Mashkovskiĭ M D, Shvarts G Ia
Farmakol Toksikol. 1979 Jan-Feb;42(1):3-7.
The antihistaminic and antiserotonin properties of 16 new tropine esters, analogues of atropine, tropacin and tropaphen, were studied. All of them were found to lessen the spasmogenic effects of histamine and serotonin. The intensity of the antihistaminic and antiserotonin action of the drugs varied depending upon the structure of the radical at the alpha-carbon atom in the acidic part of the molecule. Both types of the activity are most marked in the desoxymethyl propyl and butyl analogues of atropine. The absence of the oxymethyl group at alpha-carbon in the series of atropine analogues is shown to facilitate the manifestation of the antihistaminic activity.
研究了16种新的托品酯(阿托品、托哌辛和托帕芬的类似物)的抗组胺和抗血清素特性。发现它们均可减轻组胺和血清素的致痉挛作用。这些药物的抗组胺和抗血清素作用强度因分子酸性部分α-碳原子上基团的结构而异。两种活性在阿托品的脱氧甲基丙基和丁基类似物中最为显著。结果表明,在阿托品类似物系列中,α-碳原子上不存在羟甲基基团有利于抗组胺活性的表现。