Pharmacology of the highly selective A1 adenosine receptor agonist 2-chloro-N6-cyclopentyladenosine.

摘要: The pharmacological profile of 2-chloro-N6-cyclopentyladenosine (CCPA, CAS 37739-05-2), a highly selective A1 adenosine receptor agonist, was characterized. Its effects were compared with those the non-selective agonist 5'-N-ethylcarboxamidoadenosine (NECA). In binding studies on both rat and bovine brain, CCPA potent receptors (Ki = 1.3 0.5 nmol/l, respectively) displayed good vs A2a selectivity (500- 920-fold, respectively). functional studies, showed marked negative chronotropic activity in spontaneously beating atria (EC50 8.2 nmol/l). This effect antagonized dose-dependently by antagonist 8-cyclopentyl-1,3-dipropylxanthine (DPCPX). Langendorff model, which global ischemia induced, (3 nmol/l) prevented significantly rise diastolic pressure coronary perfusion during postischemic reperfusion. vascular preparations, responsive to stimulation, did not show any vasodilating properties up micromolar concentrations, whereas NECA had relaxing arteries 167 rabbit platelets, model sensitive only A2a-receptor elicit relevant antiaggregatory properties, found be effective (IC50 200 Likewise, an vivo platelet aggregation using non-invasive radioisotopic technique, (100 micrograms/kg, 30 min i.v. infusion) influence function, (10 decreased peak value for accumulation 35%.(ABSTRACT TRUNCATED AT 250 WORDS)