GSK163090

GSK163090 is a potent, selective and orally active 5-HT 1A/1B/1D receptor antagonist with pK i values of 9.4/8.5/9.7, respectively. GSK163090 inhibits the functional activity of serotonin reuptake transporter (SerT) with a pK i value of 6.1. GSK163090 has antidepressant and anxiolytic activities In Vitro GSK163090 (compound 36) is devoid of agonist activity at R1 receptors, but rather it demonstrates a moderate functional antagonismof the phenylephrineinduced contraction of rabbit aorta (pIC 50 =6.9). At 1 μM concentration, the ratio of the apparent permeabilities measured from basolateral-to-apical (BA) to apical-to-basolateral (AB) indicated that GSK163090 is a moderate P-glycoprotein (P-gp) substrate (BA/AB = 2.8). MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo In male Sprague-Dawley rats, GSK163090 (compound 36) treatment shows clear dose-dependent inhibition of the 8-OH-DPAT-induced hyperlocomotor activity (hLMA), with ED 50 values ranging from 0.03 to 1 mg/kg . MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:5-HT 1A Receptor 9.4 (pKi) 5-HT 1B Receptor 8.5 (pKi) 5-HT 1D Receptor 9.7 (pKi) D 2 Receptor 6.3 (pKi) D 3 Receptor 6.7 (pKi) 5-HT 2A Receptor 6 (pKi) 5-HT 2B Receptor 6.3 (pKi) 5-HT 2C Receptor 5.8 (pKi) Human 5-HT 6 Receptor

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