PMID: 15233377Jul 6, 2004Paper

Nicotinic receptor inhibition by Tetraponera ant alkaloids

Cellular and Molecular Neurobiology
William R KemJean-Claude Braekman

Abstract

1. Tetraponerines are a group of alkaloids occurring in the venoms of ants belonging to the genus Tetraponera. Eight compounds had been isolated and their structures elucidated, but their mechanisms of action had not yet been reported. We have studied the actions of several of these tetraponerines on vertebrate neuromuscular, ganglionic, and brain nicotinic acetylcholine receptors (nAChRs) using a variety of techniques including muscle contracture, cultured cell functional assays, neuronal patch clamping, and radioligand binding methods. 2. Potency for inhibition of the frog muscle carbachol-elicited contracture increased as the carbon 9 side chain alkyl group was increased in length to 10-12 carbons, then decreased when the chain was 18-carbons long. Potency differences between T-7 and T-8, which differ only in the stereochemistry of the carbon pentyl side chain were rather small. Quaternization of either N atom in a T-8 analog bearing a 10-carbon length alkyl substituent did not greatly affect potency for inhibition of the muscle response; thus the ionized form is an active form of this tetraponerine. 3. T-7 inhibited the nicotine-stimulated efflux of 86Rb from cultured PC12 cells, which primarily express alpha3-beta4 ganglio...Continue Reading

Citations

Dec 3, 2014·Toxicon : Official Journal of the International Society on Toxinology·Samira R AiliGraham M Nicholson
May 26, 2017·The Journal of Organic Chemistry·Stephen G DaviesJames E Thomson
Jul 25, 2020·Chemical Record : an Official Publication of the Chemical Society of Japan ... [et Al.]·Caroline GrundkeTill Opatz
Nov 3, 2020·Pest Management Science·Guanghu TongRyan A Shenvi
Apr 16, 2014·The Journal of Organic Chemistry·Irene BosqueJosé Brea
Oct 25, 2012·The Journal of Organic Chemistry·Irene BosqueMiguel Yus
Jan 16, 2018·The Journal of Organic Chemistry·Hina P A Khan, Tushar Kanti Chakraborty

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