Zejc A, Groczyca M, Kieć-Kononowicz K, Pawlowski M
Pol J Pharmacol Pharm. 1976 May-Jun;28(4):369-74.
In the reaction of 7-resp. 1-beta,gamma-epoxyproplderivatives of theophylline (Th) or theobromine (Tb) with piperazine and N-monoalkyl or monoarylpiperazines the corresponding 7-resp. 1-beta-hydroxy-gamma-piperazinopropyl-Th (1-8) resp. Tb (9-16) were formed. In preliminary screening some of the new compounds showed strong antagonism with histamine H1 receptor and with endogenous histamine.
在茶碱(Th)或可可碱(Tb)的7 - 分别为1 - β,γ - 环氧丙基衍生物与哌嗪以及N - 单烷基或单芳基哌嗪的反应中,相应地形成了7 - 分别为1 - β - 羟基 - γ - 哌嗪基丙基 - Th(1 - 8)和Tb(9 - 16)。在初步筛选中,一些新化合物显示出对组胺H1受体和内源性组胺有强烈的拮抗作用。