BMY 7378 dihydrochloride

BMY 7378 dihydrochloride用途

BMY 7378是α1D肾上腺素受体(α1D-AR)的选择性拮抗剂。BMY 7378与表达克隆大鼠α1D-AR的膜结合的亲和力(Ki=2 nM)高于与克隆大鼠α1A-AR(Ki=800 nM)或仓鼠α1B-AR(Ki=600 nM)结合的亲和力>100倍。BMY 7378是一种5-HT1A受体部分激动剂[1][2]。

BMY 7378 dihydrochloride名称

[ CAS 号 ]:
21102-95-4

[ 中文名 ]:
8-[2-[4-(甲氧基苯基)-1-哌嗪]乙基]-8-氮杂螺[4.5]癸烷-7,9-二酮双盐酸盐

[ 英文名 ]:
BMY 7378 dihydrochloride

[中文别名 ]:

[英文别名 ]:

BMY 7378 dihydrochloride
MFCD00153771

BMY 7378 dihydrochloride生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 心血管疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

[ 靶点 ]

rat α1A-adrenergic receptor:800 nM (Ki)

hamster alpha1B-adrenergic receptor:600 nM (Ki)

rat alpha1D-adrenergic receptor:2 nM (Ki)

5-HT1A Receptor

[体外研究]

BMY 7378对α1D肾上腺素受体亚型(pKi：仓鼠α1b肾上腺素受体6.2,人α1b肾上腺素受体7.2；牛α1c肾上腺素受体6.1,人α1c肾上腺素受体6.6；大鼠α1D肾上腺素受体8.2,人α1D肾上腺素受体9.4)具有选择性,并对大鼠主动脉α1肾上腺素受体具有高亲和力(pA2,8.9)[2]。

[参考文献]

[1]. Piascik MT, et al. The specific contribution of the novel alpha-1D adrenoceptor to the contraction of vascular smooth muscle. J Pharmacol Exp Ther. 1995;275(3):1583-1589.

[2]. Goetz AS, et al. BMY 7378 is a selective antagonist of the D subtype of alpha 1-adrenoceptors. Eur J Pharmacol. 1995;272(2-3):R5-R6.

BMY 7378 dihydrochloride物理化学性质

[ 沸点 ]:
585.6ºC at 760 mmHg

[ 熔点 ]:
196.5-198.5 °C

[ 分子式 ]:
C₂₂H₃₃Cl₂N₃O₃

[ 分子量 ]:
458.422

[ 闪点 ]:
307.9ºC

[ 精确质量 ]:
457.189911

[ PSA ]:
53.09000

[ LogP ]:
4.07140

[ 外观性状 ]:
solid | white

[ 蒸汽压 ]:
1.07E-13mmHg at 25°C

[ 储存条件 ]:
Store at RT

[ 水溶解性 ]:
H2O: soluble

BMY 7378 dihydrochlorideMSDS

详细MSDS(安全技术说明书)

BMY 7378 dihydrochloride毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: GY3996000

CHEMICAL NAME :: 1,1-Cyclopentanediacetimide, N-(2-(4-(o-methoxyphenyl)-1-piperazinyl)ethyl)-, dihydrochloride

CAS REGISTRY NUMBER :: 21102-95-4

LAST UPDATED :: 199007

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C22-H31-N3-O3.2Cl-H

MOLECULAR WEIGHT :: 458.48

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 53600 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 12,876,1969

BMY 7378 dihydrochloride安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
GY3996000

[ 海关编码 ]:
2933599090

BMY 7378 dihydrochloride制备

BMY 7378 dihydrochloride海关

[ 海关编码 ]: 2933599090

[ 中文概述 ]:
2933599090. 其他结构上有嘧啶环的化合物(包括其他结构上有哌嗪环的化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933599090. other compounds containing a pyrimidine ring (whether or not hydrogenated) or piperazine ring in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

BMY 7378 dihydrochloride文献

The Alpha-1D Is the Predominant Alpha-1-Adrenergic Receptor Subtype in Human Epicardial Coronary Arteries

J. Am. Coll. Cardiol. 54 , 1137-45, (2009)

Objectives The goal was to identify alpha-1-adrenergic receptor (AR) subtypes in human coronary arteries.

Further investigation of the in vivo pharmacological properties of the putative 5-HT1A antagonist, BMY 7378.

Eur. J. Pharmacol. 176 , 331, (1990)

The present study examined the actions of the putative 5-HT1A antagonist BMY 7378 on central pre- and postsynaptic 5-HT1A function in the rat in vivo. Unlike the direct acting 5-HT1A agonist 8-hydroxy...

Novel benzodioxopiperazines acting as antagonists at postsynaptic 5-HT1A receptors and as agonists at 5-HT1A autoreceptors: a comparative pharmacological characterization with proposed 5-HT1A antagonists.

J. Pharmacol. Exp. Ther. 268 , 337-352, (1994)

The novel benzodioxopiperazines [4-(benzodioxan-5-yl)1-[2- (benzocyclobutane-1-yl)ethyl]piperazine] (S 14489), [4-(benzodioxan-5-yl)1-(indan-2-yl)piperazine)] (S 15535) and [4-(benzodioxan-5-yl)1-[2(i...

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