THE ANTIINFLAMMATORY ACTIVITY OF TOPICALLY APPLIED NOVEL CALCIUM-CHANNEL ANTAGONISTS

Authors
DEVRIES GW MCLAUGHLIN A WENZEL MB PEREZ J HARCOURT D LEE G GARST M WHEELER LA
Citation
Gw. Devries et al., THE ANTIINFLAMMATORY ACTIVITY OF TOPICALLY APPLIED NOVEL CALCIUM-CHANNEL ANTAGONISTS, Inflammation, 19(2), 1995, pp. 261-275
Citations number
38
Categorie Soggetti
Cell Biology
Journal title
Inflammation → ACNP
ISSN journal
03603997
Volume
19
Issue
2
Year of publication
1995
Pages
261 - 275
Database
ISI
SICI code
0360-3997(1995)19:2<261:TAAOTA>2.0.ZU;2-7
Abstract
The antiinflammatory activities of two novel calcium-channel antagonis ts, AGN 190742 and AGN 190744, were evaluated in murine models of cuta neous inflammation. These 2(5H)-furanone ring compounds block both dep olarization-dependent Ca2+ entry and receptor-mediated responses in GH 3 cells. Topical application of AGN 190742 or AGN 190744 inhibits neut rophil infiltration and epidermal hyperplasia induced by repeated trea tment of mouse skin with phorbol ester. AGN 190744 also is active in a n arachidonic acid model of acute inflammation. These data suggest tha t topical application of calcium-channel antagonists can inhibit cutan eous inflammatory responses and that AGN 190742 and/or AGN 190744 may serve as useful pharmacological probes for examining these responses i n vivo.