NEW SELECTIVE HISTAMINE H-1 AGONISTS - SYNTHESIS AND PHARMACOLOGY

In this article the synthesis and histaminergic H-1 activity of a series of substituted 2-phenylhistamines are described. It appeared that substitution of the phenyl ring of these compounds influences the H-1 activity substantially. In general, substitution in para position causes a decrease in H-1 activity. However, in the meta-substitute members both increases and decreases of H-1 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 H-1 nor H-3 activity could be established.