83928-76-1 吉哌隆

吉哌隆

英文名称:4,4-Dimethyl-1-(4-(4-(pyrimidin-2-yl)piperazin-1-yl)butyl)piperidine-2,6-dione
CAS:

83928-76-1

分子式:C19H29N5O2
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吉哌隆简介

Gepirone (INN) (current developmental code name TGFK07AD; proposed brand name Travivo) or gepirone hydrochloride (USAN) is an antidepressant and anxiolytic drug of the azapirone group that was synthesized by Bristol-Myers Squibb in 1986 and has been under development for the treatment of depression but has yet to be marketed. Like other azapirones, it acts as a selective partial agonist of the 5-HT1A receptor. Gepirone has been under development in the U.S. in an extended release form (referred to as gepirone ER), but despite completing phase III clinical trials and demonstrating efficacy, it has been rejected multiple times by the FDA during the drug approval process.
Gepirone was originally developed by Bristol-Myers Squibb, but was out-licensed to Fabre-Kramer in 1993. The U.S. Food and Drug Administration (FDA) rejected approval for gepirone in 2004. It was submitted for the preregistration (NDA) phase again in May 2007 after adding additional information from clinical trials as the FDA required in 2004. However, in 2007 it once again failed to convince the FDA of its qualities for treating anxiety and depression. In December 2015, the FDA once again gave gepirone a negative review for depression due to concerns of efficacy. However, in March 2016, the FDA reversed its decision and gave gepirone ER a positive review, clearing the way for the drug to finally gain market approval in the U.S.
In addition to its antidepressant and anxiolytic properties, gepirone has been found to improve symptoms of sexual dysfunction in men and women, similarly to the marketed 5-HT1A receptor agonist flibanserin. Moreover, the pro-sexual effects appear to be independent of its antidepressant and anxiolytic effects.
Unlike its relative buspirone, gepirone has negligible affinity for the D2 receptor (30- to 50-fold lower in comparison), and its efficacy in activating the 5-HT1A is greater than that of buspirone. However, similarly to buspirone, gepirone metabolizes into 1-(2-pyrimidinyl)piperazine, which is known to act as an antagonist of the α2-adrenergic receptor.

吉哌隆基本信息

中文名称 吉哌隆 英文名称 4,4-Dimethyl-1-(4-(4-(pyrimidin-2-yl)piperazin-1-yl)butyl)piperidine-2,6-dione
中文别名

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英文别名

4,4-dimethyl-1-[4-(4-pyrimidin-2-ylpiperazin-1-yl)butyl]piperidine-2,6-dione;

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CAS号 83928-76-1 分子式 C19H29N5O2
分子量 359.46600 精确质量 359.23200
PSA 69.64000 LOGP 1.49480

吉哌隆编号系统

MDL号 MFCD00868196

安全信息

海关编码:
2933990090
SDS 1.0 中文 展开
SDS 1.0 英文 展开
1H NMR : Predict展开

核磁图谱 1H NMR : Predict

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国家名称 海关编码 海关数据更新时间 操作
中国 2933990090 2019-03 申报要素
美国 2933999700 2019-03 概述
印度 29335990 2019-03 概述
欧盟 29339980 2019-03 概述
英国 2933998090 2019-03 概述
日本 293359400 2019-03 概述
韩国 2933592090 2019-03 概述
加拿大 2933590030 2019-03 概述
吉哌隆
CAS号:83928-76-1 分子式:C19H29N5O2 分子量:359.46600

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