BMY 7378 dihydrochloride,21102-95-4

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YZ剂描述：

产品名称：BMY 7378 dihydrochloride

产品别名：8-[2-[4-(基)-1-哌嗪]乙基]-8-氮杂螺[4.5]癸烷-7,9-二酮双盐酸盐

英文别名：BMY 7378 2HCl

靶点：5-HT1A ，α1D-adrenoceptor ，Dopamine D2 receptor ，α2C-adrenoceptor ,5-HT1C ，,

CAS：21102-95-4

纯度：98%

外观：白色粉末

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

BMY-7,378 is a 5-HT1A receptor weak partial agonist/antagonist and α1D-adrenergic receptor antagonist.

溶解性：DMSO : 85 mg/mL (185.4 mM)
Ethanol : 16 mg/mL (34.9 mM)
Water : 84 mg/mL (183.2 mM)

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 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 (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.

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