PF-04995274 是一种有效的、高亲和力的、具有口服活性的部分 5-羟色胺 4 受体 (5-HT4R) 激动剂。
货号:ajcx20040
CAS:1331782-27-4
分子式:C23H32N2O6
分子量：432.5
溶解度:Chloroform: 30 mg/ml,DMF: 20 mg/ml,DMF:PBS (pH 7.2) (1:4): 0.25 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

PF-04995274 is a partial agonist of the serotonin (5-HT) receptor subtypes 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E (Kis = 0.36, 0.46, 0.15, and 0.32 nM, respectively, in a radioligand binding assay).1 It increases cAMP levels in HEK293 cells expressing 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E receptors (EC50s = 0.47, 0.36, 0.37, and 0.26 nM, respectively, for the human recombinant receptors). PF-04995274 decreases scopolamine-induced increases in the distance traveled in the Morris water maze in rats when administered at a dose of 0.032 mg/kg.

|1. Brodney, M.A., Johnson, D.E., Sawant-Basak, A., et al. Identification of multiple 5•HT4 partial agonist clinical candidates for the treatment of alzheimer's disease. J. Med. Chem. 55(21), 9240-9254 (2012).