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*  Adenosine receptor
He W, Wilder T, Cronstein BN (2013) Rolofylline, an adenosine A1 receptor antagonist, inhibits osteoclast differentiation as an ... The adenosine receptors (or P1 receptors) are a class of purinergic G protein-coupled receptors with adenosine as endogenous ... The adenosine A1 receptor has been found to be ubiquitous throughout the entire body. This receptor has an inhibitory function ... Adenosine receptors play a key role in the homeostasis of bone. The A1 receptor has been shown to stimulate osteoclast ...
*  Adenosine A2A receptor
"Time and sex-dependent effects of an adenosine A2A/A1 receptor antagonist on motivation to self-administer cocaine in rats". ... 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 ... "Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor". Genomics. 11 (1 ...
*  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. ... 1999). "Cardiac myocytes rendered ischemia resistant by expressing the human adenosine A1 or A3 receptor". FASEB J. 12 (15): ... a novel ligand that demonstrates both adenosine A(2A) receptor agonist and adenosine A(3) receptor antagonist activity". ... is an adenosine receptor, but also denotes the human gene encoding it. Adenosine A3 receptors are G protein-coupled receptors ...
*  Adenosine A1 receptor
... an adenosine A1-receptor antagonist,on diuresis and renal function in patients with acute decompensated heart failure and renal ... The adenosine A1 receptor is one member of the adenosine receptor group of G protein-coupled receptors with adenosine as ... The adenosine A1 receptor has been found to be ubiquitous throughout the entire body. Activation of the adenosine A1 receptor ... "Adenosine Receptors: A1". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology ...
*  Dipropylcyclopentylxanthine
... is a drug which acts as a potent and selective antagonist for the adenosine A1 receptor. It has high selectivity for A1 over ... "Potent adenosine receptor antagonists that are selective for the A1 receptor subtype". Molecular Pharmacology. 31 (3): 247-52. ... Chwalczuk K, Rubaj A, Swiader M, Czuczwar SJ (2008). "[Influence of the antagonist of adenosine A1 receptors, 8-cyclopentyl-1 , ... a selective high affinity antagonist radioligand for A1 adenosine receptors". Naunyn-Schmiedeberg's Archives of Pharmacology. ...
*  Rolofylline
... (KW-3902) is an experimental diuretic which acts as a selective adenosine A1 receptor antagonist. It was discovered ... an adenosine A1-receptor antagonist, on diuresis and renal function in patients with acute decompensated heart failure and ... dose-finding study of the adenosine A1 receptor antagonist rolofylline in patients with acute heart failure and renal ...
*  Bamifylline
... is a drug of the xanthine chemical class which acts as a selective adenosine A1 receptor antagonist. Theophylline ... "Effects of A1 adenosine receptor blockade by bamiphylline on ischaemic preconditioning during coronary angioplasty" (PDF). ...
*  Cardiorenal syndrome
Givertz, M. M.; Massie B. M.; Fields T. K.; Pearson L. L. (2007). "The effects of KW-3902 an adenosine A1-receptor antagonist, ... It was found that an adenosine A1-receptor antagonist called KW-3902 was able to improve kidney function in CRS patients. ... Vasopressin antagonists Tolvaptan showed to have no benefit. It is also a very costly drug. Adenosine antagonists Adenosine is ...
*  ATL-444
... is a drug which acts as a potent and reasonably selective antagonist for the adenosine receptors A1 and A2A. It has ... "Time and sex-dependent effects of an adenosine A2A/A1 receptor antagonist on motivation to self-administer cocaine in rats". ... been used to study the role of the adenosine receptor system in the reinforcing action of cocaine. CGS-15943 Doyle, S. E.; ...
*  Diprophylline
Schwabe, U; Ukena, D; Lohse, MJ (September 1985). "Xanthine Derivatives as Antagonists at A1 and A2 Adenosine Receptors". ... It acts as an adenosine receptor antagonist and phosphodiesterase inhibitor. Xanthine "International Non-Proprietary Names. ...
*  CGS-15943
"Comparison of the behavioural effects of an adenosine A1/A2-receptor antagonist, CGS 15943A, and an A1-selective antagonist, ... CGS-15943 is a drug which acts as a potent and reasonably selective antagonist for the adenosine receptors A1 and A2A, having a ... Ki of 3.3nM at A2A and 21nM at A1. It was one of the first adenosine receptor antagonists discovered that is not a xanthine ... Holtzman SG (1991). "CGS 15943, a nonxanthine adenosine receptor antagonist: effects on locomotor activity of nontolerant and ...
*  Cartazolate
... activity as antagonists of A1- and A2-adenosine receptors". Biochemical Pharmacology. 37 (4): 655-64. doi:10.1016/0006-2952(88) ... It is also known to act as an adenosine antagonist at the A1 and A2 subtypes and as a phosphodiesterase inhibitor. Cartazolate ... "Perturbation of benzodiazepine receptor binding by pyrazolopyridines involves picrotoxinin/barbiturate receptor sites". Journal ... O'Brien, Robert (1986). Receptor binding in drug research. New York: Dekker. p. 519. ISBN 0-8247-7548-1. US Patent 3966746 ...
*  SCH-58261
Popoli P, Reggio R, Pèzzola A, Fuxe K, Ferré S (July 1998). "Adenosine A1 and A2A receptor antagonists stimulate motor activity ... SCH-58261 is a drug which acts as a potent and selective antagonist for the adenosine receptor A2A, with more than 50x ... Kuzmin A, Johansson B, Gimenez L, Ogren SO, Fredholm BB (February 2006). "Combination of adenosine A1 and A2A receptor blocking ... "The non-xanthine heterocyclic compound SCH 58261 is a new potent and selective A2a adenosine receptor antagonist". The Journal ...
*  8-Phenyltheophylline
... is a drug derived from the xanthine family which acts as a potent and selective antagonist for the adenosine receptors A1 and ... Howell LL; Morse WH; Spealman RD (September 1990). "Respiratory effects of xanthines and adenosine analogs in rhesus monkeys". ... Spealman RD (1988). "Psychomotor stimulant effects of methylxanthines in squirrel monkeys: relation to adenosine antagonism". ...
*  Caffeine
... is an antagonist at all four adenosine receptor subtypes (A1, A2A, A2B, and A3), although with varying potencies. The ... specifically the A1-D1 receptor heterodimer (this is a receptor complex with 1 adenosine A1 receptor and 1 dopamine D1 receptor ... a receptor complex composed of 1 adenosine A1 receptor and 1 adenosine A2A receptor) in the axon terminal of glutamate neurons ... this is a receptor complex with 2 adenosine A2A receptors and 2 dopamine D2 receptors). The A2A-D2 receptor heterotetramer has ...
*  Caffeine-induced anxiety disorder
Caffeine acts as an antagonist of adenosine A1 and A2A receptors. Adenosine is a normal neuromodulator that activates adenosine ... A1 receptors are paired with the G-proteins of Gi-1, Gi-2, Gi-3, Go1, and Go2. The g-proteins of A1 receptors continue to ... The actions of A1 and A2A receptors oppose each other but are both inhibited by caffeine due to its function as an antagonist. ... Adenosine acts on A1 receptors to decrease opening of N-type Ca2+ channels in some hippocampal neurons, and therefore decrease ...
*  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 ...
*  Purinergic signalling
... leading to an accumulation of adenosine. On the other hand, the adenosine-receptor antagonist caffeine reverses the anti- ... The other three adenosine receptors are involved in bone formation. In Alzheimer's disease (AD), the expression of A1 and A2A ... 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 ...
*  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 ...
*  SCH-442,416
Brain adenosine A2A receptor occupancy by a novel A1/A2A receptor antagonist, ASP5854, in rhesus monkeys: relationship to ... SCH-442,416 is a highly selective adenosine A2a subtype receptor antagonist. It is widely used in its 11C radiolabelled form to ... Adenosine A2A receptors and depression. Neurology. 2003 Dec 9;61(11 Suppl 6):S82-7. PMID 14663017 Matsuya T, Takuma K, Sato K, ... In vivo imaging of adenosine A2A receptors in rat and primate brain using [11C]SCH442416. European Journal of Nuclear Medicine ...
*  DMPX
... is a caffeine analog which displays affinity to A2 adenosine receptors, in contrast to the A1 subtype receptors. DMPX had 28× ... a potent and selective in vivo antagonist of adenosine analogs. Life Sci. 1988;43(21):1671-84. PMID 3193854. ...
*  8-Cyclopentyl-1,3-dimethylxanthine
... is a drug which acts as a potent and selective antagonist for the adenosine receptors, with some selectivity for the A1 ... "Involvement of adenosine A1 and A2A receptors in the motor effects of caffeine after its acute and chronic administration". ... relation to adenosine antagonism". Psychopharmacology. 95 (1): 19-24. doi:10.1007/bf00212759. PMID 3133696. Karcz-Kubicha M; ... receptor subtype, as well as a non-selective phosphodiesterase inhibitor. It has stimulant effects in animals with slightly ...
*  PPADS
... and adenosine A1 receptors. PPADS tetrasodium salt, Santa Cruz Biotechnology Ziganshin, AU (December 1993). "PPADS selectively ... PPADS (pyridoxalphosphate-6-azophenyl-2',4'-disulfonic acid) is a selective purinergic P2X antagonist. It is able to block ... It appears to be relatively selective for P2X receptors, having no appreciable activity at α1 adrenergic, muscarinic M2 and M3 ... Lambrecht, G. (1992). "PPADS, a novel functionally selective antagonist of P2 purinoreceptor mediated responses". European ...
*  Acupuncture
The anti-nociceptive effect of acupuncture may be mediated by the adenosine A1 receptor. A 2014 review in Nature Reviews Cancer ... and that it is possible to inhibit acupuncture's analgesic effects with the opioid antagonist naloxone. Mechanical deformation ... which then triggered nearby A1 receptors "caused more tissue damage and inflammation relative to the size of the animal in mice ... such studies unnecessarily muddled a finding that local inflammation can result in the local release of adenosine with ...
*  Pharmacodynamics
... adenosine receptor antagonist, on the negative inotropic action of A(1) adenosine receptor full agonists in isolated guinea pig ... Dhalla AK, Shryock JC, Shreeniwas R, Belardinelli L (2003). "Pharmacology and therapeutic applications of A1 adenosine receptor ... Hormone receptors Neuromodulator receptors Neurotransmitter receptors General anesthetics were once thought to work by ... Upon drug binding, receptors can elicit their normal action (agonist), blocked action (antagonist), or even action opposite to ...
*  Pre-Bötzinger complex
Adenosine modulates the preBötC output via activation of the A1 and A2A receptor subtypes. An adenosine A1 receptor agonist has ... most being selective agonists or antagonists to receptor subtypes on neurons in the vicinity. Since many of these neurons ... Effects of adenosine A1 receptor activation". BMC Neuroscience. 9: 95. doi:10.1186/1471-2202-9-95. PMC 2567986 . PMID 18826652 ... Another synthetic drug specific to the adenosine A2A receptor subtype is CGS-21680 that has been shown to cause apneas in 14- ...
*  Etazolate
It acts as a positive allosteric modulator of the GABAA receptor at the barbiturate binding site, as an adenosine antagonist of ... the A1 and A2 subtypes, and as a phosphodiesterase inhibitor selective for the PDE4 isoform. It is currently in clinical trials ... ISBN 3-7643-1837-6. Williams M, Jarvis MF (February 1988). "Adenosine antagonists as potential therapeutic agents". ... Zezula J, Slany A, Sieghart W (April 1996). "Interaction of allosteric ligands with GABAA receptors containing one, two, or ...