Adenosine

Four subtypes of adenosine receptors (ARs) have been identified among vertebrates so far (A1, A2A, A2B and A3). These receptors all have a distinctive pharmacological profile, tissue distribution and effector coupling[1]. All four members are coupled to a G-protein (A1 and A3 subtypes to Gi, and A2 subtypes to Gs (GPCR-A18)). 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. More specifically, A1 and A2A receptors play a role in regulating myocardial oxygen consumption and coronary blood flow. 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. Recently, clinical evidence was found for the A3 receptor to be involved in rheumatoid arthritis, among other myocardial functions.[2] Interestingly, evidence is growing for a certain role of adenosine receptors in the field of oncology.[3]


[1] InternationalUnion of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors—an update. B.B. Fredholm, A.P. Ijzerman, K.A. Jacobson, J. Linden, C.E. Muller. Pharmacol. Rev. 2011, 63, 1-34.
[2] Clinical evidence for utilization of the A3 adenosine receptor as a target to treat rheumatoid arthritis: data from a phase II clinical trial. MH Silverman et al. J. Rheumatol.2008, 35, 41-48.
[3] Adenosine receptors and cancer. Gessi S, Merighi S, Sacchetto V, Simioni C, Borea PA. Biochim Biophys Acta. 2011, 1808, 1400-12.

 

15 Item(s)

per page
Axon ID Name Description From price
1188 Adenosine amine congener Adenosine A1 agonist €125.00
2317 BAY 60-6583 Potent and highly selective A2BAR (Adenosine) agonist €125.00
1319 CGS 21680 hydrochloride Adenosine A2A agonist €95.00
1190 Chloroadenosine, 2- Adenosine A1 and A2A agonist €65.00
1287 GR 79236 Adenosine A1 agonist €120.00
1423 KW 6002 Adenosine A2A antagonist €85.00
2076 MRS 1523 Adenosine A3 receptor antagonist €120.00
1603 Rolofylline Adenosine A1 antagonist €85.00
1852 Rolofylline metabolite M1-cis Adenosine A1 antagonist €110.00
1851 Rolofylline metabolite M1-trans Adenosine A1 antagonist €110.00
1264 SCH 442416 Adenosine A2A antagonist €90.00
2283 SCH 442416, Desmethyl Radioligand precursor of the adenosine A2A antagonist SCH 442416 €300.00
1253 SCH 58261 Adenosine A2A antagonist €90.00
1265 SDZ-WAG 994 Adenosine A1 agonist €125.00
1193 UK 432097 Adenosine A2A agonist €145.00

15 Item(s)

per page
Please wait...