The nicotinic acetylcholine receptors of zebrafish and an evaluation of pharmacological tools used for their study.

Biochemical Pharmacology
R L PapkeR Thomas Boyd

Abstract

Zebrafish (Danio rerio) have been used to study multiple effects of nicotine, for example on cognition, locomotion, and stress responses, relying on the assumption that pharmacological tools will operate similarly upon molecular substrates in the fish and mammalian systems. We have cloned the zebrafish nicotinic acetylcholine receptor (nAChR) subunits and expressed key nAChR subtypes in Xenopus oocytes including neuronal (α4β2, α2β2, α3β4, and α7) and muscle (α1β1(b)ɛδ) nAChR. Consistent with studies of mammalian nAChR, nicotine was relatively inactive on muscle-type receptors, having both low potency and efficacy. It had high efficacy but low potency for α7 receptors, and the best potency and good efficacy for α4β2 receptors. Cytisine, a key lead compound for the development of smoking cessation agents, is a full agonist for both mammalian α7 and α3β4 receptors, but a full agonist only for the fish α7, with surprisingly low efficacy for α3β4. The efficacy of cytisine for α4β2 was somewhat greater than typically reported for mammalian α4β2. The ganglionic blocker mecamylamine was most potent for blocking α3β4 receptors, least potent for α7, and roughly equipotent for the muscle receptors and the β2-containing nAChR. However, th...Continue Reading

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Citations

Oct 29, 2013·European Journal of Pharmacology·Roger L PapkeM Imad Damaj
Dec 12, 2013·Proceedings of the National Academy of Sciences of the United States of America·Elim HongMarnie E Halpern
Aug 1, 2014·PloS One·Caio MaximinoAnderson Manoel Herculano
Oct 30, 2015·Critical Reviews in Toxicology·Larry P SheetsRichard C Peffer
Mar 19, 2015·The Journal of Physiological Sciences : JPS·Eriko DaikokuFumihito Ono
Oct 29, 2014·Molecular Psychiatry·A M StewartA V Kalueff
Jan 26, 2020·Progress in Neuro-psychopharmacology & Biological Psychiatry·Talise E MüllerDenis B Rosemberg
Apr 28, 2021·Progress in Neuro-psychopharmacology & Biological Psychiatry·Luisa PonzoniMariaelvina Sala
Jun 4, 2021·Frontiers in Pharmacology·Oihane JakaKyoko Koshibu
May 16, 2021·Pharmacology, Biochemistry, and Behavior·Murilo S de AbreuAllan V Kalueff
Jul 2, 2021·Pharmacology, Biochemistry, and Behavior·Andrew B HawkeyKyoko Koshibu
Jul 16, 2021·Journal of Natural Medicines·Ainhoa AlzualdeKyoko Koshibu

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