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[2-和4-[苄基-(2-二甲基氨基乙基)氨基]嘧啶化合物的抗H1组胺和抗毒蕈碱作用]

[The anti-H1-histaminic and antimuscarinic effect of 2- and 4-[benzyl-(2-dimethylaminoethyl)amino]pyrimidine compounds].

作者信息

Maggiali C, Morini G, Mossini F, Morini G, Barocelli E, Impicciatore M

机构信息

Istituto di Chimica Farmaceutica e Tossicologica - Universita' di Parma.

出版信息

Farmaco Sci. 1988 Mar;43(3):277-91.

PMID:2901367
Abstract

This paper reports the synthesis of 2- and 4- [benzyl-(2-dimethylaminoethyl)amino]pyrimidine compounds and the evaluation of their inhibitory properties against histamine (H1), acetylcholine and barium chloride, on guinea pig isolated ileum. 4-[p.Methoxybenzyl-(2-dimethylaminoethyl)amino]-2-methoxy-pyrimidine (VIII) is shown to possess H1 receptor antagonist activity, with a potency similar to that observed for Tonzylamine. By contrast, a specific, although weak, antimuscarinic effect is displayed by 4-[benzyl-(2-dimethylaminoethyl)amino]-2-methoxy-5-methylthio-pyrimidine (XII).

摘要

本文报道了2-和4- [苄基-(2-二甲基氨基乙基)氨基]嘧啶化合物的合成及其对豚鼠离体回肠组胺(H1)、乙酰胆碱和氯化钡抑制特性的评价。4- [对甲氧基苄基-(2-二甲基氨基乙基)氨基]-2-甲氧基嘧啶(VIII)显示出具有H1受体拮抗剂活性,其效力与托恩扎胺相似。相比之下,4- [苄基-(2-二甲基氨基乙基)氨基]-2-甲氧基-5-甲硫基嘧啶(XII)表现出一种特异性的、尽管较弱的抗毒蕈碱作用。

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