57477-39-1 BRL-54443 57477-39-1

BRL54443

分子式：C14H18N2O   分子量：230.31

产品描述

BRL 54443是5-HT1E 和 5-HT1F受体激动剂，pKi分别为8.7和9.25, 对5-HT1A, 5-HT1B, 5-HT1D受体具有弱的结合亲和力。

靶点

5-HT1E

5-HT1F

5-HT1A

5-HT1B

5-HT1D

IC50

8.7 (pKi)

9.25 (pKi)

7.2 (pKi)

6.9 (pKi)

7.2 (pKi)

体外研究

BRL 54443 has also measurable affinity for the 5-HT2A receptor. BRL 54443 induces contraction with a −logEC50 of 6.52. Contraction caused by BRL 54443 is likely mediated through stimulation of 5-HT5-HT2A receptors.

体内研究

BRL 54443 induces an immediate dose-dependent maximal intragastric volume increase vs. saline.

溶解性

DMSO 46 mg/mL，水 <1 mg/mL，乙醇 2 mg/mL

稳定性

2年 -20°C粉状，6月-80°C溶于DMSO