A1 receptors. (eneuro.org)
Cell-attached recordings from RTN chemoreceptors in slices from rat or wild-type mouse pups (mixed sex) show that exposure to adenosine (1 µM) inhibits chemoreceptor activity by an A1 receptor-dependent mechanism. (eneuro.org)
These results show that adenosine activation of A1 receptors inhibits chemosensitive RTN neurons by direct activation of a G-protein-regulated inward-rectifier K + (GIRK)-like conductance, and presynaptically, by suppression of excitatory synaptic input to chemoreceptors. (eneuro.org)
Here, we show that adenosine activation of A1 receptors inhibits RTN neurons by activation of an inward rectifying K + conductance, and by selective suppression of excitatory synaptic input to chemoreceptors. (eneuro.org)
These observations confirm previous neurophysiologic studies that presynaptic adenosine A1 receptor activation inhibits glutamate release from primary afferents. (asahq.org)

The A1AR-selective full agonist MRS5474 displayed anticonvulsant activity in vivo in a model of minimal clonic seizures, without toxicity characteristic of other A1AR agonists. (nih.gov)

Adenosine A1 receptor activation increases myocardial protein S-nitrosothiols and elicits protection from ischemia-reperfusion injury in male and female hearts. (nih.gov)
30 nM) alone did not potentiate CO 2 /H + -stimulated activity, suggesting activation of A1 receptors does not limit chemoreceptor activity under these reduced conditions. (eneuro.org)
The H4 histamine receptor (H4R), also implicated in pain modulation, is expressed on T cells playing a preeminent role in its activation and release of IL-10. (bvsalud.org)
cAMP NOMAD ADORA1 Cell Line allows to assay compounds analyzing the G-Protein signalling pathway by Go involving receptor activation. (innoprot.com)
21)Protection conferred by Corticotropin-releasing hormone in rat primary cortical neurons against chemical ischemia involves opioid receptor activation. (edu.in)
A1 adenosine receptor activation reduces hypersensitivity in animal models of chronic pain, but intrathecal adenosine does not produce analgesia to acute noxious stimuli. (asahq.org)
We have used convergent modeling, mutagenesis and structure activity approaches to gather information about the three-dimensional structure of the receptors and its relationship to binding and activation functions. (nih.gov)
Another potential method of using the protective effects of AR activation has been achieved through receptor engineering. (nih.gov)
The cardioprotective effects of activation of the A 2A adenosine receptor (A 2A AR) on ischemia/reperfusion injury in the heart remain controversial. (opencardiovascularmedicinejournal.com)
Activation of adenosine receptors has been shown to reduce myocardial infarct size in experimental models. (opencardiovascularmedicinejournal.com)
[4] Activation of A 1 receptors depresses heart by negative inotropic, chronotropic, and dromotropic effects. (ijp-online.com)
Activation of A 2 receptors cause a reduction in mean arterial pressure by causing a relaxation in vascular smooth muscle cells. (ijp-online.com)

In addition, we have introduced the approach of neoceptors, also intended for eventual use in gene therapy, in which the putative agonist binding site is redesigned to accept only agonist molecules altered in a complementary fashion. (nih.gov)

The agonists, which incorporate the commercially available fluorophore BODIPY [630/650], retain potent and efficacious agonist activity, as demonstrated by their ability to inhibit cAMP accumulation in chinese hamster ovary cells expressing the human adenosine A 1 -receptor. (nottingham.edu.cn)
Substances developed as potent and selective agents acting through adenosine and P2 receptors have proven useful as pharmacological probes and have potential for treating diseases of the central nervous system, immune system, and cardiovascular system. (nih.gov)

Glutamate release evoked by the TRPV-1 receptor agonist, capsaicin, was measured. (asahq.org)
Capsaicin-evoked glutamate release was inhibited by adenosine or R-PIA (R-N6-(2- phenylisopropyl)-adenosine) in a concentration-dependent manner, with a threshold of 10 nm in both normal and nerve-ligated synaptosomes. (asahq.org)
My central area of research concerns the pharmacology and biochemistry of G protein-coupled receptors (in particular, cannabinoid, adenosine and glutamate) in the CNS and peripheral tissues. (nottingham.ac.uk)

AN - traumatic kidney injury: index KIDNEY/ inj HN - 2011 MH - Adenosine A1 Receptor Agonists UI - D058907 MN - D27.505.519.625.725.200.100.100 MN - D27.505.696.577.725.200.100.100 MS - Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS. (nih.gov)

A3 adenosine receptor agonists at low concentrations and P2Y6 receptor agonists have antiapoptotic effects. (nih.gov)
Furthermore, P2Y6 agonists promote insulin release in pancreatic islet cells. (nih.gov)

17. Adenosine A1 receptor agonists reduce hyperalgesia after spinal cord injury in rats. (nih.gov)

ADENOSINE and synthetic adenosine receptor agonists produce antinociception in a broad range of pain models in animals, including hypersensitivity from nerve injury and inflammation. (asahq.org)

Objectives: Adenosine and adenosine A1 receptor agonists exert protective effects against reperfusion injury in different tissues by mediating preconditioning. (beun.edu.tr)

Yöntemler: Denekler herbiri rastgele sekiz hayvan içeren dört gruba ayrıldı: sham kontrol, iskemi-reperfüzyon kontrol, 5'-N-etilkarboksiamidoadenozin (NECA) (non-selektif A1 /A2 agonisti, 0.1 mg/kg, i.v.) tedavili iskemi-reperfüzyon ve teofilin (non-selektif A1 /A2 antagonisti, 20 mg/kg, i.v.) tedavili iskemi-reperfüzyon. (beun.edu.tr)

D1 receptors stimulate adenylyl cyclase, triggering the production of second messenger, 3',5'-cyclic adenosine monophosphate (cAMP) that regulates protein kinase A (PKA) activity, whereas the D2 receptors have the opposite effect. (brainmatrix.com)

We investigated whether ATL 313, a new selective A 2A AR agonist, could reduce myocardial infarct size in a rat ischemia/reperfusion model. (opencardiovascularmedicinejournal.com)

The pharmacological probes designed in our section have been used to demonstrate the connection between purine receptors and apoptosis (programmed cell death). (nih.gov)

This problem might be circumvented by using low-efficacy agonists (partial agonists). (tno.nl)

10)Adipokinetic hormone signaling through the gonadotropin-releasing hormone receptor modulates egg-laying in Caenorhabditis elegans. (edu.in)
Adenosine modulates many physiological processes by activating specific adenosine receptors. (nih.gov)

Autoradiography with [11C]MPDX ex vivo demonstrated decreased A1 receptor binding in the superior colliculus of rats deprived of retino-collicular fibers by contralateral eye enucleation. (nih.gov)

Nucleoside docking to a homology model based on recently reported agonist-bound AR structures characterized the interaction of cycloalkylrelated constituents with a small hydrophobic subpocket in the A1AR. (nih.gov)

Myocardial infarction, A 2A adenosine receptor, ATL 313. (opencardiovascularmedicinejournal.com)

Compounds that bind to and stimulate ADENOSINE A1 RECEPTORS . (nih.gov)

Adenosine concentrations, mean arterial pressure (MAP), heart rate (HR), QRS duration and QT interval were evaluated. (ijp-online.com)
In the second protocol, citalopram infusion did not cause a significant change in plasma adenosine concentrations, but a significant increase observed in EHNA/NBTI groups. (ijp-online.com)

This effect is unaltered after peripheral nerve injury and thereby is unlikely to account for the enhanced analgesic efficacy of intrathecal adenosine in this setting. (asahq.org)

2)Structure of the atrial natriuretic peptide receptor extracellular domain in the unbound and hormone-bound states by single-particle electron microscopy. (edu.in)
My current focus is on receptors for purines, encompassing both adenosine receptors and P2 receptors, which are activated by ATP, UTP and other extracellular nucleotides. (nih.gov)
Recently, the involvement of extracellular loops of GPCRs have been implicated in the receptor binding of small molecules. (nih.gov)

When an agonist binds to ADORA1, Go protein is activated which, in turn, triggers a cellular response mediated by cAMP. (innoprot.com)
When an agonist binds to [Arg8]‐AVP, the Gs protein is activated which, in turn, triggers a cellular response mediated by cAMP via adenylate cyclase stimulation. (innoprot.com)
The function and signaling of dopamine depends on the effect exerted by the type of receptor it binds. (brainmatrix.com)

1997)J Mol Cell Cardiol 29:593-602] and that this decline may be caused by a decrease in coupling between adenosine A1 receptors (AdoA1R) and guanine nucleotide-binding proteins [Cai et al. (aspetjournals.org)

however, mechanisms by which adenosine regulates activity of RTN chemoreceptors is not known. (eneuro.org)

PMID- 214392 TI - Regulation of lipogenesis by adenosine 3', 5'-cyclic monophosphate in chicken liver in vitro. (nih.gov)

Adenosine is thought to act through A1AR in the nucleus of the solitary tract or pre-optic area to elicit hypothermia in rodents. (nih.gov)
Recent advances in specificity to the A1AR encourage development of these agonists for CNS disorders. (nih.gov)

Gabapentin is structurally related to the neurotransmitter GABA (gamma-aminobutyric acid) but it does not modify GABA A or GABA B radioligand binding, it is not converted metabolically into GABA or a GABA agonist, and it is not an inhibitor of GABA uptake or degradation. (nih.gov)

Compuestos que se unen a los RECEPTORES DE ADENOSINA A1, estimulándolos. (bvsalud.org)

Adenosine agonists inhibited 1 nM [3H]CGS 15943 binding with the following order of activity N6-cyclopentyladenosine (IC50 = 15 nM) greater than 2-chloroadenosine greater than (R)-N6-phenylisopropyladenosine greater than 5'-N6-ethylcarboxamidoadenosine greater than (S)N6-phenylisopropyladenosine greater than CGS 21680 greater than CV 1808 (IC50 greater than 10,000 nM). (aspetjournals.org)

1)Type I Gonadotropin-Releasing Hormone Receptor (GnRH-R) Mediates the Antiproliferative Effects of GnRH-II on Prostate Cancer Cells. (edu.in)

Therefore, we pharmacologically preconditioned male and female hearts with the adenosine A1 receptor agonist N6-cyclohexyl adenosine (CHA). (nih.gov)

Whole-cell voltage-clamp from chemosensitive RTN neurons shows that exposure to adenosine activated an inward rectifying K + conductance, and at the network level, adenosine preferentially decreased frequency of EPSCs but not IPSCs. (eneuro.org)

[5] Alternative splicing generates two isoforms of the D2 receptor, D2-short (D2s) and D2-long (D2 L ), respectively, and confers different properties that influence its signaling and pharmacology. (brainmatrix.com)

The objective of the present study was to investigate whether reduction of central acetylcholine (ACh) accumulation by adenosine receptor agonists could serve as a generic treatment against organophosphate (OP) poisoning. (tno.nl)

8)Vasoactive intestinal peptide acts via multiple signal pathways to regulate hippocampal NMDA receptors and synaptic transmission. (edu.in)

In further FCS studies, both A3 AR and A3 AR R108A underwent similar agonist-induced increases in receptor density and molecular brightness which were accompanied by a decrease in membrane diffusion after agonist treatment. (bvsalud.org)
11)Molecular evolution of multiple forms of kisspeptins and GPR54 receptors in vertebrates. (edu.in)
We are interested in correlating structure of receptors and small molecular drugs with pharmacological properties. (nih.gov)
The intracellular cAPM-PKA signaling cascades engenders all sorts of modifications of targets that include ion channels, receptors, and carries further to the molecular level. (brainmatrix.com)

13)Androgen-induced human breast cancer cell proliferation is mediated by discrete mechanisms in estrogen receptor-alpha-positive and -negative breast cancer cells. (edu.in)

19)Hippocampal dynorphin immunoreactivity increases in response to gonadal steroids and is positioned for direct modulation by ovarian steroid receptors. (edu.in)

Dopamine signals are essentially mediated by five receptors D1-D5, that are encoded by DRD1-DRD5 genes in humans. (brainmatrix.com)
The dopamine receptor regulation of cAMP impacts PKA and the downstream phosphorylation states of its many substrates. (brainmatrix.com)

Here, we have compared the membrane organization and downstream signaling of a mutant (R108A, R3.50A) of the adenosine A3 receptor (A3 AR) to that of the wild-type receptor. (bvsalud.org)
Using bimolecular fluorescence complementation, experiments showed that the R108A mutant retained the ability to recruit ß-arrestin and these receptor/arrestin complexes displayed similar membrane diffusion and organization to that observed with wild-type receptors. (bvsalud.org)
Constitutively active mutant A3 adenosine receptors, in principle, could be delivered by tissue-targeted vectors for gene therapy. (nih.gov)

These adenosine receptors play a critical role in the regulation of cellular signaling and are broadly distributed throughout the body. (nih.gov)
PMID- 214393 TI - Regulation of growth & metabolism of ovariectomised rat uterus by adenosine 3', 5'-cyclic monophosphate. (nih.gov)

inhibitor of facilitated adenosine transport). (ijp-online.com)

The application of adenosine A1 receptor agonists in regard to cerebral disorders is hampered by serious cardiovascular side effects. (tno.nl)

Anatomy13

Organisms10

Diseases1

Chemicals and Drugs201

Analytical, Diagnostic and Therapeutic Techniques and Equipment9

Psychiatry and Psychology2

Phenomena and Processes18

Disciplines and Occupations1

Health Care1

Alteration of the purinergic modulation of enteric neurotransmission in the mouse ileum during chronic intestinal inflammation. (1/122)

Comparison of effects of MgCl2 and Gpp(NH)p on antagonist and agonist radioligand binding to adenosine A1 receptors. (2/122)

Involvement of adenosine A1 and A2A receptors in the adenosinergic modulation of the discriminative-stimulus effects of cocaine and methamphetamine in rats. (3/122)

Adenosine A1 receptor agonists block the neuropathological changes in rat retrosplenial cortex after administration of the NMDA receptor antagonist dizocilpine. (4/122)

Allosteric enhancers of A1 adenosine receptors increase receptor-G protein coupling and counteract Guanine nucleotide effects on agonist binding. (5/122)

Role of direct RhoA-phospholipase D1 interaction in mediating adenosine-induced protection from cardiac ischemia. (6/122)

A1 and A2A adenosine receptor modulation of alpha 1-adrenoceptor-mediated contractility in human cultured prostatic stromal cells. (7/122)

A1 adenosine receptor upregulation and activation attenuates neuroinflammation and demyelination in a model of multiple sclerosis. (8/122)

Adenosine

Receptor, Adenosine A2A

Receptor, Adenosine A1

Purinergic P1 Receptor Agonists

Adenosine A2 Receptor Agonists

Adenosine A1 Receptor Agonists

Receptor, Adenosine A3

Adenosine Deaminase

Receptor, Adenosine A2B

Receptors, Purinergic P1

Receptors, Adenosine A2

Adenosine Kinase

Adenosine A2 Receptor Antagonists

Adenosine A1 Receptor Antagonists

Serotonin Receptor Agonists

Dopamine Agonists

Purinergic P1 Receptor Antagonists

Serotonin 5-HT1 Receptor Agonists

Xanthines

Adenosine A3 Receptor Agonists

Serotonin 5-HT2 Receptor Agonists

Adenosine-5'-(N-ethylcarboxamide)

Phenethylamines

Dose-Response Relationship, Drug

Adenosine Monophosphate

GABA Agonists

GABA-A Receptor Agonists

GABA-B Receptor Agonists

Receptors, Purinergic

Purinergic P2 Receptor Agonists

Cannabinoid Receptor Agonists

Serotonin 5-HT4 Receptor Agonists

Rats, Sprague-Dawley

Cyclic AMP

Adrenergic alpha-2 Receptor Agonists

Phenylisopropyladenosine

Theophylline

Adenosine A3 Receptor Antagonists

2-Chloroadenosine

Receptors, Opioid, kappa

Histamine Agonists

Muscarinic Agonists

Rats, Wistar

Receptors, Opioid, mu

Receptors, Dopamine D2

Serotonin Antagonists

2,3,4,5-Tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepine

Adrenergic Agonists

Baclofen

Adrenergic beta-3 Receptor Agonists

Radioligand Assay

Quinpirole

5'-Nucleotidase

Nicotinic Agonists

Receptors, Opioid, delta

Receptors, Dopamine D1

Excitatory Amino Acid Agonists

Cells, Cultured

Inosine

Piperidines

Guinea Pigs

Adrenergic beta-Agonists

Benzazepines

Calcium

8-Hydroxy-2-(di-n-propylamino)tetralin

Enkephalin, Ala(2)-MePhe(4)-Gly(5)-

Adrenergic alpha-Agonists

Cannabinoids

Adrenergic alpha-1 Receptor Agonists

Tubercidin

Receptors, Opioid

Theobromine

Muscimol

Serotonin

Receptors, Serotonin

Pyrrolidines

Adenosine Triphosphatases

Naphthalenes

Adenine Nucleotides

Receptors, Purinergic P2