6-乙基-5,6,7,8-四氢-4H-噁唑并[4,5-d]氮杂-2-胺二盐酸盐

用途

盐酸阿泽派索(B-HT 933)是一种有效的选择性α2肾上腺素受体激动剂,其α2A-、α2B-和α2C肾上腺素受体亚型的PKI分别为8.3、7.6和7.5[1]。盐酸阿泽哌索可引起浓度依赖性的蠕动收缩抑制(IC50=78.72 nM)[2]。

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名称

[ CAS 号 ]:
36067-72-8

[ 中文名 ]:
6-乙基-5,6,7,8-四氢-4H-噁唑并[4,5-d]氮杂-2-胺二盐酸盐

[ 英文名 ]:
Azepexole dihydrochloride

生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 心血管疾病

研究领域 >> 内分泌

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体

[体外研究]

在正常血糖大鼠中,交感神经诱导的血管升压反应被1和3μg/kg剂量依赖性抑制。最小(静脉注射)盐酸阿泽派索,含10和30μg/kg。min Azepexole盐酸盐不产生进一步的抑制作用。在糖尿病大鼠中,电诱导的血管升压反应为：(i)1和3μg/kg不变。盐酸阿泽派索；(ii)通过10μg/kg在所有刺激频率下显著抑制。min B-HT 933二盐酸盐；和(iii)同样抑制(即超最大抑制)30μg/kg。min Azepexole盐酸盐[1]。

[参考文献]

[1]. Altamirano-Espinoza AH, et al. Specific role of α2A - and α2B -, but not α2C -, adrenoceptor subtypes in the inhibition of the vasopressor sympathetic out-flow in diabetic pithed rats. Basic Clin Pharmacol Toxicol. 2015;117(1):31-38.

物理化学性质

[ 密度 ]:
1.126g/cm3

[ 沸点 ]:
330.9ºC at 760mmHg

[ 分子式 ]:
C₉H₁₇Cl₂N₃O

[ 分子量 ]:
254.16

[ 闪点 ]:
153.9ºC

[ 精确质量 ]:
253.07500

[ PSA ]:
55.29000

[ LogP ]:
2.80040

MSDS

详细MSDS(安全技术说明书)

毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: RQ5831345

CHEMICAL NAME :: 4H-Oxazolo(4,5-d)azepin-2-amine, 5,6,7,8-tetrahydro-6-ethyl-, dihydrochloride

CAS REGISTRY NUMBER :: 36067-72-8

LAST UPDATED :: 199712

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C9-H15-N3-O.2Cl-H

MOLECULAR WEIGHT :: 254.19

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2210 mg/kg

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

REFERENCE :: USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4259342

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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 ]:
2

[ RTECS号 ]:
RQ5831345

文献

The role of several alpha(1)- and alpha(2)-adrenoceptor subtypes mediating vasoconstriction in the canine external carotid circulation.

Br. J. Pharmacol. 132 , 1292-1298, (2001)

1. It has recently been shown that both alpha(1)- and alpha(2)-adrenoceptors mediate vasoconstriction in the canine external carotid circulation. The present study set out to identify the specific sub...

Pharmacological evidence that alpha2A- and alpha2C-adrenoceptors mediate the inhibition of cardioaccelerator sympathetic outflow in pithed rats.

Eur. J. Pharmacol. 554(2-3) , 205-11, (2007)

It has been suggested that the alpha(2)-adrenoceptors mediating cardiac sympatho-inhibition in pithed rats closely resemble the pharmacological profile of the alpha(2A)-adrenoceptor subtype. However, ...

Evidence that some imidazoline derivatives inhibit peripherally the vasopressor sympathetic outflow in pithed rats.

Auton. Neurosci. 143(1-2) , 40-5, (2008)

Imidazoline derivatives (e.g. clonidine and moxonidine) and alpha(2)-adrenoceptor agonists (e.g. B-HT 933) have been shown to inhibit sympathetically-induced [(3)H]noradrenaline release in several iso...

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