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化合物简介
Terguride (INN), also known as trans-dihydrolisuride, is a serotonin receptor antagonist and dopamine receptor agonist of the ergoline family. It is approved for and used in the treatment of hyperprolactinemia. Terguride is an oral, potent antagonist of 5-HT2B and 5-HT2A (serotonin) receptors. Serotonin stimulates the proliferation of pulmonary artery smooth muscle cells, and induces fibrosis in the wall of pulmonary arteries. Together, this causes vascular remodeling and narrowing of the pulmonary arteries. These changes result in increased vascular resistance and PAH. Due to the potential anti-proliferative and anti-fibrotic activity of terguride, this potential medicine could offer the hope of achieving reversal of pulmonary artery vascular remodeling and attenuation of disease progression.
基本信息
CAS:37686-84-3
中文别名:特麦角脲;
英文别名:S(+)-TERGURIDE;tergurid;R-(+)-TERGURIDE;Teluron;trans-Dihydro Lisuride;(5R,8S,10R)-Terguride;trans-9,10-Dihydrolisuride hydrogen maleate;TDHL;terguride;dironyl;9,10a-Dihydrolisuride;1,1-diethyl-3-(6-methyl-ergolin-8-yl)-urea;
分子式:C20H28N4O
分子量:340.463
精确质量:340.226
Psa:51.37
Logp:3.2605
中文别名:特麦角脲;
英文别名:S(+)-TERGURIDE;tergurid;R-(+)-TERGURIDE;Teluron;trans-Dihydro Lisuride;(5R,8S,10R)-Terguride;trans-9,10-Dihydrolisuride hydrogen maleate;TDHL;terguride;dironyl;9,10a-Dihydrolisuride;1,1-diethyl-3-(6-methyl-ergolin-8-yl)-urea;
分子式:C20H28N4O
分子量:340.463
精确质量:340.226
Psa:51.37
Logp:3.2605
编号系统
UNII:21OJT43Q88
物化性质
密度:1.21g/cm3
沸点:588ºC at 760 mmHg
闪点:309.4ºC
折射率:1.639
沸点:588ºC at 760 mmHg
闪点:309.4ºC
折射率:1.639
安全信息
危险品运输编码:UN 2811 6.1/PG 2
生产方法及用途
合成路线
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参考文献
Sauer; Haffer; Wachtel Synthesis, 1986 , vol. No. 12, p. 1007 - 1010
上游原料
下游产品
图谱
13C NMR : Predict









