The antiinflammatory activity of topically applied novel calcium-channel antagonists

The antiinflammatory activities of two novel calcium-channel antagonists, AGN 190742 and AGN 190744, were evaluated in murine models of cutaneous inflammation. These 2(5H)-furanone ring compounds block both depolarization-dependent Ca2+ entry and receptor-mediated responses in GH3 cells. Topical app...

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Veröffentlicht in:	Inflammation 1995-04, Vol.19 (2), p.261-275
Hauptverfasser:	De Vries, G W, McLaughlin, A, Wenzel, M B, Perez, J, Harcourt, D, Lee, G, Garst, M, Wheeler, L A
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Cutaneous Animals Anti-Inflammatory Agents, Non-Steroidal - administration & dosage Anti-Inflammatory Agents, Non-Steroidal - pharmacology Arachidonic Acid - secretion Arachidonic Acid - toxicity Calcium - metabolism Calcium Channel Blockers - administration & dosage Calcium Channel Blockers - pharmacology Chemotaxis, Leukocyte - drug effects Clobetasol - analogs & derivatives Clobetasol - pharmacology Ear, External Epidermis - drug effects Epidermis - pathology Female Humans Hyperplasia Inflammation Mice Neutrophils - drug effects Neutrophils - enzymology Neutrophils - secretion Nifedipine - pharmacology Peroxidase - analysis Phosphatidylinositol Diacylglycerol-Lyase Phosphodiesterase Inhibitors - pharmacology Phospholipases A - antagonists & inhibitors Phosphoric Diester Hydrolases - metabolism Pituitary Neoplasms - pathology Potassium Chloride - antagonists & inhibitors Pyrazoles - pharmacology Terpenes - pharmacology Tetradecanoylphorbol Acetate - toxicity Thyrotropin-Releasing Hormone - antagonists & inhibitors Tumor Cells, Cultured - drug effects
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Beschreibung
Zusammenfassung:	The antiinflammatory activities of two novel calcium-channel antagonists, AGN 190742 and AGN 190744, were evaluated in murine models of cutaneous inflammation. These 2(5H)-furanone ring compounds block both depolarization-dependent Ca2+ entry and receptor-mediated responses in GH3 cells. Topical application of AGN 190742 or AGN 190744 inhibits neutrophil infiltration and epidermal hyperplasia induced by repeated treatment of mouse skin with phorbol ester. AGN 190744 also is active in an arachidonic acid model of acute inflammation. These data suggest that topical application of calcium-channel antagonists can inhibit cutaneous inflammatory responses and that AGN 190742 and/or AGN 190744 may serve as useful pharmacological probes for examining these responses in vivo.
ISSN:	0360-3997 1573-2576
DOI:	10.1007/BF01534466