Paruszewski R, Kłodzińska A, Chojnacka-Wójcik E
Department of Drug Chemistry, Medical University, Warszawa, Poland.
Pharmazie. 1998 Feb;53(2):124-5.
Three derivatives of amino acids: (R)-Ac-Pro-BZA (1), Ac-beta Ala-BZA (2) and (S)-Ac-Arg(NO2)-BZA (3) were evaluated as potential anxiolytics. In the conflict drinking test in rats used as a model of anxiety, the tested compounds exhibited anxiolytic-like activity. Compounds 1 and 2 administered in doses of 50-100 mg/kg produced an anticonflict effect in a dose-dependent manner. A distinct effect is observed after dose of 100 mg/kg of 1 and 2, comparable to those induced by 10 mg/kg of diazepam. The anticonflict effect of 3 was weak and dose independent. It was revealed only in one mean dose (50 mg/kg) but not in the higher doses.
(R)-Ac-Pro-BZA(1)、Ac-β-Ala-BZA(2)和(S)-Ac-Arg(NO2)-BZA(3)被评估为潜在的抗焦虑药。在用作焦虑模型的大鼠冲突饮水试验中,受试化合物表现出抗焦虑样活性。化合物1和2以50-100mg/kg的剂量给药时,以剂量依赖性方式产生抗冲突效应。在100mg/kg的1和2剂量后观察到明显的效应,与10mg/kg地西泮诱导的效应相当。3的抗冲突效应较弱且与剂量无关。仅在一个平均剂量(50mg/kg)时观察到该效应,而在更高剂量时未观察到。