2-Chloro-N6-cyclopentyladenosine

2-Chloro-N6-cyclopentyladenosine是一种强效的和选择性的腺苷A1受体激动剂[1].

腺苷A1受体是腺苷的G蛋白偶联受体,在促进睡眠方面发挥着重要作用.2-Chloro-N6-cyclopentyladenosine (CCPA)是一种强效的和选择性的腺苷A1受体激动剂.CCPA抑制[3H]PIA与大鼠脑膜A1受体的结合及[3H]NECA与大鼠纹状体膜A2受体的结合,Ki值分别为0.4 和3900 nM.

另外,CCPA抑制大鼠脂肪细胞膜上的腺苷酸环化酶,IC50值为33 nM,且刺激人血小板膜上的腺苷酸环化酶活性,EC50值为3500 nM [1].在大鼠和牛的脑中,CCPA对A1受体具有高亲和力,Ki值分别为1.3和0.5 nM.在自发性跳动的大鼠心房中,CCPA抑制变时性活性,EC50值为8.2 nM [2].

在缺血/再灌注大鼠模型中,CCPA显著抑制冠状动脉灌注压和舒张压的升高[2].在兔体内,CCPA减少了40-50%的平均血压,且降低心率[3].在小鼠中,CCPA (1.4-27.6 mol/kg)增加A1受体介导的[35S]TBPS在黑质\海马\大脑皮层及纹状体膜的结合.CCPA减少GABA偶联氯离子通道功能,且诱发抗惊厥活性[4].

参考文献：
[1].  Lohse MJ, Klotz KN, Schwabe U, et al. 2-Chloro-N6-cyclopentyladenosine: a highly selective agonist at A1 adenosine receptors. Naunyn Schmiedebergs Arch Pharmacol, 1988, 337(6): 687-689.
[2].  Monopoli A, Conti A, Dionisotti S, et al. Pharmacology of the highly selective A1 adenosine receptor agonist 2-chloro-N6-cyclopentyladenosine. Arzneimittelforschung, 1994, 44(12): 1305-1312.
[3].  Concas A, Santoro G, Mascia MP, 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, 1993, 267(2): 844-851.
[4].  Sandoli D, Chiu PJ, Chintala M, et al. In vivo and ex vivo effects of adenosine A1 and A2 receptor agonists on platelet aggregation in the rabbit. Eur J Pharmacol, 1994, 259(1): 43-49.