Amoroso S, Di Renzo G, Taglialatela M, Canzoniero L M, Cragoe E J, Annunziato L
Department of Pharmacology, 2nd School of Medicine, University of Naples.
Biochem Pharmacol. 1991 May 1;41(9):1279-82. doi: 10.1016/0006-2952(91)90098-p.
Insulin dose-dependently inhibited tyrosine hydroxylase (TH) activity and increased intrasynaposomal pH (pHi) in rat striatal nerve endings. Both these effects of insulin on TH and pHi were prevented by the 5-(N-methyl-N-(guanidinocarbonylmethyl) amiloride (MGCMA), a putative selective inhibitor of the Na(+)-H+ antiporter. Interestingly when, by changing the extracellular pH (pHo), the pHi was increased, from 7.1 up to 7.5, an equivalent inhibition of TH activity occurred. The inhibitory action exerted from insulin on TH activity disappeared when the hormone was added to synaptosomes whose pHi was lowered to 6.83. Collectively, the results of the present study showed that insulin inhibited TH activity in striatal synaptosomes. This effect seems to involve the activation of the Na(+)-H+ antiporter. This exchange system once activated, may induce an intrasynaptosomal alkalinization, a condition in which TH activity is inhibited.
胰岛素呈剂量依赖性地抑制大鼠纹状体神经末梢中酪氨酸羟化酶(TH)的活性,并升高突触小体内pH值(pHi)。胰岛素对TH和pHi的这两种作用均被5-(N-甲基-N-(胍基羰基甲基))氨氯吡咪(MGCMA)所阻断,MGCMA是一种推测的Na(+)-H+反向转运体选择性抑制剂。有趣的是,当通过改变细胞外pH值(pHo)将pHi从7.1升高至7.5时,会出现对TH活性的等效抑制。当将胰岛素添加到pHi降至6.83的突触小体中时,胰岛素对TH活性的抑制作用消失。总体而言,本研究结果表明胰岛素抑制纹状体突触小体中的TH活性。这种作用似乎涉及Na(+)-H+反向转运体的激活。一旦该交换系统被激活,可能会诱导突触小体内碱化,在这种情况下TH活性会受到抑制。