2-chloro-N6-Cyclopentyladenosine (hydrate)

2-chloro-N6-Cyclopentyladenosine is an adenosine receptor agonist.1 It binds selectively to adenosine A1 receptors over A2A and A3 receptors with Ki values of 0.83, 2,300 and 42 nM, respectively, for the human recombinant receptors expressed in CHO cells. 2-chloro-N6-Cyclopentyladenosine decreases heart rate in isolated rat atria (EC50 = 8.2 nM) but does not affect vasodilation in bovine coronary arteries.2 It inhibits convulsions induced by isoniazid and pentylenetetrazole in mice when administered at a dose of 8.3 μmol/kg.3

|1. Cristalli, G., Camaioni, E., Costanzi, S., et al. Characterization of potent ligands at human recombinant adenosine receptors. Drug Develop. Res. 45(3‐4), 176-181 (1998).|2. Monopoli, A., Conti, A., Dionisotti, S., et al. Pharmacology of the highly selective A1 adenosine receptor agonist 2-chloro-N6-cyclopentyladenosine. Arzneimittelforschung 44(12), 1305-1312 (1994).|3. Concas, A., Santoro, G., Mascia, M.P., et al. Anticonvulsant doses of 2-chloro-N6-cyclopentyladenosine, an adenosine A1 receptor agonist, reduce GABAergic transmission in different areas of the mouse brain. J. Pharmacol. Exp. Ther. 267(2), 844-851 (1993).