title: Smooth muscle-depressant activity of AP-18, a putative TRPA1 antagonist in the guinea pig intestine.
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.
authors.affiliation: Department of Pharmacology and Pharmacotherapy, University Medical School of Pécs and Clinical Centre, Pécs, Hungary.
authors.forename: Lorand
authors.initials: L
authors.lastname: Bartho
authors.forename: Zsolt
authors.initials: Z
authors.lastname: Sándor
authors.forename: Dezsö
authors.initials: D
authors.lastname: Kelemen
authors.forename: Robert
authors.initials: R
authors.lastname: Papp
authors.forename: Rita
authors.initials: R
authors.lastname: Benko
mesh_terms: D000109:Acetylcholine / Q000494:pharmacology; D000818:Animals; D015220:Calcium Channels; D004558:Electric Stimulation; D005260:Female; D006168:Guinea Pigs; D006632:Histamine / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D007421:Intestine, Small / Q000187:drug effects* / Q000502:physiology; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects* / Q000502:physiology; D009419:Nerve Tissue Proteins / Q000037:antagonists & inhibitors*; D010091:Oximes / Q000494:pharmacology*; D000074025:TRPA1 Cation Channel; D050051:Transient Receptor Potential Channels / Q000037:antagonists & inhibitors*
chemical_list: C000602225:4-(4-chlorophenyl)-3-methylbut-3-en-2-oxime; D015220:Calcium Channels; D009419:Nerve Tissue Proteins; D010091:Oximes; D000074025:TRPA1 Cation Channel; C473350:TRPA1 protein, human; D050051:Transient Receptor Potential Channels; D006632:Histamine; D000109:Acetylcholine