局部应用新型钙通道拮抗剂的抗炎活性。
The antiinflammatory activity of topically applied novel calcium-channel antagonists.
作者信息
De Vries G W, McLaughlin A, Wenzel M B, Perez J, Harcourt D, Lee G, Garst M, Wheeler L A
机构信息
Department of Biological Sciences, Allergan, Inc., Irvine, California 92715, USA.
出版信息
Inflammation. 1995 Apr;19(2):261-75. doi: 10.1007/BF01534466.
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.
在皮肤炎症的小鼠模型中评估了两种新型钙通道拮抗剂AGN 190742和AGN 190744的抗炎活性。这两种2(5H)-呋喃酮环化合物可阻断GH3细胞中去极化依赖性Ca2+内流和受体介导的反应。局部应用AGN 190742或AGN 190744可抑制佛波酯反复处理小鼠皮肤所诱导的中性粒细胞浸润和表皮增生。AGN 190744在急性炎症的花生四烯酸模型中也具有活性。这些数据表明，局部应用钙通道拮抗剂可抑制皮肤炎症反应，并且AGN 190742和/或AGN 190744可能作为在体内研究这些反应的有用药理学探针。
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