Koper J G, Van der Vliet A, Van der Goot H, Timmerman H
Department of Pharmacochemistry, Free University, Amsterdam, The Netherlands.
Pharm Weekbl Sci. 1990 Dec 14;12(6):236-9. doi: 10.1007/BF01967823.
In this article the synthesis and histaminergic H1 activity of a series of substituted 2-phenylhistamines are described. It appeared that substitution of the phenyl ring of these compounds influences the H1 activity substantially. In general, substitution in para position causes a decrease in H1 activity. However, in the meta-substituted members both increases and decreases of H1 activity have been observed; thus the meta nitro and meta methoxy derivatives are four times as potent as the parent 2-phenylhistamine. As far as investigated, neither H1 nor H3 activity could be established.
本文描述了一系列取代的2-苯基组胺的合成及其组胺能H1活性。结果表明，这些化合物苯环上的取代基对H1活性有显著影响。一般来说，对位取代会导致H1活性降低。然而，在间位取代的化合物中，H1活性既有增加也有降低的情况；因此，间硝基和间甲氧基衍生物的活性是母体2-苯基组胺的四倍。就目前所研究的情况而言，未发现有H1或H3活性。
