TIME-COURSE OF INHIBITION OF BRAIN NITRIC-OXIDE SYNTHASE BY 7-NITRO INDAZOLE
TIME-COURSE OF INHIBITION OF BRAIN NITRIC-OXIDE SYNTHASE BY 7-NITRO INDAZOLE
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DOI：
10.1097/00001756-199410000-00039
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发表时间：
1994-10-03
期刊：
影响因子：
1.7
通讯作者：
MARSDEN, CD
中科院分区：
文献类型：
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作者：
MACKENZIE, GM;ROSE, S;MARSDEN, CD
7-硝基茚唑（7-NI）对大鼠纹状体、小脑、海马、大脑皮层和嗅球一氧化氮合酶（NOS）的体外抑制作用，IC50值分别为0.68 +/- 0.01 μ M、0.64 +/- 0.03 μ M、1.53 +/- 0.05 μ M、0.93 +/- 0.04 μ M和1.05 +/- 0.02 μ M （n = 6）。大鼠腹腔或口服7-NI （30 mg kg(-1)）可抑制所有五个脑区的NOS酶活性（n = 5-6）。NOS抑制（在注射后0.5 h达到最大效果）是短暂的，在4 h（口服）或24 h（口服）时完全恢复。7-NI （30 mg kg(-1)，每4 h 1次，连续注射20 h）对24 h各脑区NOS酶活性的抑制作用为51 ~ 61%。在评价一氧化氮的中枢作用时，应考虑到7-NI在肠外给药后相对短暂的NOS抑制作用。
7-NITRO indazole (7-NI) inhibits rat striatal, cerebellar, hippocampal, cerebral cortex and olfactory bulb nitric oxide synthase (NOS) in vitro with IC50 values of 0.68 +/- 0.01 mu M, 0.64 +/- 0.03 mu M, 1.53 +/- 0.05 mu M, 0.93 +/- 0.04 mu M and 1.05 +/- 0.02 mu M respectively (n = 6). Intraperitoneal (i.p.) or oral administration of 7-NI (30 mg kg(-1)) to rats inhibited NOS enzyme activity measured ex vivo in all five brain regions (n = 5-6). NOS inhibition (maximal effect, 0.5 h post-injection) was transient with complete recovery at either 4 h (oral administration) or 24 h (i.p. administration). Repeated i.p. injection of 7-NI (30 mg kg(-1), every 4 h for 20 h) inhibited NOS enzyme activity at 24 h by 51-61% in all brain regions. The relatively transient NOS inhibitory effect of 7-NI following parenteral administration should be taken into account when using this drug to evaluate the central effects of nitric oxide.