单胺氧化酶抑制剂对大鼠脑内去甲肾上腺素体外摄取与释放的影响。
Influence of MAO inhibitors on uptake and release of norepinephrine in rat brain in vitro.
作者信息
Ziance R J, Moxley K, Mullis M, Gray W
出版信息
Arch Int Pharmacodyn Ther. 1977 Jul;228(1):30-8.
MAO inhibitors of diverse chemical structures were found to inhibit the uptake of 3H-NE into chopped rat cerebral cortex in vitro. The following molar (M) IC50 values to inhibit 3H-NE uptake were obtained: iproniazid, 7.9 X 10(-4)M; pargyline, 3.1 X 10(-4)M; pheniprazine, 6.3 X 10(-6)M; phenelzine, 3.9 X 10(-6)M; tranylcypromine, 2.5 X 10(-6)M; amphetamine, 2.5 X10(-7)M. In addition to decreasing deaminative catabolism, 5 X 10(-5)M amphetamine, tranylcypromine and pheniprazine plus 10(-3)M phenelzine produced a release of 3H-NE from tissue stores into incubation media. Similar concentrations of pargyline and iproniazid were ineffective to release 3H-NE from brain tissue.
研究发现，多种化学结构的单胺氧化酶（MAO）抑制剂在体外可抑制³H-去甲肾上腺素（³H-NE）被切碎的大鼠大脑皮层摄取。获得了以下抑制³H-NE摄取的半数抑制浓度（IC50）摩尔（M）值：异烟肼，7.9×10⁻⁴M；帕吉林，3.1×10⁻⁴M；苯乙肼，6.3×10⁻⁶M；苯乙肼，3.9×10⁻⁶M；反苯环丙胺，2.5×10⁻⁶M；苯丙胺，2.5×10⁻⁷M。除了减少脱氨基分解代谢外，5×10⁻⁵M苯丙胺、反苯环丙胺和苯乙肼加10⁻³M苯乙肼可使³H-NE从组织储存中释放到孵育培养基中。类似浓度的帕吉林和异烟肼无法从脑组织中释放³H-NE。
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