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D2343

D2343用途

D2343 是一种 β2 肾上腺素能受体激动剂,也是一种 α1-肾上腺素能受体抑制剂。

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D2343名称

[ CAS 号 ]:
72734-63-5

[ 中文名 ]:
D2343

[ 英文名 ]:
D2343

[英文别名 ]:

d 2343
D2343

D2343生物活性

[ 描述 ]:

D2343 是一种 β2 肾上腺素能受体激动剂,也是一种 α1-肾上腺素能受体抑制剂。

[ 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 ]

β2-adrenoceptor[1] α1- adrenoceptor[1]

[体外研究]

D2343是一种化合物,具有与特布他林大致相同的β2-肾上腺素能受体-激动剂作用,并且还表现出α1-受体抑制活性[1]。 β2-激动剂和α1-拮抗药物D2343以浓度相关的方式抑制诱发的收缩,在9.6μM时有50％的作用[2]。

[体内研究]

已经将D2343与来自大鼠和兔子的雌激素化子宫制剂和来自同源物的子宫内膜条带中的β2-激动剂特布他林进行了比较。 D2343已经显示出能够使子宫肌肉松弛到与特布他林相同甚至更多的能力,特别是当这两种药物在兔子和大鼠的制剂中进行比较时[1]。

[参考文献]

[1]. Olsson OA, et al. The effects in myometrial preparations of D2343, a beta 2-adrenoceptor agonist possessing alpha 1-receptor blocking qualities. Acta Pharmacol Toxicol (Copenh). 1984 Nov;55(5):391-7.

[2]. Olsson OA, et al. The effect of D2343 in transmurally stimulated rabbit isthmus muscle. Acta Pharmacol Toxicol (Copenh). 1985 May;56(5):427-30.

[相关活性小分子]

D2343物理化学性质

[ 密度 ]:
1.116g/cm3

[ 沸点 ]:
506.8ºC at 760 mmHg

[ 分子式 ]:
C₂₀H₂₇NO₃

[ 分子量 ]:
329.43300

[ 闪点 ]:
260.3ºC

[ 精确质量 ]:
329.19900

[ PSA ]:
61.72000

[ LogP ]:
3.82610

[ 折射率 ]:
1.572

[ 储存条件 ]:
2-8℃

D2343毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DA4801500

CHEMICAL NAME :: Benzenemethanol, 4-hydroxy-alpha-(((3-(2-methoxyphenyl)-1,1-dimethylpr opyl)amino)methyl)-

CAS REGISTRY NUMBER :: 72734-63-5

LAST UPDATED :: 199703

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C20-H27-N-O3

MOLECULAR WEIGHT :: 329.48

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 :: 170 mg/kg

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

REFERENCE :: EPXXDW European Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #0004835

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 45 mg/kg

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

REFERENCE :: EPXXDW European Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #0004835

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 50 mg/kg

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

REFERENCE :: EPXXDW European Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #0004835

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 13 mg/kg

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

REFERENCE :: EPXXDW European Patent Application. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #0004835