A 5-HT7A and adrenergic α2 receptor antagonist
The transduction of neurobehavioral effects by serotonin (5-hydroxy tryptamine; 5-HT) is mediated by at least seven major 5-HT receptor subtypes. SB-269970 is a potent 5-HT7A antagonist (pKi = 8.9) that demonstrates >50-fold binding selectivity over 5-HT5A and >250-fold selectivity over 5-HT1, 5-HT2, 5-HT4, 5-HT6, adrenergic α1, dopamine D2, and dopamine D3 receptors.1 It is also reported to block adrenergic α2 receptors in guinea pig vas deferens.2 SB-269970 has been used to target the 5-HT7 receptor in the study of schizophrenia-like cognitive deficits.3
1.Lovell, P.J., Bromidge, S.M., Dabbs, S., et al.A novel, potent, and selective 5-HT7 antagonist: (R)-3-(2-(2-(4-Methylpiperidin-1-yl)ethyl)pyrrolidine-1-sulfonyl) phenol (SB-269970)J. Med. Chem.43(3)342-345(2000) 2.Foong, J.P.P., and Bornstein, J.C.5-HT antagonists NAN-190 and SB 269970 block α2-adrenoceptors in the guinea pigNeuroreport20(3)325-330(2009) 3.Nikiforuk, A., Kos, T., Fijal, K., et al.Effects of the selective 5-HT7 receptor antagonist SB-269970 and amisulpride on ketamine-induced schizophrenia-like deficits in ratsPLoS One8(6)1-12(2013)
动态评分
0.0