Different effects of lobeline on neuronal and muscle nicotinic receptors

Eur J Pharmacol. 2014 Sep 5:738:352-9. doi: 10.1016/j.ejphar.2014.05.057. Epub 2014 Jun 12.

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.

Keywords: Embryonic muscle nicotinic receptor; Lobeline; Neuronal nicotinic receptor alpha3beta4.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • COS Cells
  • Chlorocebus aethiops
  • Humans
  • Lobeline / pharmacology*
  • Muscles / drug effects
  • Muscles / metabolism*
  • Neurons / drug effects
  • Neurons / metabolism*
  • Nicotinic Agonists / pharmacology*
  • Organ Specificity
  • Rats
  • Receptors, Nicotinic / metabolism*

Substances

  • Nicotinic Agonists
  • Receptors, Nicotinic
  • nicotinic receptor alpha3beta2
  • Lobeline