Pharmacology 2014-01-01

Smooth muscle-depressant activity of AP-18, a putative TRPA1 antagonist in the guinea pig intestine.

Lorand Bartho, Zsolt Sándor, Dezsö Kelemen, Robert Papp, Rita Benko

Index: Pharmacology 94(3-4) , 131-4, (2014)

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Abstract

AP-18, a putative antagonist at TRPA1 receptor/ion channel, caused smooth muscle relaxation at 10-100 µmol/l. It inhibited cholinergic twitch responses evoked by electrical field stimulation of cholinergic nerves as well as contractions in response to acetylcholine and histamine in the guinea pig small intestine. AP-18 (30 µmol/l) blocked spontaneous contractions of longitudinal strips of human jejunum. It is concluded that AP-18 may have limited value in studying TRPA1-mediated responses in smooth muscles and should probably be used with care in other preparations because of possible nonspecific effects.© 2014 S. Karger AG, Basel.