4.7 Article

Different effects of lobeline on neuronal and muscle nicotinic receptors

期刊

EUROPEAN JOURNAL OF PHARMACOLOGY
卷 738, 期 -, 页码 352-359

出版社

ELSEVIER SCIENCE BV
DOI: 10.1016/j.ejphar.2014.05.057

关键词

Neuronal nicotinic receptor alpha3beta4; Embryonic muscle nicotinic receptor; Lobeline

资金

  1. Czech Science Foundation [202/09/0806, IAA500110905, P304/12/G069]

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Lobeline is a plant alkaloid known to interact with cholinergic system. The effect of lobeline on neuronal alpha 3 beta 4 receptors expressed in COS cells and muscle embryonic alpha beta gamma delta receptors naturally expressed in TE671 cells was studied using a patch clamp technique. Our results show that lobeline inhibited responses to acetylcholine in human embryonic muscle nicotinic receptor in a pseudo noncompetitive manner. The responses of rat neuronal alpha 3 beta 4 receptors to a low concentration of acetylcholine were potentiated by a mixed occupation mechanism that corresponds to competitive potentiation. This potentiation turned into voltage dependent inhibition for alpha 3 beta 4 receptors was activated by a high concentration of acetylcholine. (C) 2014 Elsevier B.V. All rights reserved.

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