21102-95-4 BMY 7378 21102-95-4BMY 7378

BMY 7378 21102-95-4BMY 7378

adrenoceptor，pKi分别为6.54 和8.2,且作为混合型5-HT1A受体激动剂和拮抗剂，pKi为8.3。
靶点
α2C-adrenoceptor
α1D-adrenoceptor
       
IC50
6.54 (pKi)
8.2 (pKi)
       
体外研究
BMY 7378 shows 10-fold selectivity for α2C-adrenoceptors over other α2-adrenoceptors with pKi of 6.54.BMY 7378 is selective for the α1D-adrenoceptor subtype (PKi: hamster α1b-adrenoceptor 6.2, human α1b-adrenoceptor 7.2; bovine α1c-adrenoceptor 6.1, human α1c-adrenoceptor 6.6; rat α1d-adrenoceptor 8.2, human α1d-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 approximay 100 times more potent than yohimbine (pA2 of 6.62) against contractions to noradrenaline in rat aorta. BMY 7378 (pA2 of 6.48) is approximay 10 times less potent than yohimbine (pA2 of 7.56) at antagonizing the contractile response to noradrenaline in human saphenous vein (α2C-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
特征