产品分类

靶点

α_2C-adrenoceptor

α_1D-adrenoceptor

IC50

6.54 (pK_i)

8.2 (pK_i)

体外研究

BMY 7378 shows 10-fold selectivity for α_2C-adrenoceptors over other α₂-adrenoceptors with pKi of 6.54.BMY 7378 is selective for the α_1D-adrenoceptor subtype (PKi: hamster α_1b-adrenoceptor 6.2, human α_1b-adrenoceptor 7.2; bovine α_1c-adrenoceptor 6.1, human α_1c-adrenoceptor 6.6; rat α_1d-adrenoceptor 8.2, human α_1d-adrenoceptor 9.4.BMY 7378 at concentration of 1 nM to 30 nM elicits inhibitory effects in a concentration-dependent manner in the rat dorsal raphe nucleus.

体内研究

BMY 7378 (pA₂ of 8.67) is approximately 100 times more potent than yohimbine (pA₂ of 6.62) against contractions to noradrenaline in rat aorta. BMY 7378 (pA₂ of 6.48) is approximately 10 times less potent than yohimbine (pA₂ of 7.56) at antagonizing the contractile response to noradrenaline in human saphenous vein (α_2C-adrenoceptor).BMY 7378 dose dependently (0.25-5 mg/kg s.c.) reduces the undetectable levels forepaw treading and head weaving induced by 8-OH-DPAT (0.75 mg/kg s.c.) in rats. BMY 7378 causes a marked and dose-dependent (0.01-1.0 mg/kg s.c.) decrease of 5-HT release in ventral hippocampus of the anaesthetized rat as detected by brain microdialysis in rats.

溶解性

DMSO 92 mg/mL，水 92 mg/mL，乙醇 20 mg/mL

稳定性

2年 -20°C粉状，6月-80°C溶于DMSO