Antiallergic Effect of ZCR-2060: Antihistaminic Action

Abstract

ABSTRACT-The antihistaminic effect of 2-[2-[4-(diphenylmethyl)-1-piperadinyl]ethoxy]benzoic acid maleate (ZCR-2060), a newly synthesized antiallergic agent, was investigated in both in vitro and in vivo studies. ZCR-2060 clearly antagonized histamine-induced contraction of isolated guinea pig ileum and trachea. In contrast, carbachol-, BaC12 and 5-hydroxytryptamine-induced contractions of isolated guinea pig ileum were slightly inhibited by higher concentrations of ZCR-2060. 3H-Mepyramine specific binding to membranes from guinea pig lung and brain were markedly inhibited by ZCR-2060 in a concentration-de pendent fashion. In the in vitro studies, the antihistaminic effect of ZCR-2060 was greater than those of cetirizine and terfenadine, but was less than that of ketotifen. In the in vivo studies, ZCR-2060 significantly inhibited the histamine-induced cutaneous reaction in rats, when administered orally 1 hr before the histamine injection. Moreover, ZCR-2060 has a long-lasting antihistaminic effect. In the in vivo studies, the antihistaminic effect of ZCR-2060 was found to be greater than that of cetirizine and terfenadine, and it was the same as that of ketotifen. Thiopental-induced sleep and spontaneous ambulatory activity in mice, however, were unaffected by ZCR-2060 at higher doses. These results indicate that ZCR-2060 has a potent, selective and long acting histamine H,-receptor antagonistic action without causing any unwanted CNS side effect.

Anti-allergic properties of Mangifera indica L. extract (Vimang) and contribution of its glucosylxanthone mangiferin

“…Then, they were injected intravenously with 1 mL of Evan's blue 1% in saline solution, and immediately received 50 mg/site of histamine intradermally into 4 sites of the shaved back, and another two sites received saline. The rats were sacrificed 30 min later, and the reaction sites were excised for measurement of extravased dye (Abe et al 1994). The amount of extravased dye was determined according to Katayama's method (Katayama et al 1981).…”