Handy R L, Wallace P, Gaffen Z A, Whitehead K J, Moore P K
Biomedical Sciences Division, King's College, University of London.
Br J Pharmacol. 1995 Nov;116(5):2349-50. doi: 10.1111/j.1476-5381.1995.tb15078.x.
1-(2-trifluoromethylphenyl)imidazole (TRIM) is a potent inhibitor of neuronal (mouse cerebellar) and inducible (lung from endotoxin-pretreated rats) isoforms of nitric oxide synthase (NOS) with IC50 values of 28.2 microM and 27.0 microM, respectively. In contrast, TRIM is a poor inhibitor of bovine aortic endothelial NOS with an IC50 of 1057.5 microM. TRIM (10-50 mg kg-1) administered i.p. exhibits dose-related antinociceptive activity in the mouse (assessed as inhibition of late phase formalin-induced hindpaw licking behaviour) with an ED50 of 85.8 mumol kg-1. In contrast, TRIM (50 mg kg-1, i.p.) failed to influence mean arterial blood pressure in the urethane-anaesthetized mouse. Thus, TRIM may be of use as an experimental tool with which to investigate the biological roles of nitric oxide (NO) within the central nervous system.
1-（2-三氟甲基苯基）咪唑（TRIM）是一种强效的一氧化氮合酶（NOS）神经元型（小鼠小脑）和诱导型（来自内毒素预处理大鼠的肺）亚型抑制剂，其IC50值分别为28.2微摩尔和27.0微摩尔。相比之下，TRIM对牛主动脉内皮NOS的抑制作用较弱，IC50为1057.5微摩尔。腹腔注射TRIM（10 - 50毫克/千克）在小鼠中表现出剂量相关的抗伤害感受活性（通过抑制晚期福尔马林诱导的后爪舔舐行为评估），ED50为85.8微摩尔/千克。相比之下，TRIM（50毫克/千克，腹腔注射）未能影响乌拉坦麻醉小鼠的平均动脉血压。因此，TRIM可用作研究一氧化氮（NO）在中枢神经系统中生物学作用的实验工具。
