Fenamates as TRP channel blockers: mefenamic acid selectively blocks TRPM3

• Published in: British journal of pharmacology Vol. 162; no. 8; pp. 1757 - 1769
• Main Authors: Klose, Chihab, Straub, Isabelle, Riehle, Marc, Ranta, Felicia, Krautwurst, Dietmar, Ullrich, Susanne, Meyerhof, Wolfgang, Harteneck, Christian
• Format: Journal Article
• Language: English
• Published: Oxford, UK Blackwell Publishing Ltd 01.04.2011; Nature Publishing Group
• Subjects: Acids; Animals; Anti-Inflammatory Agents, Non-Steroidal - pharmacology; Biological and medical sciences; Calcium - metabolism; cationic channel; fenamate; Fenamates - pharmacology; HEK293 Cells; Humans; Insulin; Insulin - metabolism; Insulin-Secreting Cells - metabolism; Medical sciences; Mefenamic Acid - pharmacology; Mice; non‐steroidal anti‐inflammatory drugs; Pancreas; pancreatic β‐cells; Pharmacology. Drug treatments; Research Papers; transient receptor potential; TRPC Cation Channels - antagonists & inhibitors; TRPM Cation Channels - antagonists & inhibitors; TRPV Cation Channels - antagonists & inhibitors; Drug; Prostaglandin-endoperoxide synthase; Enzyme; Enzyme inhibitor; non-steroidal anti-inflammatory drugs; transient receptor potential; Non steroidal antiinflammatory agent; pancreatic β-cells; Analgesic; cationic channel; Transient receptor potential channel; Mefenamic acid; Antipyretic; Anthranilic acid derivatives; Oxidoreductases; Antagonist; β Cell; fenamate; Biological receptor

BACKGROUND AND PURPOSE Fenamates are N‐phenyl‐substituted anthranilic acid derivatives clinically used as non‐steroid anti‐inflammatory drugs in pain treatment. Reports describing fenamates as tools to interfere with cellular volume regulation attracted our attention based on our interest in the rol...