Pharmacological and physiological properties of a putative ganglionic nicotinic receptor, alpha 3 beta 4, expressed in transfected eucaryotic cells

Brain Res Mol Brain Res. 1995 Jan;28(1):101-9. doi: 10.1016/0169-328x(94)00189-l.


Neuronal nicotinic acetylcholine receptor subunits alpha 3 (PCA48E) and beta 4S (ZPC13) were expressed in human embryonic kidney (HEK)-293 cells by calcium phosphate transfection. In the presence of atropine, acetylcholine (ACh) induced fast activating currents which exhibited desensitization and inward rectification. The EC50 for ACh was 202 +/- 32 microM with a Hill coefficient of 1.9 +/- 0.4. The rank order of nicotinic agonist potency was 1,1-dimethyl-4-phenylpiperozinium (DMPP) > cytisine = nicotine approximately equal to ACh. The maximal response elicited by DMPP was substantially less than that elicited by other agonists, suggesting that DMPP is a partial agonist. ACh (500 microM) responses were very effectively blocked by equimolar concentrations (100 microM) of the ganglionic antagonists d-tubocurarine, mecamylamine and hexamethonium. Equal concentrations of the potent muscle receptor antagonist decamethonium and the competitive antagonist dihydro-beta-erythroidine were much less effective. alpha bungaro-toxin (1 microM) had little effect on ACh-induced responses. This physiological and pharmacological profile is consistent with a ganglionic nicotinic response.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Acetylcholine / pharmacology*
  • Alkaloids / pharmacology
  • Atropine / pharmacology
  • Azocines
  • Dose-Response Relationship, Drug
  • Humans
  • In Vitro Techniques
  • Kidney / physiology*
  • Nicotine / pharmacology
  • Patch-Clamp Techniques
  • Quinolizines
  • Receptors, Nicotinic / physiology*


  • Alkaloids
  • Azocines
  • Quinolizines
  • Receptors, Nicotinic
  • cytisine
  • Nicotine
  • Atropine
  • Acetylcholine