Jacobsen, E. Jon; TenBrink, Ruth E.; Stelzer, Lindsay S.; Belonga, Kenneth L.; Carter, Donald B.; Im, Haesook K.; Im, Wha Bin; Sethy, Vimala H.; Tang, Andy H. published the artcile< High-Affinity Partial Agonist Imidazo[1,5-a]quinoxaline Amides, Carbamates, and Ureas at the γ-Aminobutyric Acid A/Benzodiazepine Receptor Complex>, Category: chlorides-buliding-blocks, the main research area is imidazoquinoxaline carbamate carboxamide preparation benzodiazepine receptor; anxiolytic imidazoquinoxaline carbamate carboxamide preparation; cyclopropyl oxadiazolyl imidazoquinoxalinecarboxamide preparation; urea imidazoquinoxaline preparation benzodiazepine receptor.
A series of imidazo[1,5-a]quinoxaline amides, carbamates, and ureas which have high affinity for the γ-aminobutyric acid A/benzodiazepine receptor complex was developed. Compounds within this class have varying efficacies ranging from antagonists to full agonists. However, most analogs were found to be partial agonists as indicated by [35S]TBPS and Cl- current ratios. Many of these compounds were also effective in antagonizing metrazole-induced seizures in accordance with anticonvulsant and possible anxiolytic activity. Selected quinoxalines displayed limited benzodiazepine-type side effects such as ethanol potentiation and phys. dependence in animal models. An interesting analog was 3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-N,N-dimethylimidazo[1,5-a]quinoxaline-5(4H)-carboxamide which has a partial agonist profile in vitro while possessing useful activity in animal models of anxiety such as the Vogel and Geller assays. In accordance with its partial agonist profile, 3-(5-cyclopropyl-1,2,4-oxadiazol-3-yl)-N,N-dimethylimidazo[1,5-a]quinoxaline-5(4H)-carboxamide was devoid of typical benzodiazepine side effects.
Journal of Medicinal Chemistry published new progress about Anxiolytics. 55687-19-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H5ClN2O, Category: chlorides-buliding-blocks.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics