化合物信息

Description

BMY 7378 is a multiple inhibitors of α_2C-adrenoceptor and α_1D-adrenoceptor with pK_i of 6.54 and 8.2, respectively.

Targets

IC₅₀

In Vitro

BMY 7378 shows 10-fold selectivity for α_2C-adrenoceptors over other α₂-adrenoceptors with pKi of 6.54. ^[1] 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 ^[2] BMY 7378 at concentration of 1 nM to 30 nM elicits inhibitory effects in a concentration-dependent manner in the rat dorsal raphe nucleus. ^[3]

In Vivo

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).^[1] 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. ^[4]

Clinical Trials

Features

Description