The nicotinic acetylcholine receptor of the bovine chromaffin cell, a new target for dihydropyridines

Eur J Pharmacol. 1993 Oct 15;247(2):199-207. doi: 10.1016/0922-4106(93)90078-n.

Abstract

The effects of 1,4-dihydropyridine derivatives on divalent cation transients and catecholamine release stimulated by either high K+ or the nicotinic receptor agonist dimethyl-phenyl-piperazinium (DMPP) have been compared in bovine adrenal chromaffin cells. The activation of Ca2+ entry pathways was followed by measuring 45Ca2+ or Mn2+ uptake, or by the changes of [Ca2+]i in fura-2-loaded chromaffin cells. Various dihydropyridine Ca2+ channel blockers (nimodipine, PCA50938, nifedipine, nitrendipine, furnidipine) abolished the DMPP-mediated effects, but prevented only partially the activation by high [K+]0 of 45Ca2+ uptake. The IC50 for DMPP-induced activation was around 1 microM. The L-type Ca2+ channel activator Bay K 8644 potentiated the uptake of 45Ca2+ induced by K+ depolarization at concentrations between 10 nM and 1 microM, but completely inhibited the uptake of 45Ca2+ by DMPP (IC50, 0.9 microM). Both high [K+]0 and DMPP produced membrane depolarization as measured using bis-oxonol. The DMPP-evoked, but not the K(+)-evoked membrane depolarization was prevented by Na+ removal, suggesting that the depolarization was due to Na+ entry through the acetylcholine receptor ionophore. Nimodipine at 10 microM abolished the depolarization induced by DMPP, leaving the K(+)-evoked depolarization unaffected. Tetrodotoxin (2 microM) did not affect the DMPP- or high K(+)-mediated cell depolarization. Whole-cell inward current evoked by 100 microM DMPP (IDMPP) was measured in cells voltage-clamped at -80 mV. Nimodipine (10 microM) reduced IDMPP by 36%; Bay K 8644 (10 microM) inhibited IDMPP by 67%. DMPP-evoked catecholamine release from superfused chromaffin cells was reduced by over 90% with 10 microM nimodipine; in contrast, K(+)-evoked release was decreased by 20%.(ABSTRACT TRUNCATED AT 250 WORDS)

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester / pharmacology
  • Animals
  • Calcium / metabolism
  • Calcium Radioisotopes
  • Catecholamines / metabolism
  • Cattle
  • Cytosol / metabolism
  • Dihydropyridines / pharmacology*
  • Dimethylphenylpiperazinium Iodide / antagonists & inhibitors
  • Dimethylphenylpiperazinium Iodide / pharmacology
  • Electrophysiology
  • Enterochromaffin Cells / drug effects
  • Enterochromaffin Cells / metabolism*
  • Fura-2 / pharmacology
  • Manganese / metabolism
  • Membrane Potentials / drug effects
  • Nimodipine / pharmacology
  • Potassium / pharmacology
  • Receptors, Cholinergic / drug effects*

Substances

  • Calcium Radioisotopes
  • Catecholamines
  • Dihydropyridines
  • Receptors, Cholinergic
  • Manganese
  • Dimethylphenylpiperazinium Iodide
  • Nimodipine
  • 3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester
  • Potassium
  • Calcium
  • Fura-2