西洛巴明(Cilobamine) - 药物靶点：DAT x NET_在研适应症：抑郁症_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Clobamine

靶点

DAT x NET

作用机制

DAT拮抗剂(多巴胺转运体拮抗剂)、NET抑制剂(去甲肾上腺素转运蛋白抑制剂)

治疗领域

其他疾病

在研适应症

抑郁症

非在研适应症-

原研机构

Merrell Dow Pharmaceuticals, Inc.

在研机构

Merrell Dow Pharmaceuticals, Inc.

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C17H23Cl2NO

InChIKeyMQILJMOEUMZBHK-UHFFFAOYSA-N

CAS号69429-84-1

关联

100 项与西洛巴明相关的临床结果

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100 项与西洛巴明相关的转化医学

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100 项与西洛巴明相关的专利（医药）

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1

项与西洛巴明相关的文献（医药）

1984-04-01·Fundamental and Applied Toxicology

Dose related induction of the drug metabolizing enzymes of rat liver by cilobamine

Article

作者: Z. A. Shaath ; G. A. Leeson ; J. T. Yarrington ; S. A. Biedenbach ; R. A. Okerholm

Cilobamine , an antidepressant, was investigated for its influence on the hepatic drug metabolizing enzymes ( DME ) of male Charles River CD rats. Cilobamine doses (3, 10, 30, 100, and 300 mg/kg po, as free base) were compared to sodium phenobarbital (PB) doses (3, 10, 30, 100, and 200 mg/kg po, as free acid). Compounds were given daily for 4 days and all tests were done on Day 5. Ethylmorphine n-demethylase, aniline hydroxylase, microsomal cytochrome P-450 content, relative liver weight, and recoverable microsomal protein were quantitated. The results indicated that cilobamine was an inducer of the DME but not as potent as PB. Cilobamine did not exert any inductive responses at 3 mg/kg. At 10 and 30 mg/kg some but not all test systems were increased. However, at 100 and 300 mg/kg all were increased. PB increased all systems at all doses studied. Electron micrographs of livers of rats given 100 mg/kg of cilobamine or PB revealed hypertrophy of the smooth endoplasmic reticulum. The time course of induction in rats given 100 mg/kg po showed that responses in the cilobamine rats peaked after the second dose and plateaued with later doses. Responses in PB rats increased markedly after one dose and showed a continual increase with later doses. Induction of the DME was also demonstrated in female rats.

100 项与西洛巴明相关的药物交易

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