GSK163090

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GSK163090 是一种特异性口服活性 5-HT1A/B/D 受体拮抗剂（5-HT1A/B/D 和多巴胺 D2/D3 的 pK 值：9.4/8.5/9.7 和 6.3/6.7）。

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).(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.

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 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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Endocrinology/Hormones

5-HT Receptor

5-HT1A|5-HT1B|5-HT1D|Dopamine

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844903-58-8

415.53

C25H29N5O

>98% (HPLC)

DMSO:14.29 mg/mL (34.39 mM; Need ultrasonic)

Cc1ccc(c(N2CCN(CCc3cccc(N(CCN4)C4=O)c3)CC2)ccc2)c2n1

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(-20℃)

With Ice Pack

≥ 2 years