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*  Adenosine receptor
Newer adenosine receptor agonists and antagonists are much more potent and subtype-selective, and have allowed extensive ... The role of A3 receptor is less defined in this field. Studies have shown that it plays a role in the downregulation of ... The adenosine receptors (or P1 receptors) are a class of purinergic G protein-coupled receptors with adenosine as endogenous ... Br J Pharmacol 170(6):1167-1176 "Entrez Gene: ADORA2A adenosine A2A receptor". Jacobson KA, Gao ZG (2006). "Adenosine receptors ...
*  Adenosine A2A receptor
3-e]-1,2,4-triazolo[1,5-c]pyrimidines as new A2A and A3 adenosine receptors antagonists". Journal of Medicinal Chemistry. 46 (7 ... Older research on adenosine receptor function, and non-selective adenosine receptor antagonists such as aminophylline, focused ... As a result, Adenosine receptor A2A decreases activity in the Dopamine D2 receptors. The adenosine A2A receptor has also been ... The adenosine A2A receptor, also known as ADORA2A, is an adenosine receptor, and also denotes the human gene encoding it. This ...
*  Adenosine A3 receptor
... a novel specific adenosine A(3) receptor antagonist with adenosine A(3) receptor agonists both in vitro and in vivo". Eur. J. ... is an adenosine receptor, but also denotes the human gene encoding it. Adenosine A3 receptors are G protein-coupled receptors ... adenosine receptor". Mol. Pharmacol. 63 (5): 1021-31. doi:10.1124/mol.63.5.1021. PMID 12695530. "Adenosine Receptors: A3". ... a novel ligand that demonstrates both adenosine A(2A) receptor agonist and adenosine A(3) receptor antagonist activity". ...
*  Reversine
... is known to act as an antagonist of the adenosine A3 receptor. Reversine is a potent inhibitor of the mitotic kinase ...
*  KF-26777
... is a drug which acts as a potent and selective antagonist for the adenosine A3 receptor, with sub-nanomolar affinity ( ... a new potent and selective adenosine A3 receptor antagonist". European Journal of Pharmacology. 444 (3): 133-41. doi:10.1016/ ... Baraldi PG, Tabrizi MA, Gessi S, Borea PA (January 2008). "Adenosine receptor antagonists: translating medicinal chemistry and ... A3 Ki=0.2nM) and high selectivity over the other three adenosine receptor subtypes. Simple xanthine derivatives such as ...
*  PSB-10
... is a drug which acts as a selective antagonist for the adenosine A3 receptor (ki value at human A3 receptor is 0.44 nM ... Müller CE (2003). "Medicinal chemistry of adenosine A3 receptor ligands". Current Topics in Medicinal Chemistry. 3 (4): 445-62 ... a novel high-affinity antagonist radioligand for human A(3) adenosine receptors". Bioorg Med Chem Lett. 12 (3): 501-3. doi: ... "Adenosine receptor subtype-selective antagonists in inflammation and hyperalgesia". Naunyn-Schmiedeberg's Archives of ...
*  Adenosine A2B receptor
2001). "Differential gene expression of adenosine A1, A2a, A2b, and A3 receptors in the human enteric nervous system". J. Comp ... Cacciari B, Pastorin G, Bolcato C, Spalluto G, Bacilieri M, Moro S (December 2005). "A2B adenosine receptor antagonists: recent ... The adenosine A2B receptor, also known as ADORA2B, is a G-protein coupled adenosine receptor, and also denotes the human ... "The A2b adenosine receptor mediates cAMP responses to adenosine receptor agonists in human intestinal epithelia". J. Biol. Chem ...
*  Caffeine
... is an antagonist at all four adenosine receptor subtypes (A1, A2A, A2B, and A3), although with varying potencies. The ... this is a receptor complex with 1 adenosine A1 receptor and 1 dopamine D1 receptor) and the A2A-D2 receptor heterotetramer ( ... this is a receptor complex with 2 adenosine A2A receptors and 2 dopamine D2 receptors). The A2A-D2 receptor heterotetramer has ... a receptor complex composed of 1 adenosine A1 receptor and 1 adenosine A2A receptor) in the axon terminal of glutamate neurons ...
*  Theophylline
... 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 ... asthma infant apnea Blocks the action of adenosine; an inhibitory neurotransmitter that induces sleep, contracts the smooth ...
*  Caffeine-induced anxiety disorder
Caffeine acts as an antagonist of adenosine A1 and A2A receptors. Adenosine is a normal neuromodulator that activates adenosine ... There are four well-known adenosine receptors found in the body, A1, A2A, A2B, and A3. The endogenous agonist for these ... Caffeine has been proven to act as an antagonist on adenosine receptors, which acts as a stimulant and therefore fulfills this ... Caffeine also has an excitatory effect on mesocortical cholinergic neurons by acting as an antagonist on adenosine receptors ...
*  Methoctramine
... such as nicotinic ACh receptors -at micromolar concentrations- or adenosine A3. The exact effects of methoctramine still remain ... Watson, N.; Barnes, P.J.; Maclagan, J. (1992). "Actions of methoctramine, a muscarinic M2 receptor antagonist, on muscarinic ... Gallamine triethiodide M2 receptor Muscarinic receptor Acetylcholine Jakubik, Jan; Zimcik, Pavel; Randakova, Alena; Fuksova, ... Hence, the presence of the antagonist methoctramine provokes an increase of the heart rate. In marked contrast of the above, ...
*  Adenosine
All adenosine receptor subtypes (A1, A2A, A2B, and A3) are G-protein-coupled receptors. The four receptor subtypes are further ... This is being contended and it is now considered a relative contraindication (however, selective adenosine antagonists are ... Cellular signaling by adenosine occurs through four known adenosine receptor subtypes (A1, A2A, A2B, and A3). Extracellular ... The A1 receptors couple to Gi/o and decreases cAMP levels, while the A2 adenosine receptors couple to Gs, which stimulates ...
*  Adenosine diphosphate receptor inhibitor
"Anti-platelet therapy: ADP receptor antagonists". British Journal of Clinical Pharmacology. 72 (4): 647-657. doi:10.1111/j.1365 ... 157 (1): 148.e1-148.e5. doi:10.1016/j.ahj.2008.09.017. Drepper, Michael D; Spahr, Laurent; Frossard, Jean Louis (2012-05-14). " ... P2Y12 receptor is a G-coupled receptor and is activated by adenosine diphosphate. ADP binds to the P2Y12 receptor that leads to ... Adenosine diphosphate (ADP) receptor inhibitors are a drug class of antiplatelet agents, used in the treatment of acute ...
*  Multiple electrode aggregometry
The antagonist reagent is used together with TRAP-test, and allows assessment of a positive control. Prostaglandin E1 (PGE1) is ... Thrombin receptor activating peptide-6 (TRAP-6) activates platelets through the thrombin receptor protease activated receptor-1 ... Adenosine diphosphate (ADP) is a platelet agonist. When it is added to saline-diluted whole blood in the test cuvette, it ... The GPIIb/IIIa antagonist blocks the binding of fibrinogen to the GPIIb/IIIa receptors, preventing the formation of platelet- ...
*  Hydrogen potassium ATPase
Björklund O, Shang M, Tonazzini I, Daré E, Fredholm BB (2008). "Adenosine A1 and A3 receptors protect astrocytes from hypoxic ... H2-receptor antagonists, like cimetidine (Tagamet), inhibit the signaling pathway that leads to activation of the ATPase. This ... eCollection 2015 Gessi S, Merighi S, Stefanelli A, Fazzi D, Varani K, Borea PA (2013). "A(1) and A(3) adenosine receptors ... Memory has been associated with astrocytes and the alpha3 subunit of adenosine receptor found in hydrogen/Sodium-potassium ...
*  Purinergic signalling
... leading to an accumulation of adenosine. On the other hand, the adenosine-receptor antagonist caffeine reverses the anti- ... On the other hand, nanomolar concentrations of adenosine activate A1 and A3 receptors, resulting in neutrophilic chemotaxis ... In the airways of patients with asthma, the expression of adenosine receptors is upregulated. Adenosine receptors affect ... the expression of adenosine receptors on the neutrophil, and the affinity of these receptors for adenosine. Micromolar ...
*  Adrenergic receptor
Antagonists may be used primarily in hypertension, anxiety disorder, and panic attacks. The α2 receptor couples to the Gi/o ... 81 (1): 211.e1-7. doi:10.1016/j.urology.2012.09.011. PMID 23200975. Fitzpatrick D, Purves D, Augustine G (2004). "Table 20:2". ... "Convergence of major physiological stimuli for renin release on the Gs-alpha/cyclic adenosine monophosphate signaling pathway ... a Gq coupled receptor) and α2 (a Gi coupled receptor). Phenylephrine is a selective agonist of the α receptor. β receptors have ...
*  Arachidonate 5-lipoxygenase
Montelukast, Zafirlukast, and Pranlukast are receptor antagonists for the Cysteinyl leukotriene receptor 1 which contributes to ... Leukotriene-A4 hydrolase), or are the cellular receptors responsible for mediating the cellular responses to the down-stream ... may serve as a mobile lid over ALOX5's substrate-binding site An Adenosine triphosphate (ATP) binding site; ATP is crucial for ... as well as of LTC4 and LTD4 receptor antagonists have proven inferior to corticosteroids as single drug therapy for persistent ...
*  Prostaglandin EP3 receptor
These Receptor antagonist, which block EP3 from responding to PGE2 or other agonists of this receptor, include Sulprostone, DG- ... Prostaglandin E1 (PGE1), which has one less double bond than PGE2, has the same binding affinity and potency for EP3 as PGE2. ... and pathways that inhibit adenyl cyclase which thereby lowers cellular levels of cyclic adenosine monophosphate (cAMP) to ... Eicosanoid receptor Prostaglandin E2 receptor 1 (EP1) Prostaglandin E2 receptor 2 (EP2) Prostaglandin E2 receptor 4 (EP4) ...
*  History of catecholamine research
J. W. Black; A. F. Crowther; R. G. Shanks; A. C. Dornhorst (1964). "A new adrenergic beta-receptor antagonist". The Lancet. 283 ... A. Vulpian (1856). "Note sur quelques réactions propres à la substance des capsules surrénales". Comptes Rendus de l'Académie ... In addition the vesicles contained adenosine triphosphate (ATP), with a molar noradrenaline:ATP ratio in sympathetic nerve ... he called alpha adrenotropic receptor (now α-adrenoceptor or α-adrenergic receptor), while the receptor with the second rank ...
*  Cannabinoid receptor type 1
Endogenous CB1 antagonist and CB2 agonist) Rimonabant Taranabant Lipoxin A4 - endogenous, PAM ZCZ-011 - PAM Pregnenolone - ... Through its primary action as a Gi coupled receptor, CB1 inhibits production of cyclic adenosine monophosphate (cAMP), ... Discovery and development of Cannabinoid Receptor 1 Antagonists Cannabinoid receptor Cannabinoid receptor type 2 (CB2) GRCh38: ... As a consequence, CB1 receptor antagonists can reduce drug seeking behavior in some addicts. The CB1 receptor is expressed by a ...
*  Mechanism of anoxic depolarization in the brain
... involve sigma-1 receptor ligands, to modulate Ca2+ release, NMDA receptor antagonists, to prevent Ca2+ overload, and ion ... This compensatory stimulation of glycolysis occurs because, in the turtle's brain, cytochrome a and a3 have a low affinity for ... the turtle's brain reduces its ATP consumption by suppressing its neuronal activity and gradually releasing adenosine. This re- ... They include the NMDA receptors, AMPA receptors, P2X7 purinergic receptors, pannexin channels (Panx1), transient receptor ...
*  Cannabinoid receptor type 2
Cannabinoid receptor agonists reduce gut motility in IBS patients. Application of CB2-specific antagonists has found that these ... CB2 receptor agonists cause a reduction in the intracellular levels of cyclic adenosine monophosphate (cAMP). Although the ... 11: e3. doi:10.1017/S1462399409000957. PMC 2768535 . PMID 19152719. Galiègue S, Mary S, Marchand J, Dussossoy D, Carrière D, ... Unlike the CB1 receptor, in the brain, CB2 receptors are found primarily on microglia. The CB2 receptor is expressed in some ...
*  Portopulmonary hypertension
2005;128:164-8 Wilkins et al.Sildenafil versus Endothelin Receptor Antagonist for Pulmonary Hypertension (SERAPH) study. Am J ... Prostacyclin and Prostaglandin E1: Molecular mechanisms and therapeutic utility. Prog Hemostasis Thrombosis 1991;10:307-37 Vane ... Another drug, Milrinone, a Type 3 PDE-i increases vascular smooth muscle adenosine-3,5-cyclic monophosphate concentrations to ... Use of a mixed endothelin receptor antagonist in portopulmonary hypertension: a safe and effective therapy? Gastroenterology. ...
*  12-Hydroxyheptadecatrienoic acid
Hicks, A; Monkarsh, S. P.; Hoffman, A. F.; Goodnow Jr, R (2007). "Leukotriene B4 receptor antagonists as therapeutics for ... subsequent studies showed that it was a high affinity receptor for the arachidonic acid metabolite, lipoxin A4, but also bound ... to inhibit platelet aggregation responses to various agents by stimulating platelets to raise their levels of Cyclic adenosine ... BLT1 receptor) and its low affinity BLT2 receptor (Kd=23 nM); both receptors are G protein coupled receptors that, when ligand- ...
*  Cannabidiol
... has been found to act as an antagonist of GPR55, a G protein-coupled receptor and putative cannabinoid receptor ... is most likely associated with an increase in the extracellular adenosine offer and signaling through adenosine A2A receptor. ... "Cannabis à faible teneur en THC et CBD". bag.admin.ch. Retrieved May 20, 2017. ... Cannabidiol has very low affinity for the cannabinoid CB1 and CB2 receptors but acts as an indirect antagonist of these ...