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GSK163090
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GSK163090图片
CAS NO:844903-58-8
包装与价格:
包装价格(元)
1 mg电议
5 mg电议
10 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
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。

产品描述

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).

体外活性

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).

体内活性

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.

Cas No.

844903-58-8

分子式

C25H29N5O

分子量

415.53

别名

GSK163090

储存和溶解度

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