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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.

PMID:921400
Abstract

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.

摘要

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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Arch Int Pharmacodyn Ther. 1977 Jul;228(1):30-8.
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