title: Antihistaminic and anticholinergic activities of mequitazine in comparison with clemizole.
abstract: The antihistamine and anticholinergic properties of mequitazine have been investigated and compared with those of clemizole. Both mequitazine and clemizole antagonized the effect of histamine in guinea-pig ileum competitively, the pA2 values calculated by Schild plot were 9.95 +/- 0.44 for mequitazine and 10.54 +/- 0.44 for clemizole. Mequitazine at 10(-7) M produced a parallel shift of the dose-response curve to acetylcholine in the rat duodenum, clemizole and the lower doses of mequitazine failed to modify the effect of acetylcholine. The potency of mequitazine and clemizole as H1-histamine blockers is similar, but only mequitazine at highest concentration used showed anticholinergic activity.
authors.affiliation: Department de Farmacologia i Farmacotecnia, Universitat de Valencia, Facultat de Medicina, Spain.
authors.forename: I
authors.initials: I
authors.lastname: Martinez-Mir
authors.forename: L
authors.initials: L
authors.lastname: Estañ
authors.forename: E
authors.initials: E
authors.lastname: Rubio
authors.forename: F J
authors.initials: FJ
authors.lastname: Morales-Olivas
mesh_terms: D000109:Acetylcholine / Q000494:pharmacology; D000818:Animals; D001562:Benzimidazoles / Q000494:pharmacology*; D004386:Duodenum / Q000187:drug effects; D006168:Guinea Pigs; D006632:Histamine / Q000494:pharmacology; D006634:Histamine H1 Antagonists; D066298:In Vitro Techniques; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D010276:Parasympatholytics; D010640:Phenothiazines / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains
chemical_list: D001562:Benzimidazoles; D006634:Histamine H1 Antagonists; D010276:Parasympatholytics; D010640:Phenothiazines; D006632:Histamine; D000109:Acetylcholine; C006069:mequitazine