SB-200646A 是第一个对 5-HT2B/2C 的选择性超过 5-HT2A 的拮抗剂，5-HT2B，5-HT2C 和 5-HT2A 的 pKi 值分别为 7.5、6.9 和 5.2。SB-200646A 具有口服活性，在体内具有电生理和抗焦虑特性。

SB-200646A is an orally active, selective antagonist of 5-HT2B/2C over 5-HT2A receptor with pKi of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A exerts anxiolytic and electrophysiological properties in vivo.

SB200646A (4 μM) abolishes the ethanol-induced increase in miniature inhibitory postsynaptic current (mIPSC) frequency and had no effect on basal mIPSC frequency.

SB-200646A (20 mg/kg; intravenous injection; daily; for 21 days; male albino Sprague-Dawley rats) treatment significantly decreases the number of spontaneously active ventral tegmental area (VTA) dopaminergic neurons. The i.v. administration of 4-16 mg/kg of SB-200646A significantly increases the firing rate and % events as bursts in spontaneously active VTA dopaminergic neurons and significantly increases the % events as burst in substantia nigra pars compacta (SNC) dopaminergic neurons[1].

143797-62-0

C15H15ClN4O

302.76

DMSO:225mg/mL (743.2mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years