Abstract
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 inpara position causes a decrease in h1 activity. However, in themeta-substituted members both increases and decreases of H1 activity have been observed; thus themeta nitro andmeta methoxy derivatives are four times as potent as the parent 2-phenylhistamine. As far as investigated, neither H1 nor H3 activity could be established.
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Koper, J.G., Van der Vliet, A., Van der Goot, H. et al. New selective histamine H1 agonists. Pharmaceutisch Weekblad Scientific Edition 12, 236–239 (1990). https://doi.org/10.1007/BF01967823
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DOI: https://doi.org/10.1007/BF01967823