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三肽醛,Boc-DPhe-Phe-Lysinal,是一种新型的垂体细胞钙离子通道抑制剂。

The tripeptide aldehyde, Boc-DPhe-Phe-Lysinal, is a novel Ca2+ channel inhibitor in pituitary cells.

作者信息

Makara G B, Rappay G, Garamvölgyi V, Nagy I, Dankó S, Bajusz S

机构信息

Institute of Experimental Medicine, Hungarian Academy of Sciences, Budapest.

出版信息

Eur J Pharmacol. 1988 Jun 22;151(1):147-9. doi: 10.1016/0014-2999(88)90706-6.

Abstract

The effect of Boc-DPhe-Phe-Lysinal (Boc-DPPL) on the 45Ca2+ uptake of rat anterior pituitary monolayer cultures was investigated. The compound decreased the basal Ca2+ uptake at 3 x 10(-4) mol/l. The 45Ca2+ uptake stimulated by potassium-induced depolarization was more sensitive to Boc-DPPL inhibition, a slight decrease was seen with 3 x 10(-6) mol/l and there was a half maximal inhibition at 3 x 10(-5) mol/l. Boc-DPPL is known to inhibit pituitary hormone release in similar concentrations, an effect might also be due to its calcium antagonist property.

摘要

研究了Boc-DPhe-Phe-Lysinal(Boc-DPPL)对大鼠垂体前叶单层培养物45Ca2+摄取的影响。该化合物在3×10(-4)mol/l时可降低基础Ca2+摄取。钾诱导的去极化刺激的45Ca2+摄取对Boc-DPPL的抑制更敏感,在3×10(-6)mol/l时可见轻微降低,在3×10(-5)mol/l时出现半数最大抑制。已知Boc-DPPL在相似浓度下可抑制垂体激素释放,这种作用可能也归因于其钙拮抗剂特性。

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