GSK163090 是选择性和具有口服活性的5-HT1A/1B/1D受体拮抗剂，pKi值分别为 9.4、8.5 和 9.7。它抑制血清素再摄取转运蛋白的功能活性，pKi值为 6.1，具有抗抑郁和抗焦虑活性。

GSK163090 is a specific and orally active 5-HT1A/B/D receptor antagonist (pKis: 9.4/8.5/9.7, and 6.3/6.7 for 5-HT1A/B/D, and dopamine D2/D3).

GSK163090 demonstrates clear dose-dependent inhibition of the 8-OH-DPAT-induced hyper locomotor activity (hLMA), with ED50 values ranging from 0.03 to 1 mg/kg. GSK163090 was devoid of agonist activity at R1 receptors, but rather it demonstrated a moderate functional antagonism of the phenylephrine-induced contraction of rabbit aorta (pIC50: 6.9).

The superior quality of GSK163090 was further highlighted by its commendable in vivo pharmacokinetic profile in rats and its outstanding activity in the 5-HT1A PD model, where 50% efficacy was achieved at a blood concentration of 3 ng/mL.

844903-58-8

C25H29N5O

415.53

GSK163090

DMSO:14.29 mg/mL (34.39 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years