title: New selective histamine H1 agonists. Synthesis and pharmacology.
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 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.
authors.affiliation: Department of Pharmacochemistry, Free University, Amsterdam, The Netherlands.
authors.forename: J G
authors.initials: JG
authors.lastname: Koper
authors.forename: A
authors.initials: A
authors.lastname: Van der Vliet
authors.forename: H
authors.initials: H
authors.lastname: Van der Goot
authors.forename: H
authors.initials: H
authors.lastname: Timmerman
mesh_terms: 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
chemical_list: D011969:Receptors, Histamine H1; D006632:Histamine