γ-谷氨酰多巴和γ-谷氨酰多巴胺：对血糖水平的影响。

gamma-Glutamyl DOPA and gamma-glutamyl dopamine: effect on plasma glucose levels.

作者信息

Mizoguchi H, Orlowski M, Wilk S, Green J P

出版信息

Eur J Pharmacol. 1979 Aug 1;57(2-3):239-45. doi: 10.1016/0014-2999(79)90371-6.

Abstract

gamma-Glutamyl-L-3,4-dihydroxyphenylalanine (gamma-glutamyl DOPA) and gamma-glutamyldopamine (gamma-glutamyl DA) are kidney specific prodrugs. Their effect on plasma glucose levels in the rat was compared to that of L-DOPA and dopamine (DA) after a 30 min intravenous infusion. L-DOPA and DA induced hyperglycemia after 15 min of druginfusion. A more marked and protracted elevation of plasma glucose was observed after infusion of gamma-glutamyl DA. By gamma-glutamyl DOPA had no effect on plasma glucose levels in spite of the high accumulation of DA in the pancreas after this prodrug. Of the various dopamine produrgs studied only gamma-glutamyl DOPA was not hyperglycemic in doses that are known to increase renal plasma flow in the rat. A simplified new procedure for the synthesis of gamma-glutamyl DA is described.

摘要

γ-谷氨酰-L-3,4-二羟基苯丙氨酸（γ-谷氨酰多巴）和γ-谷氨酰多巴胺（γ-谷氨酰多巴胺）是肾脏特异性前体药物。在大鼠中，经30分钟静脉输注后，将它们对血浆葡萄糖水平的影响与左旋多巴和多巴胺（DA）的影响进行了比较。输注左旋多巴和多巴胺15分钟后会导致高血糖。输注γ-谷氨酰多巴胺后，观察到血浆葡萄糖有更显著且持久的升高。尽管该前体药物在胰腺中大量积累多巴胺，但γ-谷氨酰多巴对血浆葡萄糖水平没有影响。在所研究的各种多巴胺前体药物中，只有γ-谷氨酰多巴在已知能增加大鼠肾血浆流量的剂量下不会导致高血糖。描述了一种合成γ-谷氨酰多巴胺的简化新方法。