123882-89-3

RS 64459-193 is a compound with high affinity for the 5-HT1A binding site.

RS-64459-193 is a 5-HT1A receptor partial agonist with a Ki of 24.9 nM. RS-64459-193 also shows high affinity for 5-HT2C, 5-HT2A and 5-HT7 with pKi values of 6.87, 7.02, and 7.18, respectively. RS-64459-193 is almost devoid of activity at the m 5-HT3 receptor[1].

5-HT_1A Receptor: 24.9 nM (Ki, CHO cells); human 5-HT_1A Receptor: 7.6 (pKi, Sf9); human 5-HT_1A Receptor: 7.04 (pKi); 5-HT_2C Receptor: 6.87 (pKi); Rat 5-HT_2A: 7.02 (pKi); Human 5-HT₇ Receptor: 7.18 (pKi); 5-HT₃ Receptor: <4 (pKi)

[1] M Spedding, et al. Interaction of the anxiogenic agent, RS-30199, with 5-HT1A receptors: modulation of sexual activity in the male rat. Neuropharmacology. 1998 Jun;37(6):769-80. DOI:10.1016/s0028-3908(98)00065-3