化合物简介
Bretazenil (Ro16-6028) is an imidazopyrrolobenzodiazepine anxiolytic drug which is derived from the benzodiazepine family, and was invented in 1988. It is most closely related in structure to the benzodiazepine antagonist flumazenil, although its effects are somewhat different. It is classed as a high-potency benzodiazepine due to its high affinity binding to benzodiazepine binding sites where it acts as a partial agonist. Its profile as a partial agonist and preclinical trial data suggests that it may have a reduced adverse effect profile. In particular bretazenil has been proposed to cause a less strong development of tolerance and withdrawal syndrome. Bretazenil differs from traditional 1,4-benzodiazepines by being a partial agonist and because it binds to α1, α2, α3, α4, α5 and α6 subunit containing GABAA receptor benzodiazepine receptor complexes. 1,4-benzodiazepines bind only to α1, α2, α3 and α5 GABAA benzodiazepine receptor complexes.
基本信息
中文名称
溴他西尼
英文名称
Bretazenil
中文别名
英文别名
Ro-16-6028
CAS号
84379-13-5
分子式
C19H20BrN3O3
分子量
418.284
精确质量
417.069
PSA
64.43
LOGP
3.8187
编号系统
UNII
OSZ0E9DGOJ
物化性质
密度
1.56g/cm3
沸点
594.3ºC at 760 mmHg
闪点
313.2ºC
折射率
1.685
储存条件
2-8ºC
安全信息
安全说明
S22; S24/25
合成路线