title: Antinociceptive effect of tebanicline for various noxious stimuli-induced behaviours in mice.
abstract: Tebanicline (ABT-594), an analogue of epibatidine, exhibits potent antinociceptive effects and high affinity for the nicotinic acetylcholine receptor in the central nervous system. We assessed whether tebanicline exerts an effect on various noxious stimuli and mediates the nicotine receptor or opioid receptor through stimulation. The antinociceptive effects of tebanicline were determined by noxious chemical, thermal and mechanical stimuli-induced behaviours in mice. Tebanicline had dose-dependent analgesic effects in formalin, hot-plate and tail-pressure tests. By contrast, the antinociceptive effect of tebanicline was not demonstrated in the tail-flick assay. Pre-treatment with mecamylamine, a nicotinic acetylcholine receptor antagonist, blocked the effects of tebanicline in formalin, tail-pressure and hot-plate tests. Moreover, pre-treatment with naloxone, an opioid receptor antagonist, only partially inhibited the effects of tebanicline in formalin and tail-pressure tests. Tebanicline produced antinociception in persistent chemical (formalin), acute thermal (hot-plate, but not tail-flick) and mechanical (tail-pressure) pain states. Moreover, tebanicline stimulated the nicotinic acetylcholine receptor and opioid receptor.
authors.affiliation: Laboratory of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University, 4-4-1 Komatsushima, Aoba-ku, Sendai, Miyagi 981-8558, Japan.
authors.forename: Takafumi
authors.initials: T
authors.lastname: Hayashi
authors.affiliation: Center for Experiential Pharmacy Practice, Tokyo University of Pharmacy and Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan.
authors.forename: Soh
authors.initials: S
authors.lastname: Katsuyama
authors.affiliation: Department of Physiology and Anatomy, Tohoku Medical and Pharmaceutical University, 4-4-1 Komatsushima, Aoba-ku, Sendai, Miyagi 981-8558, Japan.
authors.forename: Tohru
authors.initials: T
authors.lastname: Orito
authors.affiliation: Laboratory of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University, 4-4-1 Komatsushima, Aoba-ku, Sendai, Miyagi 981-8558, Japan.
authors.forename: Tsuneyoshi
authors.initials: T
authors.lastname: Suzuki
authors.affiliation: Department of Physiology and Anatomy, Tohoku Medical and Pharmaceutical University, 4-4-1 Komatsushima, Aoba-ku, Sendai, Miyagi 981-8558, Japan. Electronic address: s-sakura@tohoku-mpu.ac.jp.
authors.forename: Shinobu
authors.initials: S
authors.lastname: Sakurada
mesh_terms: D000700:Analgesics / Q000494:pharmacology*; D000818:Animals; D001384:Azetidines / Q000494:pharmacology*; D001522:Behavior, Animal / Q000187:drug effects*; D004347:Drug Interactions; D006930:Hyperalgesia / Q000503:physiopathology / Q000523:psychology; D007274:Injections, Intraperitoneal; D008297:Male; D051379:Mice; D009292:Narcotic Antagonists / Q000494:pharmacology; D018733:Nicotinic Antagonists / Q000494:pharmacology; D010147:Pain Measurement; D011725:Pyridines / Q000494:pharmacology*
chemical_list: C109763:5-(2-azetidinylmethoxy)-2-chloropyridine; D000700:Analgesics; D001384:Azetidines; D009292:Narcotic Antagonists; D018733:Nicotinic Antagonists; D011725:Pyridines
keywords: Endogenous opioid peptide; Formalin test; Hot-plate test; Neuronal nicotinic acetylcholine receptor; Tail-flick test; Tail-pressure test