上海一基提供BMY 7378 21102-95-4

BMY-7378
分子式：C22H31N3O3.2HCl   分子量：458.42
 
產(chǎn)品描述
BMY 7378是多靶點抑制劑，作用于α2C-adrenoceptor和α1D-adrenoceptor，pKi分別為6.54 和8.2,且作為混合型5-HT1A受體激動劑和拮抗劑，pKi為8.3。
靶點
α2C-adrenoceptor
α1D-adrenoceptor
       
IC50
6.54 (pKi)
8.2 (pKi)
       
體外研究
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.
體內(nèi)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
穩(wěn)定性
2年 -20°C粉狀，6月-80°C溶于DMSO
特征