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合成促黑素细胞激素释放抑制因子(MIF)。第三部分:L-脯氨酰-N-甲基-D-亮氨酰-甘氨酰胺和MIF对生物胺代谢的影响。

Synthetic melanocyte stimulating hormone release-inhibiting factor (MIF). Part III: effect of L-prolyl-N-methyl-D-leucyl-glycinamide and MIF on biogenic amine turnover.

作者信息

Pugsley T A, Lippmann W

出版信息

Arzneimittelforschung. 1977;27(12):2293-6.

PMID:23796
Abstract

The effect of the factor that inhibits the release of melanocyte stimulating hormone (MSH), i.e., L-prolyl-L-leucyl-glycinamide (MIF), and L-prolyl-N-methyl-D-leucyl-glycinamide, an analog, on brain norepinephrine (NE), dopamine (DA) and serotonin (5-HT) turnover was examined in rats. The analog (40 mg/kg i.p.), in a fashion similar to MIF (40 and 5 mg/kg i.p.), increased brain DA turnover; only MIF (40 mg/kg i.p.) increased endogenous DA levels. The analog (40 and 5 mg/kg i.p.) decreased brain NE turnover; MIF at the same doses was ineffective. Neither MIF nor the analog affected rat brain 5-HT turnover or the 5-HTP-induced behavioural syndrome in the mouse. These results indicate that the analog, like MIF, exerts effects on central catecholamine turnover. The different biochemical profile of the analog compared to MIF may be importance with regard to potential clinical use in the treatment of Parkinson's disease and depression.

摘要

在大鼠中研究了抑制促黑素细胞激素(MSH)释放的因子,即L-脯氨酰-L-亮氨酰-甘氨酰胺(MIF)和类似物L-脯氨酰-N-甲基-D-亮氨酰-甘氨酰胺,对脑去甲肾上腺素(NE)、多巴胺(DA)和5-羟色胺(5-HT)周转的影响。该类似物(腹腔注射40mg/kg),以类似于MIF(腹腔注射40mg/kg和5mg/kg)的方式,增加了脑DA周转;只有MIF(腹腔注射40mg/kg)增加了内源性DA水平。该类似物(腹腔注射40mg/kg和5mg/kg)降低了脑NE周转;相同剂量的MIF无效。MIF和该类似物均未影响大鼠脑5-HT周转或小鼠中5-羟色氨酸诱导的行为综合征。这些结果表明,该类似物与MIF一样,对中枢儿茶酚胺周转有影响。与MIF相比,该类似物不同的生化特征可能对于帕金森病和抑郁症治疗的潜在临床应用具有重要意义。

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