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GSK163090

CAS No. : 844903-58-8

MCE 国际站：GSK163090

产品活性：GSK163090 是一种有效的，选择性的和具有口服活性的 5-HT_1A/1B/1D 受体拮抗剂，pK_i 值分别为 9.4/8.5/9.7。GSK163090 抑制血清素再摄取转运蛋白 (SerT) 的功能活性，其 pK_i 值为 6.1。GSK163090 具有抗抑郁和抗焦虑活性。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：5-HT Receptor  |  Dopamine Receptor

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 (pIC₅₀=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).

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 ED₅₀ values ranging from 0.03 to 1 mg/kg.

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