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.
Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.
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.
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 P2Y RECEPTORS. Included under this heading are agonists for specific P2Y receptor subtypes.
A subclass of purinergic P2 receptors whose signaling is coupled through a G-PROTEIN signaling mechanism.
Compounds that bind to and stimulate PURINERGIC P2 RECEPTORS.
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.
A ligand that binds to but fails to activate the INTERLEUKIN 1 RECEPTOR. It plays an inhibitory role in the regulation of INFLAMMATION and FEVER. Several isoforms of the protein exist due to multiple ALTERNATIVE SPLICING of its mRNA.
A 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.
Uridine 5'-(tetrahydrogen triphosphate). A uracil nucleotide containing three phosphate groups esterified to the sugar moiety.
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).
Compounds that inhibit or block the activity of NEUROKININ-1 RECEPTORS.
Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.
A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.
Compounds that bind to and block the stimulation of PURINERGIC P2Y RECEPTORS. Included under this heading are antagonists for specific P2Y receptor subtypes.
The relationship between the dose of an administered drug and the response of the organism to the drug.
Drugs that selectively bind to but do not activate histamine H2 receptors, thereby blocking the actions of histamine. Their clinically most important action is the inhibition of acid secretion in the treatment of gastrointestinal ulcers. Smooth muscle may also be affected. Some drugs in this class have strong effects in the central nervous system, but these actions are not well understood.
Drugs that bind to but do not activate SEROTONIN 5-HT3 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT3 RECEPTOR AGONISTS.
A family of hexahydropyridines.
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.
A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.
A class of cell surface receptors that prefer ADENOSINE to other endogenous PURINES. Purinergic P1 receptors are widespread in the body including the cardiovascular, respiratory, immune, and nervous systems. There are at least two pharmacologically distinguishable types (A1 and A2, or Ri and Ra).
Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.
Agents that antagonize ANGIOTENSIN RECEPTORS. Many drugs in this class specifically target the ANGIOTENSIN TYPE 1 RECEPTOR.
Drugs that bind to but do not activate 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.
Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.
Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.
Drugs that bind to but do not activate SEROTONIN 5-HT2 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT2 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more specific 5-HT2 receptor subtypes.
Chemical substances which inhibit the function of the endocrine glands, the biosynthesis of their secreted hormones, or the action of hormones upon their specific sites.
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.
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.
Compounds that bind to and stimulate PURINERGIC P1 RECEPTORS.
Agents inhibiting the effect of narcotics on the central nervous system.
Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.
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.
Cell surface proteins that bind ENDOTHELINS with high affinity and trigger intracellular changes which influence the behavior of cells.
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 but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.
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.
Adenosine 5'-(trihydrogen diphosphate). An adenine nucleotide containing two phosphate groups esterified to the sugar moiety at the 5'-position.
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 but do not activate GABA-A RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-A RECEPTOR AGONISTS.
Drugs that bind to but do not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists. Classical antihistaminics block the histamine H1 receptors only.
Drugs that bind to but do not activate GABA RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.
Glycoproteins which contain sialic acid as one of their carbohydrates. They are often found on or in the cell or tissue membranes and participate in a variety of biological activities.
A class of drugs designed to prevent leukotriene synthesis or activity by blocking binding at the receptor level.
A subtype of endothelin receptor found predominantly in the VASCULAR SMOOTH MUSCLE. It has a high affinity for ENDOTHELIN-1 and ENDOTHELIN-2.
Compounds that act on PURINERGIC RECEPTORS or influence the synthesis, storage, uptake, metabolism, or release of purinergic transmitters.
Cell-surface proteins that bind SEROTONIN and trigger intracellular changes which influence the behavior of cells. Several types of serotonin receptors have been recognized which differ in their pharmacology, molecular biology, and mode of action.
A class of ionotropic glutamate receptors characterized by affinity for N-methyl-D-aspartate. NMDA receptors have an allosteric binding site for glycine which must be occupied for the channel to open efficiently and a site within the channel itself to which magnesium ions bind in a voltage-dependent manner. The positive voltage dependence of channel conductance and the high permeability of the conducting channel to calcium ions (as well as to monovalent cations) are important in excitotoxicity and neuronal plasticity.
Drugs that bind to but do not activate SEROTONIN 5-HT1 RECEPTORS, thereby blocking the actions of SEROTONIN 5-HT1 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more of the specific 5-HT1 receptor subtypes.
Use of electric potential or currents to elicit biological responses.
A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.
A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.
Purine bases found in body tissues and fluids and in some plants.
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.
Drugs that bind to nicotinic cholinergic receptors (RECEPTORS, NICOTINIC) and block the actions of acetylcholine or cholinergic agonists. Nicotinic antagonists block synaptic transmission at autonomic ganglia, the skeletal neuromuscular junction, and at central nervous system nicotinic synapses.
Cell surface receptors that are specific for INTERLEUKIN-1. Included under this heading are signaling receptors, non-signaling receptors and accessory proteins required for receptor signaling. Signaling from interleukin-1 receptors occurs via interaction with SIGNAL TRANSDUCING ADAPTOR PROTEINS such as MYELOID DIFFERENTIATION FACTOR 88.
Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.
Compounds with BENZENE fused to AZEPINES.
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.
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.
Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.
The action of a drug that may affect the activity, metabolism, or toxicity of another drug.
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.
Established cell cultures that have the potential to propagate indefinitely.
Endogenous compounds and drugs that bind to and activate SEROTONIN RECEPTORS. Many serotonin receptor agonists are used as ANTIDEPRESSANTS; ANXIOLYTICS; and in the treatment of MIGRAINE DISORDERS.
Drugs that selectively bind to but do not activate HISTAMINE H3 RECEPTORS. They have been used to correct SLEEP WAKE DISORDERS and MEMORY DISORDERS.
Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS.
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.
Peptides whose amino and carboxy ends are linked together with a peptide bond forming a circular chain. Some of them are ANTI-INFECTIVE AGENTS. Some of them are biosynthesized non-ribosomally (PEPTIDE BIOSYNTHESIS, NON-RIBOSOMAL).
An eleven-amino acid neurotransmitter that appears in both the central and peripheral nervous systems. It is involved in transmission of PAIN, causes rapid contractions of the gastrointestinal smooth muscle, and modulates inflammatory and immune responses.
Drugs that bind to but do not activate 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.
Azoles of two nitrogens at the 1,2 positions, next to each other, in contrast with IMIDAZOLES in which they are at the 1,3 positions.
Drugs that bind to but do not activate ADRENERGIC RECEPTORS. Adrenergic antagonists block the actions of the endogenous adrenergic transmitters EPINEPHRINE and NOREPINEPHRINE.
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.
A group of compounds that contain the structure SO2NH2.
Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).
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 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.
An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.
A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.
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)
Drugs that bind to but do not activate GABA-B RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-B RECEPTOR AGONISTS.
Cell surface receptors that bind BRADYKININ and related KININS with high affinity and trigger intracellular changes which influence the behavior of cells. The identified receptor types (B-1 and B-2, or BK-1 and BK-2) recognize endogenous KALLIDIN; t-kinins; and certain bradykinin fragments as well as bradykinin itself.
A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.
A subtype of endothelin receptor found predominantly in the KIDNEY. It may play a role in reducing systemic ENDOTHELIN levels.
A 21-amino acid peptide produced in a variety of tissues including endothelial and vascular smooth-muscle cells, neurons and astrocytes in the central nervous system, and endometrial cells. It acts as a modulator of vasomotor tone, cell proliferation, and hormone production. (N Eng J Med 1995;333(6):356-63)
Compounds that selectively bind to and block the activation of ADENOSINE A3 RECEPTORS.
A class of cell surface receptors for TACHYKININS with a preference for SUBSTANCE P. Neurokinin-1 (NK-1) receptors have been cloned and are members of the G protein coupled receptor superfamily. They are found on many cell types including central and peripheral neurons, smooth muscle cells, acinar cells, endothelial cells, fibroblasts, and immune cells.
Seven membered heterocyclic rings containing a NITROGEN atom.
A nonapeptide messenger that is enzymatically produced from KALLIDIN in the blood where it is a potent but short-lived agent of arteriolar dilation and increased capillary permeability. Bradykinin is also released from MAST CELLS during asthma attacks, from gut walls as a gastrointestinal vasodilator, from damaged tissues as a pain signal, and may be a neurotransmitter.
A derivative of benzodiazepine that acts on the cholecystokinin A (CCKA) receptor to antagonize CCK-8's (SINCALIDE) physiological and behavioral effects, such as pancreatic stimulation and inhibition of feeding.
Cell surface proteins that bind cholecystokinin (CCK) with high affinity and trigger intracellular changes influencing the behavior of cells. Cholecystokinin receptors are activated by GASTRIN as well as by CCK-4; CCK-8; and CCK-33. Activation of these receptors evokes secretion of AMYLASE by pancreatic acinar cells, acid and PEPSIN by stomach mucosal cells, and contraction of the PYLORUS and GALLBLADDER. The role of the widespread CCK receptors in the central nervous system is not well understood.
Elements of limited time intervals, contributing to particular results or situations.
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.
Specific molecular sites or proteins on or in cells to which VASOPRESSINS bind or interact in order to modify the function of the cells. Two types of vasopressin receptor exist, the V1 receptor in the vascular smooth muscle and the V2 receptor in the kidneys. The V1 receptor can be subdivided into V1a and V1b (formerly V3) receptors.
Drugs that bind to but do not activate SEROTONIN 5-HT4 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN RECEPTOR AGONISTS.
The D-enantiomer is a potent and specific antagonist of NMDA glutamate receptors (RECEPTORS, N-METHYL-D-ASPARTATE). The L form is inactive at NMDA receptors but may affect the AP4 (2-amino-4-phosphonobutyrate; APB) excitatory amino acid receptors.
A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients.
The observable response an animal makes to any situation.
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 cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.
Cell surface proteins that bind THROMBOXANES with high affinity and trigger intracellular changes influencing the behavior of cells. Some thromboxane receptors act via the inositol phosphate and diacylglycerol second messenger systems.
Compounds with a BENZENE fused to IMIDAZOLES.
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.
An amine derived by enzymatic decarboxylation of HISTIDINE. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and also a centrally acting neurotransmitter.
A competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.
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 class of cell surface receptors for tachykinins that prefers neurokinin A; (NKA, substance K, neurokinin alpha, neuromedin L), neuropeptide K; (NPK); or neuropeptide gamma over other tachykinins. Neurokinin-2 (NK-2) receptors have been cloned and are similar to other G-protein coupled receptors.
Compounds that inhibit or block the activity of CANNABINOID RECEPTORS.
An alkylamide found in CAPSICUM that acts at TRPV CATION CHANNELS.
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.
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.
A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.
Injections into the cerebral ventricles.
The physiological narrowing of BLOOD VESSELS by contraction of the VASCULAR SMOOTH MUSCLE.
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.
Drugs that bind to and block the activation of ADRENERGIC BETA-2 RECEPTORS.
A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.
A musculomembranous sac along the URINARY TRACT. URINE flows from the KIDNEYS into the bladder via the ureters (URETER), and is held there until URINATION.
The excretory duct of the testes that carries SPERMATOZOA. It rises from the SCROTUM and joins the SEMINAL VESICLES to form the ejaculatory duct.
An isoquinoline alkaloid obtained from Dicentra cucullaria and other plants. It is a competitive antagonist for GABA-A receptors.
Drugs that bind to and block the activation of MINERALOCORTICOID RECEPTORS by MINERALOCORTICOIDS such as ALDOSTERONE.
PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS.
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)
An octapeptide that is a potent but labile vasoconstrictor. It is produced from angiotensin I after the removal of two amino acids at the C-terminal by ANGIOTENSIN CONVERTING ENZYME. The amino acid in position 5 varies in different species. To block VASOCONSTRICTION and HYPERTENSION effect of angiotensin II, patients are often treated with ACE INHIBITORS or with ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKERS.
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.
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.
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
A histamine H1 antagonist. It has mild hypnotic properties and some local anesthetic action and is used for allergies (including skin eruptions) both parenterally and locally. It is a common ingredient of cold remedies.
A constitutively expressed subtype of bradykinin receptor that may play a role in the acute phase of the inflammatory and pain response. It has high specificity for intact forms of BRADYKININ and KALLIDIN. The receptor is coupled to G-PROTEIN, GQ-G11 ALPHA FAMILY and G-PROTEIN, GI-GO ALPHA FAMILY signaling proteins.
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).
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 class of drugs that act by selective inhibition of calcium influx through cellular membranes.
21-Amino-acid peptides produced by vascular endothelial cells and functioning as potent vasoconstrictors. The endothelin family consists of three members, ENDOTHELIN-1; ENDOTHELIN-2; and ENDOTHELIN-3. All three peptides contain 21 amino acids, but vary in amino acid composition. The three peptides produce vasoconstrictor and pressor responses in various parts of the body. However, the quantitative profiles of the pharmacological activities are considerably different among the three isopeptides.
Cell surface proteins that bind neuropeptide Y with high affinity and trigger intracellular changes which influence the behavior of cells.
A methyl xanthine derivative from tea with diuretic, smooth muscle relaxant, bronchial dilation, cardiac and central nervous system stimulant activities. Theophylline inhibits the 3',5'-CYCLIC NUCLEOTIDE PHOSPHODIESTERASE that degrades CYCLIC AMP thus potentiates the actions of agents that act through ADENYLYL CYCLASES and cyclic AMP.
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.
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.
The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.
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.
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.
Benzopyrroles with the nitrogen at the number two carbon, in contrast to INDOLES which have the nitrogen adjacent to the six-membered ring.
Cell surface proteins that bind CALCITONIN GENE-RELATED PEPTIDE with high affinity and trigger intracellular changes which influence the behavior of cells. CGRP receptors are present in both the CENTRAL NERVOUS SYSTEM and the periphery. They are formed via the heterodimerization of the CALCITONIN RECEPTOR-LIKE PROTEIN and RECEPTOR ACTIVITY-MODIFYING PROTEIN 1.
A 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.
Cell surface proteins that bind corticotropin-releasing hormone with high affinity and trigger intracellular changes which influence the behavior of cells. The corticotropin releasing-hormone receptors on anterior pituitary cells mediate the stimulation of corticotropin release by hypothalamic corticotropin releasing factor. The physiological consequence of activating corticotropin-releasing hormone receptors on central neurons is not well understood.
An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).
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.
Peptides composed of between two and twelve amino acids.
An alkaloid, originally from Atropa belladonna, but found in other plants, mainly SOLANACEAE. Hyoscyamine is the 3(S)-endo isomer of atropine.
An adenine nucleotide containing one phosphate group which is esterified to both the 3'- and 5'-positions of the sugar moiety. It is a second messenger and a key intracellular regulator, functioning as a mediator of activity for a number of hormones, including epinephrine, glucagon, and ACTH.
A soluble factor produced by MONOCYTES; MACROPHAGES, and other cells which activates T-lymphocytes and potentiates their response to mitogens or antigens. Interleukin-1 is a general term refers to either of the two distinct proteins, INTERLEUKIN-1ALPHA and INTERLEUKIN-1BETA. The biological effects of IL-1 include the ability to replace macrophage requirements for T-cell activation.
Cell surface proteins that bind TACHYKININS with high affinity and trigger intracellular changes influencing the behavior of cells. Three classes of tachykinin receptors have been characterized, the NK-1; NK-2; and NK-3; which prefer, respectively, SUBSTANCE P; NEUROKININ A; and NEUROKININ B.
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.
An angiotensin receptor subtype that is expressed at high levels in a variety of adult tissues including the CARDIOVASCULAR SYSTEM, the KIDNEY, the ENDOCRINE SYSTEM and the NERVOUS SYSTEM. Activation of the type 1 angiotensin receptor causes VASOCONSTRICTION and sodium retention.
Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS.
Cell surface proteins that bind ANGIOTENSINS and trigger intracellular changes influencing the behavior of cells.
A competitive serotonin type 3 receptor antagonist. It is effective in the treatment of nausea and vomiting caused by cytotoxic chemotherapy drugs, including cisplatin, and has reported anxiolytic and neuroleptic properties.
Nucleotides in which the base moiety is substituted with one or more sulfur atoms.
The domestic dog, Canis familiaris, comprising about 400 breeds, of the carnivore family CANIDAE. They are worldwide in distribution and live in association with people. (Walker's Mammals of the World, 5th ed, p1065)
The species Oryctolagus cuniculus, in the family Leporidae, order LAGOMORPHA. Rabbits are born in burrows, furless, and with eyes and ears closed. In contrast with HARES, rabbits have 22 chromosome pairs.
A drug that exerts an inhibitory effect on gastric secretion and reduces gastrointestinal motility. It is used clinically in the drug therapy of gastrointestinal ulcers.
A curved elevation of GRAY MATTER extending the entire length of the floor of the TEMPORAL HORN of the LATERAL VENTRICLE (see also TEMPORAL LOBE). The hippocampus proper, subiculum, and DENTATE GYRUS constitute the hippocampal formation. Sometimes authors include the ENTORHINAL CORTEX in the hippocampal formation.
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.
One of the catecholamine NEUROTRANSMITTERS in the brain. It is derived from TYROSINE and is the precursor to NOREPINEPHRINE and EPINEPHRINE. Dopamine is a major transmitter in the extrapyramidal system of the brain, and important in regulating movement. A family of receptors (RECEPTORS, DOPAMINE) mediate its action.
A 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.
AMANTADINE derivative that has some dopaminergic effects. It has been proposed as an antiparkinson agent.
A serotonin receptor (5HT-3 selective) antagonist that has been used as an antiemetic for cancer chemotherapy patients.
Drugs that bind to and activate dopamine receptors.
1,4-Diethylene dioxides. Industrial solvents. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), dioxane itself may "reasonably be anticipated to be a carcinogen." (Merck Index, 11th ed)
Cell surface receptors that bind signalling molecules released by neurons and convert these signals into intracellular changes influencing the behavior of cells. Neurotransmitter is used here in its most general sense, including not only messengers that act to regulate ion channels, but also those which act on second messenger systems and those which may act at a distance from their release sites. Included are receptors for neuromodulators, neuroregulators, neuromediators, and neurohumors, whether or not located at synapses.
Cell-surface receptors that bind LEUKOTRIENES with high affinity and trigger intracellular changes influencing the behavior of cells. The leukotriene receptor subtypes have been tentatively named according to their affinities for the endogenous leukotrienes LTB4; LTC4; LTD4; and LTE4.
Calcitonin gene-related peptide. A 37-amino acid peptide derived from the calcitonin gene. It occurs as a result of alternative processing of mRNA from the calcitonin gene. The neuropeptide is widely distributed in neural tissue of the brain, gut, perivascular nerves, and other tissue. The peptide produces multiple biological effects and has both circulatory and neurotransmitter modes of action. In particular, it is a potent endogenous vasodilator.
A statistical technique that isolates and assesses the contributions of categorical independent variables to variation in the mean of a continuous dependent variable.
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.

On the mechanism of histaminergic inhibition of glutamate release in the rat dentate gyrus. (1/619)

1. Histaminergic depression of excitatory synaptic transmission in the rat dentate gyrus was investigated using extracellular and whole-cell patch-clamp recording techniques in vitro. 2. Application of histamine (10 microM, 5 min) depressed synaptic transmission in the dentate gyrus for 1 h. This depression was blocked by the selective antagonist of histamine H3 receptors, thioperamide (10 microM). 3. The magnitude of the depression caused by histamine was inversely related to the extracellular Ca2+ concentration. Application of the N-type calcium channel blocker omega-conotoxin (0. 5 or 1 microM) or the P/Q-type calcium channel blocker omega-agatoxin (800 nM) did not prevent depression of synaptic transmission by histamine. 4. The potassium channel blocker 4-aminopyridine (4-AP, 100 microM) enhanced synaptic transmission and reduced the depressant effect of histamine (10 microM). 4-AP reduced the effect of histamine more in 2 mM extracellular calcium than in 4 mM extracellular calcium. 5. Histamine (10 microM) did not affect the amplitude of miniature excitatory postsynaptic currents (mEPSCs) and had only a small effect on their frequency. 6. Histaminergic depression was not blocked by an inhibitor of serine/threonine protein kinases, H7 (100 microM), or by an inhibitor of tyrosine kinases, Lavendustin A (10 microM). 7. Application of adenosine (20 microM) or the adenosine A1 agonist N6-cyclopentyladenosine (CPA, 0.3 microM) completely occluded the effect of histamine (10 microM). 8. We conclude that histamine, acting on histamine H3 receptors, inhibits glutamate release by inhibiting presynaptic calcium entry, via a direct G-protein-mediated inhibition of multiple calcium channels. Histamine H3 receptors and adenosine A1 receptors act upon a common final effector to cause presynaptic inhibition.  (+info)

Inhibition by adenosine receptor agonists of synaptic transmission in rat periaqueductal grey neurons. (2/619)

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)

Brain blood flow and blood pressure during hypoxia in the epaulette shark Hemiscyllium ocellatum, a hypoxia-tolerant elasmobranch. (3/619)

The key to surviving hypoxia is to protect the brain from energy depletion. The epaulette shark (Hemiscyllium ocellatum) is an elasmobranch able to resist energy depletion and to survive hypoxia. Using epi-illumination microscopy in vivo to observe cerebral blood flow velocity on the brain surface, we show that cerebral blood flow in the epaulette shark is unaffected by 2 h of severe hypoxia (0.35 mg O2 l-1 in the respiratory water, 24 C). Thus, the epaulette shark differs from other hypoxia- and anoxia-tolerant species studied: there is no adenosine-mediated increase in cerebral blood flow such as that occurring in freshwater turtles and cyprinid fish. However, blood pressure showed a 50 % decrease in the epaulette shark during hypoxia, indicating that a compensatory cerebral vasodilatation occurs to maintain cerebral blood flow. We observed an increase in cerebral blood flow velocity when superfusing the normoxic brain with adenosine (making sharks the oldest vertebrate group in which this mechanism has been found). The adenosine-induced increase in cerebral blood flow velocity was reduced by the adenosine receptor antagonist aminophylline. Aminophylline had no effect upon the maintenance of cerebral blood flow during hypoxia, however, indicating that adenosine is not involved in maintaining cerebral blood flow in the epaulette shark during hypoxic hypotension.  (+info)

Role of renal medullary adenosine in the control of blood flow and sodium excretion. (4/619)

This study determined the levels of adenosine in the renal medullary interstitium using microdialysis and fluorescence HPLC techniques and examined the role of endogenous adenosine in the control of medullary blood flow and sodium excretion by infusing the specific adenosine receptor antagonists or agonists into the renal medulla of anesthetized Sprague-Dawley rats. Renal cortical and medullary blood flows were measured using laser-Doppler flowmetry. Analysis of microdialyzed samples showed that the adenosine concentration in the renal medullary interstitial dialysate averaged 212 +/- 5.2 nM, which was significantly higher than 55.6 +/- 5.3 nM in the renal cortex (n = 9). Renal medullary interstitial infusion of a selective A1 antagonist, 8-cyclopentyl-1,3-dipropylxanthine (DPCPX; 300 pmol. kg-1. min-1, n = 8), did not alter renal blood flows, but increased urine flow by 37% and sodium excretion by 42%. In contrast, renal medullary infusion of the selective A2 receptor blocker 3, 7-dimethyl-1-propargylxanthine (DMPX; 150 pmol. kg-1. min-1, n = 9) decreased outer medullary blood flow (OMBF) by 28%, inner medullary blood flows (IMBF) by 21%, and sodium excretion by 35%. Renal medullary interstitial infusion of adenosine produced a dose-dependent increase in OMBF, IMBF, urine flow, and sodium excretion at doses from 3 to 300 pmol. kg-1. min-1 (n = 7). These effects of adenosine were markedly attenuated by the pretreatment of DMPX, but unaltered by DPCPX. Infusion of a selective A3 receptor agonist, N6-benzyl-5'-(N-ethylcarbonxamido)adenosine (300 pmol. kg-1. min-1, n = 6) into the renal medulla had no effect on medullary blood flows or renal function. Glomerular filtration rate and arterial pressure were not changed by medullary infusion of any drugs. Our results indicate that endogenous medullary adenosine at physiological concentrations serves to dilate medullary vessels via A2 receptors, resulting in a natriuretic response that overrides the tubular A1 receptor-mediated antinatriuretic effects.  (+info)

Endogenous interstitial adenosine in isolated myenteric neural networks varies inversely with prevailing PO2. (5/619)

Isolated myenteric ganglion networks were used in a perifusion protocol to characterize the response of interstitial adenosine levels to changes in prevailing PO2. The biological activity of such adenosine was assessed using inhibition of release of substance P (SP) as a functional measure of adenosine activity, and the effect of altered O2 tension on both spontaneous and elevated extracellular K+ concentration-evoked SP release from networks was determined over a range of PO2 values from hypoxic (PO2 = 54 mmHg) to hyperoxic (PO2 = 566 mmHg). Release of SP was found to be sensitive to PO2, and a linear graded relationship was obtained. Perifusion in the additional presence of the adenosine A1-receptor-selective antagonist 1,3-dipropyl-8-cyclopentylxanthine (DPCPX) revealed considerable adenosinergic inhibition with an inverse exponential relationship and hyperoxic threshold PO2. Disinhibition of evoked SP release by DPCPX in the absence of TTX was double that observed in its presence, indicating a neural source for some of the adenosine released during hypoxia. A postulated neuroprotective role for adenosine is consistent with the demonstrated relationship between interstitial adenosine and prevailing O2 tension.  (+info)

Natriuretic and diuretic actions of a highly selective adenosine A1 receptor antagonist. (6/619)

The natriuretic and diuretic action of a highly selective adenosine A1 receptor (A1AdoR) antagonist, 1,3-dipropyl-8-[2-(5,6-epoxy)norbornyl]xanthine (CVT-124), was investigated in anesthetized rats. CVT-124 (0.1 to 1 mg/kg) caused dose-dependent increases in urine flow and fractional and absolute sodium excretion of by six- to 10-fold and, at 0.1 mg/kg, increased the GFR (1.6+/-0.1 to 2.5+/-0.2 ml/min; P<0.01). There were no changes in BP or heart rate. CVT-124 reduced absolute proximal reabsorption (26+/-3 to 20+/-2 nl/min; P<0.05) despite unchanged proximally measured, single-nephron GFR (SNGFR) (42+/-5 to 44+/-4 nl/min; NS) and thereby decreased fractional proximal reabsorption (60+/-3 to 46+/-4%; P<0.05). Despite increasing distal tubular fluid flow rate (5.4+/-0.7 to 9.7+/-0.9 nl/min; P<0.001), it reduced the proximal-distal difference in SNGFR (before: 9.4+/-1.0 versus during CVT-124: 4.6+/-1.5 nl/min; P<0.01), suggesting that it had blunted the effects of the macula densa on SNGFR. Direct measurements of maximal tubuloglomerular feedback (TGF) responses were made from proximal stop flow pressure (PSF) during orthograde loop perfusion from the proximal tubule with artificial tubular fluid at 40 nl/min. TGF was blunted by intravenous CVT-124 (0.5 mg/kg; deltaPSF with vehicle: 8.3+/-0.6 versus CVT-124: 6.5+/-0.3 mm Hg; n = 9; P<0.01). In conclusion, A1AdoR blockade reduces proximal reabsorption and uncouples it from glomerular filtration. It increases distal delivery of fluid yet does not activate a macula densa-dependent fall in SNGFR because it blunts the TGF response. Natriuresis accompanied by blockade of proximal glomerulotubular balance and TGF characterizes a new class of diuretic drugs.  (+info)

Retinal ischemic preconditioning in the rat: requirement for adenosine and repetitive induction. (7/619)

PURPOSE: A brief period of ischemia can induce a remarkably complete state of ischemic tolerance in the retina, a phenomenon known as ischemic preconditioning (IPC). The mechanisms of IPC were studied in the rat retina by examining the role of adenosine as a possible mediator and determining whether IPC protection could be induced more than once in the same rat. METHODS: Retinal ischemia was produced for 60 minutes in ketamine-xylazine-anesthetized Sprague-Dawley rats, and recovery was measured using electroretinography. Twenty-four hours earlier, the IPC stimulus of 5 minutes of ischemia was applied. To test the role of adenosine as a mediator of IPC, the selective adenosine A1 receptor antagonist 8-cyclopentyl-1,3-dipropylxanthine (DPCPX; 0.45 mg/kg, 2.25 mg/kg, or 4.5 mg/kg), the A2a antagonist 8-(3-chlorostyryl)caffeine (CSC; 0.1 mg/kg or 1.0 mg/kg), or their cyclodextrin vehicle were administered 15 minutes before IPC. To examine whether exogenous adenosine administration could mimic IPC, animals received intravitreal injections of the adenosine A1 receptor stimulant adenosine amine congener (ADAC) or the A2a stimulant CGS21680, followed by ischemia 24 hours later. To test the hypothesis that IPC could be induced repeatedly without loss of protection, rats were divided to receive IPC or sham IPC, followed 10 days later by IPC or a sham procedure, and 24 hours later by 60 minutes of ischemia. RESULTS: Adenosine A1 receptor blockade with 4.5 mg/kg DPCPX administered intraperitoneally (IP) before or immediately after 5 minutes of ischemia completely blocked IPC protection, whereas lower doses resulted in partial blockade. CSC at the lowest dose (0.1 mg/kg) had no significant effect on IPC's protective effect, whereas partial blockade was found with 1.0 mg/kg CSC. A1 or A2a receptor stimulation produced partial but significant mimicking of IPC protection, effects that were antagonized by DPCPX or CSC. Ischemic preconditioning applied twice, separated by 10 days, and followed by 60 minutes of ischemia 24 hours after the second IPC stimulus, resulted in nearly identical recovery of function after ischemia compared with IPC performed one time. CONCLUSIONS: Adenosine, acting through the A1 and A2a receptors, is a critical component in the induction of ischemic tolerance after preconditioning in the retina. The neuroprotective effects of IPC in the retina are lost over time but may be reinduced by subsequent application of the IPC stimulus.  (+info)

P2 purinoceptors contribute to ATP-induced inhibition of L-type Ca2+ current in rabbit atrial myocytes. (8/619)

OBJECTIVE: Adenine compounds, including adenosine-5'-triphosphate (ATP) and adenosine (Ado), exert inhibitory effects on myocardium via P1 (subtype A1) purinoceptors. However, ATP per se is a potent activator of P2 purinoceptors. Our aim was to elucidate the respective roles of P1 and P2 purinoceptors in the actions of ATP on L-type calcium current (ICa) in rabbit atrial cells. METHODS AND RESULTS: A whole cell clamp technique was used to record ICa in single atrial cells from the rabbit heart. ATP (0.1 mumol/1-3 mmol/l) produced an inhibitory effect on ICa prestimulated by isoproterenol (ISO, 30 nmol/l), even in the presence of Ado (1 mmol/l). Both 1,3-dipropyl-8-cyclopentylxanthine (A1 blocker) and suramin (P2 blocker) partially blocked the ATP-induced inhibition of ICa, while their co-application nearly completely abolished the effect of ATP. ATP-gamma S (30 mumol/l) inhibited ISO-stimulated ICa significantly, and this inhibition was completely blocked by suramin. alpha, beta-Methylene-ADP, an inhibitor of hydrolysis of AMP to Ado, eliminated the suramin-resistant component of ICa inhibition by ATP. Pretreatment with pertussis toxin (PTX) abolished the ATP inhibition of ICa. Both intracellular dialysis with 8Br cAMP and the application of forskolin plus 3-isobutyl-1-methylxanthine also eliminated the effect of ATP. CONCLUSIONS: Both P1 and P2 purinoceptors are involved in the ATP inhibition of ISO-stimulated ICa in rabbit atrial cells. The P1 stimulation by ATP results from hydrolysis of ATP to Ado. Both the P2- and the P1-mediated effects of ATP and Ado, respectively. involve a PTX-sensitive and cAMP-dependent pathway.  (+info)

Caffeine is a naturally occurring methylxanthine that acts as a non-selective adenosine receptor antagonist. Epidemiological studies demonstrated habitual coffee drinking to be significantly associated with liver cancer survival. We aimed to investigate the effects of caffeine and its analog CGS 15943 on hepatocellular carcinoma (HCC) and pancreatic cancer adenocarcinoma (PDAC). We demonstrate that caffeine and CGS 15943 block proliferation in HCC and PDAC cell lines by inhibiting the PI3K/Akt pathway. Importantly a kinase profiling assay reveals that CGS 15943 targets specifically the catalytic subunit of the class IB PI3K isoform (p110ƴ). These data give mechanistic insight into the action of caffeine and its analogs and they identify these compounds as promising lead compounds to develop drugs that can specifically target this PI3K isoform whose key role in cancer progression is emerging.. ...
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We examined how the endogenous anticonvulsant adenosine might influence gamma-aminobutyric acid type A (GABA(A)) receptor stability and which adenosine receptors (ARs) were involved. Upon repetitive activation (GABA 500 microM), GABA(A) receptors, microtransplanted into Xenopus oocytes from neurosurgically resected epileptic human nervous tissues, exhibited an obvious GABA(A)-current (I(GABA)) run-down, which was consistently and significantly reduced by treatment with the nonselective adenosine receptor antagonist CGS15943 (100 nM) or with adenosine deaminase (ADA) (1 units/ml), that inactivates adenosine. It was also found that selective antagonists of A2B (MRS1706, 10 nM) or A3 (MRS1334, 30 nM) receptors reduced I(GABA) run-down, whereas treatment with the specific A1 receptor antagonist DPCPX (10 nM) was ineffective. The selective A2A receptor antagonist SCH58261 (10 nM) reduced or potentiated I(GABA) run-down in approximately 40% and approximately 20% of tested oocytes, respectively. The ...
Adenosine receptors (AR) belong to the G-protein coupled receptor family. There are four receptor subtypes: A1, A2A, A2B e A3. Adenosine receptor subtypes show a different distribution in the organism and are implicated in several physiopathological processes. In particular, antagonists towards A1AR are promising in the treatment of cognitive disorders. A2A antagonists seem to be involved in decrease the neurological impairment observed in Parkinson’s disease. A2B antagonists are potential therapeutic agents in asthma and diabetes. Finally, antagonists at the A3AR could be implicated in tumor growth inhibition and in glaucoma treatment. The crystallographic structure acquisition of the human A2A receptor allowed the design of new AR antagonists by the help of computational techniques. Our group is focused on the synthesis of new adenosine receptor antagonists (particularly towards A2A and A3) for their potential therapeutic use, but also as tools for pharmacological investigations on ...
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 ...
You are viewing an interactive 3D depiction of the molecule 8-phenyl-1,3-dipropyl-3,7-dihydro-1h-purine-2,6-dione (C17H20N4O2) from the PQR.
SCH 442416 is a selective adenosine A2A receptor antagonist; binds to human and rat A2A receptors with high affinity (Ki values are 0.048 and 0.5 nM respectively). Displays > 23000-fold selectivity for hA2A over hA1 in vitro with minimal affinity for h
The findings from this systematic review and meta-analysis, based on 1,109,272 study participants and 45,335 cases of type 2 diabetes, demonstrate a robust inverse association between coffee consumption and risk of diabetes. Compared with no coffee consumption, consumption of 6 cups/day of coffee was associated with a 33% lower risk of type 2 diabetes. Caffeinated coffee and decaffeinated coffee consumption were both associated with a lower risk of type 2 diabetes. The association between coffee consumption and diabetes risk was consistent for men and women and for European, U.S., and Asian populations.. There has been some debate about the role of caffeine in the development of insulin resistance and diabetes. Short-term studies in humans have shown that caffeine intake results in an acute reduction of insulin sensitivity, which may be due to adenosine receptor antagonism and increased epinephrine release caused by caffeine (36). Other studies have found that when controlling for total coffee ...
Lunell E, Svedmyr N, Andersson KE, Persson CG (1982). Effects of enprofylline, a xanthine lacking adenosine receptor antagonism, in patients with chronic obstructive lung disease. European Journal of Clinical Pharmacology. 22 (5): 395-402. doi:10.1007/bf00542541. PMID 6288396 ...
August 20, 2007 By Grendel Burrell, M.D. [1] Preliminary results of the Phase 2, 50-patient, of BG9928 (ADENTRI®), an A1 adenosine receptor antagonist in stable patients with heart failure were reported in 2003 at the American Heart Associations annual scientific session. Dr. Barry Greenberg, professor of medicine and director of the Advanced Heart Failure Program at University of California, San Diego Medical Center, and colleagues reported the results in the August 14, 2007, issue of the Journal of the American College of Cardiology, in an article titled Effects of Multiple Oral Doses of an A1 Adenosine Antagonist, BG9928, in Patients With Heart Failure: Results of a Placebo-Controlled, Dose-Escalation Study (J Am Coll Cardiol, 2007; 50:600-606, doi:10.1016/j.jacc.2007.03.059 (Published online 29 July 2007)). BG9928 is a selective inhibitor of the A1 adenosine receptor. The objective of the study was to assess the pharmacokinetics and pharmacologic effects of BG9928 (ADENTRI®) in heart ...
A method of treating cells having a reduced apical Cl.sup.- conductance, such as that characteristic of cystic fibrosis cells, by contacting cells having a reduced apical Cl.sup.- conductance with a therapeutically effective quantity of a compound that antagonizes the A.sub.1 -adenosine cell receptor and does not antagonize the A.sub.2 -adenosine cell receptor. Suitable compounds include 8-cyclopentyl-1,3-dipropylxanthine (CPX), xanthine amino congener (XAC), and therapeutically effective derivatives thereof.. ...
methyl 2-cyclopentyl-2-(methoxycarbonylamino)acetate - chemical structural formula, chemical names, chemical properties, synthesis references
Close examination of the effect of DPCPX alone showed an increase in forskolin-stimulated [3H]cAMP accumulation. This could have been secondary to DPCPX acting as either an A1-Gi-inverse agonist or a weak A1-Gs-agonist. An alternative explanation could be antagonism of secreted endogenous adenosine from the cells themselves. Concentration-response curves were therefore constructed to the antagonists alone. An augmentation of forskolin-stimulated [3H]cAMP accumulation was observed in response to all four antagonists. Furthermore, the log EC50 values of the antagonists for this response were very similar to the log KD values obtained from whole-cell binding. Closer examination of the responses to DPCPX and CGS 15943 indicated that the response curves were biphasic. When the responses were examined in the parent CHO-CRE-SPAP cells (i.e., those with the CRE-SPAP reporter but without the A1-receptor), a similar decrease in [3H]cAMP was seen at matching higher concentrations. This suggests that the ...
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 ...
Methods Thirty-two male Sprague-Dawley rats (310-360 g) were anaesthetised and divided into four equal groups (n=8 each): Saline, Saline+MA, Theophylline, and Theophylline+MA. In the two MA groups, the sparrow-pecking MA technique was applied at 30 repetitions per min for 1 min to a depth of 15-18 mm using a stainless steel acupuncture needle (0.20×40 mm). The stimulus point was located on the right tibialis anterior (TA) muscle 7-8 mm below the knee. Animals in the two theophylline groups were intra-arterially injected with 8-(p-sulphophenyl) theophylline, a non-selective adenosine receptor antagonist, at a dose of 30 mg/kg before MA. Animals in the two saline groups received control saline. Fluorescent microspheres (15 µm in diameter, yellow-green fluorescent) were used for MBF measurement in all four groups. ...
We performed experiments to test the hypothesis that endogenous adenosine acts as an essential cofactor required for eliciting angiotensin II (Ang II)-induced afferent and/or efferent arteriolar vasoconstriction. Enalaprilat (2 mg IV) was administered to anesthetized rats to reduce endogenous Ang II levels. Kidneys and blood were harvested from these animals and used for study of renal microvascular function using the in vitro blood-perfused juxtamedullary nephron technique. Arteriolar inside diameter was monitored videomicroscopically in (1) normal kidneys, (2) kidneys subjected to adenosine receptor blockade (100 mumol/L 1,3-dipropyl-8-p-sulfophenylxanthine), and (3) kidneys continuously exposed to 1 mumol/L adenosine. Under resting conditions, arteriolar diameters were similar in all three groups of kidneys, averaging 24.8 +/- 1.0 microns (n = 23) in afferent arterioles and 24.0 +/- 0.9 microns (n = 16) in efferent arterioles. In normal kidneys, adenosine (10 mumol/L) decreased both afferent ...
Synonyms for Dimethylxanthine in Free Thesaurus. Antonyms for Dimethylxanthine. 3 synonyms for theophylline: Elixophyllin, Slo-Bid, Theobid. What are synonyms for Dimethylxanthine?
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1-Cyclopentyl-2-(1-ethylbenzimidazol-2-yl)ethanol | C16H22N2O | CID 79754065 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
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Empowering human resources means: managing learning in the organization, generating a healthy communication climate building up a team spirit amongst employees at various levels. On the basis of the lessons learned output of the M&E actions we can empower the country programme teams and partners by increasing their knowledge and understanding on programme quality, impact, accountability and learning and assisting them in developing and prioritising work plans and processes to this end.. How do we integrate learning into our Programme Cycle Management?. Through moments of reflection, or sharing thoughts, questions and ideas with colleagues or beneficiaries in more informal discussions. Learning might happen as part of structured processes such as formal evaluations, or reporting requirements, or in more informal ways, for example through a conversation between a programme officer and partner on the trip back from visiting the programme. Steps you can take to promote learning include:. · Be in ...
Substantial in vitro and animal data suggest that methylxanthines, such as caffeine and theophylline, act as adenosine receptor antagonists. To test this hypothesis in humans, we first determined if theophylline would antagonize the effects of adenosine. Intravenous administration of adenosine, 80 micrograms/kg/min, increased heart rate 28 +/- 6 bpm, systolic blood pressure 19 +/- 5 mm Hg and minute ventilation 6.1 +/- 2.2 liters/min. All these changes were significantly attenuated during theophylline administration (17 +/- 3 bpm and 1 +/- 2 mm Hg and 1.6 +/- 0.6 liters/min, respectively, P less than .05), at a dose (10 mg/kg over 1 hr, followed by 1.8 micrograms/kg/min i.v.) that produced plasma theophylline levels of 17 +/- 2 micrograms/ml (94 microM). We then determined if chronic caffeine consumption resulted in upregulation of platelet adenosine receptors in eight normal volunteers. After 7 days of caffeine abstinence, the adenosine analog 5-N-ethylcarboxamidoadenosine produced a ...
Disclosed are processes for the synthesis of novel compounds that are A.sub.2B adenosine receptor antagonists, having the structure of Formula I or Formula II: ##STR00001## by cyclizing a compound of the formula (3): ##STR00002##
TY - JOUR. T1 - Microwave-assisted and conventional synthesis of benzothieno [3,2-e] [1,3,4] triazolo[4,3-c]pyrimidines. T2 - A comparative study. AU - Gaonkar, Santhosh L.. AU - Ahn, Chuljin. AU - Princia, AU - Shetty, Nitinkumar S.. PY - 2014/8/20. Y1 - 2014/8/20. N2 - Benzothieno[2,3-d]pyrimidines (2,3,4) and benzothieno[3,2-e][1,3,4] triazolo[4,3-c] pyrimidines (5a-c) were synthesized from the precursor 2-amino-7-oxo-4,5,6,7-tetrahydro-1-benzothiophene-3-carbonitrile 1 by employing the conventional method as well as the microwave irradiation technique. The precursor 2-amino-3-cyanothiophene analogue 1 was synthesized by employing the well-known Gewald reaction. In the present work it has been found that the microwave supported syntheses are more efficient than the conventional classical heating methods. The structures of all the compounds were ascertained by spectral and analytical data.. AB - Benzothieno[2,3-d]pyrimidines (2,3,4) and benzothieno[3,2-e][1,3,4] triazolo[4,3-c] pyrimidines ...
This study was undertaken in order to investigate the effect of chronic treatment with 5′-chloro-5′-deoxy-(±)-ENBA, a potent and highly selective agonist of human adenosine A1 receptor, on thermal hyperalgesia and mechanical allodynia in a mouse model of neuropathic pain, the Spared Nerve Injury (SNI) of the sciatic nerve. Chronic systemic administration of 5′-chloro-5′-deoxy-(±)-ENBA (0.5 mg/kg, i.p.) reduced both mechanical allodynia and thermal hyperalgesia 3 and 7 days post-SNI, in a way prevented by DPCPX (3 mg/kg, i.p.), a selective A1 adenosine receptor antagonist, without exerting any significant change on the motor coordination or arterial blood pressure. In addition, a single intraperitoneal injection of 5′-chloro-5′-deoxy-(±)-ENBA (0.5 mg/kg, i.p.) 7 days post-SNI also reduced both symptoms for at least two hours. SNI was associated with spinal changes in microglial activation ipsilaterally to the nerve injury. Activated, hypertrophic microglia were significantly reduced by 5
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In the present study, we have made some progress in understanding the extracellular adenosine involved in the LFS-induced depotentiation at Schaffer collateral-CA1 synapses. There are four principal observations emerged from this work. First, the time-dependent reversal of LTP by LFS was mimicked by extracellular application of adenosine and was blocked by A1 adenosine receptor antagonist DPCPX but not by A2 receptor antagonist DMPX. Although transient extracellular application of 5-HT1A receptor agonist buspirone after LTP induction could also effectively reverse previously established LTP, 5-HT1A receptor antagonist NAN-190 did not affect the LFS-induced depotentiation. Second, the source of extracellular adenosine during LFS to exert depotentiation appeared to be attributable to the efflux of cAMP that is subsequently converted into adenosine by ecto-5′-nucleotidase. However, the extracellular conversion of ATP is not the major source of adenosine underlying the LFS-induced depotentiation. ...
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 ...
Caffeine, an adenosine receptor antagonist, blocks various receptors in the brain which are activated by adenosine. Initial results of the team of researchers had already indicated that the blockade of the adenosine receptor subtype A2A in particular could play an important role. Initially, Prof. Müller and her colleagues developed an A2A antagonist in ultrapure and water-soluble form (designated MSX-3). This compound had fewer adverse effects than caffeine since it only blocks only the A2A adenosine receptor subtype, and at the same time it is significantly more effective. Over several weeks, the researchers then treated genetically altered mice with the A2A antagonist. The mice had an altered tau protein which, without therapy, leads to the early development of Alzheimers symptoms ...
Effects of adenosine receptor agonists of the A1, A2A and A3 subtypes on the proinflammatory activity of human neutrophils in ...
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Adenosine is a modulator of many physiological and pathophysiological processes in the central nervous system (CNS). Blockade of the adenosine receptors A1ARs and A2AARs has shown beneficial neuroprotective effects in animal models and in clinical studies of Parkinsonss disease (PD) and Alzheimers disease (AD). Furthermore, selective inhibitors of the monoamine oxidase A (MAO-A) are applied as adjunctive therapeutics for PD, as they protect the brains of PD patients from oxidative stress. Nevertheless, there is still no satisfactory multitarget drug approach which inhibits MAO-A and the two adenosine receptors A1ARs and A2AARs. This invention provides newly designed tricyclic xanthine derivatives which allow overcoming this problem. A variety of 69 derivatives were prepared and evaluated in radioligand binding studies at adenosine receptors and for their ability to inhibit monoamine oxidases. Potent dual-target-directed A1/A2A adenosine receptor antagonists were identified. Several compounds ...
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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 ...
Each type of adenosine receptor has different functions, although with some overlap.[3] For instance, both A1 receptors and A2A play roles in the heart, regulating myocardial oxygen consumption and coronary blood flow, while the A2A receptor also has broader anti-inflammatory effects throughout the body.[4] These two receptors also have important roles in the brain,[5] regulating the release of other neurotransmitters such as dopamine and glutamate,[6][7][8] while the A2B and A3 receptors are located mainly peripherally and are involved in processes such as inflammation and immune responses. Most older compounds acting on adenosine receptors are nonselective, with the endogenous agonist adenosine being used in hospitals as treatment for severe tachycardia (rapid heart beat),[9] and acting directly to slow the heart through action on all four adenosine receptors in heart tissue,[10] as well as producing a sedative effect through action on A1 and A2A receptors in the brain. Xanthine derivatives ...
Alkylxanthine drugs, such as theophylline, block adenosine receptors, inhibit phosphodiesterases and other enzymes, and cause the release of calcium from intracellular stores. Adenosine receptor blockade occurs at low micromolar concentrations of the drugs, while other effects occur in the millimolar concentration range. The effects of theophylline were tested on spontaneous transmitter release at the frog cutaneous-pectoris neuromuscular junction (NMJ). A change in the frequency, but not the amplitude, of miniature endplate potentials (mepps) was interpreted as a change in spontaneous transmitter release. In normal Ringers, theophylline, at concentrations of 100 microM and 1 mM, theophylline had no consistent effect on spontaneous release. In contrast, theophylline produced dual effects on mepp frequency in hyperosmotic Ringers. At 10 microM, theophylline depressed mepp frequency, while, at 100 microM and 1 mM, theophylline increased mepp rate. Since low micromolar concentrations of ...
Locomotion is generally defined as any type of motor activity that animals use, including humans, to produce activity such as walking, running, swimming, jumping, flying, and gliding. In vertebrates, these activities are controlled by a complex neural network located in the spinal cord referred to as the central pattern generator (CPG) for locomotion. Spinal CPG adjustments, rely mostly on sensory motor stretch reflexes, which provides direct excitatory feedback to the motoneurons (MNs) innervating the muscle which has been stretched, and thus sending that information to the spinal interneurons for readjustments on movements or posture. After the loss of supraspinal brain/brainstem) inputs to the spinal cord via injury or disease, locomotion is entirely directed by the CPG and the sensory information coming from periphery. Within motor control systems, neuromodulators are necessary for proper and efficient CPG function because they induce or regulate essential components of spinal network ...
The IUPHAR/BPS Guide to Pharmacology. cyclopentyladenosine ligand page. Quantitative data and detailed annnotation of the targets of licensed and experimental drugs.
Intra- and extracellular adenosine levels rise in response to physiological stimuli and with metabolic/energetic perturbations, inflammatory challenge and tissue injury. Extracellular adenosine engages members of the G-protein coupled adenosine receptor (AR) family to mediate generally beneficial acute and adaptive responses within all constituent cells of the heart. In this way the four AR sub-types - A1, A2A, A2B, and A 3Rs - regulate myocardial contraction, heart rate and conduction, adrenergic control, coronary vascular tone, cardiac and vascular growth, inflammatory-vascular cell interactions, and cellular stress-resistance, injury and death. The AR sub-types exert both distinct and overlapping effects, and may interact in mediating these cardiovascular responses. The roles of the ARs in beneficial modulation of cardiac and vascular function, growth and stress-resistance render them attractive therapeutic targets. However, interactions between ARs and with other receptors, and their ubiquitous
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This is Digital Version of (Ebook) 978-9048131433 A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics Product Will Be Delivered
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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 ...
The incubation of isolated human PMN in vitro results in the rapid accumulation of endogenous adenosine, which has profound inhibitory effects on many cell functions, including LT synthesis. In the present study, we show that when endogenous adenosine is eliminated enzymatically from PMN suspensions, or its actions blocked with receptor antagonists, human PMN respond very strongly to low micromolar concentrations of AA for the synthesis of 5-LO products. This observation contrasts with the widely held perception that resting human PMN respond poorly to exogenous AA for LTB4synthesis and that the measurable synthesis of 5-LO products in the presence of AA requires the simultaneous stimulation with another agonist. Thus, our studies establish clearly that AA can trigger, in the absence of other added PMN stimuli, an important generation of 5-LO products and that the effect of exogenous AA is highly sensitive to the inhibitory effect of adenosine A2a receptor engagement on PMN. Therefore, these ...
The protein encoded by this gene is an adenosine receptor that belongs to the G-protein coupled receptor 1 family. There are 3 types of adenosine receptors, each with a specific pattern of ligand binding and tissue distribution, and together they regulate…
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This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
Longleaf pine savannas of the southeastern United States occupy lands ranging from flat, poorly drained (even seasonally flooded) to extremely well-drained high and dry ridges. The lower, more mesic savannas are called pine flatwoods and the higher, drier stands are known as high pine. The two communities are at opposite ends of a wetness continuum, are similar in appearance, have similar fire regimes, and share many plant and animal species. Ridges within extensive areas of pine flatwoods often support more xeric species and could be considered high pine, just as low areas within high pine support flatwoods species.. The original high pine community was readily recognized by the continuous ground cover of grasses and the widely spaced longleaf pines. Today there is no virgin or old-growth high pine remaining in Florida. Examples of second growth high pine that come close to matching descriptions from early naturalists (e.g., Bartram 1791, Williams 1837) can be seen at Riverside Island in the ...
The adenosine receptors (or P1 receptors) are a class of purinergic G protein-coupled receptors with adenosine as the ... The adenosine receptors are commonly known for their antagonists caffeine and theophylline, whose action on the receptors ... Newer adenosine receptor agonists and antagonists are much more potent and subtype-selective, and have allowed extensive ... Kalda A, Yu L, Oztas E, Chen JF (October 2006). "Novel neuroprotection by caffeine and adenosine A(2A) receptor antagonists in ...
There are three known distinct classes of purinergic receptors, known as P1, P2X, and P2Y receptors. [What about P2Z,U,T?] P2X ... All of these are antiplatelet agents that block P2Y12 receptors. Data obtained from using P2 receptor-selective antagonists has ... 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 three known distinct classes of purinergic receptors, known as P1, P2X, and P2Y receptors. Cell signalling events ... receptor inhibitors. Before the expiry of its patent, the P2Y12 receptor antagonist Clopidogrel (trade name: Plavix) was the ... 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 ...
GABAA receptor involvement was demonstrated by intrathecal administration of gabazine, a GABAA antagonist, in animals receiving ... a large majority were co-labeled with purinergic antibodies. Fifty-five percent of TPH+ neurons stained for P1, 63% for P2X1, ... Intra-RVM administration of AP5 or MK-801, NMDA receptor antagonists, resulted in a reversal of the mechanical sensitivity ... Histological staining by another research group examined the distribution of purinergic receptor subtypes throughout the RVM. ...
... purinergic P1 receptor - purinergic P2 receptor - purinergic receptor - pyridine - pyrimidine - pyruvate - pyruvate oxidation ... receptor (biochemistry) - receptor antagonist - receptor protein-tyrosine kinase - recombinant fusion protein - recombinant ... 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- ...
Blocking the DAMP receptors or their signaling - RAGE small molecule antagonists, TLR4 antagonists, antibodies to DAMP-R DAMPs ... Similarly, adenosine triggers degranulation through P1 receptors. Uric acid is also an endogenous danger signal released by ... that have reached the extracellular space can also serve as danger signals by signaling through purinergic receptors. ATP and ... DAMPs and their receptors are characterized as: Two papers appearing in 1994 presaged the deeper understanding of innate immune ...
Role of Prasugrel, a Novel P2Y12 Receptor Antagonist, in the Management of Acute Coronary Syndromes. American Journal of ... Harden TK, Boyer JL, Nicholas RA (1995). „P2-purinergic receptors: subtype-associated signaling responses and structure". ... P1 receptori. adenozin. G protein spregnuti receptori P2Y receptori. nukleotidi *ATP. *ADP ... Biogeno aminski receptor - Eikozanoidni receptor (Prostaglandinski receptor) - G protein-spregnuti receptor - Imunski receptor ...
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. ...
Antagonists bind to receptors but do not activate them. This results in a receptor blockade, inhibiting the binding of agonists ... 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 P1 Receptor Antagonists. Purinergic Antagonists. Purinergic Agents. Neurotransmitter Agents. To Top ...
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 Antagonists. Purinergic Antagonists. Purinergic Agents. Neurotransmitter Agents. To Top ...
Purinergic P1 Receptor Antagonists. Purinergic Antagonists. Purinergic Agents. Neurotransmitter Agents. To Top ...
... receptor. The aim of the present study was to elucidate the effects of PD81,723 both as a … ... Purinergic P1 Receptor Agonists * Purinergic P1 Receptor Antagonists * Receptors, Purinergic P1 / genetics ... on agonist and antagonist binding and function at the human wild-type and a mutant (T277A) adenosine A1 receptor Biochem ... receptor. Our results showed opposite effects of PD81,723 on the binding of agonists and antagonists. Within the concept of a ...
Purinergic P1 Receptor Antagonists * Receptors, Purinergic P1 * 2-(4-(2-carboxyethyl)phenethylamino)-5-N- ... Adenosine mediates its effects through four receptor subtypes: the A1, A2a, A2b and A3 receptors. The A2a receptor (A2aR) is ... Purinergic P1 Receptor Antagonists * Receptors, Purinergic P1 / deficiency * Receptors, Purinergic P1 / genetics ... Aggressiveness, hypoalgesia and high blood pressure in mice lacking the adenosine A2a receptor Nature. 1997 Aug 14;388(6643): ...
Purinergic P1 Receptor Antagonists: 1 study in 3 results : IBA. *Apolipoprotein E2: 1 study in 3 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 : ...
Purinergic P1 Receptor Antagonists. Not Applicable. Interventional clinical trials:. #. Name. Status. NCT ID. Phase. Drugs. ...
PPADS is a nonselective (but nonuniversal) P2 receptor antagonist and does not block P1 receptor (Lambrecht, 2000; Lambrecht et ... a P2X purinergic receptor antagonist) were purchased from Sigma-Aldrich. Aβ1-42 synthetic peptide was purchased from American ... 4E,F) and PPADS blocks P2 receptors but not P1 receptors (Lambrecht, 2000). ... Adenosine is a signaling molecule that regulates cellular activity in the CNS through P1 purinergic receptor (Kaster et al., ...
... 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 ... ATP-induced TSP-1 expression is mediated by purinergic receptors. Astrocytes were treated with P2 antagonists (RB2 or PPADS; 50 ... Agonist and antagonist studies point to a role for P2Y4 receptors. However, other P2 receptors might be involved because RB2 ...
Update on novel purinergic P2X3 and P2X2/3 receptor antagonists and their potential therapeutic applications.,/bp:TITLE, ,bp: ... P1 or Adenosine receptors GraphId=aba11, ,Graphics CenterX=845.8450842431788 CenterY=587.9216367603486 Width= ... A selective P2X3 antagonist with potent anti-tussive effect and no taste alteration.,/bp:TITLE, ,bp:SOURCE rdf:datatype=http ... nucleotide signaling via the purinergic P2Y receptors.,/bp:TERM, ,bp:ID xmlns:rdf=http://www.w3.org/1999/02/22-rdf-syntax-ns# ...
Purinergic P1 Receptor Antagonists Triazolam and zolpidem: A comparison of their psychomotor, cognitive, and subjective effects ... Cocaine-like subjective effects of nicotine are not blocked by the D1 selective antagonist ecopipam (SCH 39166). Chausmer, A. L ...
The purinergic P2/P4 antagonist di-inosine pentaphosphate or P1-receptor antagonist sulfonylphenyl theophylline, but not the P2 ... receptor antagonist suramin, antagonized the effect of AP4A, suggesting that the observed protection is mediated through an ... anti-apoptotic mechanism and the activation of P1- and P4-purinergic receptors. AP4A also afforded protection from toxicity ... GLP-1 receptors are widely expressed in the brain and spinal cord, and our prior studies have shown that Ex-4 is ...
Purinergic P1 Receptor Agonists * Purinergic P1 Receptor Antagonists * Purinergic P1 Receptors * Eye ...
The adenosine receptors (or P1 receptors) are a class of purinergic G protein-coupled receptors with adenosine as the ... The adenosine receptors are commonly known for their antagonists caffeine and theophylline, whose action on the receptors ... Newer adenosine receptor agonists and antagonists are much more potent and subtype-selective, and have allowed extensive ... Kalda A, Yu L, Oztas E, Chen JF (October 2006). "Novel neuroprotection by caffeine and adenosine A(2A) receptor antagonists in ...
Theophylline, a purinoceptor P1 antagonist and vinpocetine, an antiischemic compound partly reversed the effect of hypoxia. ... Theophylline, a purinoceptor P1 antagonist and vinpocetine, an antiischemic compound partly reversed the effect of hypoxia. ... Theophylline, a purinoceptor P1 antagonist and vinpocetine, an antiischemic compound partly reversed the effect of hypoxia. ... Theophylline, a purinoceptor P1 antagonist and vinpocetine, an antiischemic compound partly reversed the effect of hypoxia. ...
Purinergic P1 Receptor Antagonists 49 Scopus citations * Anorectal contractility under basal conditions and during rectal ...
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. ...
4H-J and M). Other purinergic agonists that we tested, including adenosine, which activate P1 receptors, and α,β-methylene ATP ... 3E). This increased activity was diminished in the presence of the ATP receptor antagonist suramin (10 μmol/L) (Fig. 3F), ... 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 ...
... a purinergic P1 receptor antagonist which acts as a respiratory ... Mechanism of Action Purinergic P1 receptor antagonists * Orphan ...
Purinergic P1 Receptor Antagonists Medicine & Life Sciences * sapropterin Medicine & Life Sciences * Antirheumatic Agents ... but rather was completely prevented by adenosine receptor antagonists.Conclusion. Our findings support a model whereby distinct ... but rather was completely prevented by adenosine receptor antagonists.Conclusion. Our findings support a model whereby distinct ... but rather was completely prevented by adenosine receptor antagonists.Conclusion. Our findings support a model whereby distinct ...
It may be clinically important for pharmacological intervention in gliomas to associate purinergic receptor antagonists and ... Adenosine appears to act through P1 purinoceptors, although the subtype involved remains controversial, whereas ATP may involve ... A G protein mutant that inhibits thrombin and purinergic receptor activation of phospholipase A2. Gupta, S.K., Diez, E., ... Feed forward cycle of hypotonic stress-induced ATP release, purinergic receptor activation, and growth stimulation of prostate ...
There are three known distinct classes of purinergic receptors, known as P1, P2X, and P2Y receptors. [What about P2Z,U,T?] P2X ... All of these are antiplatelet agents that block P2Y12 receptors. Data obtained from using P2 receptor-selective antagonists has ... 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 ...
Activation of P2X receptors is implicated in dental pain, and receptor antagonists represent important targets for new ... Oral tissues express a variety of G-protein-coupled P2Y receptors for ATP and P1 receptors for adenosine in addition to ... The intricacies of the purinergic signaling system make it well-suited for the unique concerns of dental research, and future ... Nuclear Transport Receptor Binding Avidity Triggers a Self-healing Collapse Transition in FG-nucleoporin Molecular Brushes ...
Purinergic P1 Receptor Agonists. *Purinergic P1 Receptor Antagonists. *Purines. *Receptor, Adenosine A2A ... adenosine receptor subtypes. In contrast to their effects on antagonist-occupied receptors, amiloride analogues did not affect ... The binding modes of amiloride analogues at agonist-occupied and antagonist-occupied receptors differed markedly, which was ... Amiloride and 5-(N,N-dimethyl)amiloride (DMA) were more potent at A(1) receptors than at A(3) receptors, while 5-(N,N- ...
Purinergic Antagonists. MeSH PA. D058915. Purinergic P1 Receptor Antagonists. MeSH PA. D019141. Respiratory System Agents. ...
Adenosine A2A Receptors * Purinergic P1 Receptor Antagonists * Fructose-Bisphosphate Aldolase * Peritoneal Macrophages ... Adenosine A2a receptor-mediated, normoxic induction of HIF-1 through PKC and PI-3K-dependent pathways in macrophages. ... Fingerprint Dive into the research topics of Adenosine A2a receptor-mediated, normoxic induction of HIF-1 through PKC and PI- ...
Purinergic P1 Receptor Antagonists. *RNA, Messenger/metabolism. *Receptor, Adenosine A3. *Receptors, Purinergic P1/metabolism* ... receptor antagonist (MRS1191) but not by an A(2) receptor antagonist (3,7-dimethyl-1-propargylxanthine [DMPX]). The A(3) ... AK-T cells express mRNA coding for A(2A), A(2B) and A(3) receptors, but little or no mRNA coding for A(1) receptors. The ... Adenosine acts through an A3 receptor to prevent the induction of murine anti-CD3-activated killer T cells.. Hoskin DW1, Butler ...
Purinergic P1 Receptors * Adenosine * Renal Cell Carcinoma * Immunotherapy * Purinergic P1 Receptor Antagonists ... Adenosine 2A receptor blockade as an immunotherapy for treatment-refractory renal cell cancer. Fong, L., Hotson, A., Powderly, ... Contribution of immune cells to glucocorticoid receptor expression in breast cancer. Gandhi, S., Elkhanany, A., Oshi, M., Dai, ... BL-8040, a CXCR4 antagonist, in combination with pembrolizumab and chemotherapy for pancreatic cancer: the COMBAT trial. ...
  • Binding (saturation and displacement experiments) and functional adenosine 3',5'-cyclic monophosphate studies were performed, and differential effects of allosteric enhancer PD81,723 on agonists and antagonists were observed on the wild-type (wt) and mutant adenosine A(1) receptor. (nih.gov)
  • Our results showed opposite effects of PD81,723 on the binding of agonists and antagonists. (nih.gov)
  • 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)
  • Primary cultures of cerebellar granule cells were exposed chronically to A 1 adenosine receptor agonists and antagonists. (elsevier.com)
  • Hettinger-Smith, BD, Leid, M & Murray, TF 1996, ' Chronic exposure to adenosine receptor agonists and antagonists reciprocally regulates the A 1 adenosine receptor-adenylyl cyclase system in cerebellar granule cells ', Journal of Neurochemistry , vol. 67, no. 5, pp. 1921-1930. (elsevier.com)
  • Adenosine receptors: development of selective agonists and antagonists. (wikipathways.org)
  • This involvement suggests the possible use of purinergic agonists and antagonists as therapeutic targets for ocular inflammation. (ucm.es)
  • Various agonists and antagonists are involved in the inhibition and induction of purinergic signalling, which causes alterations in the responsive cells. (springeropen.com)
  • Methods: Spinal cord cultures were treated with adenosine receptor agonists and antagonists. (northwestern.edu)
  • Adenosine mediates its effects through four receptor subtypes: the A1, A2a, A2b and A3 receptors. (nih.gov)
  • This recent knowledge of purinergic receptors' effects on chronic pain provide promise in discovering a drug that specifically targets individual P2 receptor subtypes. (wikipedia.org)
  • 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)
  • 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)
  • 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)
  • therefore, it may be useful in evaluating the role of LPA and its receptor subtypes involved in biological actions. (aspetjournals.org)
  • 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)
  • 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)
  • Comparative pharmacology of human adenosine receptor subtypes - characterization of stably transfected receptors in CHO cells. (biomedsearch.com)
  • Four adenosine receptor subtypes of the family of G protein-coupled receptors, designated A1, A2A, A2B and A3 are currently known. (biomedsearch.com)
  • In this study we present for the first time the comparative pharmacology of all known human adenosine receptor subtypes. (biomedsearch.com)
  • These cells are valuable systems for further characterization of specific receptor subtypes and for the development of new ligands. (biomedsearch.com)
  • 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)
  • 5 Using Ca2+ channel subtype-selective antagonists, CADO inhibition appeared to target multiple channel subtypes, with the inhibition of o-conotoxin GVIA-sensitive calcium channels being more prominent. (gotomydoctor.com)
  • 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)
  • 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)
  • Antagonism of the adenosine receptor by caffeine leads to an increased LPS-induced inflammatory reaction and an increase in (subclinical) tissue damage? (clinicaltrials.gov)
  • Caffeine (4mg/kg) is used as an adenosine receptor antagonist. (clinicaltrials.gov)
  • The adenosine receptors are commonly known for their antagonists caffeine and theophylline, whose action on the receptors produces the stimulating effects of coffee, tea and chocolate. (wikipedia.org)
  • Xanthine derivatives such as caffeine and theophylline act as non-selective antagonists at A1 and A2A receptors in both heart and brain and so have the opposite effect to adenosine, producing a stimulant effect and rapid heart rate. (wikipedia.org)
  • Theophylline and caffeine are nonselective adenosine antagonists that are used to stimulate respiration in premature infants. (wikipedia.org)
  • Xanthines (e.g. caffeine) specifically block adenosine receptors, and are known to induce a stimulating effect to one's behavior. (wikipedia.org)
  • CB(1) and A(1) receptors are the main targets for the effects of two of the most heavily consumed psychoactive substances worldwide: Δ(9)-tetrahydrocannabinol (THC, a CB(1) receptor agonist) and caffeine (an adenosine receptor antagonist). (strath.ac.uk)
  • A(1) receptor levels were increased following chronic caffeine administration. (strath.ac.uk)
  • This study shows that A(1) receptors exert a negative modulatory effect on CB(1)-mediated inhibition of GABA and glutamate release, and provides the first evidence of chronic caffeine-induced alterations on the cannabinoid system in the cortex and hippocampus, with functional implications in spatial memory. (strath.ac.uk)
  • The stimulant effects of caffeine on locomotor behaviour in mice are mediated through its blockade of adenosine A(2A) receptors. (ac.be)
  • In the present study, the effect of adenosine (A1 and A2 receptor agonist), caffeine (A2A receptor antagonist), theophylline (A2A receptor antagonist) and their combination was studied in anxiety related behaviours using elevated zero maze and elevated plus maze paradigms and compared their various behavioural profiles. (bvsalud.org)
  • OBJECTIVE: Studies have demonstrated that methylxanthines, such as caffeine, are A1 and A2 adenosine receptor antagonists found in the brain, heart, lungs, peripheral vessels, and platelets. (bvsalud.org)
  • 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)
  • The adenosine antagonists caffeine and 8-p-sulfophenyltheophylline produced alterations in A 1 adenosine receptor homeostasis that were antipodal to those associated with agonist treatment. (elsevier.com)
  • Minor stimulants such as caffeine, which act as adenosine receptor antagonists, can also potentiate behavioral activation. (elsevier.com)
  • We first demonstrate that acute mortality is related to prolonged apnea and that a single acute injection of the adenosine receptor antagonist caffeine can completely prevent TBI-induced mortality when given immediately following the TBI. (elsevier.com)
  • Immunodeficient nonobese diabetic-severe combined immunodeficiency-IL-2 receptor γnull mice were injected with human peripheral blood mononuclear cells, and subsequently injected with the CD39/CD73 antagonist αβ-methylene-ADP (APCP) (50 mg kg-1) or saline for 7 days, or the AR antagonist caffeine (10 mg kg-1) or saline for 14 days. (unboundmedicine.com)
  • Acute and chronic caffeine administration differentially alters striatal gene expression in wild-type and adenosine A(2A) receptor-deficient mice. (ox.ac.uk)
  • These results indicate that, depending on the dose, the blockade of A(2A)-R or A(1) receptors by caffeine is preferentially revealed leading to highly differential alterations in striatal gene expression and they also suggested the central role of these two receptors on the control of dopaminergic functions. (ox.ac.uk)
  • Caffeine keeps you awake by blocking adenosine receptors. (wikipedia.org)
  • These effects of sleep deprivation are counteracted by the adenosine receptor antagonist caffeine, implying involvement of the adenosine neuromodulator/receptor system. (cdc.gov)
  • To examine a role for adenosine A(2A) receptors, we investigated whether variation of the A(2A) receptor gene (ADORA2A) modified effects of caffeine on PVT and SWA after sleep deprivation. (cdc.gov)
  • Genetic basis of apnoea of prematurity and caffeine treatment response: role of adenosine receptor polymorphisms: genetic basis of apnoea of premat. (cdc.gov)
  • Caffeine treatment reduces the frequency of apnoea of prematurity (AOP) and eliminates the need for mechanical ventilation by acting as a nonspecific inhibitor of adenosine A1 and adenosine 2A receptors. (cdc.gov)
  • Our results indicate a role for adenosine receptor gene polymorphisms in susceptibility to AOP and BPD and in interindividual variability to caffeine response. (cdc.gov)
  • Physiological roles of A1 and A2A adenosine receptors in regulating heart rate, body temperature, and locomotion as revealed using knockout mice and caffeine. (semanticscholar.org)
  • Heart rate (HR), body temperature (Temp), locomotor activity (LA), and oxygen consumption (O(2)C) were studied in awake mice lacking one or both of the adenosine A(1) or A(2A) receptors (A(1)R or A(2A)R, respectively) using telemetry and respirometry, before and after caffeine administration. (semanticscholar.org)
  • Caffeine reduces hypnotic effects of alcohol through adenosine A2A receptor blockade. (semanticscholar.org)
  • Modulation of paracetamol antinociception by caffeine and by selective adenosine A2 receptor antagonists in mice. (semanticscholar.org)
  • Treatment of primary cultures of rat cortical astrocytes with extracellular ATP caused an increase in TSP-1 expression in a time- and concentration-dependent manner and was inhibited by antagonists of P2 and P1 purinergic receptors. (pnas.org)
  • 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)
  • Platelet-derived growth factor stimulated synthesis of TSP in a human glial cell line ( 28 ) and transforming growth factor-β1 induced TSP-1 mRNA in astrocytes ( 29 ), but the potential role of extracellular ATP and P2 receptor signaling in TSP-1 expression and release in astrocytes has not been investigated. (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)
  • 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)
  • These data suggest that central ATP, acting on purinergic P2 receptors, reduces water intake induced by intracellular and extracellular dehydration. (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)
  • 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)
  • There are two types of NTs: Concentrative nucleoside transporters (CNTs): Na+-dependent symporters Equilibrative nucleoside transporters (ENTs): Na+-independent passive transporters The extracellular concentration of adenosine can be regulated by NTs, possibly in the form of a feedback loop connecting receptor signaling with transporter function. (wikipedia.org)
  • Extracellular AMP is hydrolyzed to adenosine by ecto-5'-nucleotidase (eN) as well as by APs. (wikipedia.org)
  • Nucleotides and nucleosides act as potent extracellular messengers via the activation of the family of cell-surface receptors termed purinergic receptors. (biomedcentral.com)
  • 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)
  • 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)
  • Intracellularly, ATP is stored at very high levels (from 5 to 10mmol/l), which can quickly be degraded by ubiquitous extracellular nucleotidases after connecting to specific receptors under physiological conditions. (thefreelibrary.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. (springer.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)
  • Presence of ATP in the extracellular milieu activates the P2X and P2Y purinergic signalling cascade. (springeropen.com)
  • Responses were preserved in the absence of extracellular calcium and inhibited by P2Y 2 R antagonists. (frontiersin.org)
  • Extracellular nucleotides, signalling via purinergic receptors, are actually known to take part in a wide variety of natural procedures. (onetownmanyvoices.com)
  • Furthermore, a recently available research using ATP analogues shown that P2X1 and P2X7 receptors will also be mixed up in regulation of bone tissue mineralisation by extracellular nucleotides [21]. (onetownmanyvoices.com)
  • Pursuing membrane harm or necrosis, all cells can?launch ATP in to the extracellular environment, that may then act within an autocrine/paracrine way to influence community purinergic signalling. (onetownmanyvoices.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)
  • Extracellular adenosine critically modulates ischemic brain injury, at least in part through activation of the A 1 adenosine receptor. (jneurosci.org)
  • These results suggest that intrastriatal administration of ATP causes P2X receptor-mediated cell death in the striatum and support the hypothesis that extracellular ATP can be an important mediator of neuropathological events of brain injuries. (ajou.ac.kr)
  • CysLT1 receptor is a target for extracellular nucleotide- induced heterologous desensitization: a possible feedback mechanism in. (lookformedical.com)
  • Inhibitors of purinergic receptors include clopidogrel, prasugrel and ticlopidine, as well as ticagrelor. (wikipedia.org)
  • 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 inhibitors of these receptors will be the effective therapeutic targets in managing OC. (springeropen.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)
  • Boosts in bone tissue mineralisation had been also noticed when osteoblasts had been cultured using the ATP discharge inhibitors, NEM and brefeldin A, aswell much like P2X1 and P2X7 receptor antagonists. (onetownmanyvoices.com)
  • Adenosine receptor-blocking xanthines as inhibitors of phosphodiesterase isozymes. (semanticscholar.org)
  • 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)
  • 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)
  • 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)
  • each receptor continues to be cloned, characterised and shows distinctive pharmacology and tissues appearance [4,5]. (onetownmanyvoices.com)
  • The purinergic P2/P4 antagonist di-inosine pentaphosphate or P1-receptor antagonist sulfonylphenyl theophylline, but not the P2-receptor antagonist suramin, antagonized the effect of AP4A, suggesting that the observed protection is mediated through an anti-apoptotic mechanism and the activation of P1- and P4-purinergic receptors. (jove.com)
  • Theophylline, a purinoceptor P 1 antagonist and vinpocetine, an antiischemic compound partly reversed the effect of hypoxia. (elsevier.com)
  • Only the A 1 /A 2A receptor antagonist theophylline (5.0-15.0mg/kg) and the A 2A antagonist MSX-3 (2.0mg/kg) increased spontaneous locomotion and rearing. (elsevier.com)
  • Although adenosine antagonists did not affect c-Fos expression on their own, theophylline and MSX-3, but not CPT, attenuated haloperidol induction of c-Fos expression. (elsevier.com)
  • Once in the body, theophylline is released and acts as a phosphodiesterase inhibitor, adenosine receptor blocker, and histone deacetylase activator. (drugbank.ca)
  • Theophylline also binds to the adenosine A2B receptor and blocks adenosine mediated bronchoconstriction. (drugbank.ca)
  • P1 receptors are preferentially activated by adenosine and P2Y receptors are preferentially more activated by ATP. (wikipedia.org)
  • 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)
  • P1 are G-protein-coupled receptors activated by adenosine. (alzforum.org)
  • 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)
  • In contrast, inhibition of NF-κB activation by MTX was not mediated via BH 4 depletion and JNK activation in FLSs, but rather was completely prevented by adenosine receptor antagonists.Conclusion. (elsevier.com)
  • We found that A(1) receptor activation attenuated the CB(1)-mediated inhibition of GABA and glutamate release and this interaction was manifested at the level of G-protein activation. (strath.ac.uk)
  • Among the most important are inhibition of cyclic nucleotide PHOSPHODIESTERASES, antagonism of ADENOSINE RECEPTORS, and modulation of intracellular calcium handling. (drugcentral.org)
  • 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)
  • 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)
  • Adenosine A2AR antagonists improve 6-OHDA -motor deficit and this effect seems to be mediated by the inhibition of A2A presynaptic receptors in substantia nigra pars compacta . (bvsalud.org)
  • 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)
  • This UTP-responsive P2Y receptor was found to be P2Y 4 , evidenced by the inhibition of UTP effect in the presence of 100 μM reactive blue 2, an antagonist at rat P2Y 4 . (ejao.org)
  • CADO inhibition of barium currents was also sensitive to the A1 antagonist 1,3-dipropyl-8-cyclopentylxanthine (DPCPX). (gotomydoctor.com)
  • 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)
  • This can be calculated for a given antagonist by determining the concentration of antagonist needed to elicit half inhibition of the maximum biological response of an agonist . (lookformedical.com)
  • Bailey MA (2004) Inhibition of bicarbonate reabsorption in the rat proximal tubule by activation of luminal P2Y1 receptors. (springer.com)
  • The adenosine receptors (or P1 receptors) are a class of purinergic G protein-coupled receptors with adenosine as the endogenous ligand. (wikipedia.org)
  • P2X receptors are ligand-gated ion channels, whereas the P1 and P2Y receptors are G protein-coupled receptors. (wikipedia.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)
  • The latter can be further subdivided into the G-protein-coupled P2Y receptors (P2YRs) and the ionotropic P2X receptors (P2XRs) [ 9 ]. (springeropen.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)
  • The P2 receptors react to nucleotides including ATP, adenosine diphosphate (ADP),?uridine triphosphate (UTP) and uridine diphosphate (UDP) and?are additional subdivided in to the P2X ligand-gated ion stations as well as the P2Con G-protein-coupled receptors [2,3]. (onetownmanyvoices.com)
  • Update and subclassification of the P2Y G protein-coupled nucleotide receptors: from molecular mechanisms and pathophysiology to therapy. (axonmedchem.com)
  • The notion of xanthine-insensitivity of the A3 receptor should be dropped at least for the human receptor as xanthines with submicromolar affinity were found. (biomedsearch.com)
  • After binding onto a specific purinergic receptor, adenosine causes a negative chronotropic effect due to its influence on cardiac pacemakers. (wikipedia.org)
  • ATP provokes the activation of specific purinergic receptors in the plasma membrane (Fig. 1 . (springeropen.com)
  • The effects of UTP and ATP were prevented by both wide-range and specific purinergic antagonists. (frontiersin.org)
  • Modulation of murine dendritic cell function by adenine nucleotides and adenosine: involvement of the A(2B) receptor. (ac.be)
  • Released nucleotides can be hydrolyzed extracellularly by a variety of cell surface-located enzymes referred to as ectonucleotidases that control purinergic signalling. (wikipedia.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)
  • 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)
  • P2Y receptors can be stimulated by a wider range of nucleotides such as ATP, ADP, UTP, UDP and UDP-glucose. (axonmedchem.com)
  • 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)
  • 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)
  • In the presence of GTP all receptors were converted to a single low affinity state indicating functional coupling to endogenous G proteins. (biomedsearch.com)
  • Expressed by neurons and astroglia, the A2A receptor couples to Gs proteins that raise the levels of the second messenger cAMP in the cytosol. (alzforum.org)
  • 1997), the long-term decrease in receptors belong to the heptahelical family of receptors seizure threshold brought about by repeated electrical and are coupled to heterotrimeric G proteins. (gotomydoctor.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)
  • Differential allosteric modulation by amiloride analogues of agonist and antagonist binding at A(1) and A(3) adenosine receptors. (nih.gov)
  • Recent research has identified a role for microglial P2X receptors in neuropathic pain and inflammatory pain, especially the P2X4 and P2X7 receptors. (wikipedia.org)
  • CONCLUSION: Despite all of the exciting results obtained on the bench, few antagonists of P2 receptors advanced to the clinical trials, and once they reach this stage, the effectiveness of the therapy is not guaranteed, as in the example of P2X7 antagonists. (bvsalud.org)
  • Thus several preclinical studies demonstrate the involvement of the P2X7 receptor (P2X7R) in the control of Mycobacterium tuberculosis (MTB) infection. (bvsalud.org)
  • Nevertheless, one idea that seems overlooked by the "purinergic community" is the use of the high-conductance channel associated with P2X7R to increase the passage of hydrophilic drugs to the cytoplasm of cells that express the P2X7 pore, a potential method for a drug delivery system. (bvsalud.org)
  • 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)
  • 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)
  • Stimulation of the adenosine receptor could potentially lead to a decrease in inflammation and tissue damage. (clinicaltrials.gov)
  • Stimulation of the A1 receptor has a myocardial depressant effect by decreasing the conduction of electrical impulses and suppressing pacemaker cell function, resulting in a decrease in heart rate. (wikipedia.org)
  • 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)
  • 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)
  • We also found that exogenous ATP protected Aβ42-mediated reduction in synaptic molecules, such as NMDA receptor 2A and PSD-95, through P2 purinergic receptors and prevented Aβ42-induced spine reduction in cultured primary hippocampal neurons. (jneurosci.org)
  • Presynaptically, it reduces synaptic vesicle release while post synaptically it has been found to stabilize the magnesium on the NMDA receptor. (wikipedia.org)
  • 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)
  • is an uncompetitive antagonist of the NMDA receptor . (lookformedical.com)
  • Most older compounds acting on adenosine receptors are nonselective, with the endogenous agonist adenosine being used in hospitals as treatment for severe tachycardia (rapid heart beat), and acting directly to slow the heart through action on all four adenosine receptors in heart tissue, as well as producing a sedative effect through action on A1 and A2A receptors in the brain. (wikipedia.org)
  • The A1, together with A2A receptors of endogenous adenosine play a role in regulating myocardial oxygen consumption and coronary blood flow. (wikipedia.org)
  • Macrophage production and secretion of these homeostatic factors are controlled by endogenous purinergic signals. (diabetesjournals.org)
  • Regulation of plasma membrane ion transport by endogenous purinergic receptors was assessed in a distal renal (A6) cell line. (elsevier.com)
  • 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)
  • Barrett RJ, Droppleman DA (1993) Interactions of adenosine A1 receptor-mediated renal vasoconstriction with endogenous nitric oxide and ANG II. (springer.com)
  • Ryanodine reduced calcium activity in the boutons, whereas the ATP antagonist adenosine-5′-O-(α, β- methylene diphosphate) reduced calcium activity in both the boutons and vascular tone. (arvojournals.org)
  • 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)
  • 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)
  • 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)
  • 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)
  • Purinergic receptors, also known as purinoceptors, are a family of plasma membrane molecules that are found in almost all mammalian tissues. (wikipedia.org)
  • The term purinergic receptor was originally introduced to illustrate specific classes of membrane receptors that mediate relaxation of gut smooth muscle as a response to the release of ATP (P2 receptors) or adenosine (P1 receptors). (wikipedia.org)
  • Nucleotide receptors may effect their responses through primary activation of membrane chloride channels. (elsevier.com)
  • 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)
  • 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)
  • Purines and pyrimidines act on P1 and P2 purinergic receptors, which are widely expressed in the plasma membrane in various cell types. (bvsalud.org)
  • Purinergic receptors sit on the plasma membrane and are activated by ATP or its breakdown products ADP, AMP, and adenosine. (alzforum.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)
  • P2X receptors mediate a large variety of responses including fast transmission at central synapses, contraction of smooth muscle cells, platelet aggregation, macrophage activation, and apoptosis. (wikipedia.org)
  • Studies using local administration of cannabinoid agonists have shown that peripheral, spinal, and supraspinal cannabinoid receptors mediate cannabinoid-induced antinociception. (cognizantcommunication.com)
  • 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)
  • Furthermore, we found that the protective role of ATP is mediated by the P2 purinergic receptor signaling pathway. (jneurosci.org)
  • The current study aimed to explore the role of the CD39/CD73 pathway and adenosine receptor (AR) blockade in a humanized mouse model of GVHD. (unboundmedicine.com)
  • Geraghty NJ, Watson D, Sluyter R. Pharmacological blockade of the CD39/CD73 pathway but not adenosine receptors augments disease in a humanized mouse model of graft-versus-host disease. (unboundmedicine.com)
  • TY - JOUR T1 - Pharmacological blockade of the CD39/CD73 pathway but not adenosine receptors augments disease in a humanized mouse model of graft-versus-host disease. (unboundmedicine.com)
  • The Pannexin-1 channel (PANX1) is an integral component of the P2X/P2Y purinergic signaling pathway and the key contributor to pathophysiological ATP release. (wikipedia.org)
  • It has been thought that P2X 2 receptors in OSC provide parasensory K + efflux pathway in response to intense noise exposure. (ejao.org)
  • 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)
  • 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)
  • Specific A1 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)
  • Therefore, we studied the effects of intracerebroventricular (icv) injections of ATP (100, 200 and 300 nmol/µL) alone or combined with DPCPX or PPADS (P1 and P2 purinergic antagonists, respectively, 25 nmol/µL) on water intake induced by water deprivation. (bvsalud.org)
  • ZM241385, DPCPX, MRS1706 are inverse agonists with different relative intrinsic efficacies on constitutively active mutants of the human adenosine A2B receptor. (wikipathways.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)
  • Immunohistochemical analysis of A 1 receptor abundance was conducted in EtOH-naïve and EtOH pretreated slice cultures at 15 DIV. Results: Twenty-four hour exposure to DPCPX in EtOH-naïve slice cultures did not produced neurotoxicity in any region of slice cultures. (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 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)
  • 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)
  • 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)
  • Further, we also intend to highlight purinergic signalling as a novel therapeutic target in treating OC. (springeropen.com)
  • Conclusion: Selective, high-affinity adenosine A 2a antagonists merit consideration as therapeutic agents for the treatment of ALS. (northwestern.edu)
  • These two receptors also have important roles in the brain, regulating the release of other neurotransmitters such as dopamine and glutamate, while the A2B and A3 receptors are located mainly peripherally and are involved in processes such as inflammation and immune responses. (wikipedia.org)
  • These ligand-gated ion channels are nonselective cation channels responsible for mediating excitatory postsynaptic responses, similar to nicotinic and ionotropic glutamate receptors. (wikipedia.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)
  • 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)
  • 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)
  • Contractile responses of the sphincter to EFS were unaffected by the muscarinic receptor antagonist atropine (1 µM), but were almost completely abolished by the adrenergic neuron blocker guanethidine (10 µM). (edu.au)
  • Therefore, purinergic responses in the perivascular retinal tissue during relaxation of VSMCs were studied. (arvojournals.org)
  • 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)
  • Pharmacological examination showed that the ATP responses are primarily mediated by P2X purinergic receptors. (frontiersin.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)
  • 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)
  • P2Y receptors are coupled to protein kinase cascades, and signaling studies demonstrated that blockade of mitogen-activated protein kinases or Akt inhibited ATP- and UTP-induced TSP-1 expression. (pnas.org)
  • Studies have found that blockade of the A1 Receptor suppresses the osteoclast function, leading to increased bone density. (wikipedia.org)
  • Absence of the adenosine A(2A) receptor or its chronic blockade decrease ethanol withdrawal-induced seizures in mice. (ac.be)
  • Conversely, blockade of adenosine A1 receptors from the presymptomatic stage significantly attenuated motor disease progression and induced a non-significant increase of median survival in ALS mice. (elsevier.com)
  • 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)
  • Potent adenosine receptor antagonists that are selective for the A1 receptor subtype. (wikipathways.org)
  • BLU-5937: A selective P2X3 antagonist with potent anti-tussive effect and no taste alteration. (wikipathways.org)
  • The non-xanthine heterocyclic compound SCH 58261 is a new potent and selective A2a adenosine receptor antagonist. (wikipathways.org)
  • 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)
  • 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 ACh effects are diminished in the presence of atropine or M3 muscarinic receptor antagonist and in SCs lacking M3 receptors. (frontiersin.org)
  • 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)
  • 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)
  • The study suggested the involvement of adenosinergic receptor system in anxiety related behaviours. (bvsalud.org)
  • Researchers have elucidated the involvement of these receptors in the host response to infections. (biomedcentral.com)
  • The adenosine receptor system warrants further examination in this regard, as recent evidence has implicated adenosine receptor involvement in the behavioral effects of both EtOH exposure and withdrawal. (elsevier.com)
  • Taken together, these results demonstrate the involvement of different purinergic receptors and signaling in GC, and the pattern of expression changes in tumoral cells, and this change likely directs ATP and nucleotide signaling from antiproliferative effects in healthy tissues to proliferative effects in cancer. (frontiersin.org)
  • 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)
  • 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)
  • 100 nM), or the purinoceptor antagonists 8- phenyltheophyline (P1 receptors) or suramin (P2 receptors). (edu.au)
  • Both of these metabotropic receptors are distinguished by their reactivity to specific activators. (wikipedia.org)
  • 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)
  • Babich V, Vadnagara K, Di Sole F (2015) Dual effect of adenosine a1 receptor activation on renal O2 consumption. (springer.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)
  • All of these are antiplatelet agents that block P2Y12 receptors. (wikipedia.org)
  • However, the use of antagonists for P2 receptors in clinical therapy, with the exception of P2Y12, is a great challenge. (bvsalud.org)
  • Despite this, P2Y12 receptor antagonists have a history of success and have been used in therapy for at least two decades to prevent thrombosis in patients at risk for myocardial infarctions. (bvsalud.org)
  • Furthermore clopidogrel, PLXNC1 a P2Y12 receptor 600734-02-9 supplier antagonist broadly prescribed to lessen the chance of coronary attack and heart stroke, inhibits bone tissue cell function and reduces trabecular bone tissue [18]. (onetownmanyvoices.com)
  • In this article, we report that purinergic signaling participates in the production and secretion of TSP-1. (pnas.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)
  • Purinergic signaling is important not only in short-term regulation of vascular tone but also in long-term regulation of vascular remodeling (i.e., vascular cell proliferation, migration, and death) [ 15 - 21 ]. (hindawi.com)
  • 1 - 4 Retinal blood flow is regulated primarily by the tone of resistance arterioles, which is influenced by a number of signaling molecules, including purinergic compounds released from the retinal tissue. (arvojournals.org)
  • 16 However, the anatomic basis for purinergic signaling during the relaxation of retinal arterioles is unknown. (arvojournals.org)
  • Elements of the purinergic signaling system are involved in many processes in health and disease conditions [3]. (thefreelibrary.com)
  • Only in 2006, ATP was finally recognized as a cotransmitter in both the peripheral and central nervous systems (CNS) [9, 10, 14], and the purinergic signaling was recognized as a system involved in many nonneuronal and neuronal mechanisms [12]. (thefreelibrary.com)
  • In this work, we studied in detail purinergic signaling in the gastric adenocarcinoma-derived cell lines: AGS, MKN-45, and MKN-74, and compared them to a nontumoral epithelial cell line: GES-1. (frontiersin.org)
  • Evidences show that purinergic signaling is involved in processes associated with health and disease, including noncommunicable, neurological, and degenerative diseases. (hindawi.com)
  • 2] Signaling at Purinergic P2X Receptors. (axonmedchem.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)
  • 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)
  • 1] Purinergic signaling in the nervous system: an overview. (axonmedchem.com)
  • Adenosine receptors are known to transactivate Trk receptors, leading us to examine the effects of manipulating of adenosine receptor signaling on Trk signaling and excitotoxic sensitivity. (northwestern.edu)
  • Conversely, activating adenosine A 2a receptors in the absence of BDNF signaling makes motor neurons vulnerable to excitotoxic challenge. (northwestern.edu)
  • 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)
  • 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)
  • 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)
  • Both binding and functional assays support the allosteric interactions of amiloride analogues with A(3) receptors. (nih.gov)
  • Here we investigate the role of the A2a receptor by disrupting the gene in mice. (nih.gov)
  • SCH 58261 and ZM 241385 differentially prevent the motor effects of CGS 21680 in mice: evidence for a functional 'atypical' adenosine A(2A) receptor. (ac.be)
  • Adenosine A2A receptor knockout mice are partially protected against drug-induced catalepsy. (ac.be)
  • Because A 2A antagonists were expected to be more selective for reversing the effects of the D 2 antagonist haloperidol, A 2A receptor knockout (A 2A RKO) mice were also assessed. (elsevier.com)
  • Meanwhile, the related adenosine A2A receptor may impair memory, as knocking it out improved the performance of both wild-type and AD transgenic mice in behavioral tasks. (alzforum.org)
  • The volume of cerebral infarction, as well as the associated neurological deficit induced by transient filament occlusion of the middle cerebral artery, were significantly attenuated in A 2A receptor knock-out mice. (jneurosci.org)
  • This neuroprotective phenotype of A 2A receptor-deficient mice was observed in different genetic backgrounds, confirming A 2A receptor disruption as its cause. (jneurosci.org)
  • Up 4 A structurally contains both purine and pyrimidine moieties, which activate purinergic receptors. (hindawi.com)
  • Then, ATP will activate purinergic P2 receptors present in sensory nerve endings, the iris, the ciliary body, or other tissues surrounding the anterior chamber of the eye to produce uveitis/endophthalmitis. (ucm.es)
  • There are currently four types of adenosine receptors found in the heart. (wikipedia.org)
  • Within the field of purinergic signalling, these receptors have been implicated in learning and memory, locomotor and feeding behavior, and sleep. (wikipedia.org)
  • thus, in a matter of years, we will have an evolution in the field of purinergic therapy. (bvsalud.org)
  • 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)
  • The present study was designed to determine whether P1 adenosine receptor ligands affected disease progression in a transgenic model of ALS. (elsevier.com)
  • The cannabinoid CB(1) receptor-mediated modulation of γ-aminobutyric acid (GABA) release from inhibitory interneurons is important for the integrity of hippocampal-dependent spatial memory. (strath.ac.uk)
  • Therefore, a complete understanding of purinergic system could potentially unveil possible markers or relevant pathways for pathological processes, mainly related to human degeneration. (thefreelibrary.com)
  • In contrast to the adenosine A 2 receptor agonist 5′-N-ethylcarboxamidoadenosine, nucleotide analogues had no discernible effect on cytosolic adenosine 3′,5′-cyclic monophosphate levels or adenylyl cyclase activity. (elsevier.com)
  • This study demonstrates that nucleotide receptors in this model of renal epithelium initiate distinct regulation of Na-K-Cl cotransport. (elsevier.com)
  • Launch Purinergic receptors are categorized as P1 adenosine and P2 ATP receptors predicated on their selectivity for adenosine and nucleotide agonists. (eaap2017.org)
  • It is believed that ATP functions as a pronociceptive neurotransmitter, acting at specific P2X and P2Y receptors in a systemized manner, which ultimately (as a response to noxious stimuli) serve to initiate and sustain heightened states of neuronal excitability. (wikipedia.org)
  • 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)
  • Although preliminary, these results indicate that purinergic receptors are putative pharmacological targets that should be further explored in future studies. (biomedcentral.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)
  • 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)
  • 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)
  • The regulation of vascular tone in the endothelium of blood vessels is mediated by purinergic signalling. (wikipedia.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)
  • 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)
  • Currently, many research groups and pharmaceutical companies are working on the development of specific antagonist molecules for each receptor subtype that could be used as new medicines to treat their respective disorders. (bvsalud.org)