A selective A1R agonist
N6-Cyclopentyladenosine is a selective agonist at adenosine 1 receptors (A1Rs) (Kis = 2.3, 790, and 43 nM for A1R, A2R, and A3R receptors, respectively, in transfected CHO cells).[1],[2] When microinjected into the rat brainstem, it increases blood pressure and heart rate.[3] It is effective for pain in normal and nerve-injured rats and shows anticonvulsant activity in a rat model of generalized seizures.[4],[5]
Reference:
[1]. Klotz, K.-N. Adenosine receptors and their ligands. Naunyn-Schmiedeberg's Arch. Pharmacol. 362(4), 382-391 (2000).
[2]. Klotz, K.-N., Hessling, J., Hegler, J., et al. Comparative pharmacology of human adenosine receptor subtypes - characterization of stably transfected receptors in CHO cells. Naunyn-Schmiedeberg's Arch. Pharmacol. 357, 1-9 (1998).
[3]. Barraco, R.A., el-Ridi, M.R., Ergene, E., et al. Adenosine receptor subtypes in the brainstem mediate distinct cardiovascular response patterns. Brain Res. Bull. 26(1), 59-84 (1991).
[4]. Gong, Q.-J., Li, Y.-Y., Xin, W.-J., et al. Differential effects of adenosine A1 receptor on pain-related behavior in normal and nerve-injured rats. Brain Res. 1361, 23-30 (2010).
[5]. Jaishree, J., Kumaresan, S., Sudha, S., et al. Individual and combined effects of N6-cyclopentyladenosine, flunarizine and diazepam on aminophylline-induced recurrent generalized seizures in mice. Pol. J. Pharmacol. 55(4), 559-564 (2003).
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