New selective histamine H1 agonists. Synthesis and pharmacology.
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.
Koper
J G
JG
Department of Pharmacochemistry, Free University, Amsterdam, The Netherlands.
Van der Vliet
A
A
Van der Goot
H
H
Timmerman
H
H
D000818:Animals; D006168:Guinea Pigs; D006321:Heart / Q000187:drug effects; D006632:Histamine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D009130:Muscle, Smooth / Q000187:drug effects; D011969:Receptors, Histamine H1 / Q000737:chemistry / Q000187:drug effects* / Q000502:physiology
D011969:Receptors, Histamine H1; D006632:Histamine