Substituted pyrrolecarboxamide compounds are disclosed. These compounds are highly selective agonists, antagonists or inverse agonists for GABA
A
brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABA
A
brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Alzheimer's dementia, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABA
A
receptors in tissue samples.
揭示了取代
吡咯甲酰胺化合物。这些化合物是高度选择性的
GABAA脑受体的激动剂、拮抗剂或逆向激动剂,或者是
GABAA脑受体的激动剂、拮抗剂或逆向激动剂的前药,因此在焦虑、抑郁、阿尔茨海默病痴呆、睡眠和癫痫障碍、苯二氮卓类药物过量以及增强记忆的诊断和治疗中非常有用。此外,还提供了包括包装的药物组合物在内的制药组合物。该发明的化合物还可用作定位组织样本中
GABAA受体的探针。