T-226296(T-226296) - 药物靶点：MCHR1_在研适应症：肥胖_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

MCHR1

作用机制

MCHR1抑制剂(黑色素浓缩激素受体-1抑制剂)

治疗领域

内分泌与代谢疾病

在研适应症

肥胖

非在研适应症-

原研机构

Takeda Pharmaceuticals LLC

在研机构

Takeda Chemical Industries Ltd.

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-

关联

100 项与 T-226296 相关的临床结果

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100 项与 T-226296 相关的转化医学

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100 项与 T-226296 相关的专利（医药）

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1

项与 T-226296 相关的文献（医药）

2006-07-01·European Journal of Pharmacology3区 · 医学

Lack of efficacy of melanin-concentrating hormone-1 receptor antagonists in models of depression and anxiety

3区 · 医学

Article

作者: Ana M. Basso ; Natalie A. Bratcher ; Marlon D. Cowart ; Chen Zhao ; Minghua Sun ; Martin Schmidt ; Gerard B. Fox ; Kelly B. Gallagher ; Anil Vasudevan ; Timothy A. Esbenshade ; Lynne E. Rueter ; Philip R. Kym ; Michael E. Brune ; Rajesh Iyengar ; Christine A. Collins ; Arthur A. Hancock ; Andrew J. Souers

The aim of this study was to validate melanin-concentrating hormone (MCH)-1 receptor antagonism as a potential treatment of mood disorders. We attempted to replicate the effects previously reported with SNAP-7941 and expanded the investigation to three other orally bioavailable MCH-1 receptor antagonists with good brain penetration. SNAP-7941 (3-30 mg/kg, i.p.) and T-226296 (5-60 mg/kg, p.o.) (+/- racemate), were evaluated in the rat forced swim and mouse tail suspension tests. (+)SNAP-7941 (3-10 mg/kg, p.o.) was also tested in a modified 5-min rat forced swim protocol as previously reported. A-665798 (3-30 mg/kg, p.o.) and A-777903 (3-30 mg/kg, p.o.) were tested in mouse tail suspension and rat Vogel tests. None of the compounds showed meaningful efficacy in the paradigms tested. The lack of efficacy with four structurally different MCH-1 receptor antagonists does not support a role for therapeutic treatment of depression/anxiety via this mechanism of action.

100 项与 T-226296 相关的药物交易

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