Kaiser F C, Palmer G C, Wallace A V, Carr R D, Fraser-Rae L, Hallam C
Department of Biology, Fisons Corporation, Research and Development, Rochester, NY 14603.
Neuroreport. 1992 Oct;3(10):922-4. doi: 10.1097/00001756-199210000-00026.
The angiotensin II receptor antagonist, DUP 753 (Losartan), was compared with diazepam for antianxiety properties in the rat using the elevated plus-maze. Oral diazepam (5 mg kg-1) resulted in a significantly greater number of entries of rats into the open arms of the maze, an increase in time spent in the open arms and a decreased time spent in the closed arms. Oral doses of DUP 753 likewise resulted in significantly greater numbers of entries into the open arms (active at 0.0001, 0.001, 0.01 and 0.1 mg kg-1), increased time spent on the open arms (active at 0.0001-0.01 mg kg-1) and a decreased time spent in the closed arms (active at 0.0001, 0.01 and 0.1 mg kg-1). Larger (1.0 mg kg-1) or smaller (0.00001 mg kg-1) doses of DUP 753 were not active.
使用高架十字迷宫,将血管紧张素II受体拮抗剂DUP 753(氯沙坦)与地西泮在大鼠体内的抗焦虑特性进行了比较。口服地西泮(5毫克/千克)使大鼠进入迷宫开放臂的次数显著增加,在开放臂停留的时间增加,在封闭臂停留的时间减少。口服不同剂量的DUP 753同样使进入开放臂的次数显著增加(在0.0001、0.001、0.01和0.1毫克/千克时具有活性),在开放臂停留的时间增加(在0.0001 - 0.01毫克/千克时具有活性),在封闭臂停留的时间减少(在0.0001、0.01和0.1毫克/千克时具有活性)。更大剂量(1.0毫克/千克)或更小剂量(0.00001毫克/千克)的DUP 753没有活性。