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.
A purinergic P2X neurotransmitter receptor that plays a role in pain sensation signaling and regulation of inflammatory processes.
Compounds that bind to and block the stimulation of PURINERGIC P2X RECEPTORS. Included under this heading are antagonists for specific P2X receptor subtypes.
Compounds that bind to and stimulate PURINERGIC P2X RECEPTORS. Included under this heading are agonists for specific P2X receptor subtypes.
A subclass of purinergic P2 receptors that signal by means of a ligand-gated ion channel. They are comprised of three P2X subunits which can be identical (homotrimeric form) or dissimilar (heterotrimeric form).
A purinergic P2X neurotransmitter receptor involved in sensory signaling of TASTE PERCEPTION, chemoreception, visceral distension, and NEUROPATHIC PAIN. The receptor comprises three P2X3 subunits. The P2X3 subunits are also associated with P2X2 RECEPTOR subunits in a heterotrimeric receptor variant.
A subclass of purinergic P2Y receptors that have a preference for ATP and UTP. The activated P2Y2 receptor acts through a G-PROTEIN-coupled PHOSPHATIDYLINOSITOL and intracellular CALCIUM SIGNALING pathway.
A widely distributed purinergic P2X receptor subtype that plays a role in pain sensation. P2X4 receptors found on MICROGLIA cells may also play a role in the mediation of allodynia-related NEUROPATHIC PAIN.
A subclass of purinergic P2Y receptors that have a preference for ATP and ADP. The activated P2Y1 receptor signals through the G-PROTEIN-coupled activation of PHOSPHOLIPASE C and mobilization of intracellular CALCIUM.
Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.
Compounds that bind to and stimulate PURINERGIC P2Y RECEPTORS. Included under this heading are agonists for specific P2Y receptor subtypes.
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.
A subclass of purinergic P2 receptors whose signaling is coupled through a G-PROTEIN signaling mechanism.
A purinergic P2X neurotransmitter receptor involved in sensory signaling of TASTE PERCEPTION, chemoreception, visceral distension and NEUROPATHIC PAIN. The receptor comprises three P2X2 subunits. The P2X2 subunits also have been found associated with P2X3 RECEPTOR subunits in a heterotrimeric receptor variant.
Drugs that bind to and block the activation of PURINERGIC RECEPTORS.
Compounds that bind to and activate PURINERGIC RECEPTORS.
An adenine nucleotide containing three phosphate groups esterified to the sugar moiety. In addition to its crucial roles in metabolism adenosine triphosphate is a neurotransmitter.
A subclass of purinergic P2Y receptors that have a preference for ADP binding and are coupled to GTP-BINDING PROTEIN ALPHA SUBUNIT, GI. The P2Y12 purinergic receptors are found in PLATELETS where they play an important role regulating PLATELET ACTIVATION.
A purinergic P2X neurotransmitter receptor found at high levels in the BRAIN and IMMUNE SYSTEM.
A purinergic P2X neurotransmitter receptor found at sympathetically innervated SMOOTH MUSCLE. It may play a functional role regulating the juxtoglomerular apparatus of the KIDNEY.
Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.
Uridine 5'-(tetrahydrogen triphosphate). A uracil nucleotide containing three phosphate groups esterified to the sugar moiety.
A polyanionic compound with an unknown mechanism of action. It is used parenterally in the treatment of African trypanosomiasis and it has been used clinically with diethylcarbamazine to kill the adult Onchocerca. (From AMA Drug Evaluations Annual, 1992, p1643) It has also been shown to have potent antineoplastic properties.
This is the active form of VITAMIN B 6 serving as a coenzyme for synthesis of amino acids, neurotransmitters (serotonin, norepinephrine), sphingolipids, aminolevulinic acid. During transamination of amino acids, pyridoxal phosphate is transiently converted into pyridoxamine phosphate (PYRIDOXAMINE).
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 stimulate ADENOSINE A1 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.
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).
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 strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.
A 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.
Compounds that bind to and block the stimulation of PURINERGIC P2Y RECEPTORS. Included under this heading are antagonists for specific P2Y receptor subtypes.
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.
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.
Signal transduction mechanisms whereby calcium mobilization (from outside the cell or from intracellular storage pools) to the cytoplasm is triggered by external stimuli. Calcium signals are often seen to propagate as waves, oscillations, spikes, sparks, or puffs. The calcium acts as an intracellular messenger by activating calcium-responsive proteins.
The relationship between the dose of an administered drug and the response of the organism to the drug.
Endogenous compounds and drugs that bind to and activate GAMMA-AMINOBUTYRIC ACID receptors (RECEPTORS, GABA).
Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS.
Endogenous compounds and drugs that bind to and activate GABA-A RECEPTORS.
Endogenous compounds and drugs that bind to and activate GABA-B RECEPTORS.
Compounds that interact with and stimulate the activity of CANNABINOID RECEPTORS.
Endogenous compounds and drugs that specifically stimulate SEROTONIN 5-HT4 RECEPTORS.
Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
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.
Adenosine 5'-(trihydrogen diphosphate). An adenine nucleotide containing two phosphate groups esterified to the sugar moiety at the 5'-position.
Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS.
A calcium-activated enzyme that catalyzes the hydrolysis of ATP to yield AMP and orthophosphate. It can also act on ADP and other nucleoside triphosphates and diphosphates. EC 3.6.1.5.
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.
Compounds that act on PURINERGIC RECEPTORS or influence the synthesis, storage, uptake, metabolism, or release of purinergic transmitters.
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 selectively bind to and activate ADENOSINE A3 RECEPTORS.
The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM.
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 but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.
Drugs that bind to and activate adrenergic receptors.
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 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 group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed)
Drugs that bind to 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.
Established cell cultures that have the potential to propagate indefinitely.
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 selective D1 dopamine receptor agonist used primarily as a research tool.
Compounds that bind to and activate ADRENERGIC BETA-3 RECEPTORS.
A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D2-class receptor genes contain INTRONS, and the receptors inhibit ADENYLYL CYCLASES.
A series of heterocyclic compounds that are variously substituted in nature and are known also as purine bases. They include ADENINE and GUANINE, constituents of nucleic acids, as well as many alkaloids such as CAFFEINE and THEOPHYLLINE. Uric acid is the metabolic end product of purine metabolism.
A 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 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.
A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity.
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.
A dopamine D2/D3 receptor agonist.
Drugs that selectively bind to and activate alpha adrenergic receptors.
Compounds that bind to and activate ADRENERGIC ALPHA-1 RECEPTORS.
Drugs that bind to and activate cholinergic receptors.
Drugs that bind to and activate excitatory amino acid receptors.
Use of electric potential or currents to elicit biological responses.
An interleukin-1 subtype that is synthesized as an inactive membrane-bound pro-protein. Proteolytic processing of the precursor form by CASPASE 1 results in release of the active form of interleukin-1beta from the membrane.
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.
A family of hexahydropyridines.
A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.
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.
Compounds with BENZENE fused to AZEPINES.
An enkephalin analog that selectively binds to the MU OPIOID RECEPTOR. It is used as a model for drug permeability experiments.
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.
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.
Compounds having the cannabinoid structure. They were originally extracted from Cannabis sativa L. The most pharmacologically active constituents are TETRAHYDROCANNABINOL; CANNABINOL; and CANNABIDIOL.
Drugs that selectively bind to and activate beta-adrenergic receptors.
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.
Purine bases found in body tissues and fluids and in some plants.
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.
Unstriated and unstriped muscle, one of the muscles of the internal organs, blood vessels, hair follicles, etc. Contractile elements are elongated, usually spindle-shaped cells with centrally located nuclei. Smooth muscle fibers are bound together into sheets or bundles by reticular fibers and frequently elastic nets are also abundant. (From Stedman, 25th ed)
A 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 process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.
Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).
The action of a drug that may affect the activity, metabolism, or toxicity of another drug.
A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.
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 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.
N-Isopropyl-N-phenyl-adenosine. Antilipemic agent. Synonym: TH 162.
Nucleotides in which the base moiety is substituted with one or more sulfur atoms.
A disulfide opioid pentapeptide that selectively binds to the DELTA OPIOID RECEPTOR. It possesses antinociceptive activity.
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.
A musculomembranous sac along the URINARY TRACT. URINE flows from the KIDNEYS into the bladder via the ureters (URETER), and is held there until URINATION.
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 excretory duct of the testes that carries SPERMATOZOA. It rises from the SCROTUM and joins the SEMINAL VESICLES to form the ejaculatory duct.
OXAZINES with a fused BENZENE ring.
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).
A subclass of cannabinoid receptor found primarily on immune cells where it may play a role modulating release of CYTOKINES.
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.
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.
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.
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.
Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.
A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.
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 selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.
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 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.
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.
Histamine substituted in any position with one or more methyl groups. Many of these are agonists for the H1, H2, or both histamine receptors.
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.
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.
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.
Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.
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.
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.
Elements of limited time intervals, contributing to particular results or situations.
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.
Agents inhibiting the effect of narcotics on the central nervous system.
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 neuropeptide Y with high affinity and trigger intracellular changes which influence the behavior of cells.
A neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system.
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.
A subclass of phospholipases that hydrolyze the phosphoester bond found in the third position of GLYCEROPHOSPHOLIPIDS. Although the singular term phospholipase C specifically refers to an enzyme that catalyzes the hydrolysis of PHOSPHATIDYLCHOLINE (EC 3.1.4.3), it is commonly used in the literature to refer to broad variety of enzymes that specifically catalyze the hydrolysis of PHOSPHATIDYLINOSITOLS.
A subset of GABA RECEPTORS that signal through their interaction with HETEROTRIMERIC G-PROTEINS.
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.
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.
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.
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.
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.
Substances used for their pharmacological actions on any aspect of neurotransmitter systems. Neurotransmitter agents include agonists, antagonists, degradation inhibitors, uptake inhibitors, depleters, precursors, and modulators of receptor function.
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)
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 subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.
One of the catecholamine NEUROTRANSMITTERS in the brain. It is derived from TYROSINE and is the precursor to NOREPINEPHRINE and EPINEPHRINE. Dopamine is a major transmitter in the extrapyramidal system of the brain, and important in regulating movement. A family of receptors (RECEPTORS, DOPAMINE) mediate its action.
The study of the generation and behavior of electrical charges in living organisms particularly the nervous system and the effects of electricity on living organisms.
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
Cell-surface proteins that bind dopamine with high affinity and trigger intracellular changes influencing the behavior of cells.
The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.
A uracil nucleotide containing a pyrophosphate group esterified to C5 of the sugar moiety.
The physical activity of a human or an animal as a behavioral phenomenon.
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)
A dopamine D1 receptor agonist that is used as an antihypertensive agent. It lowers blood pressure through arteriolar vasodilation.
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.
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 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.
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.
Any drugs that are used for their effects on dopamine receptors, on the life cycle of dopamine, or on the survival of dopaminergic neurons.
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.-.
An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent.
A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL 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.
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).
An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.
A highly potent and specific histamine H2 receptor agonist. It has been used diagnostically as a gastric secretion indicator.
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.
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.
Drugs that bind to but do not activate alpha-adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists. Adrenergic alpha-antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma.
Interstitial space between cells, occupied by INTERSTITIAL FLUID as well as amorphous and fibrous substances. For organisms with a CELL WALL, the extracellular space includes everything outside of the CELL MEMBRANE including the PERIPLASM and the cell wall.
An enzyme of the lyase class that catalyzes the formation of CYCLIC AMP and pyrophosphate from ATP. EC 4.6.1.1.
A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.
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.
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.
Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. Muscarinic antagonists have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system.
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.
Naturally occurring or experimentally induced animal diseases with pathological processes sufficiently similar to those of human diseases. They are used as study models for human diseases.
A class of 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)
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.
The most common inhibitory neurotransmitter in the central nervous system.
The rate dynamics in chemical or physical systems.
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.
Refers to animals in the period of time just after birth.
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.
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.
Cell-surface proteins that bind epinephrine and/or norepinephrine with high affinity and trigger intracellular changes. The two major classes of adrenergic receptors, alpha and beta, were originally discriminated based on their cellular actions but now are distinguished by their relative affinity for characteristic synthetic ligands. Adrenergic receptors may also be classified according to the subtypes of G-proteins with which they bind; this scheme does not respect the alpha-beta distinction.
A subclass of G-protein coupled SEROTONIN receptors that couple preferentially to GI-GO G-PROTEINS resulting in decreased intracellular CYCLIC AMP levels.
The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.

Expression of both P1 and P2 purine receptor genes by human articular chondrocytes and profile of ligand-mediated prostaglandin E2 release. (1/458)

OBJECTIVE: To assess the expression and function of purine receptors in articular chondrocytes. METHODS: Reverse transcriptase-polymerase chain reaction (RT-PCR) was used to screen human chondrocyte RNA for expression of P1 and P2 purine receptor subtypes. Purine-stimulated prostaglandin E2 (PGE2) release from chondrocytes, untreated or treated with recombinant human interleukin-1alpha (rHuIL-1alpha), was assessed by radioimmunoassay. RESULTS: RT-PCR demonstrated that human articular chondrocytes transcribe messenger RNA for the P1 receptor subtypes A2a and A2b and the P2 receptor subtype P2Y2, but not for the P1 receptor subtypes A1 and A3. The P1 receptor agonists adenosine and 5'-N-ethylcarboxamidoadenosine did not change PGE2 release from chondrocytes. The P2Y2 agonists ATP and UTP stimulated a small release of PGE2 that was potentiated after pretreatment with rHuIL-1alpha. PGE2 release in response to ATP and UTP cotreatment was not additive, but release in response to coaddition of ATP and bradykinin (BK) or UTP and BK was additive, consistent with ATP and UTP competition for the same receptor site. The potentiation of PGE2 release in response to ATP and UTP after rHuIL-1alpha pretreatment was mimicked by phorbol myristate acetate. CONCLUSION: Human chondrocytes express both P1 and P2 purine receptor subtypes. The function of the P1 receptor subtype is not yet known, but stimulation of the P2Y2 receptor increases IL-1-mediated PGE2 release.  (+info)

A comparison of an A1 adenosine receptor agonist (CVT-510) with diltiazem for slowing of AV nodal conduction in guinea-pig. (2/458)

1. The purpose of this study was to compare the pharmacological properties (i.e. the AV nodal depressant, vasodilator, and inotropic effects) of two AV nodal blocking agents belonging to different drug classes; a novel A1 adenosine receptor (A1 receptor) agonist, N-(3(R)-tetrahydrofuranyl)-6-aminopurine riboside (CVT-510), and the prototypical calcium channel blocker diltiazem. 2. In the atrial-paced isolated heart, CVT-510 was approximately 5 fold more potent to prolong the stimulus-to-His bundle (S-H interval), a measure of slowing AV nodal conduction (EC50 = 41 nM) than to increase coronary conductance (EC50 = 200 nM). At concentrations of CVT-510 (40 nM) and diltiazem (1 microM) that caused equal prolongation of S-H interval (approximately 10 ms), diltiazem, but not CVT-510, significantly reduced left ventricular developed pressure (LVP) and markedly increased coronary conductance. CVT-510 shortened atrial (EC50 = 73 nM) but not the ventricular monophasic action potentials (MAP). 3. In atrial-paced anaesthetized guinea-pigs, intravenous infusions of CVT-510 and diltiazem caused nearly equal prolongations of P-R interval. However, diltiazem, but not CVT-510, significantly reduced mean arterial blood pressure. 4. Both CVT-510 and diltiazem prolonged S-H interval, i.e., slowed AV nodal conduction. However, the A1 receptor-selective agonist CVT-510 did so without causing the negative inotropic, vasodilator, and hypotensive effects associated with diltiazem. Because CVT-510 did not affect the ventricular action potential, it is unlikely that this agonist will have a proarrythmic action in ventricular myocardium.  (+info)

Purification of A1 adenosine receptor-G-protein complexes: effects of receptor down-regulation and phosphorylation on coupling. (3/458)

We examined the effects of exposing A1 adenosine receptors (A1ARs) to an agonist on the stability and phosphorylation state of receptor-guanine nucleotide-binding regulatory protein (R-G-protein) complexes. Non-denatured recombinant human A1ARs extended on the N-terminus with hexahistidine (His6) and the FLAG (Asp-Tyr-Lys-Asp-Asp-Asp-Asp-Lys) epitope (H/F) were purified to near homogeneity from stably transfected Chinese-hamster ovary (CHO)-K1 cells. Purified receptors have pharmacological properties similar to receptors in membranes. G-proteins were co-purified with 15+/-2% of H/F-A1AR unless receptor-G-protein (R-G) complexes were uncoupled by pre-treating cell membranes with GTP. By silver staining, purified A1AR-G-protein complexes contain receptors, G-protein alpha and beta subunits and an unidentified 97 kDa protein. Pretreating intact cells with N6-cyclopentyladenosine (CPA) for 24 h decreased both the total number of receptors measured in membranes and the number of purified A1ARs by about 50%. In contrast, pretreating cells with CPA decreased the number of R-G complexes measured in membranes (54+/-6%) significantly less than it decreased the number of purified R-G complexes (78+/-3%) as detected by 125I-N6-(4-aminobenzyl)adenosine binding or by Western blotting Gialpha2. The effect of CPA to decrease the fraction of receptors purified as R-G complexes was not associated with any change in low-level A1AR phosphorylation (found on serine), or low-level phosphorylation of G-protein alpha or beta subunits or the 97 kDa protein. These experiments reveal a novel aspect of agonist-induced down-regulation, namely a diminished stability of receptor-G-protein complexes that is manifested as uncoupling during receptor purification.  (+info)

Inhibition by adenosine receptor agonists of synaptic transmission in rat periaqueductal grey neurons. (4/458)

1. The actions of selective adenosine A1 and A2 receptor agonists were examined on synaptic currents in periaqueductal grey (PAG) neurons using patch-clamp recordings in brain slices. 2. The A1 receptor agonist 2-chloro-N-cyclopentyladenosine (CCPA), but not the A2 agonist, 2-p-(2-carboxyethyl)phenethylamino-5'-N-ethylcarboxamidoadenosine (CGS21680), inhibited both electrically evoked inhibitory (eIPSCs) and excitatory (eEPSCs) postsynaptic currents. The actions of CCPA were reversed by the A1 receptor antagonist 8-cyclopentyl-1, 3-dipropylxanthine (DPCPX). 3. In the absence or presence of forskolin, DPCPX had no effect on eIPSCs, suggesting that concentrations of tonically released adenosine are not sufficient to inhibit synaptic transmission in the PAG. 4. CCPA decreased the frequency of spontaneous miniature action potential-independent IPSCs (mIPSCs) but had no effect on their amplitude distributions. Inhibition persisted in nominally Ca2+-free, high Mg2+ solutions and in 4-aminopyridine. 5. The CCPA-induced decrease in mIPSC frequency was partially blocked by the non-selective protein kinase inhibitor staurosporine, the specific protein kinase A inhibitor 8-para-chlorophenylthioadenosine-3',5'-cyclic monophosphorothioate (Rp-8-CPT-cAMPS), and by 8-bromoadenosine cyclic 3',5' monophosphate (8-Br-cAMP). 6. These results suggest that A1 adenosine receptor agonists inhibit both GABAergic and glutamatergic synaptic transmission in the PAG. Inhibition of GABAergic transmission is mediated by presynaptic mechanisms that partly involve protein kinase A.  (+info)

A3 adenosine receptors regulate Cl- channels of nonpigmented ciliary epithelial cells. (5/458)

Adenosine stimulates Cl- channels of the nonpigmented (NPE) cells of the ciliary epithelium. We sought to identify the specific adenosine receptors mediating this action. Cl- channel activity in immortalized human (HCE) NPE cells was determined by monitoring cell volume in isotonic suspensions with the cationic ionophore gramicidin present. The A3-selective agonist N6-(3-iodobenzyl)-adenosine-5'-N-methyluronamide (IB-MECA) triggered shrinkage (apparent Kd = 55 +/- 10 nM). A3-selective antagonists blocked IB-MECA-triggered shrinkage, and A3-antagonists (MRS-1097, MRS-1191, and MRS-1523) also abolished shrinkage produced by 10 microM adenosine when all four known receptor subtypes are occupied. The A1-selective agonist N6-cyclopentyladenosine exerted a small effect at 100 nM but not at higher or lower concentrations. The A2A agonist CGS-21680 triggered shrinkage only at high concentration (3 microM), an effect blocked by MRS-1191. IB-MECA increased intracellular Ca2+ in HCE cells and also stimulated short-circuit current across rabbit ciliary epithelium. A3 message was detected in both HCE cells and rabbit ciliary processes using RT-PCR. We conclude that human HCE cells and rabbit ciliary processes possess A3 receptors and that adenosine can activate Cl- channels in NPE cells by stimulating these A3 receptors.  (+info)

Role of K+ channels in A2A adenosine receptor-mediated dilation of the pressurized renal arcuate artery. (6/458)

1. Adenosine A2A receptor-mediated renal vasodilation was investigated by measuring the lumenal diameter of pressurized renal arcuate arteries isolated from the rabbit. 2. The selective A2A receptor agonist CGS21680 dilated the arteries with an EC50 of 130 nM. The CGS21680-induced vasodilation was, on average, 34% less in endothelium-denuded arteries. 3. The maximum response and the EC50 for CGS21680-induced vasodilation in endothelium-intact arteries were not significantly affected by incubation with the K+ channel blockers apamin (100 nM), iberiotoxin (100 nM), 3,4-diaminopyridine (1 mM), glibenclamide (1 microM) or Ba2+ (10 microM). However, a cocktail mixture of these blockers did significantly inhibit the maximum response by almost 40%, and 1 mM Ba2+ alone or 1 mM Ba2+ in addition to the cocktail inhibited the maximum CGS21680-response by 58% and about 75% respectively. 4. CGS21680-induced vasodilation was strongly inhibited when the extracellular K+ level was raised to 20 mM even though the dilator response to 1 microM levcromakalim, a K(ATP) channel opener drug, was unaffected. 5. CGS21680-induced vasodilation was inhibited by 10 microM ouabain, an inhibitor of Na+/K(+)-ATPase, but ouabain had a similar inhibitory effect on vasodilation induced by 30 nM nicardipine (a dihydropyridine Ca2+ antagonist) or 1 microM levcromakalim. 6. The data suggest that K+ channel activation does play a role in A(2A) receptor-mediated renal vasodilation. The inhibitory effect of raised extracellular K+ levels on the A(2A) response may be due to K(+)-induced stimulation of Na+/K(+)-ATPase.  (+info)

Chronic administration of adenosine A3 receptor agonist and cerebral ischemia: neuronal and glial effects. (7/458)

We have previously shown that chronic administration of the selective A3 receptor agonist N6-(3-iodobenzyl)-5'-N-methylcarboxoamidoadenosine (IB-MECA) leads to a significant improvement of postocclusive cerebral blood flow, and protects against neuronal damage and mortality induced by severe forebrain ischemia in gerbils. Using immunocytochemical methods we now show that chronic with IB-MECA results in a significant preservation of ischemia-sensitive microtubule associated protein 2 (MAP-2), enhancement of the expression of glial fibrillary acidic protein (GFAP), and a very intense depression of nitric oxide synthase in the brain of postischemic gerbils. These changes demonstrate that the cerebroprotective actions of chronically administered IB-MECA involve both neurons and glial cells, and indicate the possibility of distinct mechanisms that are affected in the course of chronic administration of the drug.  (+info)

Effects of dexamethasone on airway hyper-responsiveness to the adenosine A1 receptor agonist cyclo-pentyl adenosine in an allergic rabbit model. (8/458)

1. New Zealand White (NZW) rabbits were immunized within 24 h of birth with Alternaria tenuis in aluminium hydroxide (Al (OH)3) (i.p.) or sham immunized (saline plus Al (OH)3 i.p.) and subsequently injected with the allergen (i.p.) or sham-immunized for the next 3 months. At 3 months of age, baseline airway responsiveness was assessed using cyclo-pentyl adenosine (CPA). Bronchoalveolar lavage (BAL) was performed in all animals and samples of peripheral blood were collected from some animals for estimation of dexamethasone levels. In some animals, blood was collected at the end of the experiment and cellular function was assessed by measurement of ex vivo proliferation of mononuclear cells in response to phytohaemagglutinin (PHA). 2. Allergen immunization significantly increased baseline airway responsiveness to inhaled CPA (P<0.05) in comparison with sham-immunized animals, at 3 months after immunization. Dexamethasone (0.5 mg kg(-1) day(-1)) treatment for 1 month did not modify this established airway hyper-responsiveness to CPA. Dexamethasone treatment did not affect either total or differential cell numbers in BAL fluid during the 4 week period, although significant plasma levels of dexamethasone were achieved in dexamethasone treated animals. 3. Treatment of rabbits with dexamethasone (0.1 mg kg(-1) i.p.), 6 h prior to each allergen injection from the neonatal stage, significantly reduced baseline airway hyper-responsiveness to CPA measured at 3 months (P<0.05). There was no significant difference in either total or differential cell numbers in BAL fluid, or any difference in mitogen-induced proliferation of mononuclear cells between dexamethasone and vehicle treated rabbits. 4. These results suggest that introduction of glucocorticosteroids in early life can prevent baseline airway hyper-responsiveness to inhaled CPA in allergic rabbits. However, once established, such underlying airway hyper-responsiveness is difficult to resolve, even with prolonged treatment with glucocorticosteroids.  (+info)

In a recent prospective, double-blind, randomized multicenter phase 3 trial, ADVANCE (Adenosine versus Regadenoson Comparative Evaluation for Myocardial Perfusion Imaging), the A2A selective adenosine receptor agonist, regadenoson, was shown to be noninferior to the nonselective vasodilator, adenosine, for detecting myocardial ischemia (1). The overall visual agreement was comparably low (in the low 60% range) for the adenosine-regadenoson and for the adenosine-adenosine comparisons. Conversely, when quantitative analysis was applied, regadenoson induced virtually identical results to adenosine-regarding the size and severity of left ventricular perfusion defect size and extent of ischemia (2). What are the regulatory implications of these findings? Should the regulatory bodies rely on subjective visual interpretation of myocardial perfusion studies, on objective quantitative programs to appraise the comparability between vasodilators, or both? What is the true standard?. In order to avoid the ...
The ITU World Radiocommunication Conference 2012 (WRC-12) ran between 23 January and 17 February 2012, but preparation started shortly after the previous Conference, WRC-07 set its agenda.. A key Agenda Item was AI-1.23 - 500kHz. The result was the creation of the 472-479kHz allocation to the service. It also set the agenda for the following conference, WRC-15, which considered a 5MHz allocation.. Here you will find reports on the progress of the WRC-12 Conference from UK/RSGB delegate Colin Thomas G3PSM ...
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TY - JOUR. T1 - Chronic exposure to adenosine receptor agonists and antagonists reciprocally regulates the A1 adenosine receptor-adenylyl cyclase system in cerebellar granule cells. AU - Hettinger-Smith, Barbara D.. AU - Leid, Mark. AU - Murray, Thomas F.. PY - 1996/11. Y1 - 1996/11. N2 - Chronic treatment with the adenosine receptor antagonist caffeine evokes an up-regulation of A1 adenosine receptors and increased coupling of the receptor to G proteins in rat brain membranes. However, chronic agonist exposure has not been explored. Primary cultures of cerebellar granule cells were exposed chronically to A1 adenosine receptor agonists and antagonists. Exposure to the A1 adenosine receptor agonist N6-cyclopentyladenosine resulted in (1) a time- and concentration-dependent reduction in the density of receptors labeled by 1,3[3H]dipropyl-8-cyclopentylxanthine, (2) an enhanced ability of guanyl nucleotides to decrease the fraction of A1 adenosine receptor sites displaying high affinity for ...
Effects of adenosine receptor agonists of the A1, A2A and A3 subtypes on the proinflammatory activity of human neutrophils in ...
A series of new 2-alkynyl and 2-cycloalkynyl derivatives of adenosine-5-N-ethyluronamid(NECA) and of N-ethyl-l-deoxy-l-(6-amino-2-hexynyl-9H-purin-9-yl)-b-D-ribofuranuronamid(1e, HENECA), bearing hydroxy, amino, chloro, and cyano groups in the side chain, were synthesized. The compounds were studied in binding and functional assays to assess their potency for the A2 compared to A1 adenosine receptor. The presence of an a-hydroxyl group in the alkynyl chain of NECA derivatives accounts for the A2 agonist potency, leading to compounds endowed with sub-nanomolar affinity in binding studies. However, these analogues also possess good A1 receptor affinity resulting in low A2 selectivity. From functional experiments the 4-hydroxy-l-butynyl(6) and the 4-(2-tetrahydro-2H-pyranyloxy)-l-butynyl (16) derivatives appear to be very potent in inducing vasorelaxation without appreciable effect on heart rate. The new compounds were also tested as inhibitors of platelet aggregation induced by ADP. ...
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TY - JOUR. T1 - Modulating P1 Adenosine Receptors in Disease Progression of SOD1G93A Mutant Mice. AU - Armida, Monica. AU - Matteucci, Alessandra. AU - Pèzzola, Antonella. AU - Baqi, Younis. AU - Müller, Christa E. AU - Popoli, Patrizia. AU - Potenza, Rosa Luisa. PY - 2019/5. Y1 - 2019/5. N2 - Amyotrophic lateral sclerosis (ALS) is a fatal progressing neurodegenerative disease; to date, despite the intense research effort, only two therapeutic options, with very limited effects, are available. The purinergic system has been indicated as a possible new therapeutic target for ALS, but the results are often contradictory and generally confused. The present study was designed to determine whether P1 adenosine receptor ligands affected disease progression in a transgenic model of ALS. SOD1G93A mice were chronically treated, from presymptomatic stage, with a selective adenosine A2A receptor agonist (CGS21680), antagonist (KW6002) or the A1 receptor antagonist DPCPX. Body weight, motor performance ...
... -First A2A Adenosine Receptor Agonist Approved for Use as Pharmacolo... Stress Agent in Myocardial Perfusion Imaging- ...PALO ALTO Calif. and DEERFIELD Ill. April 10 FirstCall/...Lexiscan is the first A2A adenosine receptor agonist shown to be safe...,CV,Therapeutics,and,Astellas,Announce,FDA,Approval,for,Lexiscan(TM),(regadenoson),Injection,biological,advanced biology technology,biology laboratory technology,biology device technology,latest biology technology
Thank you for sharing this Journal of Pharmacology and Experimental Therapeutics article.. NOTE: We request your email address only to inform the recipient that it was you who recommended this article, and that it is not junk mail. We do not retain these email addresses.. ...
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Letter Letter to FCC Chairman Pai Requesting any Technical Analysis that the FCC has Conducted or Reviewed on Out-of-Band Emissions Limits Follow up to September 30 Letter Sent to FCC Chairmain Pai Attachments U.S. Proposal on WRC-19 Agenda Item 1.13, submitted by FCC on March 19 Slide deck from the 3rd ITU Inter-regional Workshop on WRC-19 Preparation, dated September 5, 2019 Study prepared by NOAA and NASA, Results from NASA/NOAA Sharing Studies on WRC-19 Agenda Item 1.13 Study … Continue Reading September 12, 2019 ...
The review summarizes data evaluating the role of adenosine receptor signaling in murine hematopoietic functions. The studies carried out utilized either non-selective activation of adenosine receptors induced by elevation of extracellular adenosine or by administration of synthetic adenosine analogs having various proportions of selectivity for a particular receptor. Numerous studies have described stimulatory effects of non-selective activation of adenosine receptors, manifested as enhancement of proliferation of cells at various levels of the hematopoietic hierarchy. Subsequent experimental approaches, considering the hematopoiesis-modulating action of adenosine receptor agonists with a high level of selectivity to individual adenosine receptor subtypes, have revealed differential effects of various adenosine analogs. Whereas selective activation of A(1) receptors has resulted in suppression of proliferation of hematopoietic progenitor and precursor cells, that of A(3) receptors has led to ...
Recent evidence indicates that topical application of adenosine A(2A) receptor agonists, unlike growth factors, increases the rate at which wounds close in normal animals and promotes wound healing in diabetic animals as well as growth factors, yet neither the specific adenosine receptor involved no …
37] Liaison statement to Joint Task Group 4-5-6-7 (copy to Working Parties (4A, 4B, 4C 5B, 5C, 5D, 6A, 7B, 7C, 7D, 1A, 3K, 3M) for information) - WRC-15 Agenda item 1.1 - Sharing considerations for the 5-6 GHz frequency range for WRC-15 Agenda item 1.1 ...
ITU HFBC software is consistent with the general principles set out in Article 12 and the specifications in Res.535(Rev.WRC-03) . It was developed in close consideration with Administrations, broadcasters, and existing HFBC regional coordination groups. ...
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Our work demonstrates that human endothelial cells of disparate origin are characterized by differential expression of adenosine receptor subtypes. HUVECs express mRNA for A2A and A2B receptors at a ratio of 10:1, and this preferential gene expression agrees well with the typical pharmacological phenotype of A2A receptor-mediated simulation of adenylate cyclase by adenosine analogs. Using complementary techniques, RT-PCR, and gene expression array, we found that A1 and A3 adenosine receptors are not expressed in HUVECs. Previous studies in HUVECs have suggested a potential role of A1 receptor in maintaining endothelial barrier function4 and of A1 and A3 receptors in modulation of tissue factors expression.6 The apparent contradiction between these results and ours can be explained by the use of nonselective concentrations of adenosine receptor ligands in previous studies.. HMEC-1 also express only A2A and A2B mRNA, but in contrast to HUVECs, they express predominantly A2B receptor mRNA, with a ...
The involvement of a guanine-nucleotide-binding regulatory protein (G protein) in the relaxing responses to adenosine receptor agonists was investigated in bovine coronary vessels. Ring segments of left anterior descending artery branches were suspended in organ baths for measurement of isometric tension. The adenosine analogs, 5-N-ethylcarboxamidoadenosine (NECA) and 2-chloroadenosine (CAD) caused concentration-dependent relaxations of coronary rings contracted with KCl. The relaxing effects of NECA and CAD were antagonized by the adenosine receptor antagonist 8-phenyltheophylline indicating the involvement of an adenosine receptor. In a separate series of experiments, incubation with cholera toxin inhibited the relaxing responses to NECA, CAD and isoproterenol but not those produced by sodium nitroprusside. Treatment with forskolin did not reduce the relaxing responses to NECA or CAD. N-ethylmaleimide and NaF/AlCl3 caused significant inhibition of the relaxations produced by both NECA and ...
Corresponding Author: Anaclet Ngezahayo Department of Cell Physiology and Biophysics, Institute of Cell Biology and Biophysics, Leibniz University Hannover, Herrenhäuser Straße 2, Hannover, 30419 (Germany ...
SMC announces that Can-Fite BioPharma has published the results of a study using STAM™ model in International Journal of Molecular Medicine.. Title: The A3 adenosine receptor agonist, namodenoson, ameliorates non-alcoholic steatohepatitis in mice. The A3 adenosine receptor agonist, namodenoson, ameliorates non‑alcoholic steatohepatitis in mice (spandidos-publications.com). ...
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Regadenoson is an A2A adenosine receptor agonist that causes coronary vasodilation and used for myocardial perfusion imagining. Manufactured by Astellas and FDA approved April 10, 2008.
Agenda Item 1.23 - 500kHz Progress through Committee 4 (COM4) was a little easier than expected and the frequency band 472-479kHz will be allocated to the amateur service, on a Secondary basis. This is subject to no further objections being received during the two final readings through the plenary meetings, of which the first blue reading is […]. Continue Reading. ...
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人們在19世紀末時同時使用著三個不同的電單位制,分別為:CGS靜電單位制,又稱高斯單位制,簡稱ESU;CGS電機械單位,簡稱EMU;以及用於配電系統的米-千克-秒制(國際單位制)。[24]在試圖根據因次分析用長度、質量及時間表達電單位時,科學家遇到了諸多困難──在使用ESU或EMU時,物理量會具有不同的因次。[16]1900年,喬瓦尼·吉奧爾吉(英语:Giovanni Giorgi)發表了一篇論文,提倡在當時的三個基本單位以外,再加一個基本單位,電單位不一致的問題迎刃而解。這第四個單位可以是電流、電壓和電阻中的其中一個。[25]. 19世紀後期至20世紀初期,人們採用了一系列不一致的單位制,在質量上有的用克,有的用公斤;在長度上有的用厘米,有的用米。例如有:表達功率的「Pferdestärke」(公制馬力)、[26][註 3]表達滲透性(英语:Permeability (earth ...
Vasodilator stress with adenosine or dipyridamole is an alternative to exercise stress with myocardial perfusion imaging for the detection of coronary artery disease. Although the safety of adenosine and dipyridamole has been well established, undesirable side effects including chest pain, headache, dyspnea, and atrioventricular conduction abnormalities do occur in a majority of patients.1-4 In addition, both adenosine and dipyridamole produce severe bronchoconstriction when given to asthmatics. Because of its ultrashort half-life, adenosine must be administered by a constant IV infusion.. Whereas adenosine-induced coronary vasodilatation is mediated primarily by stimulation of the A2A receptor subtype on vascular smooth muscle, the side effects described above are believed to be caused by stimulation of 1 or more of the other 3 adenosine receptor subtypes, A1, A2B, and A3.5 The discovery of highly selective and relatively short-acting adenosine receptor A2A agonists6-9 has opened the ...
Nicholls, J, Skene, DJ and Hourani, SMO (1997) Use of a newly developed technique to isolate rat pinealocytes and study the effects of adenosine agonists on melatonin production ...
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This is a pretty good hit rate. Generally virtual screening campaigns are lucky to have a hit rate of a few percent. Curiously, the authors also found a similarly high hit rate during a past VS campaign against the well-known β2 adrenergic receptor. What could be responsible for this high hit rate against GPCRs? The reasons are interesting. One reason could be that GPCRs are very well adapted to bind small molecules in compact pockets, enclosing them and forming many kinds of productive interactions. But more intriguingly, as the authors have noted earlier, there is biogenic bias in favor of certain target-specific chemotypes in commercial libraries that are screened, both during VS as well as HTS. This in turn reflects the biases of medicinal chemists in picking and synthesizing certain kinds of chemotypes based on the importance of drug targets and past successes in hitting these targets. GPCRs clearly are enormously important, and GPCR-friendly ligand chemotypes thus constitute a large ...
Diamond I, Mochly-Rosen D, Gordon AS. In Alcohol and seizures: basic mechanisms and clinical concepts. Porter R, Mattson R, Kramer J and Diamond I (eds). FA Davis, Philadelphia, pp 79-86, (1990). ...
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Adenosine acts as a break in biological systems, having inhibiting effects, but caffeine doesnt just stop this break, it also makes other neurotransmitters more active. For instance, it prevents breakdown of acetylcholine (ACh), so ACh sticks around longer, increasing its effect ...
This study is a 12-month, dose-level blinded, multicenter study of 2 inhaled dose levels of CVT-301 for the treatment of up to 5 OFF episodes per day in PD patients experiencing motor fluctuations (OFF episodes). All patients will receive active treatment, but patients will be blinded to dose level. This will serve as an extension to the CVT-301-004 study for those patients who participated in that study and remain eligible for this study. In addition, patients who previously completed the CVT-301-003, CVT-301-009 and CVT-301-005 (observational arm completers), as well as CVT-301 naïve patients may be enrolled if they meet the CVT-301-004E eligibility criteria ...
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Adenosine A2A Receptor Agonist Polydeoxyribonucleotide Alleviates Interstitial Cystitis-Induced Voiding Dysfunction by Suppressing Inflammation and Apoptosis in Rats
ウサギ・ポリクローナル抗体 ab106143 交差種: Hu 適用: WB,IHC-P,ICC/IF…Adenosine Receptor A2a抗体一覧…画像、プロトコール、文献などWeb上の情報が満載のアブカムの Antibody…
Heres Subject Delta from NECA modded with an LED inside courtesy of my Bioshock Light-up tutorial where you can create your own. Hes basically the NECA figure hollowed out with the LED kit inside and the drill a bit bloodies up. I also modded his left hand with the flame plasmid you get! ...
"Comparative hydrolysis of P2 receptor agonists by NTPDases 1, 2, 3 and 8". Purinergic Signalling. 1 (2): 193-204. doi:10.1007/ ... "Impact of ectoenzymes on p2 and p1 receptor signaling". Pharmacology of Purine and Pyrimidine Receptors. Advances in ... NTPDase1 hydrolyzes P2 receptor ligands, namely ATP, ADP, UTP and UDP with similar efficacy. NTPDase1 can therefore effect P2 ... Sepúlveda C, Palomo I, Fuentes E (2016). "Role of adenosine A2b receptor overexpression in tumor progression". Life Sciences. ...
Off-cells were also activated by UTP, but lacked any response to adenosine, a P1 agonist. Activation of off-cells by ATP was ... Histological staining by another research group examined the distribution of purinergic receptor subtypes throughout the RVM. ... On-cells displayed a greater response to P2X agonists vs P2Y agonists. For example, α,β-methylene ATP, a P2X agonist, activated ... On- and off-cells were both activated by local administration of ATP, a P1 and P2 agonist, whereas neutral cells were inhibited ...
There are three known distinct classes of purinergic receptors, known as P1, P2X, and P2Y receptors. Cell signalling events ... The following list of proposed medications is based on the workings of the purinergic signalling system: Diquafosol - Agonist ... The purinergic signalling complex of a cell is sometimes referred to as the "purinome". Purinergic receptors, represented by ... Purinergic receptors are specific classes of membrane receptors that mediate various physiological functions such as the ...
The adenosine receptors (or P1 receptors) are a class of purinergic G protein-coupled receptors with adenosine as the ... Newer adenosine receptor agonists and antagonists are much more potent and subtype-selective, and have allowed extensive ... Most older compounds acting on adenosine receptors are nonselective, with the endogenous agonist adenosine being used in ... The adenosine A1 receptor has been found to be ubiquitous throughout the entire body. This receptor has an inhibitory function ...
There are three known distinct classes of purinergic receptors, known as P1, P2X, and P2Y receptors. [What about P2Z,U,T?] P2X ... which is an agonist and has a high preference for the purinergic receptor type 1 isoform (P2Y1R), significantly contributes to ... P1 receptors are preferentially activated by adenosine and P2Y receptors are preferentially more activated by ATP. P1 and P2Y ... IUPHAR GPCR Database - Adenosine receptors IUPHAR GPCR Database - P2Y receptors Purinergic+Receptors at the US National Library ...
There are two main types of purinergic receptors, P1 binding to adenosine, and P2 binding to ATP or ADP, presenting different ... In general terms, platelet activation initiated by agonist takes to a signaling cascade that leads to an increase of the ... Therefore, there are four main transmembrane receptor types: G protein coupled receptors (GPCRs), tyrosine kinase receptors ( ... PAR1 and PAR4 receptors), platelet-derived thromboxane A2 (TxA2) (TP receptor) and ADP (P2Y1 and P2Y12 receptors) that is ...
... purinergic P1 receptor - purinergic P2 receptor - purinergic receptor - pyridine - pyrimidine - pyruvate - pyruvate oxidation ... Inverse agonist - invertebrate peptide receptor - invertebrate photoreceptor - Ion channel - ion channel gating - Ionic bond - ... interleukin receptor - interleukin-1 receptor - interleukin-2 receptor - interleukin-3 - interleukin-3 receptor - intermediate ... G protein-coupled receptor - G3P - GABA - GABA receptor - GABA-A receptor - gag-onc fusion protein - galanin - gamete - gamma- ...
Receptor. (ligands). P0 (adenine). *Agonists: 8-Aminoadenine. *Adenine. P1. (adenosine). *Agonists: 2-(1-Hexynyl)-N- ... Purinergic signalling. *Pyrophosphates. Hidden categories: *Chemical articles with multiple compound IDs. *Multiple chemicals ... ADP interacts with a family of ADP receptors found on platelets (P2Y1, P2Y12, and P2X1), which leads to platelet activation.[14 ... P2Y1 receptors initiate platelet aggregation and shape change as a result of interactions with ADP. ...
This results in a receptor blockade, inhibiting the binding of agonists and inverse agonists. Receptor antagonists can be ... Eicosanoid receptor (Prostaglandin receptor). *Protease-activated receptor. *Neurotransmitter receptor. *Purinergic receptor. * ... GABA receptors: GABA-A, GABA-C. GABA. Cl− , HCO−3 [11]. Glutamate receptors: NMDA receptor, AMPA receptor, and Kainate receptor ... toll-like receptors (TLRs), killer activated and killer inhibitor receptors (KARs and KIRs), complement receptors, Fc receptors ...
Purinergic Agents. *Purinergic Agonists. *Purinergic P1 Receptor Agonists. *Purines. *Ribonucleosides. *Sensory System Agents ... Adenosine receptor A2a. MPIMGSSVYITVELAIAVLAILGNVLVCWAVWLNSNLQNVTNYFVVSLAA.... yes. agonist. Adenosine receptor A2b. ... Adenosine receptor A1. MPPSISAFQAAYIGIEVLIALVSVPGNVLVIWAVKVNQALRDATFCFIVS.... yes. agonist. Adenosine receptor A3. ... This effect may be mediated through the drugs activation of cell-surface A,sub,1,/sub, and A,sub,2,/sub, adenosine receptors. ...
Purinergic P1 Receptor Antagonists. Purinergic Antagonists. Purinergic Agents. Neurotransmitter Agents. Analgesics. Sensory ... The adenosine receptor is known for its anti-inflammatory actions and could therefore be a potential target in the treatment of ... Antagonism of the adenosine receptor by caffeine leads to an increased LPS-induced inflammatory reaction and an increase in ( ... Stimulation of the adenosine receptor could potentially lead to a decrease in inflammation and tissue damage. ...
Purinergic P1 Receptor Agonists. Purinergic Agonists. Purinergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ...
Purinergic P1 Receptor Agonists. Purinergic Agonists. Purinergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ...
Purinergic P1 Receptor Agonists. Purinergic Agonists. Purinergic Agents. Neurotransmitter Agents. Molecular Mechanisms of ...
Purinergic Agents. *Purinergic Agonists. *Purinergic P1 Receptor Agonists. *Purines. *Ribonucleosides. *Sensory System Agents ... Adenosine receptor A1 MPPSISAFQAAYIGIEVLIALVSVPGNVLVIWAVKVNQALRDATFCFIVS... yes. agonist. Adenosine receptor A2b ... Adenosine receptor A3 MPNNSTALSLANVTYITMEIFIGLCAIVGNVLVICVVKLNPSLQTTTFYF... yes. agonist. Adenosine receptor A2a ... Adenosine may exert its pharmacologic effects by activation of purine (cell surface A1 and A2 adenosine) receptors, as well as ...
... receptor. The aim of the present study was to elucidate the effects of PD81,723 both as a … ... has been shown to allosterically enhance agonist binding and function at the adenosine A(1) ... Purinergic P1 Receptor Agonists * Purinergic P1 Receptor Antagonists * Receptors, Purinergic P1 / genetics ... We investigated its effect on the human wild-type in relation to a mutant (T277A) adenosine A(1) receptor for which agonists ...
... yet neither the specific adenosine receptor involved no … ... receptor agonists, unlike growth factors, increases the rate at ... Purinergic P1 Receptor Agonists * Receptor, Adenosine A2A * Receptors, Purinergic P1 / genetics * Receptors, Purinergic P1 / ... Recent evidence indicates that topical application of adenosine A(2A) receptor agonists, unlike growth factors, increases the ... To determine which adenosine receptor is involved and whether adenosine receptor-mediated stimulation of angiogenesis plays a ...
Purinergic P1 Receptor Agonists: 1 study in 2 results : IBA. *Leukemia Inhibitory Factor: 1 study in 2 results : IBA ... Purinergic P1 Receptors (Adenosine Receptor): 4 studies in 23 results : IBA. *Adenosine: 4 studies in 22 results : FDA 19 ... Drug Receptors (Drug Receptor): 1 study in 1 result : IBA. *T-Cell Antigen Receptors (T-Cell Receptor): 1 study in 1 result : ... MT2 Melatonin Receptor: 1 outcome in 1 result : IBA. *Melanocortin Receptors (Melanocortin Receptor): 1 outcome in 1 result : ...
P1 or Adenosine receptors GraphId=aba11, ,Graphics CenterX=845.8450842431788 CenterY=587.9216367603486 Width= ... Agonist binding Antagonist binding GraphId=bf23c, ,Graphics CenterX=359.7505800464012 CenterY=36.67343387470957 Width= ... Update on novel purinergic P2X3 and P2X2/3 receptor antagonists and their potential therapeutic applications.,/bp:TITLE, ,bp: ... nucleotide signaling via the purinergic P2Y receptors.,/bp:TERM, ,bp:ID xmlns:rdf=http://www.w3.org/1999/02/22-rdf-syntax-ns# ...
... agonist order ATP , ADP , AMP , ADO), purinergic nucleotides like ATP are not strong agonists of P1 receptors which are ... P1 receptors have A1, A2a, A2b, and A3 subtypes (A as a remnant of old nomenclature of adenosine receptor), all of which are ... axons and glia activates purinergic membrane receptors known as P2. The P2Y receptors are metabotropic, i.e. G protein-coupled ... purinergic receptors.. In humans, this signaling role is important in both the central and peripheral nervous system. Activity- ...
Purinergic Agents. *. Purinergic Agonists. *. Purinergic P1 Receptor Agonists. *. Sensory System Agents. *. Vasodilator Agents ...
... and concentration-dependent manner and was inhibited by antagonists of P2 and P1 purinergic receptors. Agonist studies revealed ... which could lead to activation of P1 purinergic receptors. As one approach to assess the involvement of P2 and P1 receptors in ... the P2Y1 agonist 2MeSADP and the P1 agonist, adenosine, did not stimulate release of TSP-1. UTP can activate three P2 receptors ... an agonist of P2Y1 receptors, and 2′,3′-O-(4-benzoyl)benzoyl-ATP (BzATP), an agonist of P2X receptors, were weak or ineffective ...
"Comparative hydrolysis of P2 receptor agonists by NTPDases 1, 2, 3 and 8". Purinergic Signalling. 1 (2): 193-204. doi:10.1007/ ... "Impact of ectoenzymes on p2 and p1 receptor signaling". Pharmacology of Purine and Pyrimidine Receptors. Advances in ... NTPDase1 hydrolyzes P2 receptor ligands, namely ATP, ADP, UTP and UDP with similar efficacy. NTPDase1 can therefore effect P2 ... Sepúlveda C, Palomo I, Fuentes E (2016). "Role of adenosine A2b receptor overexpression in tumor progression". Life Sciences. ...
4H-J and M). Other purinergic agonists that we tested, including adenosine, which activate P1 receptors, and α,β-methylene ATP ... an agonist with preference for P2Y6 receptors, as well as to MRS2768 (10 μmol/L), an agonist with preference for P2Y2 receptors ... We quantified changes in purinergic receptor transcript levels and found that numerous purinergic receptors were downregulated ... Purinergic signals regulate macrophage physiology and secretion. Quantification of mRNA levels of the purinergic receptors P2X7 ...
Oral tissues express a variety of G-protein-coupled P2Y receptors for ATP and P1 receptors for adenosine in addition to ... When these receptors are combined with the plethora of extracellular enzymes capable of manipulating extracellular agonist ... The intricacies of the purinergic signaling system make it well-suited for the unique concerns of dental research, and future ... Activation of P2X receptors is implicated in dental pain, and receptor antagonists represent important targets for new ...
Pharmacological examination showed that the ATP responses are primarily mediated by P2X purinergic receptors. Interestingly, ... Pharmacological examination showed that the ATP responses are primarily mediated by P2X purinergic receptors. Interestingly, ... The ACh effects are diminished in the presence of atropine or M3 muscarinic receptor antagonist and in SCs lacking M3 receptors ... Previously, we showed that superficially located microvillous cells (MCs) in the MOE expressing transient receptor potential ...
Purinergic receptors activated by extracellular nucleotides (adenosine 5′-triphosphate (ATP) and uridine 5′-triphosphate (UTP ... P2Y2 receptor agonist with enhanced stability protects the heart from ischemic damage in vitro and in vivo. Purinergic Signal 9 ... ATP P2X receptors P2Y receptors P1 receptors Rat embryo Heart Cardiomyocyte FLIPR Calcium mobilization ... Responses mediated by agonists specific for P2Y receptors subtypes showed that P2Y receptors (P2Y1, P2Y2, P2Y4 and P2Y6) were ...
The extracellular adenosine formed acts as an agonist of purinergic P1 receptors. They also can produce and hydrolyze ... They hydrolyze extracellular nucleotides and thus can control their availability at purinergic P2 receptors. They generate ... The erythropoietin receptor transmembrane domain mediates complex formation with viral anemic and polycythemic gp55 proteins.. ... Ecto-nucleotidases play a pivotal role in purinergic signal transmission. ...
... specific bradykinin or ATP receptor agonists (B1 receptor agonist Sar-[D-Phe8]-des-Arg9-Bradykinin, P2X receptor agonist α, β ... or pan-P1 adenosine receptor antagonist (CGS15493), suggesting the response to ATP in our experimental paradigm was largely ... highlighting the redundancy and complexity of purinergic signalling. ... B2 receptor antagonist HOE140, adenosine receptor antagonist CGS15943, P2×2/3,3 receptor antagonist RO4) were used to examine ...
Purinergic P1 Receptor Agonists. *. Treatment of Paroxysmal Supraventricular Tachycardia and Rate Control in Atrial ...
Purinergic P1 Receptor Agonists * Purinergic P1 Receptor Antagonists * Purinergic P1 Receptors * Eye ... Fingerprint Dive into the research topics of Intravitreous Injection of Adenosine or Its Agonists Causes Breakdown of the ... Intravitreous Injection of Adenosine or Its Agonists Causes Breakdown of the Blood-Retinal Barrier. ...
Purinergic P1 Receptors * Purinergic P1 Receptor Agonists * Purinergic P1 Receptor Antagonists * Pharmaceutical Chemistry ... Adenosine receptors as targets for therapeutic intervention. Suvarna, B., 01-01-2013, In: Kathmandu University Medical Journal. ...
Purinergic P1 Receptor Agonists * Immune System * Macrophage Inflammatory Proteins * N-(oxo-5,6-dihydrophenanthridin-2-yl)-N,N- ...
"Comparative hydrolysis of P2 receptor agonists by NTPDases 1, 2, 3 and 8". Purinergic Signalling. 1 (2): 193-204. doi:10.1007/ ... Kukulski F, Lévesque SA, Sévigny J (2011-01-01). "Impact of ectoenzymes on p2 and p1 receptor signaling". Advances in ... Yegutkin GG (May 2008). "Nucleotide- and nucleoside-converting ectoenzymes: Important modulators of purinergic signalling ... NTPDase1 hydrolyzes P2 receptor ligands, namely ATP, ADP, UTP and UDP with similar efficacy.[6] NTPDase1 can therefore affect ...
Purinergic P1 Receptor Agonists Medicine & Life Sciences * Neurology Chemical Compounds * Enzymes Medicine & Life Sciences ... in animal models of epilepsy and pain with an improved preclinical therapeutic window over direct acting ADO receptor agonists. ... in animal models of epilepsy and pain with an improved preclinical therapeutic window over direct acting ADO receptor agonists. ... in animal models of epilepsy and pain with an improved preclinical therapeutic window over direct acting ADO receptor agonists. ...
This effect was likely mediated via adenosine A1 receptor (A1R), as the selective A1R agonist ADAC (1 µM) conferred a higher ... Purinergic Signalling and Aminoglycoside Ototoxicity: The role of P1 and P2 receptors. ResearchSpace/Manakin Repository. Login ... Purinergic Signalling and Aminoglycoside Ototoxicity: The role of P1 and P2 receptors. Lin, Ching Yu ... Activation of P1/adenosine receptors (AR), on the other hand, partially protected the organ of Corti against neomycin-induced ...
... rather than a P1, purinergic effect.7 Moreover, increased release of nitric oxide may be involved in eliciting this response in ... blockade of an autocrine/paracrine pathway to define receptor preference of an agonist. J Biol Chem. 1998;273:23093-23097. ... Capacity for Purinergic Control of Renin Promoter via P2Y11 Receptor and cAMP Pathways. Louise van der Weyden, David J. Adams, ... Purinergic-P(2Y) receptors stimulate renin secretion by rat renal cortical slices. J Pharmacol Exp Ther. 1993;266:160-163. ...
Local delivery of adenosine receptor agonists to promote bone regeneration and defect healing. Lopez, C. D., Bekisz, J. M., ... The Role of Adenosine Receptor Activation in Attenuating Cartilaginous Inflammation. Bekisz, J. M., Lopez, C. D., Corciulo, C ...
Purinergic P1 Receptor Agonists * Purinergic P1 Receptors * Reperfusion * Respiration * Respiratory Insufficiency * Seizures ...
  • Caffeine (4mg/kg) is used as an adenosine receptor antagonist. (clinicaltrials.gov)
  • Caffeine is an adenosine receptor antagonist. (clinicaltrials.gov)
  • The aim of the present study was to elucidate the effects of PD81,723 both as an allosteric enhancer and as an antagonist on the adenosine A(1) receptor. (nih.gov)
  • Using an in vitro model of CNS trauma that stimulates release of ATP, we found that TSP-1 expression increased after mechanical strain and was completely blocked by a P2 receptor antagonist and by inhibition of p38/mitogen-activated protein kinase and Akt, thereby indicating a major role for P2 receptor/protein kinase signaling in TSP-1 expression induced by trauma. (pnas.org)
  • The ACh effects are diminished in the presence of atropine or M3 muscarinic receptor antagonist and in SCs lacking M3 receptors. (frontiersin.org)
  • Human serosal visceral nociceptor mechanosensitivity is attenuated by treatment with the transient receptor potential channel, vanilloid 4 (TRPV 4 ) antagonist (HC067047), highlighting the therapeutic potential of TRPV 4 blockade for the treatment of visceral pain. (bmj.com)
  • The hemodynamic effects of R-N 6 -(phenylisopropyl)-adenosine (R-PIA, a A 1 selective adenosine receptor agonist) and the antagonistic effects of 8-phenyltheophylline (a nonselective adenosine receptor antagonist) and glibenclamide (ATP sensitive potassium channel antagonist) were investigated in 72 anesthetized Sprague-Dawley rats. (elsevier.com)
  • Differential allosteric modulation by amiloride analogues of agonist and antagonist binding at A(1) and A(3) adenosine receptors. (nih.gov)
  • The diuretic drug amiloride and its analogues were found previously to be allosteric modulators of antagonist binding to A(2A) adenosine receptors. (nih.gov)
  • In this study, the possibility of the allosteric modulation by amiloride analogues of antagonist binding at A(1) and A(3) receptors, as well as agonist binding at A(1), A(2A), and A(3) receptors, was explored. (nih.gov)
  • Thus, amiloride analogues are allosteric inhibitors of antagonist binding at A(1), A(2A), and A(3) adenosine receptor subtypes. (nih.gov)
  • The binding modes of amiloride analogues at agonist-occupied and antagonist-occupied receptors differed markedly, which was demonstrated in all three subtypes of adenosine receptors tested in this study. (nih.gov)
  • Chronic treatment with the adenosine receptor antagonist caffeine evokes an up-regulation of A 1 adenosine receptors and increased coupling of the receptor to G proteins in rat brain membranes. (elsevier.com)
  • Antagonist exposure (1) increased the density of A 1 adenosine receptors in cerebellar granule cell membranes, (2) blunted the effect of guanyl nucleotides on receptor coupling to G proteins, and (3) increased the functional coupling of receptors to adenylyl cyclase inhibition. (elsevier.com)
  • These effects of CCPA were attenuated by the adenosine A1-receptor antagonist 8-cyclopentyl-1,3-dipropylxanthine at 10(-7) M. In additional experiments, CCPA exhibited similar effectiveness in reducing the spontaneous heart rate of immature and mature hearts, an effect also mediated by activation of adenosine A1 receptors. (umassmed.edu)
  • Neither the change in [Ca 2+ ] i nor the stimulation of cotransport was abolished by the adenosine receptor antagonist 8-{4-[N-(2-aminoethyl)carbamoylmethoxy]-phenyl}-1,3-dipropylxanthine (XAC). (elsevier.com)
  • With the cells overexpressing LPA 1 , LPA 2 , or LPA 3 , we examined the selectivity and mode of inhibition by Ki16425 against the LPA-induced actions and compared them with those of dioctyl glycerol pyrophosphate (DGPP 8:0), a recently identified antagonist for LPA receptors. (aspetjournals.org)
  • SOD1G93A mice were chronically treated, from presymptomatic stage, with a selective adenosine A2A receptor agonist (CGS21680), antagonist (KW6002) or the A1 receptor antagonist DPCPX. (elsevier.com)
  • The non-xanthine heterocyclic compound SCH 58261 is a new potent and selective A2a adenosine receptor antagonist. (wikipathways.org)
  • 1. A method of enhancing an immune response in a host, comprising administering to the host an A.sub.2a receptor antagonist in combination or alternation with a checkpoint inhibitor. (patents.com)
  • These effects of DPCPX in EtOH withdrawn female and male slices were prevented by co-exposure to either the A 1 agonist CCPA or the NMDA receptor antagonist APV for 24 hours. (elsevier.com)
  • In competition with antagonist radioligand biphasic curves were observed for agonists. (biomedsearch.com)
  • Aki Y, Tomohiro A, Nishiyama A et al (1997) Effects of KW-3902, a selective and potent adenosine A1 receptor antagonist, on renal hemodynamics and urine formation in anesthetized dogs. (springer.com)
  • The cyclic pyridoxine-alpha4, 5-monophosphate, compound 2 (MRS 2219), was found to be a selective potentiator of ATP-evoked responses at rat P2X1 receptors with an EC50 value of 5.9 +/- 1.8 microM, while the corresponding 6-azophenyl-2',5'-disulfonate derivative, compound 3 (MRS 2220), was a selective antagonist. (edu.au)
  • The P2 receptor antagonist reactive blue 2, but not pyridoxal-phosphate-6-azophenyl-2',4'-disulphonic acid (PPADS) attenuated ATP-induced striatal injury. (ajou.ac.kr)
  • Pharmacology of Purine and Pyrimidine Receptors. (wikipedia.org)
  • In fact, adenosine receptor activation can subtypes of P1 receptors can be distinguished from one even prevent the acquisition of amygdala kindling (Abdul- another by receptor pharmacology or by examination of the signal transduction pathways to which the individual receptors couple. (gotomydoctor.com)
  • For example, the A1 adenosine receptor *Author for correspondence at: Department of Medical subtype is classically associated with the inhibition of Pharmacology and Toxicology, The Texas A&M Univ. (gotomydoctor.com)
  • Comparative pharmacology of human adenosine receptor subtypes - characterization of stably transfected receptors in CHO cells. (biomedsearch.com)
  • In this study we present for the first time the comparative pharmacology of all known human adenosine receptor subtypes. (biomedsearch.com)
  • Advances in the pharmacology of purinergic neurotransmission has led to the development of new strategies to enhance the endogenous actions of ADO and to limit the neuroexcitatory effects of ATP. (cognizantcommunication.com)
  • Two of these strategies, the development of selective adenosine kinase inhibitors and P2X 3 receptor-selective antagonists, are highlighted in this review of the recent developments in the pharmacology of purinergic modulation of nociceptive signaling. (cognizantcommunication.com)
  • The present understanding of opioid pharmacology has been influenced by discoveries relating to the mechanisms that operate on G-protein-coupled receptor (GPCR) signaling. (cognizantcommunication.com)
  • From these results obtained, it is hypothesized that adenosine receptors in carotid body are A 2 -receptor subtype mediating the pressor effect of adenosine and its analogue, the negative chronotropic or/and inotropic effects of adenosine and its analogue are involved in their hypotensive action, and ATP-sensitive K + channels coupled by adenosine receptors may be activated by adenosine to mediate its effects. (elsevier.com)
  • The P2Y1 receptor is activated by adenosine diphosphate (ADP), whereas, at P2Y2, ATP and uridine-5′-triphosphate (UTP) are equipotent. (royalsocietypublishing.org)
  • P1 are G-protein-coupled receptors activated by adenosine. (alzforum.org)
  • Macrophage production and secretion of these homeostatic factors are controlled by endogenous purinergic signals. (diabetesjournals.org)
  • Endogenous adenosine increases coronary flow by activation of both A2A and A2B receptors in mice. (ac.be)
  • In the heart, endogenous adenosine attenuates the beta-adrenergic-elicited increase in contractile performance via activation of adenosine A1 receptors. (umassmed.edu)
  • Regulation of plasma membrane ion transport by endogenous purinergic receptors was assessed in a distal renal (A6) cell line. (elsevier.com)
  • The RVM contains high levels of both the neurokinin 1 receptor and its endogenous ligand, Substance P (SP). (wikipedia.org)
  • The P2X subfamily includes seven receptors, P2X1-P2X7, for which ATP is the primary endogenous ligand [ 6 ]. (royalsocietypublishing.org)
  • The release of endogenous nucleotides represents a critical first step for the initiation of purinergic signaling. (physiology.org)
  • In the presence of GTP all receptors were converted to a single low affinity state indicating functional coupling to endogenous G proteins. (biomedsearch.com)
  • Barrett RJ, Droppleman DA (1993) Interactions of adenosine A1 receptor-mediated renal vasoconstriction with endogenous nitric oxide and ANG II. (springer.com)
  • The adenosine receptors (or P1 receptors [1] ) are a class of purinergic G protein-coupled receptors with adenosine as the endogenous ligand . (wikipedia.org)
  • This nucleoside, acting at one or more of its receptors, is a potent endogenous anti-inflammatory mediator. (biomedcentral.com)
  • adenosine) receptors, as well as relax vascular smooth muscles through the reduction in calcium uptake by inhibition of slow inward calcium current and activation of adenylate cyclase in smooth muscle cells. (rcsb.org)
  • In normal Ca (1.8 mM), addition of sufficient Mg to reduce m to less than half the control value did not alter the degree of inhibition produced by adenosine receptor agonists. (northwestern.edu)
  • Agents which displace Ca from storage sites and also inhibit phosphodiesterases increased m.e.p.p.f in the virtual absence of extracellular Ca and increased the level of inhibition produced by adenosine receptor agonists. (northwestern.edu)
  • The difference in the inhibition profile of Ki16425 and DGPP 8:0 was exploited for the evaluation of receptor subtypes involved in responses to LPA in A431 cells. (aspetjournals.org)
  • Adenosine A2A receptors mediate GABAergic inhibition of respiration in immature rats. (wikipathways.org)
  • Further, this sex difference is not related to effects of EtOH exposure on A1 receptor abundance, but likely reflects increased NMDA receptor-mediated signaling downstream of A 1 inhibition in females. (elsevier.com)
  • The effects induced by P2Y11 receptor activation were oppositely modulated by PKA or MAPK inhibition, in line with the dual nature of the Gs- and Gq-coupled receptor. (unich.it)
  • 6 Our results indicate that the anti-convulsant e ects CADO in the basolateral amygdala may be mediated, in part, by the A1 receptor-dependent inhibition of voltage gated calcium channels. (gotomydoctor.com)
  • Various agonists and antagonists are involved in the inhibition and induction of purinergic signalling, which causes alterations in the responsive cells. (springeropen.com)
  • Bailey MA (2004) Inhibition of bicarbonate reabsorption in the rat proximal tubule by activation of luminal P2Y1 receptors. (springer.com)
  • They hydrolyze extracellular nucleotides and thus can control their availability at purinergic P2 receptors. (scienceopen.com)
  • Biological actions of NTPDases are a consequence (at least in part) of the regulated phosphohydrolytic activity on extracellular nucleotides and consequent effects on P2-receptor signaling. (scienceopen.com)
  • Purinergic receptors activated by extracellular nucleotides (adenosine 5′-triphosphate (ATP) and uridine 5′-triphosphate (UTP)) are well known to exert physiological effects on the cardiovascular system, whether nucleotides participate functionally in embryonic heart development is not clear. (springer.com)
  • Modulation of murine dendritic cell function by adenine nucleotides and adenosine: involvement of the A(2B) receptor. (ac.be)
  • 9 These P2Y receptors are expressed in a variety of tissues and can be differentiated pharmacologically on the basis of their selectivity for adenosine (ATP, ADP) and uridine (UTP, UDP) nucleotides. (ahajournals.org)
  • The nucleoside adenosine and nucleotides including adenine mononucleotides like ADP and ATP and dinucleotides such as P1,P4-diadenosine tetraphosphate (Ap4A), and P1,P5-diadenosine pentaphosphate (Ap5A) are present in different ocular locations and therefore they may contribute/modulate inflammatory processes. (ucm.es)
  • In summary, adenosine and nucleotides can activate receptors in ocular structures susceptible to suffer from inflammatory processes. (ucm.es)
  • It consists of P1 receptors, with adenosine as the agonist, and P2 receptors, activated by nucleotides (e.g., adenosine 5'-triphosphate - ATP). (bvsalud.org)
  • Purinergic signalling (or signaling: see American and British English differences) is a form of extracellular signalling mediated by purine nucleotides and nucleosides such as adenosine and ATP. (wikipedia.org)
  • Released nucleotides can be hydrolyzed extracellularly by a variety of cell surface-located enzymes referred to as ectonucleotidases that control purinergic signalling. (wikipedia.org)
  • Macrophages and thymocytes express various purinergic nucleotide receptors that, in the presence of ATP and other nucleotides, regulate immune development and microbial infections ( 3 , 10 ). (asm.org)
  • At P2Y4 and P2Y6, the uridine nucleotides UTP and uridine diphosphate (UDP) are preferred agonists, respectively. (royalsocietypublishing.org)
  • Affinity for extracellular nucleotides ranges from the low nanomolar level (P2Y receptors) to the high micromolar level (P2X7 receptor). (royalsocietypublishing.org)
  • This wide range of affinities of P2 receptors for extracellular nucleotides confers a remarkable plasticity to purinergic signalling, allowing the detection of minute as well as large changes of agonist concentration within the extracellular space. (royalsocietypublishing.org)
  • Last but not least, nucleotides ligate specific plasma membrane receptors that confer a remarkable specificity to their signalling. (royalsocietypublishing.org)
  • Essentially every cell in a mammalian organism leaks or releases these mediators, and carries receptors for nucleotides of which seven ionotropic (P2X) and at least eight metabotropic (P2Y) receptor subtypes have been identified and characterized to date. (springer.com)
  • Nucleotides and nucleosides act as potent extracellular messengers via the activation of the family of cell-surface receptors termed purinergic receptors. (biomedcentral.com)
  • Notably, the isolated application of purinergic antagonists was sufficient to change the basal proliferation of AGS cells, indicating that nucleotides released by the cells can act as paracrine/autocrine signals. (frontiersin.org)
  • The control of the levels of extracellular nucleotides adenine and adenosine and the consequent signaling by purinergic receptors induced by them is critical in maintaining the physiological processes [5]. (thefreelibrary.com)
  • These pathological conditions can be associated with disturbance in the signaling mediated by nucleotides and nucleosides of adenine, in expression or activity of extracellular ectonucleotidases and in activation of P2X and P2Y receptors. (hindawi.com)
  • Stimulation of the adenosine receptor could potentially lead to a decrease in inflammation and tissue damage. (clinicaltrials.gov)
  • The actions of extracellular ATP are a result of stimulation of P2-type purinergic receptors, which are categorized into ligand-gated ion channels (P2X 1-7 ) or metabotropic heptahelical G protein-coupled receptors (P2Y 1,2,4,6,11-14 ) ( 12 ). (pnas.org)
  • These results demonstrate that adenosine receptor stimulation differentially modulates the LPS-induced production of IL-10, TNF-α, and NO in vitro and in vivo. (utmb.edu)
  • Activation of nucleotide receptors with extracellular ATP and nucleotide analogues increased intracellular calcium concentration ([Ca 2+ ] i ) primarily by release of intracellular calcium stores, with relative potency of agonists similar to that seen for stimulation of Na-K-Cl cotransport. (elsevier.com)
  • To address possible mechanisms for stimulation of Na-K-Cl cotransport by the nucleotide receptor, 125 I efflux and patch-clamp studies were used to measure chloride secretion. (elsevier.com)
  • The results showed that neither the stimulation nor the blockade of adenosine A2A receptors modified the progressive loss of motor skills or survival of mSOD1G93A mice. (elsevier.com)
  • TIF) pone.0096281.s002.tif (268K) GUID:?7633F6F9-B387-4CFD-A0C2-D441980E9525 Abstract Background Novel developmental functions have already been related to the P2X7 receptor (P2X7R) including proliferation stimulation and neural differentiation. (eaap2017.org)
  • The stimulation of A2A receptor reduced the overexpression of the EMT-related markers, mainly through the cAMP-dependent PKA pathway, as confirmed by cell pre-treatment with Myr-PKI. (unich.it)
  • Both A1 and P2Y1 receptor stimulation exacerbated the TGF-β1-driven effects, which were reduced by cell pre-treatment with the MAPK inhibitor PD98059, according to the increased ERK1/2 phosphorylation upon receptor activation. (unich.it)
  • On murine T lymphocytes the A2aR is highly expressed ( 20 ), and after T-cell receptor (TCR) stimulation, A2aR mRNA levels increase by a factor of ∼10 ( 16 ). (physiology.org)
  • Moreover, the clinical examples provided by use of adenosine to treat supraventricular tachycardias and ATP/UTP to stimulate airway secretion indicate that pharmacological stimulation of purinergic receptors can be useful therapeutically. (elsevier.com)
  • The function of the AMPA and NMDA receptors is associated with long-term potentiation, LTP, which is caused by the stimulation of protein kinases by Ca 2+ ions, and long-term depression, LTD, which results from the low influx of Ca 2+ ions and the activation of phosphatases. (scirp.org)
  • Within the concept of a simplified two-state receptor model, it is possible that the effects of PD81,723 are mainly "allosteric", enhancing the binding of adenosine A(1) agonists and inhibiting the binding of antagonists/inverse agonists. (nih.gov)
  • RMI 12,330A (7 X 10(‐6) to 7 X 10(‐5) M), an adenylate cyclase inhibitor, occluded the effects of adenosine receptor agonists on ACh release. (northwestern.edu)
  • Regadenoson is an selective low-affinity (Ki= 1.3 µM) A2A receptor agonist that mimics the effects of adenosine in causing coronary vasodilatation and increasing myocardial blood flow. (drugbank.ca)
  • Methods: The current studies examined effects of adenosine A 1 receptor manipulation on neuronal injury in EtOH-naïve and EtOH-withdrawn male and female rat hippocampal slice cultures. (elsevier.com)
  • Agmon Y, Dinour D, Brezis M (1993) Disparate effects of adenosine A1- and A2-receptor agonists on intrarenal blood flow. (springer.com)
  • 2-Chloro-N 6 -cyclopentyladenosine (CCPA), an agonist of A 1 adenosine receptors, at 0.5 mg/kg diminished LPS-induced plasma TNF-α concentrations, but enhanced LPS-induced IL-10 levels only at the highest dose used (2 mg/kg). (utmb.edu)
  • Similar to CCPA, the adenosine A1-receptor agonist R-N6-(2-phenylisopropyl)adenosine reduced the Iso-elicited contractile response more in immature than in mature hearts, albeit with less effectiveness than CCPA. (umassmed.edu)
  • 2-Chloro-N6-[3H]cyclopentyladenosine ([3H]CCPA)--a high affinity agonist radioligand for A1 adenosine receptors. (wikipathways.org)
  • 2 CADO, adenosine, and the A1 subtype-selective agonists N6-(L-2-Phenylisopropyl)adenosine (R- PIA) and 2-chloro-N6-cyclopentyladenosine (CCPA) reversibly modulated whole cell Ba2+ currents in a concentration-dependent fashion. (gotomydoctor.com)
  • The A1 subtype showed the typical pharmacological profile with 2-chloro-N6-cyclopentyladenosine (CCPA) as the agonist with the highest affinity and a marked stereoselectivity for the N6-phenylisopropyladenosine (PIA) diastereomers. (biomedsearch.com)
  • Specific A 1 antagonists include 8-Cyclopentyl-1,3-dipropylxanthine (DPCPX), and Cyclopentyltheophylline (CPT) or 8-cyclopentyl-1,3- dipropylxanthine (CPX), while specific agonists include 2-chloro-N(6)-cyclopentyladenosine ( CCPA ). (wikipedia.org)
  • Moreover, unlike the WT A(3)AR, the entire pool of internalized mutant A(3)AR is able to recycle back to the plasma membrane following agonist removal. (edgehill.ac.uk)
  • The receptor levels on the cell surface generally recover on withdrawal of the agonist, because of either translocation of the sequestered A1AR back to plasma membrane or de novo synthesis of A1AR. (elsevier.com)
  • Withdrawal of the agonist after a 24-h exposure resulted in rapid recovery of plasma membrane A1AR. (elsevier.com)
  • in the presence of millimolar concentrations of external ATP effluxed from the macrophages or other mammalian cells ( 1 , 7 , 9 , 25 ), the surface-associated P2Z receptors of macrophages and other phagocytic or inflammatory cells are activated, thereby altering the permeability of the plasma membrane. (asm.org)
  • however, we now know that ATP also plays a fundamental physiological role as a pleiotropic extracellular messenger of cell-to-cell communication acting at plasma membrane receptors named P2 purinergic receptors [ 1 ]. (royalsocietypublishing.org)
  • and determining the mechanisms responsible for receptor expression and insertion into the plasma membrane and for receptor desensitization, recycling, and termination of signaling. (elsevier.com)
  • ATP provokes the activation of specific purinergic receptors in the plasma membrane (Fig. 1 . (springeropen.com)
  • Purinergic receptors sit on the plasma membrane and are activated by ATP or its breakdown products ADP, AMP, and adenosine. (alzforum.org)
  • however, the precise role of each LPA receptor subtype has not yet been fully characterized. (aspetjournals.org)
  • Potent adenosine receptor antagonists that are selective for the A1 receptor subtype. (wikipathways.org)
  • While ATP primarily acts as a proinflammatory signal on purinergic P2 receptors, its degradation product adenosine signals through P1 purinergic receptors, mediating both anti- and proinflammatory effects depending on the receptor subtype. (physiology.org)
  • Depending on the P2 receptor subtype and signaling pathways involved, these receptors trigger and mediate short-term (acute) processes that affect cellular metabolism, adhesion, activation or migration. (springer.com)
  • Using specific inhibitors for each purinergic receptor subtype, Delekate found that blocking P2Y1 returned astrocyte signaling to normal in the APPPS1 mice. (alzforum.org)
  • Newer adenosine receptor agonists and antagonists are much more potent and subtype-selective, and have allowed extensive research into the effects of blocking or stimulating the individual adenosine receptor subtypes, which is now resulting in a new generation of more selective drugs with many potential medical uses. (wikipedia.org)
  • Abebe W, Hussain T, Olanrewaju H et al (1995) Role of nitric oxide in adenosine receptor-mediated relaxation of porcine coronary artery. (springer.com)
  • While P2Y and P1 subtypes are G-protein-coupled metabotropic receptors, P2X receptors are resembled as homo- or hetero-trimeric ligand-gated ion stations from seven feasible subunits. (eaap2017.org)
  • In 1985, a pharmacological approach was proposed to distinguish between two types of P2 receptors: ionotropic P2X and metabotropic P2Y receptors [ 3 ]. (hindawi.com)
  • She first confirmed that the astrocytes were hyperactive, then tested whether these star-shaped cells were simply responding to neuronal activity by blocking either neuronal transmission or the astrocyte metabotropic glutamate receptors that sense it. (alzforum.org)
  • The metabolic degradation of ATP to adenosine (ADO) provides an array of purinergic signaling molecules that can interact with a large population of cell surface receptors that include the ATP-sensitive ionotropic P2X and metabotropic P2Y receptor superfamilies, as well as the P1 ADO-sensitive G-protein-coupled receptors. (cognizantcommunication.com)
  • Burnstock G (1978) A basis for distinguishing two types of purinergic receptor. (springer.com)
  • However, receptor accumulation into endosomes is dependent upon prior G-protein-coupled receptor kinase (GRK)-mediated phosphorylation of the receptor's carboxyl terminus, as replacement of the carboxyl-terminal domain of the human A(1)AR with the 14 GRK-phosphorylated amino acids of the rat A(3)AR confers rapid agonist-mediated endosomal accumulation of the resulting chimeric A(1)CT3AR. (edgehill.ac.uk)
  • G protein-coupled estrogen receptor 1 (GPER) is a membrane-associated estrogen receptor (ER) associated with rapid estrogen-mediated effects. (bvsalud.org)
  • Four distinct subtypes of P1 receptors have been identified: adenosine A1, A2a, A2b, and A3 receptors (R) which are G protein coupled ( 10 ). (physiology.org)
  • Four adenosine receptor subtypes of the family of G protein-coupled receptors, designated A1, A2A, A2B and A3 are currently known. (biomedsearch.com)
  • The latter can be further subdivided into the G-protein-coupled P2Y receptors (P2YRs) and the ionotropic P2X receptors (P2XRs) [ 9 ]. (springeropen.com)
  • The P2YR subtypes are typical G protein-coupled receptors (GPCRs), which typically consist of seven transmembrane domains connected by three extracellular and three intracellular loops. (biomedcentral.com)
  • P2 receptors are activated by ATP or ADP, and can be either ionotropic, in which case they are called P2X, or G-protein-coupled, called P2Y. (alzforum.org)
  • There are currently four types of adenosine receptors found in the heart. (wikipedia.org)
  • NTPDase1 can therefore effect P2 receptor activation and functions. (wikipedia.org)
  • We conclude that TSP-1 expression can be regulated by activation of P2Y receptors, particularly P2Y 4 , coupled to protein kinase signaling pathways and suggest that purinergic signaling may be an important factor in TSP-1-mediated cell-matrix and cell-cell interactions such as those occurring during development and repair. (pnas.org)
  • In this study, we show that extracellular ATP, through the activation of P2Y 4 receptors, stimulates TSP-1 expression and release in astrocytes and that this nucleotide-induced increase is mediated by protein kinase signaling pathways. (pnas.org)
  • The mechanism of ATPγS-mediated increase in ototoxicity was investigated using neomycin Texas-red conjugate to determine putative changes in neomycin uptake following P2X receptor activation. (auckland.ac.nz)
  • Activation of P1/adenosine receptors (AR), on the other hand, partially protected the organ of Corti against neomycin-induced hair cell loss. (auckland.ac.nz)
  • The increase in LPS-induced IL-10 production and suppression of LPS-induced TNF-α and NO production caused by adenosine receptor activation may explain some of the immunomodulatory actions of adenosine released in excess during inflammatory and/or ischemic insult. (utmb.edu)
  • On the mechanism by which adenosine receptor activation inhibits the release of acetylcholine from motor nerve endings. (northwestern.edu)
  • The results are consistent with the hypothesis that activation of extracellular adenosine receptors on adenylate cyclase inhibits evoked ACh release by reducing the affinity for Ca of an intracellular component of the secretory apparatus. (northwestern.edu)
  • Fingerprint Dive into the research topics of 'On the mechanism by which adenosine receptor activation inhibits the release of acetylcholine from motor nerve endings. (northwestern.edu)
  • Background: The death of motor neurons in amyotrophic lateral sclerosis (ALS) is believed to result, in part, from unrestrained activation of glutamate receptors (excitotoxicity). (northwestern.edu)
  • Results: We show here that adenosine A 2a antagonists can reduce activation of Trk receptors and are neuroprotective. (northwestern.edu)
  • Overall, in contrast with our original hypothesis, these results indicate that immature hearts display greater sensitivity than mature hearts to the antiadrenergic effect of adenosine A1-receptor activation. (umassmed.edu)
  • Nucleotide receptors may effect their responses through primary activation of membrane chloride channels. (elsevier.com)
  • Furthermore, the P2X7R comes with an intracellular domains that lovers receptor activation to intracellular signaling occasions and it is classically associated with apoptosis [4], [5]. (eaap2017.org)
  • Activation of adenosine receptors is related to an antidepressant activity. (bvsalud.org)
  • It involves the activation of purinergic receptors in the cell and/or in nearby cells, thereby regulating cellular functions. (wikipedia.org)
  • These results strongly imply that the secreted ATP-utilizing enzymes of V. cholerae modulate the external ATP levels of the macrophage and mast cells, leading to their accelerated death, presumably through activation of P2Z receptors. (asm.org)
  • Since macrophage cell death leads to the death of the engulfed pathogen ( 17 , 25 ), activation of the purinergic receptors is an accepted part of the phagocytic process. (asm.org)
  • Adenosine receptor activation and nociception. (semanticscholar.org)
  • In addition, activation of the P2X7 receptor, present on immune cells, triggers membrane permeabilization to medium-sized molecules and thereby may permit the cellular exit of ATP ( 28 ). (physiology.org)
  • Aside from its action on the endothelium, A2aR agonists inhibit T-cell activation through increasing cAMP levels, which acts immunosuppressive ( 39 ). (physiology.org)
  • 1997). This anticonvulsant activity of CADO highly integrative role in the sense/memory-response is dose-dependent and blocked by ca eine, suggesting that pathway and is believed to occupy a pivotal position in activation of adenosine heptahelical receptors in the the regulation of fear and anxiety. (gotomydoctor.com)
  • BM-MSCs and LA-MSCs inhibited activation and aggregation of stimulated platelets independent of the agonist used. (biomedcentral.com)
  • The tumour microenvironment is characterised by the extracellular release of high levels of ATP, which is followed by the activation of P1 adenosinergic and P2 purinergic signalling systems. (springeropen.com)
  • The activation of P2Y 12 and P2Y 1 purinergic receptors expressed in the platelets promotes epithelial-mesenchymal transition (EMT). (springeropen.com)
  • Adenosine-dependent regulation of renal function in healthy and diseased kidney is mediated by activation of the four types of P1 purinergic adenosine receptors (A 1 AR, A 2A AR, A 2B AR, A 3 AR). (springer.com)
  • Al-Mashhadi RH, Skott O, Vanhoutte PM et al (2009) Activation of A(2) adenosine receptors dilates cortical efferent arterioles in mouse. (springer.com)
  • Awad AS, Huang L, Ye H et al (2006) Adenosine A2A receptor activation attenuates inflammation and injury in diabetic nephropathy. (springer.com)
  • Babich V, Vadnagara K, Di Sole F (2015) Dual effect of adenosine a1 receptor activation on renal O2 consumption. (springer.com)
  • A pyridoxine cyclic phosphate and its 6-azoaryl derivative selectively potentiate and antagonize activation of P2X1 receptors. (edu.au)
  • Extracellular adenosine critically modulates ischemic brain injury, at least in part through activation of the A 1 adenosine receptor. (jneurosci.org)
  • This rapid breakdown results in the activation of a multiplicity of receptor subtypes, which can mediate physiological processes such as proliferation, differentiation, migration, and cell death [16]. (thefreelibrary.com)
  • Pharmacological examination showed that the ATP responses are primarily mediated by P2X purinergic receptors. (frontiersin.org)
  • Ki16425 inhibited LPA-induced guanosine 5′- O -(3-thio)triphosphate binding as well as LPA receptor binding to membrane fractions with a same pharmacological specificity as in intact cells. (aspetjournals.org)
  • Pharmacological characterization of a simple behavioral response mediated selectively by central adenosine A1 receptors, using in vivo and in vitro techniques. (semanticscholar.org)
  • The great progress in understanding the contributors to these diverse aspects of purinergic signaling - ABC family members, nucleotidase, diphosphokinases, and individual receptors - offers many potential options for development of pharmacological strategies that modify gastrointestinal function through specific targeting of the rich and interconnected network of purinergic signaling cascades. (elsevier.com)
  • Overall, the pharmacological characteristics of the human receptors are similar to other species with some species-specific characteristics. (biomedsearch.com)
  • The CHO cells with stably transfected adenosine receptors provide an identical cellular background for such a pharmacological characterization. (biomedsearch.com)
  • Although preliminary, these results indicate that purinergic receptors are putative pharmacological targets that should be further explored in future studies. (biomedcentral.com)
  • To overcome these pharmacological limitations, we explored the consequences of deleting the A 2A adenosine receptor on brain damage after transient focal ischemia. (jneurosci.org)
  • Together with complimentary pharmacological studies, these data suggest that A 2A receptors play a prominent role in the development of ischemic injury within brain and demonstrate the potential for anatomical and functional neuroprotection against stroke by A 2A receptor antagonists. (jneurosci.org)
  • The role of purinergic system in schizophrenia is related to the effect of adenosine and nucleotide receptors on dopaminergic and glutamatergic neurotransmission. (bvsalud.org)
  • While early studies focused on the role of purinergic receptors in neurotransmission, it soon became obvious that extracellular ATP and its hydrolyzed derivative adenosine had important roles in immune regulation. (hindawi.com)
  • Purinergic Signalling. (wikipedia.org)
  • Purinergic signalling is involved in several processes including neurologic, endocrine, and immune system signalling. (wikipathways.org)
  • There is increasing evidence of purinergic signalling in regulating cochlear response to injury. (auckland.ac.nz)
  • On the other hand, adenosine receptor signalling is known to increase cellular antioxidant responses and this could be the main mechanism underlying protection from neomycin-induced hair cell death. (auckland.ac.nz)
  • Based on these studies, it was postulated that ATP and adenosine regulate different aspects of the cochlear response to stress and injury, and that the balance of P1 and P2 receptor signalling is important for cochlear survival under stress. (auckland.ac.nz)
  • The purinergic signalling system consists of transporters, enzymes and receptors responsible for the synthesis, release, action, and extracellular inactivation of (primarily) ATP and its extracellular breakdown product adenosine. (wikipedia.org)
  • Cell signalling events initiated by P1 and P2Y receptors have opposing effects in biological systems. (wikipedia.org)
  • The regulation of vascular tone in the endothelium of blood vessels is mediated by purinergic signalling. (wikipedia.org)
  • Furthermore, ubiquitous distribution in all tissues makes P2 receptors one of the most common and versatile signalling systems in the human body. (royalsocietypublishing.org)
  • The nucleotide-degrading system plays a critical role in purinergic signalling because, besides degrading ATP, and therefore terminating P2 receptor-targeted signalling, it also generates adenosine, an additional powerful modulator of cell functions acting at P1 receptors [ 10 ]. (royalsocietypublishing.org)
  • Furthermore, research on these signalling systems indicates an expanding field of opportunities to specifically target the purinergic receptors for the treatment of OC. (springeropen.com)
  • In this review, we have described the complex purinergic signalling mechanism involved in the development of OC and discussed the merits of targeting the components involved in the purinergic signalling pathway. (springeropen.com)
  • It has also been established that this signalling pathway, mainly the P2Y receptors, has a key function as it alters the drug pathways in the OC cells [ 13 ]. (springeropen.com)
  • In this review, we aim to summarise the correlative role of ATPs, ectonucleotidases, platelets and adenosine in the purinergic signalling pathway. (springeropen.com)
  • Further, we also intend to highlight purinergic signalling as a novel therapeutic target in treating OC. (springeropen.com)
  • General outline of purinergic signalling in ovarian cancer. (springeropen.com)
  • Presence of ATP in the extracellular milieu activates the P2X and P2Y purinergic signalling cascade. (springeropen.com)
  • 3'-Aminoadenosine-5'-uronamides: discovery of the first highly selective agonist at the human adenosine A3 receptor. (naver.com)
  • ZM241385, DPCPX, MRS1706 are inverse agonists with different relative intrinsic efficacies on constitutively active mutants of the human adenosine A2B receptor. (wikipathways.org)
  • Novel N6-substituted adenosine 5'-N-methyluronamides with high selectivity for human adenosine A3 receptors reduce ischemic myocardial injury. (wikipathways.org)
  • Abstract -Renin secretion can be stimulated by ATP via purinergic P2Y receptors. (ahajournals.org)
  • abstract = "The process by which adenosine receptor agonists inhibit the evoked release of acetylcholine (ACh) was studied at motor nerve endings to frog skeletal muscle. (northwestern.edu)
  • abstract = "Exposure of cells to adenosine receptor (AR) agonists leads to receptor uncoupling from G proteins and downregulation of the A1AR. (elsevier.com)
  • After binding onto a specific purinergic receptor, adenosine causes a negative chronotropic effect due to its influence on cardiac pacemakers. (wikipedia.org)
  • The effects of UTP and ATP were prevented by both wide-range and specific purinergic antagonists. (frontiersin.org)
  • Astrocytes express both P2Y and P2X receptors ( 13 - 18 ), and these receptors are coupled to protein kinase cascades, including mitogen-activated protein kinases (MAPKs) and protein kinase B/Akt ( 14 , 15 , 19 , 20 ), that mediate gene expression ( 21 , 22 ). (pnas.org)
  • Purinergic receptors are specific classes of membrane receptors that mediate various physiological functions such as the relaxation of gut smooth muscle, as a response to the release of ATP or adenosine. (wikipedia.org)
  • into the basolateral amygdala suppresses seizure activity P1 purinoreceptors are believed to mediate the e ects following amygdala kindling (Abdul-Ghani et al. (gotomydoctor.com)
  • Studies using local administration of cannabinoid agonists have shown that peripheral, spinal, and supraspinal cannabinoid receptors mediate cannabinoid-induced antinociception. (cognizantcommunication.com)
  • E ) summary from the RTN (N = 7 vessels) and cortex (N = 5 vessels) data show that t-ACPD caused vasoconstriction of RTN arterioles under control conditions but not in the presence of PPADS, suggesting purinergic signaling most likely from astrocytes mediate constriction of arterioles in the RTN. (elifesciences.org)
  • In: Straub RW, Bolis L (eds) Cell membrane receptors for drugs and hormones: a multidisciplinary approach. (springer.com)
  • To examine the mechanism(s) underlying A1AR downregulation and recovery, we treated ductus deferens tumor (DDT 1 MF-2) cells with the agonist R-phenylisopropyladenosine (R-PIA) and showed a decrease in membrane A 1 AR levels by 24 h, which was associated with an unexpected 11-fold increase in A 1 AR mRNA. (elsevier.com)
  • Extracellular purines, particularly adenosine-5'-tri-phosphate (ATP) and adenosine are potent regulators of many cellular and tissue processes through pathways activated by action on the P1 and P2 receptors. (auckland.ac.nz)
  • Amiloride and 5-(N,N-dimethyl)amiloride (DMA) were more potent at A(1) receptors than at A(3) receptors, while 5-(N,N-hexamethylene)amiloride (HMA) was more potent at A(3) receptors. (nih.gov)
  • these compounds were more potent than P1 agonists. (umassmed.edu)
  • For A2A adenosine receptors CGS 21680 (2-[p-(2-carboxyethyl)phenylethylamino]-5'-N-ethylcarboxamidoadeno sine) and N-ethylcarboxamidoadenosine (NECA) were found to be the most potent agonists followed by R- and S-PIA with minor stereoselectivity. (biomedsearch.com)
  • NECA was the most potent agonist with an EC50-value of 2.3 microM whereas all other compounds tested were active at concentrations in the high micromolar range. (biomedsearch.com)
  • The N6-benzyl substituted derivatives of adenosine-5'-N-methyluronamide (MECA) turned out to be the most potent agonists. (biomedsearch.com)
  • Selective P1 - and P2-receptor agonists could be used to regulate hepatic metabolism, and the use of receptor antagonists might provide an alternative strategy for limiting tissue damage caused by colonic inflammation. (elsevier.com)
  • A. Battastini and colleagues present an overview of the various roles of purinergic signaling in gliomas. (hindawi.com)
  • Roman, RM & Fitz, JG 1999, ' Emerging roles of purinergic signaling in gastrointestinal epithelial secretion and hepatobiliary function ', Gastroenterology , vol. 116, no. 4, pp. 964-979. (elsevier.com)
  • The responsiveness of embryonic cardiomyocytes (E) 12 to P2 receptor agonists by measuring Ca 2+ influx did not present response to ATP, but responses to P2 agonists were detected in cardiomyocytes taken from E14 and E18 rats. (springer.com)
  • 1987). Unlike A1 receptors, A2 adenosine receptors appear to couple to cholera toxin- Neurons were prepared from coronal brain slices of juvenile sensitive G proteins and can stimulate cyclic AMP male rats (*P17 ± P28) as previously described (McCool & accumulation. (gotomydoctor.com)
  • ASP5854 ameliorated A(2A) agonist 2-[p-(2-carboxyethyl) phenethylamino]-5'-N-ethylcarboxamidoadenosine (CGS21680)- and haloperidol-induced catalepsy in mice, with the minimum effective doses of 0.32 and 0.1 mg/kg, respectively, and it also improved haloperidol-induced catalepsy in rats at doses higher than 0.1 mg/kg. (curehunter.com)
  • The inhibitors of these receptors will be the effective therapeutic targets in managing OC. (springeropen.com)
  • This study demonstrates that nucleotide receptors in this model of renal epithelium initiate distinct regulation of Na-K-Cl cotransport. (elsevier.com)
  • Adenosine receptors, in particular adenosine receptors, present anti-inflammatory action in acute and chronic retinal inflammation. (ucm.es)
  • This involvement suggests the possible use of purinergic agonists and antagonists as therapeutic targets for ocular inflammation. (ucm.es)
  • It is now recognized that purinergic signaling not only regulates neurotransmission and inflammation, but also influences diverse biological pathways, such as cell survival, proliferation, differentiation, lipid synthesis, and cell motility. (hindawi.com)
  • Previously, we showed that superficially located microvillous cells (MCs) in the MOE expressing transient receptor potential channel M5 (TRPM5) are cholinergic and chemoresponsive and that they play an important role in maintaining odor responses and olfactory-guided behavior under challenging chemical environment. (frontiersin.org)
  • Thus, serosal afferents (putative nociceptors) were used to investigate the effect of tegaserod, and transient receptor potential channel, vanilloid 4 (TRPV 4 ) modulation on mechanical responses. (bmj.com)
  • Responses mediated by agonists specific for P2Y receptors subtypes showed that P2Y receptors (P2Y 1 , P2Y 2 , P2Y 4 and P2Y 6 ) were also present in both E14 and E18 cardiomyocytes. (springer.com)
  • Lysophosphatidic acid (LPA) exerts a variety of biological responses through specific receptors: three subtypes of the EDG-family receptors, LPA 1 , LPA 2 , and LPA 3 (formerly known as EDG-2, EDG-4, and EDG-7, respectively), and LPA 4 /GPR23, structurally distinct from the EDG-family receptors, have so far been identified. (aspetjournals.org)
  • Ki16425 inhibited several responses specific to LPA, depending on the cell types, without any appreciable effect on the responses to other related lipid receptor agonists, including sphingosine 1-phosphate. (aspetjournals.org)
  • Interestingly, recent evidence suggests that purinergic signaling influences the severity of alloimmune responses. (hindawi.com)
  • As highlighted by P. Chernogorova and R. Zeiser, these studies suggest potential clinical use of recombinant ectonucleotidases or adenosine receptor agonists for regulation of alloimmune responses which can be tailored according to the clinical situation. (hindawi.com)
  • Described are uses of A.sub.2a adenosine receptor antagonists and agonists to provide long term modulation of immune responses. (patents.com)
  • A.sub.2a receptor antagonists in particular are provided to enhance immune responses by reducing T-cell mediated tolerance to antigenic stimuli and agonists are provided to enhance effectiveness of immunosuppressive agents. (patents.com)
  • Therefore, purinergic responses in the perivascular retinal tissue during relaxation of VSMCs were studied. (arvojournals.org)
  • The sequential hydrolysis of ATP by the ectonucleotidases CD39 and CD73 generates adenosine, which creates an immune suppressive microenvironment by inhibiting the T and NK cell responses via the A2A adenosine receptor. (springeropen.com)
  • Immune cells express various P2Rs, and purinergic signaling mechanisms have been shown to play key roles in the regulation of many aspects of immune responses. (biomedcentral.com)
  • In GES-1 cells, ATP and UTP induced similar responses and the combination of P2X and P2Y receptor antagonists was able to block them. (frontiersin.org)
  • NCS-1 also regulates the activity of IP 3 receptor, an intracellular calcium ion channel (which is crucial in the regulation of calcium homeostasis ), interacts with the IP kinases , which trigger intracellular signaling cascades, and modulates the activity of presynaptic calcium channels . (bvsalud.org)
  • P2X7R receptor-promoted intracellular calcium mineral fluxes had been attained at lower Bz-ATP ligand concentrations in undifferentiated and in neural-differentiated cells in comparison to various other studies. (eaap2017.org)
  • We have utilized whole-cell voltage-clamp electrophysiology to examine the modulatory e ects of CADO and other adenosine receptor agonists on voltage-gated calcium channels in dissociated basolateral amygdala neurons. (gotomydoctor.com)
  • Functional studies revealed a strong contribution of P2Y 2 Rs in intracellular calcium increases, elicited by adenosine-triphosphate (ATP), uridine-triphosphate (UTP), and the P2Y 2 R agonist MRS2768. (frontiersin.org)
  • Forskolin treatment of cerebellar granule cells did not affect receptor density, suggesting that cyclic AMP is not involved in the regulation of A 1 adenosine receptor expression. (elsevier.com)
  • Its effects include the regulation of receptors, ion channels and enzymes , which intervene in multiple neuronal functions. (bvsalud.org)
  • Maiken Nedergaard's group demonstrated that neuronal differentiation is normally along with a proclaimed down-regulation of purinergic signaling as well as Morusin the neural progenitor cells themselves had been the foundation of regional ATP secretion [14]. (eaap2017.org)
  • Purinergic system plays a role in the regulation of many psychological processes, including mood and activity. (bvsalud.org)
  • 1991). However, direct regulation studies outlined below, infusion of the non-selective of postsynaptic processes by amygdala adenosine receptors adenosine receptor agonist 2-chloroadenosine (CADO) has not been examined. (gotomydoctor.com)
  • Over the last decade, new concepts have been gradually substantiated, such as receptor preference for the regulation of certain classes of G-proteins in cells, agonists' selection of G-protein classes for internalizing their effects, and the regulation of the functional state of G a subunits and G bg dimers shuttling between activated receptors and effectors during agonist signal propagation. (cognizantcommunication.com)
  • NTPDase1 hydrolyzes P2 receptor ligands, namely ATP, ADP, UTP and UDP with similar efficacy. (wikipedia.org)
  • The present study was designed to determine whether P1 adenosine receptor ligands affected disease progression in a transgenic model of ALS. (elsevier.com)
  • These cells are valuable systems for further characterization of specific receptor subtypes and for the development of new ligands. (biomedsearch.com)
  • Some of these compounds are still derived from adenosine or from the xanthine family, but researchers in this area have also discovered many selective adenosine receptor ligands that are entirely structurally distinct, giving a wide range of possible directions for future research. (wikipedia.org)
  • RT-PCR showed the presence of P2X2 and P2X4 receptor transcripts on E14 cardiomyocytes with a lower expression of P2X3 and P2X7 receptors. (springer.com)
  • Our results show that specific P2 receptor subtypes are present in embryonic rat cardiomyocytes, including P2X7 and P2Y 4 receptors that have not been identified in adult rat cardiomyocytes. (springer.com)
  • Conclusions In embryonic cells, P2X7R activity and appearance is normally upregulated, preserving proliferation, while upon induction to neural differentiation P2X7 receptor activity and appearance must be suppressed. (eaap2017.org)
  • Furthermore, we showed that A1, A2A, P2Y1, P2Y11, and P2X7 purine receptor agonists modulated the TGF-β1-induced EMT through the involvement of PKA and/or MAPK/ERK signaling. (unich.it)
  • Differently, P2X7 receptor induced, per se, similar and not additive effects compared to TGF-β1, after prolonged cell exposure to BzATP. (unich.it)
  • Several of these compounds have shown significant beneficial effects in animal models of epilepsy and pain with an improved preclinical therapeutic window over direct acting ADO receptor agonists. (elsevier.com)
  • The purinergic system has been indicated as a possible new therapeutic target for ALS, but the results are often contradictory and generally confused. (elsevier.com)
  • Our data confirm that the modulation of adenosine receptors can elicit very different (and even opposite) effects during the progression of ALS course, thus strengthens the importance of further studies to elucidated their real therapeutic potential in this pathology. (elsevier.com)
  • Update on novel purinergic P2X3 and P2X2/3 receptor antagonists and their potential therapeutic applications. (wikipathways.org)
  • A(1) adenosine receptor agonists: medicinal chemistry and therapeutic potential. (wikipathways.org)
  • The potential therapeutic opportunities provided by molecular identification of these 18 receptors are just beginning to be defined. (elsevier.com)
  • Cannabinoid agonists, which act at the cannabinoid 1 (CB 1 ) receptor and cannabinoid 2 (CB 2 ) receptor, have a number of physiological effects and considerable therapeutic potential, in particular as analgesics. (cognizantcommunication.com)
  • In obese and diabetic states, macrophage expression of purinergic receptors MMP9 and IL-10 is reduced. (diabetesjournals.org)
  • Previously, we found that the expression of purinergic P2Y 2 receptor (P2Y 2 R) is increased in GC samples as compared to adjacent healthy mucosa taken from GC-diagnosed patients. (frontiersin.org)
  • This study explored the role of endogenously formed adenosine in modulating NF-κB activity and cytokine/chemokine release from murine Treg and effector T cells (Teff) including key enzymes/purinergic receptors of extracellular ATP catabolism. (physiology.org)
  • The Impact of Purinergic System Enzymes on Noncommunicable, Neurological, and Degenerative Diseases. (thefreelibrary.com)
  • Astrocytes near plaques overexpress the P2Y1 purinergic receptor, which appears to be involved in astrocyte hyperactivation. (alzforum.org)
  • Reactive astrocytes (red) strongly express P2Y1 receptors (green, overlap in yellow) around Aβ plaques (blue). (alzforum.org)
  • Here, we show in rat that purinergic signaling, possibly through P2Y 2/4 receptors, in the retrotrapezoid nucleus (RTN) maintains arteriole tone during high CO 2 /H + and disruption of this mechanism decreases the CO 2 ventilatory response. (elifesciences.org)
  • Three recent reports have examined the relationship between the level of extracellular ATP, the mechanisms underlying purinergic receptors participating in the infection mechanism of HIV-1 in the cell. (biomedcentral.com)
  • CO 2 /H + -induced vasoconstriction of RTN arterioles is mediated by a purinergic dependent mechanism involving P2Y 2/4 receptors. (elifesciences.org)
  • In confirmation of this mechanism of action, recent studies in both animals and patients suggest that adenosine-receptor antagonists, among which is caffeine, reverse or prevent the anti-inflammatory effects of methotrexate. (biomedcentral.com)
  • Regarding the A3 receptor, selective agonists like N6-(3-iodobenzyl)-5′-N-methylcarboxamidoadenosine (CF101) have been used for the treatment of inflammatory ophthalmic diseases such as dry eye and uveoretinitis. (ucm.es)
  • Adenosine receptors: development of selective agonists and antagonists. (wikipathways.org)
  • Mutation of Thr277 to Ala not only decreased agonist affinity but also inhibited the effects of PD81,723. (nih.gov)
  • While a Cys(302,305)Ala-mutated rat A(3)AR mutant internalizes significantly faster than the wild-type (WT) receptor in response to agonist exposure, analogous mutation of the human A(1)AR (Cys(309)Ala) had no effect on receptor internalization. (edgehill.ac.uk)
  • Köles L, Fürst S, Illes P (2007) Purine ionotropic (P2X) receptors. (springer.com)
  • These results suggest a putative role of purine receptors as target for anti-fibrotic agents. (unich.it)