A 5-HT7A and adrenergic α2 receptor antagonist
SB269970 HCl is a potent and selective antagonist of 5-HT7 receptor with pKi value of 8.3 [1].
SB269970 is a selective antagonist of 5-HT7 receptor. It shows at least 100-fold selective against 5-HT7 over a variety of receptors and enzymes. SB269970 prevents 5-CT from binding to h5-HT7(a) in H293 cells and human cloned 5-HT7 receptor in guinea-pig cerebral cortex membranes with pKi values of 8.9 and 8.3, respectively. SB269970 also inhibits adenylyl cyclase activity stimulated by 5-CT both in 5-HT7(a)/ HEK293 (pA2 of 8.5) membranes and in guinea-pig hippocampus (pKB of 8.3). In vehicle-treated animals, SB269970 almost completely inhibits the 5-CT-induced hypothermia with ED50 value of 2.96mg/kg [1].
参考文献:
[1] Hagan J J, Price G W, Jeffrey P, et al. Characterization of SB-269970-A, a selective 5-HT7 receptor antagonist. British journal of pharmacology, 2000, 130(3): 539-548.
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