CP-601927 是一种选择性的 α4β2 nAChR 部分激动剂(Ki=1.2 nM; EC50=2.6 μM)。CP-601927 具有良好的脑渗透性以及具有抗抑郁样特性。
CP-601927 is a selective α4β2 nicotinic acetylcholine receptor (nAChR) partial agonist (Ki=1.2 nM; EC50=2.6 μM). CP-601927 shows good brain penetration and antidepressant-like properties[1][2].
CP-601927 (0.125 mg/kg-1.5 mg/kg; i.p.; C57BL/6J male mice) has antidepressant-like activity in animal models[2].
[1]. Campion SN, et al. Toxicity study in juvenile rats with the α4β2 nicotinic acetylcholine receptor partial agonist CP-601,927. Birth Defects Res B Dev Reprod Toxicol. 2011;92(4):323-332.
[2]. Mineur YS, et al. α4β2 nicotinic acetylcholine receptor partial agonists with low intrinsic efficacy have antidepressant-like properties. Behav Pharmacol. 2011;22(4):291-299.
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