α-甲基氨基酸及其衍生物对离体组织标本的研究。

An investigation of alpha-methyl amino-acids and their derivatives on isolated tissue preparations.

作者信息

Gulati O D, Parikh H M, Ringe S Y, Sherlekar M L

出版信息

Br J Pharmacol. 1970 Dec;40(4):689-701. doi: 10.1111/j.1476-5381.1970.tb10647.x.

DOI:10.1111/j.1476-5381.1970.tb10647.x

PMID:5495174

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1702915/

Abstract

The ability of alpha-methyl amino-acids and their corresponding amines to restore the sympathomimetic actions of tyramine, and the uptake of the amino-acids and the amines, were studied in isolated tissue preparations obtained from reserpine pretreated animals.2. Tyramine relaxed isolated rat ileum preparations from non-reserpinized rats but not from reserpine treated animals. alpha-Methyldopa, alpha-methylnoradrenaline and lower concentrations of metaraminol restored the responses of reserpinized preparations. alpha-Methyldopamine, alpha-methyl-m-tyrosine, alpha-methyl-p-tyrosine and higher concentrations of metaraminol did not do so. The restoring effect of alpha-methyldopa was blocked by disulphiram. alpha-Methyl-p-tyrosine or alpha-methyl-m-tyrosine blocked the restoring action of alpha-methyldopa but not of alpha-methylnoradrenaline. Cocaine blocked the restoration of responses to tyramine by alpha-methylnoradrenaline but not by alpha-methyldopa. alpha-Methyldopa and alpha-methylnoradrenaline failed to restore responses to tyramine in the presence of sodium-free Tyrode solution.3. Tyramine increased the perfusion pressure in isolated rabbit ear preparations obtained from non-reserpinized animals but was very much less active in preparations obtained from reserpine treated animals. alpha-Methyldopa, alpha-methyl-m-tyrosine, alpha-methylnoradrenaline, alpha-methyl-p-tyrosine and metaraminol restored the effects of tyramine. alpha-Methyldopamine did not do so. The restoring effect of alpha-methyldopa and alpha-methyl-m-tyrosine was blocked by disulfiram. alpha-Methyl-p-tyrosine blocked the restoring effect of alpha-methyl-m-tyrosine.4. Tyramine produced positive inotropic effects in isolated rabbit heart preparations. This was either reduced or absent in preparations obtained from reserpine pretreated animals. alpha-Methyldopa, alpha-methylnoradrenaline, alpha-methyl-m-tyrosine and metaraminol restored the responses to tyramine. alpha-Methyldopamine and alpha-methyl-p-tyrosine did not do so.

摘要

在从经利血平预处理的动物获得的离体组织制备物中，研究了α-甲基氨基酸及其相应胺类恢复酪胺拟交感神经作用的能力，以及氨基酸和胺类的摄取情况。
酪胺可使未用利血平处理的大鼠的离体回肠制备物松弛，但对经利血平处理的动物的制备物则无此作用。α-甲基多巴、α-甲基去甲肾上腺素和较低浓度的间羟胺可恢复经利血平处理的制备物的反应。α-甲基多巴胺、α-甲基间酪氨酸、α-甲基对酪氨酸和较高浓度的间羟胺则不能。α-甲基多巴的恢复作用被双硫仑阻断。α-甲基对酪氨酸或α-甲基间酪氨酸可阻断α-甲基多巴的恢复作用，但不阻断α-甲基去甲肾上腺素的恢复作用。可卡因可阻断α-甲基去甲肾上腺素对酪胺反应的恢复作用，但不阻断α-甲基多巴的恢复作用。在无钠的台氏液存在下，α-甲基多巴和α-甲基去甲肾上腺素未能恢复对酪胺的反应。
酪胺可使从未用利血平处理的动物获得的离体兔耳制备物的灌注压升高，但对经利血平处理的动物的制备物的作用则弱得多。α-甲基多巴、α-甲基间酪氨酸、α-甲基去甲肾上腺素、α-甲基对酪氨酸和间羟胺可恢复酪胺的作用。α-甲基多巴胺则不能。α-甲基多巴和α-甲基间酪氨酸的恢复作用被双硫仑阻断。α-甲基对酪氨酸可阻断α-甲基间酪氨酸的恢复作用。
酪胺可使离体兔心制备物产生正性肌力作用。在经利血平预处理的动物的制备物中，这种作用要么减弱要么消失。α-甲基多巴、α-甲基去甲肾上腺素、α-甲基间酪氨酸和间羟胺可恢复对酪胺的反应。α-甲基多巴胺和α-甲基对酪氨酸则不能。