PMID: 2438238Jan 1, 1987

CI-922--a novel, potent antiallergic compound--I. Inhibition of mediator release in vitro

International Journal of Immunopharmacology
L J RobichaudR L Adolphson

Abstract

CI-922 (3,7-dimethoxy-4-phenyl-N-1H-tetrazol-5-yl-4H-furo[3,2-b]-indole- 2-carboxamide, L-arginine salt) is a novel antiallergy compound which inhibits the release of the inflammatory mediators histamine and leukotriene (LT) from stimulated cells. CI-922 showed potent, effective inhibition of antigen-induced mediator release from human basophils and isolated guinea pig lung. The drug inhibited ragweed or housedust-induced histamine release from basophils of allergic human donors (IC50 = 8.6 microM). The antiallergy agents proxicromil (IC50 = 80 microM) and cromolyn (100 microM) were less potent than CI-922 or inactive, respectively. In fragmented lung from actively sensitized guinea pigs, CI-922 (IC50 = 1.5 microM), blocked the antigen-induced production of LT and was a more potent inhibitor of histamine release (IC50 = 13.4 microM) than proxicromil (IC50 = 72.9 microM), or cromolyn (inactive at 1 mM). CI-922 (IC50 = 0.9 microM) completely inhibited repeated contractions of guinea pig lung strips that were induced by low antigen concentration in the presence of antihistamine (H1). Nordihydroguaiaretic acid (NDGA) (IC50 = 2.8 microM), proxicromil (IC50 = 6.2 microM) and the LT antagonist FPL-55712 (IC50 = 3.3 microM) also were f...Continue Reading

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Citations

Jan 1, 1987·International Journal of Immunopharmacology·R L AdolphsonL J Robichaud
Feb 19, 2011·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Ghassan ShattatMoyad Shahwan
May 30, 2017·EFSA Journal·EFSA Panel on Animal Health and Welfare (AHAW)Christoph Winckler
Dec 7, 2019·Beilstein Journal of Organic Chemistry·Hoang Huy DoPeter Langer

Related Concepts

3,7-dimethoxy-4-phenyl-N-(1H-tetrazol-5-yl)-4H-furo-(3,2-b)-indole-2-carboxamide 1-arginate
Metazoa
Azoles
Carboptic
Cavia porcellus
Histamine Release
Indoles
Leukocytes
Lung
Inotropism

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