Different effects of lobeline on neuronal and muscle nicotinic receptors.

Eur J Pharmacol

Institute of Physiology, Academy of Sciences of the Czech Republic, v.v.i., Vídeňská 1083, 142 20 Prague 4, Czech Republic. Electronic address:

Published: September 2014

AI Article Synopsis

  • Lobeline is a plant alkaloid that interacts with the cholinergic system, specifically affecting neuronal α3β4 receptors and muscle embryonic αβγδ receptors.
  • The study used the patch-clamp technique to reveal that lobeline inhibits acetylcholine responses in muscle nicotinic receptors in a pseudo-noncompetitive way.
  • For rat neuronal α3β4 receptors, lobeline initially enhances responses to low acetylcholine concentrations but switches to voltage-dependent inhibition at high acetylcholine levels.

Article Abstract

Lobeline is a plant alkaloid known to interact with cholinergic system. The effect of lobeline on neuronal α3β4 receptors expressed in COS cells and muscle embryonic αβγδ 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 α3β4 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 α3β4 receptors was activated by a high concentration of acetylcholine.

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Source
http://dx.doi.org/10.1016/j.ejphar.2014.05.057DOI Listing

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