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

Il Farmaco; edizione scientifica Pub Date : 1988-03-01
C Maggiali, G Morini, F Mossini, G Morini, E Barocelli, M Impicciatore
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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).

[2-和4-[苄基-(2-二甲氨基乙基)氨基]嘧啶化合物的抗h1组胺和抗毒蕈碱作用]。
本文报道了2-和4-[苄基-(2-二甲氨基乙基)氨基]嘧啶化合物在豚鼠离体回肠上的合成及其对组胺(H1)、乙酰胆碱和氯化钡的抑制性能。4-[p.甲氧基苄基-(2-二甲氨基乙基)氨基]-2-甲氧基嘧啶(VIII)显示具有H1受体拮抗剂活性,其效力与Tonzylamine相似。相比之下,4-[苄基-(2-二甲氨基乙基)氨基]-2-甲氧基-5-甲基硫代嘧啶(XII)具有特异性但较弱的抗毒蕈碱作用。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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