Receptor, Adenosine A2A
Receptor, Adenosine A1
Receptor, Adenosine A3
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.
Receptor, Adenosine A2B
Adenosine A2 Receptor Agonists
Receptors, Adenosine A2
A purine nucleoside that has hypoxanthine linked by the N9 nitrogen to the C1 carbon of ribose. It is an intermediate in the degradation of purines and purine nucleosides to uric acid and in pathways of purine salvage. It also occurs in the anticodon of certain transfer RNA molecules. (Dorland, 28th ed)
Receptors, Purinergic P1
Adenosine A2 Receptor Antagonists
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.
Adenosine A1 Receptor Antagonists
Purinergic P1 Receptor Antagonists
Adenosine A3 Receptor Antagonists
Serotonin Receptor Agonists
Dose-Response Relationship, Drug
Serotonin 5-HT1 Receptor Agonists
Nucleic Acid Conformation
Serotonin 5-HT2 Receptor Agonists
Molecular Sequence Data
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
3,7-Dimethylxanthine. The principle alkaloid in Theobroma cacao (the cacao bean) and other plants. A xanthine alkaloid that is used as a bronchodilator and as a vasodilator. It has a weaker diuretic activity than THEOPHYLLINE and is also a less powerful stimulant of smooth muscle. It has practically no stimulant effect on the central nervous system. It was formerly used as a diuretic and in the treatment of angina pectoris and hypertension. (From Martindale, The Extra Pharmacopoeia, 30th ed, pp1318-9)
Cannabinoid Receptor Agonists
Serotonin 5-HT4 Receptor Agonists
Adrenergic alpha-2 Receptor 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.
Receptors, Purinergic P2
Receptors, Opioid, kappa
Receptors, Dopamine D2
Nucleoside Transport Proteins
Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.
The 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.
Receptors, Opioid, mu
A GAMMA-AMINOBUTYRIC ACID derivative that is a specific agonist of GABA-B RECEPTORS. It is used in the treatment of MUSCLE SPASTICITY, especially that due to SPINAL CORD INJURIES. Its therapeutic effects result from actions at spinal and supraspinal sites, generally the reduction of excitatory transmission.
Receptors, Dopamine D1
Receptors, Opioid, delta
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.
Drugs that bind to and activate nicotinic cholinergic receptors (RECEPTORS, NICOTINIC). Nicotinic agonists act at postganglionic nicotinic receptors, at neuroeffector junctions in the peripheral nervous system, and at nicotinic receptors in the central nervous system. Agents that function as neuromuscular depolarizing blocking agents are included here because they activate nicotinic receptors, although they are used clinically to block nicotinic transmission.
Purinergic P2 Receptor Antagonists
Purinergic P2Y Receptor Agonists
8-Bromo Cyclic Adenosine Monophosphate
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.
Rats, Inbred Strains
Adrenergic alpha-1 Receptor Agonists
A methylxanthine naturally occurring in some beverages and also used as a pharmacological agent. Caffeine's most notable pharmacological effect is as a central nervous system stimulant, increasing alertness and producing agitation. It also relaxes SMOOTH MUSCLE, stimulates CARDIAC MUSCLE, stimulates DIURESIS, and appears to be useful in the treatment of some types of headache. Several cellular actions of caffeine have been observed, but it is not entirely clear how each contributes to its pharmacological profile. Among the most important are inhibition of cyclic nucleotide PHOSPHODIESTERASES, antagonism of ADENOSINE RECEPTORS, and modulation of intracellular calcium handling.
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.
Cyclic AMP-Dependent Protein Kinases
A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)
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.
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.
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.
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.
Disease Models, Animal
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)
The voltage differences across a membrane. For cellular membranes they are computed by subtracting the voltage measured outside the membrane from the voltage measured inside the membrane. They result from differences of inside versus outside concentration of potassium, sodium, chloride, and other ions across cells' or ORGANELLES membranes. For excitable cells, the resting membrane potentials range between -30 and -100 millivolts. Physical, chemical, or electrical stimuli can make a membrane potential more negative (hyperpolarization), or less negative (depolarization).
The increase in a measurable parameter of a PHYSIOLOGICAL PROCESS, including cellular, microbial, and plant; immunological, cardiovascular, respiratory, reproductive, urinary, digestive, neural, musculoskeletal, ocular, and skin physiological processes; or METABOLIC PROCESS, including enzymatic and other pharmacological processes, by a drug or other chemical.
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.
Purinergic P2X Receptor Agonists
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.
Receptor, Cannabinoid, CB1
The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.
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.
Regulatory proteins that act as molecular switches. They control a wide range of biological processes including: receptor signaling, intracellular signal transduction pathways, and protein synthesis. Their activity is regulated by factors that control their ability to bind to and hydrolyze GTP to GDP. EC 3.6.1.-.
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.
Striped GRAY MATTER and WHITE MATTER consisting of the NEOSTRIATUM and paleostriatum (GLOBUS PALLIDUS). It is located in front of and lateral to the THALAMUS in each cerebral hemisphere. The gray substance is made up of the CAUDATE NUCLEUS and the lentiform nucleus (the latter consisting of the GLOBUS PALLIDUS and PUTAMEN). The WHITE MATTER is the INTERNAL CAPSULE.
Enkephalin, D-Penicillamine (2,5)-
Cell surface receptors that bind glucagon with high affinity and trigger intracellular changes which influence the behavior of cells. Activation of glucagon receptors causes a variety of effects; the best understood is the initiation of a complex enzymatic cascade in the liver which ultimately increases the availability of glucose to body organs.
Receptors, Adrenergic, beta
Receptor, Cannabinoid, CB2
Serotonin 5-HT3 Receptor Agonists
Adenosine A2A receptor
"Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ... adenosine (YT-146), a selective adenosine A2 receptor agonist, involve the opening of glibenclamide-sensitive K+ channels". ... "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ... As a result, Adenosine receptor A2A decreases activity in the Dopamine D2 receptors. The adenosine A2A receptor has also been ...
... which triggers intracellular signal transduction via both adenosine A1 and A2 receptors[disambiguation needed], and that the ... expression of sulfonylurea receptor 2B in dermal papilla cells might play a role in the production of adenosine. Minoxidil ... Moreover, minoxidil contains a nitric oxide moiety and may act as a nitric oxide agonist. This may cause follicles in the ... Minoxidil is an adenosine 5'-triphosphate-sensitive potassium channel opener, causing hyperpolarization of cell membranes. ...
Adenosine A1 receptor
The adenosine A1 receptor is one member of the adenosine receptor group of G protein-coupled receptors with adenosine as ... Activation of the adenosine A1 receptor by an agonist causes binding of Gi1/2/3 or Go protein. Binding of Gi1/2/3 causes an ... Caffeine may reduce cerebral blood flow in premature infants, it is presumed by blocking vascular A2 ARs. Thus, it may prove ... A1 receptors are also present in smooth muscle throughout the vascular system. The adenosine A1 receptor has been found to be ...
"Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ... This is a valuable guide to design potential 5HT1D receptor agonists. When sumatriptan binds there is major conformational ... 5-hydroxytryptamine (serotonin) receptor 1D, also known as HTR1D, is a 5-HT receptor, but also denotes the human gene encoding ... Goadsby, P.J., Serotonin 5-HT1B/1D receptor agonists in migraine - Comparative pharmacology and its therapeutic implications. ...
The A1 receptors couple to Gi/o and decreases cAMP levels, while the A2 adenosine receptors couple to Gs, which stimulates ... Nakav S, Chaimovitz C, Sufaro Y (2008). Bozza P (ed.). "Anti-Inflammatory Preconditioning by Agonists of Adenosine A1 Receptor ... All adenosine receptor subtypes (A1, A2A, A2B, and A3) are G-protein-coupled receptors. The four receptor subtypes are further ... Cellular signaling by adenosine occurs through four known adenosine receptor subtypes (A1, A2A, A2B, and A3). Extracellular ...
1992). "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor.". Genomics ... highly potent 5-HT1D receptor agonist.". Journal of medicinal chemistry 42 (3): 526-31. PMID 9986723. doi:10.1021/jm9805945. ... 5-HT1D receptor (5-hidroksitriptaminski (serotoninski) receptor 1D, HTR1D) je 5-HT receptor. On je kodiran istoimenim genom. ... Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A • ...
Adenosine A3 receptor
Cordeaux Y, Briddon SJ, Alexander SP, Kellam B, Hill SJ (March 2008). "Agonist-occupied A3 adenosine receptors exist within ... 1999). "Cardiac myocytes rendered ischemia resistant by expressing the human adenosine A1 or A3 receptor". FASEB J. 12 (15): ... 1997). "Adenosine inhibits neutrophil degranulation in activated human whole blood: involvement of adenosine A2 and A3 ... a novel specific adenosine A(3) receptor antagonist with adenosine A(3) receptor agonists both in vitro and in vivo". Eur. J. ...
Adenosine A2A receptor antagonist
... the therapeutic potential for both agonists and antagonists of the adenosine receptors was highlighted for A2 receptors, and in ... Adenosine A1-A2A receptor heteromers: new targets for caffeine in the brain. Frontiers in Bioscience. Volume 13. Pages 2391- ... Adenosine A2A receptor antagonists are a class of drugs that blocks adenosine at the adenosine A2A receptor. Notable adenosine ... In order to be able to characterize the function of adenosine A2 receptors, potent and selective A2-receptor antagonists were ...
Adenozinski A2A receptor
1992). "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor.". Genomics ... 1992). "Vasodilatory effects of adenosine A2 receptor agonists CGS 21680 and CGS 22492 in human vasculature.". Eur. J. ... "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics 11 (1): ... a selective adenosine A2 receptor agonist, involve the opening of glibenclamide-sensitive K+ channels". Eur. J. Pharmacol. 213 ...
... and reduces inflammation and innate immunity nonselective adenosine receptor antagonist, antagonizing A1, A2, and A3 receptors ... Daly JW, Jacobson KA, Ukena D (1987). "Adenosine receptors: development of selective agonists and antagonists". Prog Clin Biol ... or rather its adenosine-antagonist behavior). Mandal, Ananya. "Caffeine Pharmacology". Website Medical News. Archived from the ... asthma infant apnea Blocks the action of adenosine; an inhibitory neurotransmitter that induces sleep, contracts the smooth ...
Adenozinski A3 receptor - Википедија, слободна енциклопедија
2002). „A3 adenosine receptors in human astrocytoma cells: agonist-mediated desensitization, internalization, and down- ... 1999). „Cardiac myocytes rendered ischemia resistant by expressing the human adenosine A1 or A3 receptor.". FASEB J. 12 (15): ... 1997). „Adenosine inhibits neutrophil degranulation in activated human whole blood: involvement of adenosine A2 and A3 ... a novel ligand that demonstrates both adenosine A(2A) receptor agonist and adenosine A(3) receptor antagonist activity". ...
Molecular and epigenetic mechanisms of alcoholism
Katsura, M., Shibasaki, M., Hayashida, S., Torigoe, F., Tsujimura, A., Ohkuma, S. (2006) Increase in expression of a1 and a2/d1 ... BDNF binds TrkB receptors whose subsequent activation results in dimerization and autophosphorylation of the receptor. In its ... Funk, C.K. and Koob, G.F. (2007). A CRF2 agonist administered into the central nucleus of the amygdala decreases ethanol self- ... Pandey, S.C., Roy, A., Zhang, H. (2003). The decreased phosphorylation of cyclic adenosine monophosphate (cAMP) response ...
TP (TXA2). *Agonists: Carbocyclic thromboxane A2. *I-BOP. *Thromboxane A2 ... All of the prostanoid receptors are G protein-coupled receptors belonging to the Subfamily A14 of the rhodopsin-like receptor ... Prostaglandin receptors or prostanoid receptors represent a sub-class of cell surface membrane receptors that are regarded as ... Thromboxane A2 receptor. TP. TXA=PGH2,,PGD2=PGE2=PGF2α=PGI2. contractile. Gq alpha subunit. stimulates PLC & IP3; raises Ca ...
Cysteinyl leukotriene receptor 2
TP (TXA2). *Agonists: Carbocyclic thromboxane A2. *I-BOP. *Thromboxane A2 ... "Leukotriene Receptors: CysLT2". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ... leukotriene receptor activity. • cysteinyl leukotriene receptor activity. • galanin receptor activity. Cellular component. • ... Cysteinyl leukotriene receptor 2, also termed CYSLTR2, is a receptor for cysteinyl leukotrienes (LT) (see leukotrienes# ...
Prostaglandin DP2 receptor
TP (TXA2). *Agonists: Carbocyclic thromboxane A2. *I-BOP. *Thromboxane A2 ... with the C5a receptor, Formyl peptide receptor 1, and Formyl peptide receptor 2 receptors. DP2 has little or no such amino acid ... prostaglandin D receptor activity. • G-protein coupled receptor activity. • prostaglandin J receptor activity. • prostaglandin ... "DP2 receptor - Prostanoid receptors - IUPHAR/BPS Guide to PHARMACOLOGY". www.guidetopharmacology.org.. ...
പ്രോസ്റ്റാഗ്ലാൻഡിൻ EP3 റിസപ്റ്റർ - വിക്കിപീഡിയ
... a selective agonist for PGE2 receptor subtype 3". Journal of Leukocyte Biology. 68 (2): 187-93. PMID 10947062.. ... "Prostanoid Receptors: EP3". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ... TP (TXA2). *Agonists: Carbocyclic thromboxane A2. *I-BOP. *Thromboxane A2 ... prostaglandin receptor activity. • signal transducer activity. • prostaglandin E receptor activity. • protein binding. ...
It binds in a reversible fashion to the adenosine triphosphate (ATP) binding site of the receptor. For the signal to be ... Ephrins (A1, A2, A3, A4, A5, B1, B2, B3). *Erythropoietin (see here instead) ... Decoy receptors: LEVI-04 (p75NTR-Fc). PDGF. *Agonists: Becaplermin. *Platelet-derived growth factor (A, B, C, D) ... It is a receptor tyrosine kinase inhibitor, which acts on the epidermal growth factor receptor (EGFR). ...
Tyrosine kinase inhibitor
... and later gefitinib and erlotinib aiming at the EGF receptor. Sunitinib, an inhibitor of the receptors for FGF, PDGF and VEGF ... Ephrins (A1, A2, A3, A4, A5, B1, B2, B3). *Erythropoietin (see here instead) ... TKIs operate by four different mechanisms: they can compete with adenosine triphosphate (ATP), the phosphorylating entity, the ... Agonists: des(1-3)IGF-1. *Insulin-like growth factor-1 (somatomedin C) ...
Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist | PNAS
1991) Activity of N6-substituted 2-chloroadenosines at A1 and A2 adenosine receptors. J Med Chem 34(12):3388-3390. ... 2007) New fluorescent adenosine A1-receptor agonists that allow quantification of ligand-receptor interactions in microdomains ... A1 receptor agonists in a cardiac cell ischemia model involves cooperative activation of adenosine A2A and A2B receptors by ... 2010) A novel highly selective adenosine A1 receptor agonist VCP28 reduces ischemia injury in a cardiac cell line and ischemia- ...
A Category Names List - Drug Information Portal - U.S. National Library of Medicine
Adenosine A2 Receptor Agonists (4) • Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS. MeSH ... Adenosine A1 Receptor Antagonists (3) • Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS. MeSH ... Adenosine A2A Receptor Agonists (0) see Adenosine A2 Receptor Agonists. Adenosine A2A Receptor Antagonists (0) see Adenosine A2 ... Adenosine A2B Receptor Agonists (0) see Adenosine A2 Receptor Agonists. Adenosine A2B Receptor Antagonists (0) see Adenosine A2 ...
Selective Glycogen Synthase Kinase 3 Inhibitors Potentiate Insulin Activation of Glucose Transport and Utilization In Vitro and...
Selectivity against receptors was tested on the MDS "Profiling" panel, including adenosine A1; adrenergic (α1 and α2 ... including insulin receptor substrate 1 (IRS-1), by the tyrosine kinase activity of activated insulin receptor (6,7). Tyrosine- ... phospholipase A2 and C; and tyrosine hydroxylase (Celle LEvescault, France). ... nonselective and β1 and β2); calcium channel type L; dopamine D1 and D2; estrogen α; GABAA (agonist site and sodium channel); ...
Metabolic features of chronic fatigue syndrome | PNAS
2007) Adenosine A1 and A2 receptor agonists reduce endotoxin-induced cellular energy depletion and oedema formation in the lung ... 2011) P2 receptors and extracellular ATP: A novel homeostatic pathway in inflammation. Front Biosci (Schol Ed) 3:1443-1456. ... Plasma adenosine was decreased in females (Table 3, Females). Plasma adenosine is produced from ATP and ADP released from cell ... 2015) Bile acid-activated receptors, intestinal microbiota, and the treatment of metabolic disorders. Trends Mol Med 21(11):702 ...
Medicinal Chemistry and Therapeutic Potential of Agonists, Antagonists and Allosteric Modulators of A1 Adenosine Receptor:...
Keywords:A1 adenosine receptors, A1 AR agonists, partial agonists, antagonists and allosteric modulators, pharmacology of A1 AR ... Szentmiklosi AJ, Galajda Z, Cseppento Á, et al. The Janus face of adenosine: antiarrhythmic and proarrhythmic actions. Curr ... Keywords: A1 adenosine receptors, A1 AR agonists, partial agonists, antagonists and allosteric modulators, pharmacology of A1 ... A1 adenosine receptor agonists, antagonists, and allosteric modulators. In: ed, The Adenosine Receptors Springer. 2018; pp. 59- ...
Molecular probes for adenosine receptors - Patent # 5248770 - PatentGenius
These probes bind to A.sub.2 and A.sub.3 adenosine receptors and aid in quantifying and characterizing the receptors. The ... This application discloses probes for adenosine receptors which are functionalized congeners of the following compound: ##STR1# ... which are agonists for A-1 and A-2 adenosine receptors and the sensitivity for quantitativeanalysis of xanthine amine congeners ... the binding properties of the functionalized congener to the A-1 adenosine receptor site or the A-2 adenosine receptor, ...
Adenosine-5'-(N-ethylcarboxamide) - NECA Summary Report | CureHunter
A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity. ... Adenosine A2A Receptor (Adenosine A2A Receptors) 6. Pentylenetetrazole (Metrazol) 7. Adenosine A1 Receptor ... Subscribe to New Research on Adenosine-5-(N-ethylcarboxamide) A stable adenosine A1 and A2 receptor agonist. Experimentally, ... 05/01/1998 - "The effect of serotonergic agents was studied on the adenosine A2 receptor agonist NECA-induced catalepsy in mice ...
Renal Adenosine in Health and Disease | Springer for Research & Development
... renal function in healthy and diseased kidney is mediated by activation of the four types of P1 purinergic adenosine receptors ... Agmon Y, Dinour D, Brezis M (1993) Disparate effects of adenosine A1- and A2-receptor agonists on intrarenal blood flow. Am J ... Kim M, Chen SW, Park SW et al (2009) Kidney-specific reconstitution of the A1 adenosine receptor in A1 adenosine receptor ... Levens N, Beil M, Schulz R (1991) Intrarenal actions of the new adenosine agonist CGS 21680A, selective for the A2 receptor. J ...
Application # 2017/0143726. ADENOSINE RECEPTOR AGONISTS AND ANTAGONISTS TO MODULATE T CELL RESPONSES - Patents.com
A.sub.2a receptor antagonists in particular are provided to enhance imm ... Described are uses of A.sub.2a adenosine receptor antagonists and agonists to provide long term modulation of immune responses ... 1990) The adenosine/neutrophil paradox resolved: human neutrophils possess both A1 and A2 receptors that promote chemotaxis and ... partial agonists at the receptor. In certain instances, non-selective agonists are also useful. Nonselective adenosine receptor ...
Frontiers | Selective Antagonism of A1 Adenosinergic Receptors Strengthens the Neuromodulation of the Sensorimotor Network...
This study explored whether selective pharmacological antagonism of the adenosine A1 receptor subtype synergizes with ESS, ... We hypothesized that selective pharmacological antagonism of A1 receptors during ESS would produce facilitatory effects in ... We hypothesized that selective pharmacological antagonism of A1 receptors during ESS would produce facilitatory effects in ... We demonstrated that ESS combined with the blockage of A1 receptors increased the magnitude of the endogenous modulation and ...
JCI - Volume 87, Issue 5
... suggesting that ATP gamma S inhibition occurs independent of AVP and A1 adenosine receptors and of phospholipase A2 activity. ... Analysis of T cell receptor genes revealed identical rearrangements of T cell receptor beta chain genes, suggesting clonality ... The compound ATP gamma S inhibits agonist-stimulated adenylate cyclase activity in solubilized and in isobutylmethylxanthine ( ... ATP receptor regulation of adenylate cyclase and protein kinase C activity in cultured renal LLC-PK1 cells.. ...
Why Does Caffeine Delay Exercise-Induced Fatigue?
... hypothesis that intracerebroventricular CNS administration of the selective adenosine A1 and A2 receptor agonist NECA ... However, A2b and A3 receptors are relatively less active than A1 and A2a receptors under normal physiological conditions. If ... study to determine the effects of intracerebroventricular injection of caffeine and the adenosine A1 and A2 receptor agonist 5 ... CNS administration of the adenosine receptor agonist NECA inhibited treadmill run time to fatigue and spontaneous locomotor ...
JCI - ATP receptor regulation of adenylate cyclase and protein kinase C activity in cultured renal LLC-PK1 cells.
... suggesting that ATP gamma S inhibition occurs independent of AVP and A1 adenosine receptors and of phospholipase A2 activity. ... The compound ATP gamma S inhibits agonist-stimulated adenylate cyclase activity in solubilized and in isobutylmethylxanthine ( ... ATP receptor regulation of adenylate cyclase and protein kinase C activity in cultured renal LLC-PK1 cells.. R J Anderson, R ... The rank order potency of inhibition by ATP analogues suggests that a P2y type of ATP receptor is involved in this inhibition. ...
Would calcium or potassium channels be responsible for cardiac arrest produced by adenosine and ATP in the right atria of...
... an adenosine A1 receptor antagonist. Effects of adenosine A2 and A3 receptors agonists and antagonists were also investigated. ... a selective adenosine A1 receptor antagonist. The selective adenosine A2 and A3 receptors antagonists did not alter the ... Right atria of adult Wistar rats were used to evaluate the effects of adenosine, ATP and CPA (an adenosine A1 receptor agonist ... Adenosine A1 receptor activation by adenosine and ATP produces cardiac arrest in the right atrium of Wistar rats predominantly ...
EPO - T 0964/98 (Purines/MERRELL) of 22.1.2002
... is related to prodrugs of adenosine receptor ligands, in general, ie A1- as well as A2-adenosine receptor agonists and ... Document (4) describes in Table III the binding constants for 8-(phenylisopropyl)xanthines at A1- and A2-adenosine receptors. ... Since, according to Table 1 of the application in suit the IC50 adenosine A2 is higher than the IC50 adenosine A1 for racemic N ... As it is said in the application in suit that the claimed compounds provide a selective A1-adenosine receptor antagonistic ...
Repeated Dosing with Oral Allosteric Modulator of Adenosine A1 Receptor Produces Tolerance in Rats with Neuropathic Pain |...
Repeated administration of selective adenosine A1 and A2 receptor agonists in the spontaneously hypertensive rat: Tolerance ... The A1 receptor is primarily coupled to the Gi/o class of G proteins. Chronic activation of A1 receptors has been tested in ... Long-term exposure of PD 81,723, a well-studied A1 receptor modulator, down-regulates A1 receptors to a small degree. 32 ... functions controlled by adenosine receptors result in some undesirable side effects from direct adenosine receptor agonists, ...
WikiGenes - Adora1 - adenosine A1 receptor
... adenosine A1 receptor agonist) and 5-N-ethylcarboxamidoadenosine (NECA, adenosine A1/A2 receptor agonist) reduced, while N6-[2 ... Adenosine receptor subtypes and vasodilatation in rat skeletal muscle during systemic hypoxia: a role for A1 receptors. Bryan, ... an adenosine A1 receptor agonist .. *Activation of adenosine A1-receptor pathway induces edema formation in the pancreas of ... Adenosine activity was manipulated by microperfusing nephrons with adenosine A1 receptor blocker, A1-agonist, or 5- ...
Local Antinociceptive and Hyperalgesic Effects in the Formalin Test After Peripheral Administration of Adenosine Analogues in...
On the other hand adenosine analogues have been shown to possess antinociceptive effects after peripheral and intrathecal ... Adenosine administered to humans has been reported to induce pain after intravenous administration. ... the effect of peripheral administration of adenosine agonists with different affinities for the A1 and A2 adenosine receptors ... with high affinity for the A1 receptor, N-ethylcarboxamide-adenosine (NECA) with almost equal affinity for the A1 and A2 ...
WikiGenes - ADORA2A - adenosine A2a receptor
... a mixed adenosine A1 and A2 receptor agonist, nor CGS 21680, a selective adenosine A2A receptor agonist, affected nucleoside ... Adenosine A2A receptors in diffuse dermal fibrosis: pathogenic role in human dermal fibroblasts and in a murine model of ... Chlorofuryl-triazolo-quinazolinamine (CGS-15943; 1 micromol/L), an adenosine A1 and A2 receptor antagonist, and ... Effect of adenosine receptor agonists on release of the nucleoside analogue [3H]formycin B from cultured smooth muscle DDT1 MF- ...
Patients being sought for clinical trial treating weak respiratory muscles after spinal cord injury
Nantwi KD and Goshgarian HG (2002). Actions of specific adenosine receptor A1 and A2 agonists and antagonists in recovery of ... of adenosine A1 receptors by either endogenously released adenosine or the administration of selective receptor agonists causes ... Specific adenosine A1 and A2 agonists and antagonists were used in an electrophysiological study. 3. Our results demonstrate ... 2. The present study was designed to assess the relative contributions of adenosine A1 and A2 receptors in inducing functional ...
Adenosine A1 Receptor Antibody 55026-1-AP | Proteintech
Adenosine A1 Receptor antibody Rabbit Polyclonal from Proteintech validated in Western Blot (WB), Immunohistochemistry (IHC), ... antagonizing the activity of adenosine A2 receptor (PMID: 15539423). A number of selective agonists and antagonists of ... Adenosine A1 receptor (ADORA1, also known as A1AR) is one of four subtypes of adenosine receptors that belong to a superfamily ... Adenosine A1 Receptor Polyclonal antibody. Adenosine A1 Receptor Polyclonal Antibody for IHC, WB, ELISA. ...
Drug CategoriesBrowse DrugBank Categories - DrugBank
Adenosine A2 Receptor Agonists. Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS.. 4. 3. Details. ... Adenosine A1 Receptor Agonists. Not Available. 1. 0. Details. Adenosine A1 Receptor Antagonists. Compounds that bind to and ... Adenosine A2 Receptor Antagonists. Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.. 4. ... Adenosine. A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivativ... more. 11. 99. Details. ...
Activation of adenosine A<sub>1</sub> receptors underlies anticonvulsant effect of...
Adenosine A2 Receptor Agonists Medicine & Life Sciences * bicuculline methiodide Medicine & Life Sciences ... title = "Activation of adenosine A1 receptors underlies anticonvulsant effect of CGS21680",. abstract = "Focal injection of the ... These results indicate that the low affinity of CGS21680 for adenosine A1 receptors is sufficient to account for the ... These results indicate that the low affinity of CGS21680 for adenosine A1 receptors is sufficient to account for the ...
Protective effect of adenosine receptors against lipopolysaccharide-induced acute lung injury | Lung Cellular and Molecular...
Adenosine A1 and A2 receptor agonists reduce endotoxin-induced cellular energy depletion and oedema formation in the lung. Eur ... Comparison of the potency of adenosine as an agonist at human adenosine receptors expressed in Chinese hamster ovary cells. ... LPS treatment significantly decreased transcription of A1 and A2B receptors but not A2A and A3 receptors (Fig. 7). Adenosine ... qPCR analyses of adenosine receptor (A1, A2A, A2B, A3) mRNA expression from murine lung tissues at 6 h. A and C: LPS and LPS/ ...
US Patent Application for ORALLY ACTIVE A1 ADENOSINE RECEPTOR AGONISTS Patent Application (Application #20020091099 issued July...
... thioxa and azacycloalkyl substituted adenosine derivative and a method for using the composition as an A1 adenosine receptor ... lsqb;0004] There are at least two subtypes of adenosine receptors in the heart: A1 and A2. Each subtype effects different ... Justia Patents Adenosine Or DerivativeUS Patent Application for ORALLY ACTIVE A1 ADENOSINE RECEPTOR AGONISTS Patent Application ... there is no role for the A2 receptor in modulating the function of this channel. Stimulation of the adenosine A1 receptor ...
Caffeine Induces Dopamine and Glutamate Release in the Shell of the Nucleus Accumbens | Journal of Neuroscience
1989) Inhibition of nigrostriatal release of dopamine in the rat by adenosine receptor agonists: A1 receptor mediation. ... 1996) Adenosine A1 and A2 receptors modulate extracellular dopamine levels in rat striatum. Neurosci Lett 212:53-56. ... Because caffeine is a nonselective adenosine receptor antagonist, the selective adenosine A1 receptor antagonist CPT and the ... in particular adenosine A1 receptors and A2A receptors (Daly and Fredholm, 1998). In the striatum, adenosine plays an important ...
Pesquisa | Portal Regional da BVS
The adenosine A1 receptor-selective agonist, CHA, appeared most potent in this modulatory effect when compared to the A2- ... suggested A1 receptor activation by NECA and CGS-21680. The functional similarity between GABAB and adenosine A1, receptors ... Intrastriatal (IST) administration of adenosine A1-, A1 = A2-, and As-selective agonists, R(-)N6-(2-phenylisopropyl)adenosine ( ... 5. Accentuation by the A1- and A2-selective adenosine agonists was significantly attenuated by the A1-selective antagonist 8- ...
Adenosine A2A receptor - Wikipedia
"Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ... adenosine (YT-146), a selective adenosine A2 receptor agonist, involve the opening of glibenclamide-sensitive K+ channels". ... "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ... As a result, Adenosine receptor A2A decreases activity in the Dopamine D2 receptors. The adenosine A2A receptor has also been ...
Limitation of Infarct Size and No-Reflow by Intracoronary Adenosine Depends Critically on Dose and Duration | JACC:...
1992) The effects of intravenous infusions of selective adenosine A1-receptor and A2-receptor agonists on myocardial ... whereas high concentrations of adenosine limited neutrophil recruitment (via A2A and A2B receptors) (18). ... Lower local concentrations of adenosine have been noted to promote neutrophil recruitment (via the A1 and A3 adenosine receptor ... Adenosine bolus did not attenuate neutrophil influx into the no-reflow area, whereas adenosine infusion demonstrated a trend (p ...
Pesquisa | Portal Regional da BVS
Renal nerves do not influence the inhibition of renin release mediated by A1 adenosine receptors. In vivo, A2-receptor agonist ... RESULTS: Infusions of A1 and A2 agonists produced comparable hypotensive effects. During A1 agonist administration, the heart ... and A2 (2-hexynil-5-N-ethyl-carboxamido-adenosine) adenosine-receptor agonists were studied in two groups of anaesthetized ... agonist administration. Heart rate significantly decreased during A1 agonist infusion, but it did not change during A2 agonist ...
AntagonistAntagonistsSubtypesNECAStimulationInhibitionEffect of adenosineEndogenousAbstractModulationPhysiologicalPharmacologicalSubtypeNitric oxideSignal TransductionAdministration of adenosineDecreasesCaffeineLevels of adenosineProteinIntrathecalRelief of neuropathic painGPCRRole of adenosine receptorsLigandInhibitAntagonismHigh affinityA2aRMiceInhibitsVitroExtracellular adenosineAdenylate cyclaseCompoundsPotentAllosteric adenosine receptorDEAMINASESpecific receptorsIschemiaGlutamateNeuronsGPCRsSerotoninInhibitoryAdenylyl cyclase activityCCPANeuropathic painActivation of adenosineAnti-inflammatoryRegulationSelectivityHypoxiaMacrophagesEthylEffectsPurinergicResponsesDerivativesRadioligandClinical
- 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)
- 1. A method of enhancing an immune response in a host, comprising administering to the host an A.sub.2a receptor antagonist in combination or alternation with a checkpoint inhibitor. (patents.com)
- NECA was chosen for the study because caffeine is a nonselective adenosine receptor antagonist, and it is not known which of the four subtypes of adenosine receptors may be involved in an effect of caffeine on fatigue. (innovations-report.com)
- Right atria of adult Wistar rats were used to evaluate the effects of adenosine, ATP and CPA (an adenosine A1 receptor agonist), in the presence and absence of DPCPX, an adenosine A1 receptor antagonist. (ovid.com)
- The effects of adenosine, CPA and ATP were inhibited by DPCPX, a selective adenosine A1 receptor antagonist. (ovid.com)
- Theophylline** Theophylline is an adenosine receptor antagonist. (rutgers.edu)
- These effects could be reproduced by the administration of a selective adenosine A1 receptor antagonist but not by a selective adenosine A2A receptor antagonist. (jneurosci.org)
- Caffeine, the adenosine A1 antagonist 8-cyclopentyltheophylline (CPT), and the adenosine A2A antagonist 5-amino-7-(2-phenylethyl)2-(2-furyl)-pyrazolo-[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine (SCH 58261) were administered intraperitoneally in all experiments. (jneurosci.org)
- The encoded protein (the A2A receptor) is abundant in basal ganglia, vasculature, T lymphocytes, and platelets and it is a major target of caffeine, which is a competitive antagonist of this protein. (wikipedia.org)
- R-PIA inhibition (0.01 æM = 141.97 ± 15.79 vs control = 244.77 ± 13.79 ng/mg t.w.) of PRL release was blocked by 1 æM cyclopentyltheophylline, a specific A1 receptor antagonist (1 æM = 212.360 ± 26.560 ng/mg t.w.), whereas cyclopentyltheophylline alone (0.01, 0.1, 1 æM) had no effect. (bvsalud.org)
- Tbe 2',3'-dideoxy analogue of the potent A\(_1\) receptor agonist, N\(^6\)-cyclohexyladenosine (CHA), was synthesized as a potential antagonist for the A\(_1\) adenosine receptor. (uni-wuerzburg.de)
- Competition of 2-alkynyladenosines 2a-d for the antagonist radioligand [\(^3\)H]DPCPX and for the agonist [\(^3\)H]CCPA gave K\(_i\) values in the nanomolar range, and the compounds showed moderate A\(_2\) selectivity. (uni-wuerzburg.de)
- Rabbits were pretreated topically with the moderately selective adenosine A 1 antagonist 8-(p-sulfophenyl)theophyline (8-SPT) or the adenosine A 2 antagonist 3,7-dimethyl-l-propargylxanthine (DMPX). (arvojournals.org)
- CADO inhibition of barium currents was also sensitive to the A1 antagonist 1,3-dipropyl-8-cyclopentylxanthine (DPCPX). (gotomydoctor.com)
- Consistent with a role for CXCR7 in cell survival and adhesion, a specific, high affinity small molecule antagonist to CXCR7 impedes in vivo tumor growth in animal models, validating this new receptor as a target for development of novel cancer therapeutics. (rupress.org)
- Xanthine amine congener, a specific A1 receptor antagonist, failed to reverse the suppression by adenosine of tumor necrosis factor release, whereas CGS15943A, an A2 receptor antagonist, did reverse suppression by adenosine and 5-n-ethylcarboxamidadenosine. (duke.edu)
- Doxofylline does not demonstrate direct inhibition of any histone deacetylase (HDAC) enzymes or known PDE enzyme isoforms and did not act as an antagonist at A2 or A2 receptors. (drugbank.ca)
- DPCPX is a potent and selective A1 adenosine receptor antagonist, both in vitro and in vivo. (emmx.com)
- 1,3-Dipropyl-8-phenylxanthine is a selective A1 adenosine antagonist. (emmx.com)
- PSB 36 is a Potent and selective A1 adenosine receptor antagonist with binding affinities of 0.12, 187, 552, 6500 and 2300 nM for rA1, hA2B, rA2A, rA3 and hA3 receptors respectively. (emmx.com)
- SLV 320 is a potent and selective adenosine A1 receptor antagonist (Ki values are 1, 200, 398 and 3981 nM at human A1, A3, A2A and A2B receptors respectively). (emmx.com)
- PSB 1115 is a highly selective, water-soluble, human A2B adenosine receptor antagonist. (emmx.com)
- NMDA receptor antagonist. (emmx.com)
- The non-selective adenosine receptor agonist (adenosine-5′N-ethylcarboxamide, NECA) and the A2AR agonist (CGS21680) stimulated cell proliferation by up to 20-40% which was attenuated by A2B (PSB603 and MRS1754) and A2A (SCH442416) receptor selective antagonists but not by the A1 receptor antagonist (PSB36). (cf.ac.uk)
- Antagonist-agonist combinations as therapies for heroin addiction : back to the future? (isni.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)
- Caffeine is a competitive antagonist at adenosine receptors. (kzeng.info)
- In competition with antagonist radioligand biphasic curves were observed for agonists. (biomedsearch.com)
- E)-8-(3-Chlorostyryl)-1,3,7-trimethylxanthine, a caffeine derivative acting both as antagonist of adenosine A2A receptors and as inhibitor of MAO-B. (harvard.edu)
- A2A antagonist prevents dopamine agonist-induced motor complications in animal models of Parkinson's disease. (harvard.edu)
- The pre-treatment of mice with DPCPX (2mg/kg, i.p., a selective adenosine A1 receptor antagonist) or ZM241385 (1mg/kg, i.p., a selective adenosine A2A receptor antagonist) did not prevent the effect of fluoxetine (32 mg/kg, i.p., a preferential serotonin reuptake inhibitor) in the FST. (unboundmedicine.com)
- 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. (uniroma1.it)
- 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. (uniroma1.it)
- 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. (uniroma1.it)
- This review provides an overview of the medicinal chemistry and therapeutic potential of various agonists/partial agonists, antagonists and allosteric modulators of A1 AR, with a particular emphasis on their current status and future perspectives in clinical settings. (eurekaselect.com)
- A1 adenosine receptors, A1 AR agonists, partial agonists, antagonists and allosteric modulators, pharmacology of A1 AR, structure- activity relationships of A1 AR. (eurekaselect.com)
- A1 adenosine receptor agonists, antagonists, and allosteric modulators. (eurekaselect.com)
- These studies support the future investigation of the optimal dosage, methods of delivery, and systemic effects of the synergistic application of A1 antagonists and spinal stimulation in the intact and injured spinal cord. (frontiersin.org)
- Described are uses of A.sub.2a adenosine receptor antagonists and agonists to provide long term modulation of immune responses. (patents.com)
- A.sub.2a receptor antagonists in particular are provided to enhance immune responses by reducing T-cell mediated tolerance to antigenic stimuli and agonists are provided to enhance effectiveness of immunosuppressive agents. (patents.com)
- 0004] This application relates to uses of A.sub.2a adenosine receptor agonists and antagonists to modulate T-cell mediated tolerance to antigenic stimuli. (patents.com)
- Effects of adenosine A2 and A3 receptors agonists and antagonists were also investigated. (ovid.com)
- The selective adenosine A2 and A3 receptors antagonists did not alter the chronotropic response of adenosine. (ovid.com)
- Behavioral effects of A1- and A2-selective adenosine agonists and antagonists: evidence for synergism and antagonism. (nih.gov)
- Older research on adenosine receptor function, and non-selective adenosine receptor antagonists such as aminophylline, focused mainly on the role of adenosine receptors in the heart, and led to several randomized controlled trials using these receptor antagonists to treat bradyasystolic arrest. (wikipedia.org)
- Evidence for the involvement of A1 (inhibitory) and A2 (stimulatory) adenosine receptors in regulating cell growth of these tumor cells was obtained through plating efficiency studies based on the relative potency of adenosine agonists and antagonists. (nus.edu.sg)
- These enhancing effects of agonists were blocked by selective antagonists, 8-cyclophenyl-1,3-dipropylxanthine (DPCPX) and 9-chloro-2-(2-furyl)[1,2,4]triazolo[1,5-c]quinalzolin-5-amine (CGS15943), respectively. (edu.au)
- Modulation of paracetamol antinociception by caffeine and by selective adenosine A2 receptor antagonists in mice. (semanticscholar.org)
- This study suggests an unappreciated "man-made" immunological pathogenesis whereby consumption of the food-, beverage-, and medication-derived adenosine receptor antagonists may modify an individual's inflammatory status and lead to excessive organ damage during acute inflammation. (jimmunol.org)
- To investigate the mechanisms involved in cannabidiol (CBD)-induced neuroprotection in hypoxic-ischemic (HI) immature brain, forebrain slices from newborn mice underwent oxygen and glucose deprivation in the presence of vehicle, or CBD alone or with selective antagonists of cannabinoid CB(1) and CB(2), and adenosine A(1) and A(2) receptors. (unboundmedicine.com)
- 2 Although selective agonists A 2 were shown to have no antinociceptive effect, A 1 receptors have been clearly identified to produce antinociception in the spinal cord by using selective agonists and antagonists. (asahq.org)
- 11,14,15 Thus, the effects of adenosine or T62 after nerve injury are totally abolished by destruction of noradrenergic terminals or administration of α 2 -adrenoceptor antagonists. (asahq.org)
- 2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists. (nih.gov)
- In this study we developed a refined pharmacophore model for antagonists of the human adenosine A1 receptor, based on features of known pyrimidine and purine derivatives. (nih.gov)
- Neuroprotection by caffeine and more specific A2A receptor antagonists in animal models of Parkinson's disease. (harvard.edu)
- Monoamine oxidase B inhibition and neuroprotection: studies on selective adenosine A2A receptor antagonists. (harvard.edu)
- Adenosine A2A antagonists as neurotherapeutics: crossing the bridge. (harvard.edu)
- Therapeutic potential of adenosine A(2A) receptor antagonists in Parkinson's disease. (harvard.edu)
- Adenosine A2A receptor antagonists for Parkinson's disease: rationale, therapeutic potential and clinical experience. (harvard.edu)
- Adenosine receptor antagonists alter the stability of human epileptic GABAA receptors. (uniroma1.it)
- Influences of different adenosine receptor subtypes on catalepsy in mice. (nih.gov)
- Adenosine A1 receptor (ADORA1, also known as A1AR) is one of four subtypes of adenosine receptors that belong to a superfamily of protein G-coupled receptors. (ptglab.com)
- The gene encodes a protein which is one of several receptor subtypes for adenosine. (wikipedia.org)
- There are at least two subtypes of adenosine receptors in the heart: A1 and A2. (justia.com)
- First, a detection method for each of the adenosine receptor subtypes was developed using reverse transcriptase polymerase chain reaction (RT-PCR). (edu.au)
- Optimization of conditions for multiplex PCR was conducted, allowing it to detect several adenosine receptor subtypes simultaneously, and it was proven to be partially successful. (edu.au)
- Treatment of cells with selective adenosine analogues for the A1 and A2A subtypes, 2-chloro-N6-cyclopentyladenosine (CCPA, 100 nM) and 2-[4-(2-carboxylethyl)phenylamino]-5'-N-ethylcarboxamido (CGS21680, 30 and 100 nM), respectively, enhanced the differentiation induced by serum deprivation at day 7 by approximately 60% and 70%, respectively. (edu.au)
- 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)
- Adenosine which has four subtypes of A1, A2a, A2b and A3, is an endogenous protein nucleotide. (biomedcentral.com)
- Four subtypes of adenosine receptors (ARs) have been identified among vertebrates so far ( A1 , A2A , A2B and A3 ). (axonmedchem.com)
- As a result, stimulation of A1 and A3 subtypes in general results in neurotransmission through the inhibition of adenylate cyclase and phospholipase C , whereas stimulation of the A2 subtypes leads to enhanced neurotransmission. (axonmedchem.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 all human subtypes were stably transfected into Chinese hamster ovary (CHO) cells in order to be able to study their pharmacological profile in an identical cellular background utilizing radioligand binding studies (A1, A2A, A3) or adenylyl cyclase activity assays (A2B). (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)
- 1 Both A 1 andA 2 subtypes of adenosine receptors are present in the substantia gelationosa. (asahq.org)
- Subtype-specific functions have been identified for many genetically defined receptor subtypes, but several pharmacologically defined receptor responses still await clarification of the roles played by different receptor subtypes. (guwsmedical.info)
- Closely related receptor subtypes may have very different anatomical distribution patterns and opposing functional effects in the cardiovascular system. (guwsmedical.info)
- The researchers' hypothesis is the foundation of a new study to determine the effects of intracerebroventricular injection of caffeine and the adenosine A1 and A2 receptor agonist 5'-N-ethylcarboxamidoadenosine (NECA) on treadmill run time to fatigue in rats. (innovations-report.com)
- The drugs chosen were, R-phenylisopropyl-adenosine (R-PIA) with high affinity for the A1 receptor, N-ethylcarboxamide-adenosine (NECA) with almost equal affinity for the A1 and A2 receptor and 2-(2-aminoethylamino)-carbonylethylphenylethylamino-adenosin e (APEC) with high affinity for the A2 receptor. (nih.gov)
- To test this hypothesis, we examined the effects of pre- and posttreatment of adenosine and 5′- N -ethylcarboxamidoadenosine (NECA), a nonselective stable AR agonist, on LPS-induced lung injury. (physiology.org)
- Mice were given vehicle or LPS intratracheally followed by adenosine, NECA, or vehicle instilled via the internal jugular vein. (physiology.org)
- Importantly, posttreatment with adenosine or NECA recovers lung vascular barrier and reduces inflammation induced by LPS challenge. (physiology.org)
- A crystal structure of the A2A receptor bound with the agonist NECA and a G protein-mimic has been published in 2016 (PDB code: 5g53). (wikipedia.org)
- The adenosine agonists, 5'-N-(ethyl)carboxamido-adenosine (NECA), cyclohexyladenosine, cyclopentyladenosine, 2-chloroadenosine and R- and S-phenylisopropyladenosine (R- and S-PIA), protected animals against seizures in a dose-dependent, and extremely potent manner. (elsevier.com)
- Quantitative autoradiographic analysis of the distribution of tritiated adenosine agonists 30 min after microinjection in the PPC reveals that [ 3 H]NECA diffuses to a significantly greater extent than R-[ 3 H]PIA, which may contribute to the relatively greater potency of the former compound in suppressing bicuculline methiodide-induced seizures. (elsevier.com)
- Binding of [\(^3\)H]NECA to A\(_2\) receptors of rat striatal membranes was inhibited by compounds 2a-d with K\(_i\) values ranging from 2.8 to 16.4 nM. (uni-wuerzburg.de)
- that a human neuroblastoma cell line, IMR32, could be induced to differentiate into cells that have a more neuronal morphology, with long neurites, by an adenosine receptor agonist 5'-N-ethylcarboxamideadenosine (NECA) 2. (edu.au)
- Adenosine and NECA stimulated a twofold increase in chromogranin A secretion in BON-1 cells. (cf.ac.uk)
- For A2A adenosine receptors CGS 21680 (2-[p-(2-carboxyethyl)phenylethylamino]-5'-N-ethylcarboxamidoadeno sine) and N-ethylcarboxamidoadenosine (NECA) were found to be the most potent agonists followed by R- and S-PIA with minor stereoselectivity. (biomedsearch.com)
- NECA was the most potent agonist with an EC50-value of 2.3 microM whereas all other compounds tested were active at concentrations in the high micromolar range. (biomedsearch.com)
- The A3 receptor was characterized utilizing the nonselective agonist [3H]NECA. (biomedsearch.com)
- Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS. (nih.gov)
- Although DPCPX significantly increased the yield of repetitive stimulation in intact spinal cords, the effects of A1 antagonism on motor evoked responses after an acute spinal transection was not detected. (frontiersin.org)
- Now, a team of researchers from the University of South Carolina has hypothesized that the blockade of adenosine receptors by caffeine may be the most likely mechanism of CNS stimulation and delayed fatigue. (innovations-report.com)
- Theophylline-induced respiratory recovery following cervical spinal cord hemisection is augmented by serotonin 2 receptor stimulation. (rutgers.edu)
- The present study was designed to specifically determine if concurrent stimulation of 5-HT2 receptors may enhance motor recovery induced by theophylline alone. (rutgers.edu)
- Stimulation of the A1 adenosine receptor induces two distinct physiological responses. (justia.com)
- Stimulation of the adenosine A1 receptor accordingly shortens the duration and decreases the amplitude of the action potential of AV nodal cells and subsequently prolongs the refractory period of the cells. (justia.com)
- These results demonstrate that adenosine receptor stimulation differentially modulates the LPS-induced production of IL-10, TNF-α, and NO in vitro and in vivo. (utmb.edu)
- To investigate the role of A 2A adenosine receptors in adaptive responses to chronic intermittent dopamine receptor stimulation, we compared the behavioral sensitization elicited by repeated l -DOPA treatment in hemiparkinsonian wild-type (WT) and A 2A adenosine receptor knock-out (A 2A KO) mice. (jneurosci.org)
- Unlike IMR32, PC12 cells, a rat adrenal pheochromocytoma cell line, resembling human neuroblastoma cell lines and also expressing the A2 subtype of adenosine receptors, was shown not to differentiate under stimulation of the A2A subtype of adenosine receptors 3. (edu.au)
- Pharmacological stimulation by an A2AR agonist results in the inhibition of proliferation ( 4 ), cytokine production ( 5 ), the cytotoxicity of T cells ( 6 ), and the activation of monocytes ( 7 ) and granulocytes ( 8 ). (jimmunol.org)
- In contrast to nitric oxide and similar to angiotensin II, sympathoadrenergic stimulation by phenylephrine or by baroreflex activation only slightly enhanced MR [ A2 ]. (uni-freiburg.de)
- Besides, 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. (axonmedchem.com)
- 3-5 The spinal administration of adenosine itself does not produce analgesia in normal rats to acute noxious stimulation. (asahq.org)
- 7 A common problem with administration of direct agonists, such as adenosine itself, is adverse effects caused by stimulation of all receptors, not just those involved in the therapeutic effect. (asahq.org)
- The EC50 of each derivative is shown in Table I. Also shown in Table I is the ability of each derivative to stimulate cAMP production in PC 12 cells, a function of agonist stimulation of adenosine A 2 receptors. (blogspot.in)
- Adenosine A2A receptors in neuroadaptation to repeated dopaminergic stimulation: implications for the treatment of dyskinesias in Parkinson's disease. (harvard.edu)
- Adenosine A2A receptor stimulation potentiates nitric oxide release by activated microglia. (harvard.edu)
- In this study, we demonstrate that, following TLR stimulation, macrophages upregulate the adenosine 2b receptor (A2bR) to enhance their sensitivity to immunosuppressive extracellular adenosine. (jimmunol.org)
- After TLR stimulation, macrophages alter their metabolism and release low levels of ATP, which is rapidly converted into immunosuppressive adenosine via CD39-mediated hydrolysis. (jimmunol.org)
- Background and purpose: Desensitization of somatodendritic 5-HT1A receptors is involved in the mechanism of action of several antidepressants, but the rapidity of this effect and the amount of agonist stimulation needed are unclear. (cancer-colorectal.com)
- Insulin indirectly relieves GS inhibition ( 4 , 5 ) through a signaling cascade beginning with phosphorylation of substrates, including insulin receptor substrate 1 (IRS-1), by the tyrosine kinase activity of activated insulin receptor ( 6 , 7 ). (diabetesjournals.org)
- Bailey MA (2004) Inhibition of bicarbonate reabsorption in the rat proximal tubule by activation of luminal P2Y1 receptors. (springer.com)
- The rank order potency of inhibition by ATP analogues suggests that a P2y type of ATP receptor is involved in this inhibition. (jci.org)
- The compound ATP gamma S inhibits agonist-stimulated adenylate cyclase activity in solubilized and in isobutylmethylxanthine (IBMX) and quinacrine pretreated membranes, suggesting that ATP gamma S inhibition occurs independent of AVP and A1 adenosine receptors and of phospholipase A2 activity. (jci.org)
- To avoid these undesirable effects, indirect approaches, such as allosteric adenosine receptor modulation or inhibition of adenosine kinase 9,10 or adenosine deaminase, 11 have been examined and show antinociceptive effects in neuropathic rats. (asahq.org)
- These results suggest that inhibition of PRL secretion after A1 receptor activation by R-PIA is mediated by a Gi protein -dependent mechanism. (bvsalud.org)
- In A431 cells adenosine evoked a biphasic response in which a low concentration (~10 μM) produced inhibition of colony formation but at higher concentrations (up to 100 μM) this inhibition was progressively reversed. (nus.edu.sg)
- 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)
- 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)
- Inhibition of rat ventricular automaticity by adenosine. (semanticscholar.org)
- Through a reorganization of these heteroreceptor complexes upon chronic dopaminergic treatment a pathological and prolonged inhibition of D2R receptor protomer signaling can develop with motor inhibition and wearing off of the therapeutic effects of levodopa and dopamine receptor agonists. (springer.com)
- Accordingly, the tissue hypoxia caused by limited blood supply may lead to an increase of local adenosine levels, probably because of insufficient ATP production and the inhibition of adenosine-metabolizing enzyme ( 14 , 15 , 16 ). (jimmunol.org)
- their activation leads to increased proliferation and secretion of chromogranin A. Targeting adenosine signal pathways, specifically inhibition of A2 receptors, may thus be a useful addition to the therapeutic management of neuroendocrine tumours. (cf.ac.uk)
- The mechanisms of the cardiovascular effects of caffeine include the blocking of adenosine receptors and the inhibition of phosphodiesterases. (kzeng.info)
- The first was the A , receptor mediated inhibition of isoproterenol stimulated cAMP accumulation in DDT cells. (blogspot.in)
Effect of adenosine7
- Babich V, Vadnagara K, Di Sole F (2015) Dual effect of adenosine a1 receptor activation on renal O2 consumption. (springer.com)
- From these results obtained, it is hypothesized that adenosine receptors in carotid body are A 2 -receptor subtype mediating the pressor effect of adenosine and its analogue, the negative chronotropic or/and inotropic effects of adenosine and its analogue are involved in their hypotensive action, and ATP-sensitive K + channels coupled by adenosine receptors may be activated by adenosine to mediate its effects. (elsevier.com)
- This study investigated the involvement of 5-HT1 and 5-HT2 receptors in the antidepressant-like effect of adenosine in the mouse forced swimming test (FST). (unboundmedicine.com)
- Taken together, the results indicate that the antidepressant-like effect of adenosine in the FST appears to be mediated, at least in part, by an interaction with 5-HT1A receptors. (unboundmedicine.com)
- TY - JOUR T1 - Involvement of 5-HT1A receptors in the antidepressant-like effect of adenosine in the mouse forced swimming test. (unboundmedicine.com)
- Little, however, is known about the effect of adenosine on myeloid cells. (springer.com)
- Considering that tumor associated macrophages (TAM) and myeloid-derived suppressor cells (MDSC) constitute up to 20 % of OvCA tissue, we investigated the effect of adenosine on myeloid cells and explored a possible contribution of myeloid cells to adenosine generation in vitro and ex vivo. (springer.com)
- Barrett RJ, Droppleman DA (1993) Interactions of adenosine A1 receptor-mediated renal vasoconstriction with endogenous nitric oxide and ANG II. (springer.com)
- We demonstrated that ESS combined with the blockage of A1 receptors increased the magnitude of the endogenous modulation and postponed the decay of responses that occur during ESS alone. (frontiersin.org)
- As a breakdown product of ATP, adenosine is an endogenous purine nucleoside that modulates many physiological processes in all cells of the body. (physiology.org)
- The A2AR is expressed in lung tissues, where it is activated by endogenous/exogenous adenosine or A2AR agonists and where it exerts anti-inflammatory effects ( 24 , 39 , 45 ). (physiology.org)
- Heteromers consisting of adenosine A1/A2A, dopamine D2/A2A and D3/A2A, glutamate mGluR5/A2A and cannabinoid CB1/A2A have all been observed, as well as CB1/A2A/D2 heterotrimers, and the functional significance and endogenous role of these hybrid receptors is still only starting to be unravelled. (wikipedia.org)
- This rise in endogenous levels of adenosine then leads to the activation of ocular adenosine receptors and is in part responsible for the ocular hypotensive action of epinephrine. (arvojournals.org)
- The mechanism of physiologically relevant increases in the levels of endogenous adenosine to enable the adenosine-mediated down-regulation of inflammation in hypoxic areas of inflamed tissues is supported by observations of the obstruction of blood perfusion in inflamed tissue ( 13 ). (jimmunol.org)
- In the presence of GTP all receptors were converted to a single low affinity state indicating functional coupling to endogenous G proteins. (biomedsearch.com)
- 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. (uniroma1.it)
- I(GABA) run-down from wt mice was not affected by 2-CA, suggesting maximal ARs activity by endogenous adenosine. (uniroma1.it)
- abstract = "Adenosine released into the extracellular space by immunologic and nonimmunologic stimuli has been shown to regulate various immune functions. (utmb.edu)
- The concepts of allosteric modulation and biased agonism are revolutionizing modern approaches to drug discovery, particularly in the field of G protein-coupled receptors (GPCRs). (pnas.org)
- Biochemical and pharmacological role of A1 adenosine receptors and their modulation as novel therapeutic strategy In: ed Protein Reviews. (eurekaselect.com)
- Among these indirect approaches, allosteric adenosine receptor modulation represents a novel drug development direction to potentiate A1 receptor function and agonist binding via a conformation change. (asahq.org)
- The actions of the A2A receptor are complicated by the fact that a variety of functional heteromers composed of a mixture of A2A subunits with subunits from other unrelated G-protein coupled receptors have been found in the brain, adding a further degree of complexity to the role of adenosine in modulation of neuronal activity. (wikipedia.org)
- The modulation of cell growth by adenosine was found to be receptor-mediated. (nus.edu.sg)
- In this review we propose that adenosine could be a key element in the development of new strategies for limit lipoinflammation and regulate metabolic homeostasis through modulation of adipocyte-macrophage dialog. (elsevier.es)
- ADENOSINE is recognized to play a role in modulation of nociceptive transmission in the spinal cord. (asahq.org)
- Adenosine A2A receptors and metabotropic glutamate 5 receptors are co-localized and functionally interact in the hippocampus: a possible key mechanism in the modulation of N-methyl-D-aspartate effects. (harvard.edu)
- Adenosine is a purine nucleoside, responsible for the regulation of a wide range of physiological and pathophysiological conditions by binding with four G-protein-coupled receptors (GPCRs), namely A1, A2A, A2B and A3 adenosine receptors (ARs). (eurekaselect.com)
- In particular, A1 AR is ubiquitously present, mediating a variety of physiological processes throughout the body, thus represents a promising drug target for the management of various pathological conditions. (eurekaselect.com)
- Adenosine-a physiological or pathophysiological agent? (eurekaselect.com)
- However, A2b and A3 receptors are relatively less active than A1 and A2a receptors under normal physiological conditions. (innovations-report.com)
- Adenosine mediates many physiological functions via activation of extracellular receptors. (nus.edu.sg)
- Adenosine is a multi-functional physiological molecule found abundantly in the body. (edu.au)
- 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)
- Li, YL , He, RR & Ho, SY 1994, ' Effects of 8-phenyltheophylline and glibenclamide on cardiovascular responses to adenosine and R-N 6 (phenylisopropyl)-adenosine in anesthetized rats ', Chinese Journal of Physiological Sciences , vol. 10, no. 2, pp. 97-104. (elsevier.com)
- Under normal physiological conditions, adenosine is present in sufficient concentrations to activate A 1 and A 2a receptors. (kzeng.info)
- These receptors are widely expressed in different cell types of the heart and blood vessels, where they mediate the actions of a variety of hormones growth factors, neurotransmitters, biologically active peptides, and local mediators, and are consequently involved in the regulation of numerous cellular processes and physiological functions. (guwsmedical.info)
- This study explored whether selective pharmacological antagonism of the adenosine A1 receptor subtype synergizes with ESS, thereby increasing motor response. (frontiersin.org)
- We hypothesized that selective pharmacological antagonism of A1 receptors during ESS would produce facilitatory effects in spinal sensorimotor networks detected as an increased amplitude of spinally-evoked motor potentials and sustained duration of ESS induced activity. (frontiersin.org)
- Pharmacological characterization of the anticonvulsant response in the prepiriform cortex revealed a significant correlation between the potency of adenosine analogs as anticonvulsants and their respective affinities for adenosine A 1 receptors in vitro. (elsevier.com)
- Molecular cloning and functional characterization of a human 5-HT1B serotonin receptor: a homologue of the rat 5-HT1B receptor with 5-HT1D-like pharmacological specificity. (wikipedia.org)
- The A1 subtype showed the typical pharmacological profile with 2-chloro-N6-cyclopentyladenosine (CCPA) as the agonist with the highest affinity and a marked stereoselectivity for the N6-phenylisopropyladenosine (PIA) diastereomers. (biomedsearch.com)
- 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)
- Genetic and pharmacological inactivation of the adenosine A2A receptor attenuates 3-nitropropionic acid-induced striatal damage. (harvard.edu)
- Genetic and pharmacological inactivation of adenosine A2A receptor reveals an Egr-2-mediated transcriptional regulatory network in the mouse striatum. (harvard.edu)
- Conditional neural knockout of the adenosine A(2A) receptor and pharmacological A(2A) antagonism reduce pilocarpine-induced tremulous jaw movements: studies with a mouse model of parkinsonian tremor. (harvard.edu)
- This is the first example showing that it is feasible to modulate and even enhance the pharmacological profile of a ligand of a GPCR based on conjugation to a nanocarrier and the precise structure of the linking group, which was designed to interact with distal extracellular regions of the 7 transmembrane-spanning receptor. (biomedcentral.com)
- Moreover, adenosine inhibited neuronal differentiation in mouse dorsal root ganglion cells presumably via the A1 subtype 4. (edu.au)
- 2 CADO, adenosine, and the A1 subtype-selective agonists N6-(L-2-Phenylisopropyl)adenosine (R- PIA) and 2-chloro-N6-cyclopentyladenosine (CCPA) reversibly modulated whole cell Ba2+ currents in a concentration-dependent fashion. (gotomydoctor.com)
- 1992). "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor. (wikipedia.org)
- Note that receptor subtype distributions have not been indicated for all receptor classes (e.g., prostanoid receptors and somatostatin receptors) with complex and incompletely known expression patterns. (guwsmedical.info)
- Abebe W, Hussain T, Olanrewaju H et al (1995) Role of nitric oxide in adenosine receptor-mediated relaxation of porcine coronary artery. (springer.com)
- Moreover, minoxidil contains a nitric oxide moiety and may act as a nitric oxide agonist. (wikipedia.org)
- Experimental studies with experimental rodent models and cultures (cardiac myocytes, endothelial cells) indicate that moderate alcohol exposure can promote anti-inflammatory processes involving adenosine receptors, protein kinase C (PKC), nitric oxide synthase, heat shock proteins, and others which could underlie cardioprotection. (pubmedcentralcanada.ca)
- Adenosine Receptors: Structure, Distribution, and Signal Transduction. (eurekaselect.com)
- The effect of minoxidil is mediated by adenosine, which triggers intracellular signal transduction via both adenosine A1 and A2 receptors[disambiguation needed], and that the expression of sulfonylurea receptor 2B in dermal papilla cells might play a role in the production of adenosine. (wikipedia.org)
- Although the signal transduction mechanisms associated with adrenergic receptor activation are diverse, studies have identified a relationship between the ocular hypotensive action of adrenergic agonists in their ability to stimulate adenylate cyclase. (arvojournals.org)
Administration of adenosine2
- The aim of the present study was to investigate the effect of peripheral administration of adenosine agonists with different affinities for the A1 and A2 adenosine receptors on a persistent pain stimulus using the formalin test. (nih.gov)
- In protocol B, risk zones were similar, but administration of adenosine resulted in significant reductions in infarct size from 59 ± 3% of the area-at-risk in control swine to 46 ± 4% (p = 0.02), and no-reflow from 49 ± 6% of the infarct area to 26 ± 6% (p = 0.03). (onlinejacc.org)
- As a result, Adenosine receptor A2A decreases activity in the Dopamine D2 receptors. (wikipedia.org)
- BAY 60-6583 is a potent adenosine A2B receptor agonist that decreases fMLP-induced superoxide production in neutrophils at low concentrations (1-10 nM). (emmx.com)
- There were no differences between brain tissue from control and caffeine-treated rats in number and affinity of adenosine binding sites or in receptor-mediated increasesmore » (A2 adenosine receptor) and decreases (A1 adenosine receptor) in cAMP accumulation. (kzeng.info)
- This suggests that caffeine, because of its ability to block adenosine A1 receptors, shares neurochemical properties with other psychostimulants, which could contribute to the widespread consumption of caffeine-containing beverages. (jneurosci.org)
- The main mechanism of action of caffeine in the brain seems to be a nonselective competitive blockade of adenosine receptors, in particular adenosine A1 receptors and A2A receptors ( Daly and Fredholm, 1998 ). (jneurosci.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)
- Effects of caffeine could be mediated by its action on several different targets such as cAMP phosphodiesterase, phosphatidylinositol-3 kinase, and adenosine receptors ( 1 , 2 ). (jimmunol.org)
- The behavioral activation by caffeine is largely accounted for by the antagonism of tonic activation of the A2A adenosine receptor (A2AR) 3 in the brain ( 1 ). (jimmunol.org)
- Its principal action is adenosine antagonism, and there are a number of caffeine analogs with variable affinities for A1 and A2 receptors [ 2 ]. (hindawi.com)
- Receptor up-regulation during chronic drug treatment has been proposed to be the mechanism of tolerance to the behavioral stimulant effects of caffeine. (kzeng.info)
- However, adenosine continues to be released even with caffeine in your bloodstream. (kzeng.info)
- It promotes wakefulness by blocking adenosine A 2A receptors (A 2A Rs) in the brain, but the specific neurons on which caffeine acts to produce arousal have not been identified. (kzeng.info)
- We propose, therefore, that up-regulation of adenosine receptors may underlie the development of tolerance to the CNS effects of caffeine. (kzeng.info)
- In early pathological stages of HD and even in symptomatic patients with a grade of 0 on Vonsattelâ s neuropathological severity in HD scale, both D 2 R and A 2A R are significantly and differentially downregulated when compared with D 1 R. 6 These data suggest a selective functional alteration in â ¦ Caffeine hijacks the receptors, artificially controlling your energy levels. (kzeng.info)
- Tolerance occurs as caffeine binds the adenosine receptors in the body, leading to an antagonizing effect and as adenosine is needed, the brain dumps greater and greater amounts of adenosine into circulation, as well as increases cell receptor number (increasing chances of binding adenosine), so there is an increased need to increase the population of caffeine molecules, and so on and so forth. (kzeng.info)
- C57BL/6J and DBA/2J mice were used to determine if possible differences in the behavioral response to caffeine might be related to differences in A1 adenosine receptors. (kzeng.info)
- Mice heterozygous for both A1 and A(2A) adenosine receptor genes show similarities to mice given long-term caffeine. (harvard.edu)
- Pathophysiological roles for purines: adenosine, caffeine and urate. (harvard.edu)
- Neuroprotection by caffeine in the MPTP model of parkinson's disease and its dependence on adenosine A2A receptors. (harvard.edu)
- Contradictary evidence activiation of A1 inhibit acetylcholine release Ach is important in memory storage Agonist of A1 DO Not effect the memory improving effect of Caffeine, can even increase it in some cases. (coursehero.com)
Levels of adenosine2
- In the study of differentiation, the use of the designed PCR primers was not quantitative to measure the levels of adenosine receptors due to variations of the expressions levels of the glyceraldehyde-3-phosphate dehydrogenase (GAPDH) gene, a house-keeping gene commonly used as the internal control in PCR or northern blot analysis. (edu.au)
- In ovarian cancer, high levels of adenosine are due to tumor-specific expression of the ectonucleotidases CD39/ENTPD1 and CD73/ecto-5′-nucleotidase [ 7 ] which synergistically catalyze the degradation of extracellular immune-stimulatory ATP to immune-inhibitory adenosine. (springer.com)
- G protein-coupled receptors (GPCRs) are the largest family of cell surface proteins and tractable drug targets ( 1 , 2 ). (pnas.org)
- ATP receptor regulation of adenylate cyclase and protein kinase C activity in cultured renal LLC-PK1 cells. (jci.org)
- Furthermore, adenosine significantly attenuated protein degradation of A2A and A3 receptors induced by LPS. (physiology.org)
- This protein is a member of the G protein-coupled receptor (GPCR) family which possess seven transmembrane alpha helices, as well as an extracellular N-terminus and an intracellular C-terminus. (wikipedia.org)
- The activity of the encoded protein, a G protein-coupled receptor family member, is mediated by G proteins which activate adenylyl cyclase, which induce synthesis of intracellular cAMP. (wikipedia.org)
- The A2A receptor binds with the Gs protein at the intracellular site of the receptor. (wikipedia.org)
- In this role, it functions similarly to programmed cell death-1 (PD-1) and cytotoxic t-lymphocyte associated protein-4 (CTLA-4) receptors, namely to suppress immunologic response and prevent associated tissue damage. (wikipedia.org)
- Abundant extracellular adenosine can then bind to the A2A receptor resulting in a Gs-protein coupled response, resulting in the accumulation of intracellular cAMP, which functions primarily through protein kinase A to upregulate inhibitory cytokines such as transforming growth factor-beta (TGF-β) and inhibitory receptors (i.e. (wikipedia.org)
- My central area of research concerns the pharmacology and biochemistry of G protein-coupled receptors (in particular, cannabinoid, adenosine and glutamate) in the CNS and peripheral tissues. (nottingham.ac.uk)
- G protein-coupled receptor list: recommendations for new pairings with cognate ligands. (nottingham.ac.uk)
- 1989). "Selective amplification and cloning of four new members of the G protein-coupled receptor family. (wikipedia.org)
- 2002). "Oligomerization of G-protein-coupled receptors shown by selective co-immunoprecipitation. (wikipedia.org)
- The GPCR complexes can also contain ion channel receptors, receptor tyrosine kinases (RTKs), sets of G protein interacting proteins and/or transmitter transporters increasing their integrative capability (Borroto-Escuela et al. (springer.com)
- A2AR is a G s protein-coupled receptor, and ligand binding to A2AR increases intracellular cAMP. (jimmunol.org)
- but these techniques are difficult to apply to low-density G protein-coupled receptors such as adenosine receptors. (aspetjournals.org)
- Adenosine A1 and A2A receptor regulation of protein phosphatase 2A in the murine heart. (harvard.edu)
- An approach to use multivalent dendrimer carriers for delivery of nucleoside signaling molecules to their cell surface G protein-coupled receptors (GPCRs) was recently introduced. (biomedcentral.com)
- The multicomponent modular nature of G protein-coupled receptor (GPCR) systems provides cells with numerous potential combinations by which to transduce signals. (aspetjournals.org)
- This approach has yielded important information regarding the types of pathways (i.e., the class of G protein and cognate downstream effectors) that are characteristically activated by a given receptor and, thereby, the types of alterations in cell function that are elicited. (aspetjournals.org)
- The current dogma is that high-affinity protein-protein interactions determine the identity of the G protein with which a particular GPCR interacts and, in turn, dictates the biochemical pathways that are activated by that receptor. (aspetjournals.org)
- 12,13 An adenosine receptor modulator, T62, belonging to a group of thiophene compounds first described a decade ago, 14 has been shown to reduce mechanical allodynia in spinal nerve-injured rats after oral, parenteral, or intrathecal application. (asahq.org)
- On the other hand adenosine analogues have been shown to possess antinociceptive effects after peripheral and intrathecal administration in animals. (nih.gov)
- Effects of intrathecal injection of the adenosine receptor agonists R-phenylisopropyl-adenosine and N-ethylcarboxamide-adenosine on nociception and motor function in the rat. (nih.gov)
- We aimed to study efficacy of intrathecal injection of adenosine for post-operative radicular pain after lumbar discectomy. (biomedcentral.com)
- Forty patients with unilevel lumbar discectomy who had radicular lower limb pain were treated by 1000 micrograms of intrathecal injection of adenosine in this single-arm prospective open-label trial between November 2015 to October 2016. (biomedcentral.com)
- This study suggests that intrathecal injection of 1000 micrograms adenosine is a safe and effective method for post-operative neuropathic pain management after uni-level disk surgeries. (biomedcentral.com)
- Intrathecal injection of 500-2000 micrograms of adenosine has been associated with spinal hyperalgesia and allodynia [ 6 ]. (biomedcentral.com)
- Since studies regarding postoperative analgesic effects of adenosine are not sufficient to overcome controversy in the literature, in this study, we aimed to determine the efficacy of intrathecal adenosine injection for relief of neuropathic pain after lumbar uni-level discectom. (biomedcentral.com)
- This is a single-arm prospective open-label trial investigating intrathecal adenosine injection for relief of the neuropathic pain after lumbar uni-level discectomy in 40 patients with history of uni-level lumbar discectomy in the last 3-6 months and chief complaint of postoperative radicular neuropathic pain which was conducted at the Emam Reza Educational Hospital, Tabriz, Iran. (biomedcentral.com)
- Adenosine-a drug commonly administered intravenously (into a vein) to treat certain types of abnormal heart rhythms-has been found to reduce areas of allodynia (pain caused by a stimulus that does not normally cause pain) after intrathecal, but not intravenous administration in people with neuropathic pain. (clinicaltrials.gov)
- Intrathecal clonidine relieves pain by actions on a2-adrenoceptors in the spinal cord, whereas adenosine relieves pain by actions on A1 adenosine receptors. (clinicaltrials.gov)
- Researchers believe that intrathecal adenosine and clonidine may prove to be excellent painkillers for nerve pain. (clinicaltrials.gov)
Relief of neuropathic pain1
- Among several novel approaches that seem promising in relief of neuropathic pain, adenosine receptor agonists have attracted considerable attention. (asahq.org)
- The adenosine A 1 GPCR (A 1 AR) is a major therapeutic target for cardioprotection, but current agents acting on the receptor are clinically limited for this indication because of on-target bradycardia as a serious adverse effect. (pnas.org)
- There is also lack of knowledge on the stoichiometry of the participating receptor protomers in GPCR heteroreceptor complexes. (springer.com)
- Various GPCR and receptor tyrosine kinases have been localized in caveolae or caveolin-rich cellular fractions along with many of the molecules critical for transducing the signals initiated by these types of receptors: e.g. (aspetjournals.org)
- Some GPCR are enriched or excluded from caveolae whereas certain GPCR reportedly translocate out of or into caveolae upon activation by an agonist. (aspetjournals.org)
Role of adenosine receptors1
- 2] Interestingly, evidence is growing for a certain role of adenosine receptors in the field of oncology . (axonmedchem.com)
- In the current study, we have rationally designed a novel A 1 AR ligand (VCP746)-a hybrid molecule comprising adenosine linked to a positive allosteric modulator-specifically to engender biased signaling at the A 1 AR. (pnas.org)
- The crystallographic structure of the adenosine A2A receptor reveals a ligand binding pocket distinct from that of other structurally determined GPCRs (i.e., the beta-2 adrenergic receptor and rhodopsin). (wikipedia.org)
- In contrast, heroic doses of the A2 selective ligand, 2-phenylaminoadenosine, afforded no protection against seizures. (elsevier.com)
- Adenosine has diverse actions as a ligand on many different types of cells and tissues acting via specific receptors. (edu.au)
- Unlike many other chemokine receptors, ligand activation of CXCR7 does not cause Ca 2+ mobilization or cell migration. (rupress.org)
- Acute and chronic effects of the benzodiazepine receptor ligand FG 7142: proconvulsant properties and kindling. (isni.org)
- Drugs that inhibit ADENOSINE DEAMINASE activity. (nih.gov)
- A1 agonists, through their ability to inhibit the catecholamine induced increase in cAMP, should have beneficial effects in the failing heart where increased sympathetic tone causing enhanced cAMP has been associated with increased likelihood of ventricular arrhythmias and sudden death. (justia.com)
- anxiety have implicated the basolateral complex (BLA), as Previous work has demonstrated that adenosine receptors being centrally important in both the acquisition and may act presynaptically in the amygdala to inhibit both expression of fear/apprehension-related behaviours (re- excitatory and inhibitory transmission (Heinbockel & viewed in Davis, 1992). (gotomydoctor.com)
- The major adenosine receptor complexes in the striato-pallidal GABA neurons can be the A2AR-D2R and A2AR-D2R-mGluR5 receptor complexes, in which A2AR protomers and mGluR5 protomers can allosterically interact to inhibit D2R protomer signaling. (springer.com)
- It only displays an inhibitory action against PDE2A1 and antagonism at adenosine A(2A) at high concentrations [A31642]. (drugbank.ca)
- 3H]2-(2-benzofuranyl)-2-imidazoline: a new selective high affinity radioligand for the study of rabbit brain imidazoline I2 receptors. (isni.org)
- The adoption of these updated criteria assisted us in synthesizing a series of 1-deazapurines with consistently high affinity as inverse agonists for the adenosine A1 receptor. (nih.gov)
- Outcomes Receptor binding "type":"entrez-nucleotide","attrs":"text":"F13714″,"term_id":"747841″,"term_text":"F13714″F13714 exhibited high affinity for rat hippocampal 5-HT1A receptors and human Baricitinib being 5-HT1A receptors indicated in CHO cells (p K can be.e.m.: 10.010.05 and 10.400.09, respectively, n =3), in keeping with previous findings in rat cortex (Koek et al . (cancer-colorectal.com)
- It has been shown that an A2AR agonist protects against ischemia-reperfusion injury in porcine allogeneic lung transplantation ( 23 ). (physiology.org)
- Several studies have also suggested that the beneficial effects of adenosine occur through the effects of the A2AR and A2BR ( 7 , 22 , 27 , 43 ). (physiology.org)
- The genetic elimination of A2A adenosine receptors (A2AR) was shown to disengage the critical immunosuppressive mechanism and cause the dramatic exacerbation of acute inflammatory tissue damage by T cells and myeloid cells. (jimmunol.org)
- The anti-inflammatory effect of A2AR agonist has been demonstrated in inflammation in vivo, including ischemia/reperfusion injury ( 9 , 10 ), airway inflammation ( 11 ), and T cell-dependent acute hepatitis ( 12 ). (jimmunol.org)
- ASP5854 ameliorated A(2A) agonist 2-[p-(2-carboxyethyl) phenethylamino]-5'-N-ethylcarboxamidoadenosine (CGS21680)- and haloperidol-induced catalepsy in mice, with the minimum effective doses of 0.32 and 0.1 mg/kg, respectively, and it also improved haloperidol-induced catalepsy in rats at doses higher than 0.1 mg/kg. (curehunter.com)
- Cell counts, EBDA extravasation, as well as levels of proteins and inflammatory cytokines were decreased in adenosine-treated mice. (physiology.org)
- In this study we report that i.p. pretreatment of mice with CGS-21680 HCl (CGS), a selective agonist of A 2 adenosine receptors, at 0.2 to 2 mg/kg caused an augmentation of plasma IL-10 levels induced by i.p. injection of LPS, but decreased plasma levels of LPS-induced TNF-α. (utmb.edu)
- Finally, repeated l -DOPA treatment reversed the 6-OHDA-induced reduction of striatal dynorphin mRNA in WT but not A 2A KO mice, raising the possibility that the A 2A receptor may contribute to l -DOPA-induced behavioral sensitization by facilitating adaptations within the dynorphin-expressing striatonigral pathway. (jneurosci.org)
- To characterize the third regulatory mechanism in more detail, mice were studied that are genetically deficient in TGF due to targeted deletion of the gene coding for A1 adenosine receptors (A1AR), the major signaling pathway of TGF [ O19 ]. (uni-freiburg.de)
- Castillo A et al: "The neuroprotective effect of cannabidiol in an in vitro model of newborn hypoxic-ischemic brain damage in mice is mediated by CB(2) and adenosine receptors. (unboundmedicine.com)
- TY - JOUR T1 - The neuroprotective effect of cannabidiol in an in vitro model of newborn hypoxic-ischemic brain damage in mice is mediated by CB(2) and adenosine receptors. (unboundmedicine.com)
- Forebrain adenosine A2A receptors contribute to L-3,4-dihydroxyphenylalanine-induced dyskinesia in hemiparkinsonian mice. (harvard.edu)
- I(GABA) run-down in pyramidal neurons was equivalent in A1 receptor-deficient and wt neurons but much larger in neurons from A2A receptor-deficient mice, indicating that, in mouse cortex, GABA(A)-receptor stability is tonically influenced by A2A but not by A1 receptors. (uniroma1.it)
- Their theory is based on the fact that adenosine is produced within the body and inhibits neuronal excitability and synapse transmission. (innovations-report.com)
- Adenosine also inhibits the release of most brain excitatory neurotransmitters, particularly dopamine (DA), and may reduce DA synthesis. (innovations-report.com)
- 2'-MeCCPA is a potent and highly selective agonist at A1 adenosine receptors (Ki values are 3.3, 9580, 37600 and 1150 nM for human recombinant A1, A2A, A2B and A3 receptors respectively), which acts as a full agonist and inhibits forskolin-stimulated adenylyl cyclase activity in rat cortical membranes with an IC50 value of 13.1 nM. (emmx.com)
- In the present study, we investigated the role of the activation of adenosine A1 receptors by (R)-N6-(2-phenylisopropyl) adenosine (R-PIA) at the pituitary level in in vitro PRL secretion . (bvsalud.org)
- In vitro data showed that adenosine stimulated a three- to fourfold increase in cAMP levels in BON-1 and KRJ-1 cells. (cf.ac.uk)
- Signaling through A 2A adenosine receptors (A 2A R) regulates T lymphocyte expansion and modulates T cell receptor (TCR)-mediated effector functions in vitro. (aspetjournals.org)
- showed that radioligand binding to A2 receptors dramatically increases during monocyte differentiation in vitro. (aspetjournals.org)
- After Anxa3 downregulation, the growth of A549 and LTEP-a2 LADC cells was slowed and they showed decreased migration and invasion in vitro. (cancerindex.org)
- We have recently shown that extracellular adenosine enhances human pulmonary (EC) barrier via activation of adenosine receptors (ARs) in cell cultures. (physiology.org)
- Extracellular adenosine gathers in response to cellular stress and breakdown through interactions with hypoxia induced HIF-1α. (wikipedia.org)
- Patterns of A2A Extracellular Adenosine Receptor Expression in Different Functional Subsets of Human Peripheral T Cells. (aspetjournals.org)
- In this study, we investigated the effect of IFN-γ on TLR-activated macrophages, and we reveal that IFN-γ sustains inflammatory macrophage activation by attenuating their sensitivity to extracellular adenosine. (jimmunol.org)
- In sturlies on adenylate cyclase 2',3'-dideoxy-N\(^6\)-cyclohexyladenosine (ddCHA) did not show agonist properties at A\(_1\) or at A\(_2\) receptors. (uni-wuerzburg.de)
- A 30- to 45-fold selectivity for platelet A\(_2\) receptors compared to A\(_1\) receptors was found for compounds 8a-c in adenylate cyclase studies. (uni-wuerzburg.de)
- Striatal D/sub 1/ receptors and their activity were characterized by (/sup 3/H)SCH23390 binding parameters and D/sub 1/ receptor-stimulated adenylate cyclase activity in striatal membranes. (kzeng.info)
- Compounds that selectively bind to and activate ADENOSINE A2 RECEPTORS. (nih.gov)
- These low molecular weight compounds activated glycogen synthase at ∼100 nmol/l in cultured CHO cells transfected with the insulin receptor and in primary hepatocytes isolated from Sprague-Dawley rats, and at 500 nmol/l in isolated type 1 skeletal muscle of both lean Zucker and ZDF rats. (diabetesjournals.org)
- that the claimed compounds would have an A1-adenosine receptor antagonistic activity. (epo.org)
- The protective effects of a series of stable adenosine analogs against generalized seizures inititated by focal injection of bicuculline methiodide into the rat prepiriform cortex (PPC) were studied by microinjection of these compounds into this brain area. (elsevier.com)
- These data suggest that the antiseizure activity of these compounds in the PPC results from activation of A 1 adenosine receptors. (elsevier.com)
- Compounds which are able to block adenosine receptors are commonly found in tea, chocolate, and coffee. (kzeng.info)
- Compounds of this invention prepared according to the method of Example 1 were tested in two functional models specific for adenosine A, receptor agonist function. (blogspot.in)
- Allosteric enhancer of A1 AR is found to be potent for the treatment of neuropathic pain, culminating the side effects related to off-target tissue activation of A1 AR. (eurekaselect.com)
- N-Methyl-5-tert-butyltryptamine: A novel, highly potent 5-HT1D receptor agonist. (wikipedia.org)
- MRS 1706 is a potent and selective adenosine A2B receptor inverse agonist (Ki values are 1.39, 157, 112 and 230 nM for human A2B, A1, A2A and A3 receptors respectively). (emmx.com)
- The N6-benzyl substituted derivatives of adenosine-5'-N-methyluronamide (MECA) turned out to be the most potent agonists. (biomedsearch.com)
Allosteric adenosine receptor1
- T62 (2-amino-3-(4-chlorobenzoyl)-5,6,7,8-tetrahydrobenzothiophen) is an allosteric adenosine receptor modulator that enhances adenosine binding to the A1 receptor through a conformation change. (asahq.org)
- Adenosine deaminase-resistant, synthetic adenosine analogues were used and demonstrated enhancement of differentiation. (edu.au)
- Adenosine binds to specific receptors in the brain to prepare your body for sleep. (kzeng.info)
- Because adenosine production increases in hypoxia, the issue of a role of the nucleoside in the renal injury following ischemia reperfusion has been studied extensively. (springer.com)
- Experimental evidence supports the notion that adenosine protects against ischemia-induced acute kidney injury by directly acting on renal endothelial and tubular A 1 AR. (springer.com)
- Adenosine is produced in response to trauma, ischemia, and hypoxia and plays an important role in preventing excessive tissue damage. (ptglab.com)
- Background Despite the clear cardioprotective effects of adenosine, when administered prior to ischemia, studies on cardioprotection by adenosine when administered at reperfusion have yielded contradictory results in both pre-clinical and clinical settings. (onlinejacc.org)
- Preconditioning of cardiomyocytes with either A 1 or A 3 AR agonists protects against myocardial ischemia. (biomedcentral.com)
- In the striatum, adenosine plays an important role as a modulator of both dopamine and glutamate neurotransmission. (jneurosci.org)
- The A2A receptor is also expressed in the brain, where it has important roles in the regulation of glutamate and dopamine release, making it a potential therapeutic target for the treatment of conditions such as insomnia, pain, depression, and Parkinson's disease. (wikipedia.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)
- 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)
- Inactivation of neuronal forebrain A receptors protects dopaminergic neurons in a mouse model of Parkinson's disease. (harvard.edu)
- In addition to the receptor types shown in Figure 4.1, GPCRs in the central nervous system (such as a2-adrenoceptors that regulate the sympathetic nervous system), GPCRs located in endocrine organs (through regulation, for example, of renin release) and receptors involved in metabolic regulation exert profound effects on cardiovascular health and disease and may constitute therapeutic targets. (guwsmedical.info)
- The important roles that some types of GPCRs have in cardiovascular diseases through effects mediated by receptors located on blood cells (e.g., many types of prostanoid receptors) or acting via enzymatic mechanisms (e.g., thrombin receptors) will not be discussed here. (guwsmedical.info)
- KANNA 20:1 extract (Sceletium tortuosum) Kanna works by interacting with the brain`s dopamine and serotonin receptors, promotes healthy wellbeing, and is used as a mood enhancer. (flippingbook.com)
- 1992). "Human serotonin 1D receptor is encoded by a subfamily of two distinct genes: 5-HT1D alpha and 5-HT1D beta." . (wikipedia.org)
- Primary structure and functional characterization of a human 5-HT1D-type serotonin receptor. (wikipedia.org)
- 2004). "Candidate genes for anorexia nervosa in the 1p33-36 linkage region: serotonin 1D and delta opioid receptor loci exhibit significant association to anorexia nervosa. (wikipedia.org)
- 2007). "The serotonin 5-HT1D receptor gene and attention-deficit hyperactivity disorder in Chinese Han subjects. (wikipedia.org)
- These results suggest that adenosine A 1 receptors may participate in the normal inhibitory regulation of the PPC, a forebrain area which may play a significant role in the pathobiology of epilepsy. (elsevier.com)
Adenylyl cyclase activity1
- The relative potencies of agonists for the A2B adenosine receptor could only be tested by measurement of receptor-stimulated adenylyl cyclase activity. (biomedsearch.com)
- 2-Chloro-N 6 -cyclopentyladenosine (CCPA), an agonist of A 1 adenosine receptors, at 0.5 mg/kg diminished LPS-induced plasma TNF-α concentrations, but enhanced LPS-induced IL-10 levels only at the highest dose used (2 mg/kg). (utmb.edu)
- The tritiated analogue of 2-chloro-N6-cyclopentyladenosine (CCPA), an adenosine derivative with subnanomolar affinity and a 10000-fold selectivity for A1 adenosine receptors, has been examined as a new agonist radioligand. (uni-wuerzburg.de)
Activation of adenosine1
- 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)
- Moreover, adenosine protects against renal ischemic reperfusion injury by the anti-inflammatory effect of enhancing the activity of regulatory T cell and by attenuating the inflammatory injury produced by neutrophils via A 2 AR activation. (springer.com)
- Although, adenosine activating its receptors (A 1 , A 2A , A 2B and A 3 ) is able to differentially modulate the function of adipocytes and macrophages, in order to avoid the reduction of insulin sensitivity and generate an anti-inflammatory state in subject with obesity. (elsevier.es)
- Adenosine has an analgesic and anti-inflammatory role and its injections are used for perioperative pain management. (biomedcentral.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)
- Although adenosine agonists were shown to attenuate pain behaviors in a variety of animal models, adenosine agonists are also implicated in the regulation of many physiologic processes, especially cardiovascular and neurologic, which either reduce the activity of excitable tissues ( e.g. , by slowing heart rate) or increase the delivery of metabolic substrates ( e.g. , inducing vasodilation). (asahq.org)
- In addition, adenosine A1 receptor regulation after chronic oral T62 administration was examined. (asahq.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)
- To understand the role of A 2A Rs in the regulation of immune response, we investigated the expression levels of this receptor in different functional lymphocyte subsets. (aspetjournals.org)
- suggesting a differentiation-dependent regulation of p2x7 receptor expression. (aspetjournals.org)
- In the search for more selective A2-receptor agonists and on the basis that appropriate substitution at C2 is known to impart selectivity for A\(_2\) receptors, 2-alkynyladenosines 2a-d were resynthesized and evaluated in radioligand binding, adenylate cycla.se, and platelet aggregation studies. (uni-wuerzburg.de)
- In order to improve this selectivity, the correaponding 2-alkynyl derivatives of adenosine-5'-N-ethyluronamide 8a-d were synthesized and tested. (uni-wuerzburg.de)
- displays 890-fold selectivity for rat A1 receptors over A2A receptors (Ki values are 0.19 and 170 nM respectively). (emmx.com)
- 100-fold selectivity over hA1, hA2A and hA3 receptors. (emmx.com)
- The ratio of the relative potency of each compound in stimulating either an A, receptor or an A 2 receptor effect is termed the selectivity of each compound for the A, receptor. (blogspot.in)
- 300-fold and 45-fold selectivity toward A2A and A3 receptors, respectively. (nih.gov)
- IFN-γ priming of macrophages selectively prevents the induction of the A2bR in macrophages to mitigate sensitivity to adenosine and to prevent this regulatory transition. (jimmunol.org)
- Thus, we propose a novel mechanism whereby IFN-γ contributes to host defense by desensitizing macrophages to the immunoregulatory effects of adenosine. (jimmunol.org)
- Thus, the generation of adenosine by macrophages is an important mechanism that prevents overactive inflammatory responses. (jimmunol.org)
- Generation of biologically active adenosine by TAM-like macrophages was measured in luciferase-based reporter assays. (springer.com)
- 12. The probe as recited in claim 11, wherein said label comprises .sup.19 F bonded to said adenosine nucleus by reacting the adenosine nucleus with ethyl trifluoracetate or heptafluorobutyryl anhydride, wherein at least one of the fluorineatoms in a fluoro substituent is .sup.19 F. (patentgenius.com)
- Focal injection of the adenosine A 2A receptor agonist CGS21680 (2-[p-(2-carboxyethyl)phenylethylamino]-5′-N-ethyl-carboxamidoadenosine) in the rat prepiriform cortex produced a reduction in the severity of bicuculline methiodide-induced motor seizures. (elsevier.com)
- the hypothesis is that this bitopic mode would result in unique receptor conformations that will signal to desirable pathways while sparing those pathways mediating undesirable effects. (pnas.org)
- Thus, this study provides proof of concept that bitopic ligands can be designed as biased agonists to promote on-target efficacy without on-target side effects. (pnas.org)
- However, treatment with full A1 AR agonists has been associated with numerous challenges like cardiovascular side effects, off-target activation as well as desensitization of A1 AR leading to tachyphylaxis. (eurekaselect.com)
- In this regard, partial agonists of A1 AR have been found to be beneficial in enhancing insulin sensitivity and subsequently reducing blood glucose level, while avoiding severe CVS side effects and tachyphylaxis. (eurekaselect.com)
- Borea PA, Gessi S, Merighi S, Varani K. Adenosine as a multi-signalling guardian angel in human diseases: when, where and how does it exert its protective effects? (eurekaselect.com)
- Effects of adenosine on tubular transport are most pronounced in the proximal tubule where the nucleoside stimulates NaCl reabsorption in the subnormal concentration range while inhibiting transport at elevated levels. (springer.com)
- Agmon Y, Dinour D, Brezis M (1993) Disparate effects of adenosine A1- and A2-receptor agonists on intrarenal blood flow. (springer.com)
- Beach RE, Good DW (1992) Effects of adenosine on ion transport in rat medullary thick ascending limb. (springer.com)
- Beach RE, Watts BA 3rd, Good DW et al (1991) Effects of graded oxygen tension on adenosine release by renal medullary and thick ascending limb suspensions. (springer.com)
- These multiple physiologic functions controlled by adenosine receptors result in some undesirable side effects from direct adenosine receptor agonists, including headache, nausea, 5 motor weakness, 6,7 chest pain, and atrioventricular block, 8 which limit their clinical application. (asahq.org)
- Objectives In the absence of effective clinical pharmacotherapy for prevention of reperfusion-mediated injury, this study re-evaluated the effects of intracoronary adenosine on infarct size and no-reflow in a porcine model of acute myocardial infarction using clinical bolus and experimental high-dose infusion regimens. (onlinejacc.org)
- In previous studies, we demonstrated biphasic purinergic effects on prolactin (PRL) secretion stimulated by an adenosine A2 agonist. (bvsalud.org)
- The mechanism(s) of these confusing effects of adenosine on neuronal differentiation require examination. (edu.au)
- In contrast with other xanthine derivatives, doxofylline does not significantly bind to adenosine alpha-1 or alpha-2 receptors and lacks stimulating effects. (drugbank.ca)
- these effects are mediated by CB(2) and adenosine, mainly A(2A), receptors. (unboundmedicine.com)
- 3) Glibenclamide (5 and 10 mg/kg) could attenuate the initial pressor and delayed depressor effects with bradycardia induced by adenosine (1 μmol/kg). (elsevier.com)
- Functional effects of adenosine were investigated in proliferation-experiments with CD4 + T cells and specific inhibitors. (springer.com)
- TCAs also block histamine-H1 receptors, α1-adrenergic receptors and muscarinic receptors, which accounts for their sedative, hypotensive and anticholinergic effects (e. g. blurred vision, dry mouth, constipation, urinary retention), respectively. (storysteel.gq)
- The purpose of this study is to determine the effects of clonidine and adenosine on nerve pain. (clinicaltrials.gov)
- Thus, rapid 5-HT1A autoreceptor desensitization by high-efficacy agonists may accelerate the onset of the therapeutic effects of antidepressants. (cancer-colorectal.com)
- Furthermore, they raise the possibility that the maladaptive dyskinetic responses to chronic l -DOPA treatment in Parkinson's disease may be attenuated by A 2A receptor inactivation. (jneurosci.org)
- This review is focused mainly on direct receptor-mediated control of myocardial functions and constriction and relaxation responses of the vascular walls. (guwsmedical.info)
- Both adenosine and xanthine derivatives bind competitively to A-1 and A-2 adenosine receptors. (patentgenius.com)
- There is provided exceptionally stable and useful pro-drugs that are esters of N6-oxa, thia, thioxa and azacycloalkyl substituted adenosine derivatives that are selective adenosine type 1 receptor agonists, and as such, are potentially useful agents for the treatment cardiovascular diseases and central nervous system disorders. (justia.com)
- An object of this invention are novel pro-drugs of heterocyclic substituted adenosine derivatives. (justia.com)
- Another object of this invention are pro-drugs of heterocyclic substituted adenosine derivatives that are converted in the mammalian body to become useful A1 receptor agonists. (justia.com)
- Still another object of this invention are pro-drugs of heterocyclic substituted adenosine derivatives that are useful for treating supraventricular tachycardias, including atrial fibrillation, atrial flutter, and AV nodal re-entrant tachycardia in mammals and especially humans. (justia.com)
- 2-(4,5-dihydro-1H-imidazol-2-yl)indazole (indazim) derivatives as selective I(2) imidazoline receptor ligands. (isni.org)
- Information about the lymphocyte subset-specific expression of adenosine receptors would be useful, but it has been difficult to obtain sufficient quantities of cells to analyze expression of Ado receptors in biochemical or radioligand binding assays, particularly in the minor subpopulations of lymphocytes. (aspetjournals.org)
- This forms the basis of the clinical utility of A1 receptor agonists for the treatment of supraventricular tachycardias, including atrial fibrillation, atrial flutter, and AV nodal re-entrant tachycardia. (justia.com)
- The clinical utility of A1 agonists therefore would be in the treatment of acute and chronic disorders of heart rhythm, especially those diseases characterized by rapid heart rate where the rate is driven by abnormalities in the atria. (justia.com)
- Recently, clinical evidence was found for the A3 receptor to be involved in rheumatoid arthritis , among other myocardial functions. (axonmedchem.com)
- 2] Clinical evidence for utilization of the A3 adenosine receptor as a target to treat rheumatoid arthritis: data from a phase II clinical trial. (axonmedchem.com)
- Tecadenoson is an adenosine A1 agonist which had been in phase II clinical evaluation by Gilead Sciences for treatment of atrial fibrillation. (blogspot.in)