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溴莫尼定

溴莫尼定用途

Brimonidine (UK 14304) 是完全的α2肾上腺素受体激动剂。

溴莫尼定名称

[ CAS 号 ]:
59803-98-4

[ 中文名 ]:
溴莫尼定

[ 英文名 ]:
Brimonidine

[中文别名 ]:

[英文别名 ]:

brimonidinum
5-bromo-6-(imidazolin-2-ylamino)-quinoxaline
MFCD00153878
Brimonidine [INN:BAN]
Bromoxidine
Brimonidine
5-bromo-6-(2-imidazolin-2-ylamino)quinoxaline
UNII-E6GNX3HHTE
[3H]-Brimonidine
UK 14,304

溴莫尼定生物活性

[ 描述 ]:

Brimonidine (UK 14304) 是完全的α2肾上腺素受体激动剂。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体

研究领域 >> 其他

[ 靶点 ]

α2-adrenergic Receptor.

[体外研究]

[3H]溴莫尼定(UK 14304)是α2-肾上腺素能受体的完全激动剂。 [3H]溴莫尼定(UK 14304)标记人脑中至少2个特异性结合位点,它们都具有α2-肾上腺素能结合位点的特征。 GTP降低了这两个位点的激动剂结合,但在每个位点具有不同的效力[1-3]。

[参考文献]

[1]. Andorn, A.C., M.A. Carlson, and R.C. Gilkeson, Specific [3H]UK 14,304 binding in human cortex occurs at multiple high affinity states with alpha 2-adrenergic selectivity and differing affinities for GTP. Life Sci, 1988. 43(22): p. 1805-12.

[2]. Cambridge, D., UK-14,304, a potent and selective alpha2-agonist for the characterisation of alpha-adrenoceptor subtypes. Eur J Pharmacol, 1981. 72(4): p. 413-5.

[3]. Chopin, P., F.C. Colpaert, and M. Marien, Effects of alpha-2 adrenoceptor agonists and antagonists on circling behavior in rats with unilateral 6-hydroxydopamine lesions of the nigrostriatal pathway. J Pharmacol Exp Ther, 1999. 288(2): p. 798-804.

[相关活性小分子]

溴莫尼定物理化学性质

[ 密度 ]:
1.8±0.1 g/cm3

[ 沸点 ]:
432.6±55.0 °C at 760 mmHg

[ 熔点 ]:
207.5 °C

[ 分子式 ]:
C₁₁H₁₀BrN₅

[ 分子量 ]:
292.135

[ 闪点 ]:
215.4±31.5 °C

[ 精确质量 ]:
291.011963

[ PSA ]:
62.20000

[ LogP ]:
0.96

[ 外观性状 ]:
黄色固体

[ 蒸汽压 ]:
0.0±1.0 mmHg at 25°C

[ 折射率 ]:
1.798

[ 储存条件 ]:
Store at RT

[ 水溶解性 ]:
45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: <0.8 mg/mL

溴莫尼定MSDS

详细MSDS(安全技术说明书)

溴莫尼定毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: VD1200000

CHEMICAL NAME :: 6-Quinoxalinamine, 5-bromo-N-(4,5-dihydro-1H-imidazol-2-yl)-

CAS REGISTRY NUMBER :: 59803-98-4

LAST UPDATED :: 199612

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C11-H10-Br-N5

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 :: 160 mg/kg

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

REFERENCE :: JKXXAF Japanese Kokai Tokyo Koho Patents. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #81-02912

溴莫尼定安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301

[ 警示性声明 ]:
P301 + P310

[ 危害码 (欧洲) ]:
T:Toxic;

[ 风险声明 (欧洲) ]:
R25;R36/37/38

[ 安全声明 (欧洲) ]:
S26-S36-S45

[ 危险品运输编码 ]:
UN 2811 6.1/PG 3

[ WGK德国 ]:
-

[ RTECS号 ]:
VD1200000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1

[ 海关编码 ]:
2934999090

溴莫尼定上下游产品

溴莫尼定上游产品

溴莫尼定下游产品

溴莫尼定制备

5-溴-6-喹啉胺和硫氰酸铵缩合后，生成物再和乙二胺环合，得到溴莫尼定。

溴莫尼定海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 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

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

溴莫尼定文献

A Comparison of the Anorectic Effect and Safety of the Alpha2-Adrenoceptor Ligands Guanfacine and Yohimbine in Rats with Diet-Induced Obesity.

PLoS ONE 10 , e0141327, (2015)

The search for drugs with anorectic activity, acting within the adrenergic system has attracted the interest of researchers. Partial α2-adrenoceptor agonists might offer the potential for effective an...

Brimonidine reduces TGF-beta-induced extracellular matrix synthesis in human Tenon's fibroblasts.

BMC Ophthalmol. 15 , 54, (2015)

Brimonidine is a highly selective α2 adrenergic agonist that has been widely used in anti-glaucoma eyedrops. The aim of this study was to investigate its putative anti-fibrotic role in the fibrosis ca...

Dilute brimonidine to improve patient comfort and subconjunctival hemorrhage after LASIK.

J. Refract. Surg. 29(7) , 469-75, (2013)

To investigate whether dilute brimonidine (0.025%) reduces patient discomfort, subconjunctival hemorrhage, and injection after LASIK without a significant increase in the rate of flap complications or...

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