Dimaprit Inhibition of Zymosan-stimulated Beta-glucuronidase Release from Human Granulocytes

Overview

Journal Agents Actions

Specialty Pharmacology

Date 1980 Apr 1

PMID 6446228

Citations 3

Authors

W W Busse

W Cooper

C Anderson

Affiliations

Soon will be listed here.

Abstract

Histamine inhibits the in vitro release of granulocytic lysosomal beta-glucuronidase when incubated with complement activated zymosan particles and this is an H2-receptor response. The highly specific histamine H2-receptor agonist, dimaprit, also inhibits this secretory enzyme release but is less potent (-log molar ED50 6.71 with histamine vs. -log ED50 5.97 with dimaprit, p less than 0.05). No change in beta-glucuronidase release was found with the H1-agonst, 2-(2 pyridyl)-ethylamine. The antagonist activity of metiamide was similar with the two agonists (KB = 2.9 x 10(-8) M with histamine and KB = 3.6 x 10(-8) M with dimaprit). Diphenhydramine did not change the granulocyte response to either histamine or dimaprit.

Citing Articles

Histamine-induced inhibition of leukotriene biosynthesis in human neutrophils: involvement of the H2 receptor and cAMP.

Flamand N, Plante H, Picard S, Laviolette M, Borgeat P Br J Pharmacol. 2004; 141(4):552-61.

PMID: 14744809 PMC: 1574237. DOI: 10.1038/sj.bjp.0705654.

Histamine-induced inhibition of lymphocyte proliferation and lysosomal enzyme release from polymorphs may not be mediated via H1- or H2-receptors.

Vickers M, Milliner K, Martin D, Ganellin C Agents Actions. 1982; 12(5-6):630-4.

PMID: 6219553 DOI: 10.1007/BF01965071.

Autacoid and beta-adrenergic agonist modulation of N-formylmethionyl-leucyl-phenylalanine evoked lysosomal enzyme release from human neutrophils.

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