Inhibition of endogenous acetylcholine release by blockade of voltage-dependent calcium channels in enteric neurons of the guinea-pig colon

J Pharm Pharmacol. 1993 May;45(5):449-52. doi: 10.1111/j.2042-7158.1993.tb05574.x.

Abstract

The effects on acetylcholine release from the guinea-pig colon of the N-type calcium channel blocker omega-conotoxin GVIA (omega-conotoxin), the L-type calcium channel blocker nifedipine and the putative blocker of T-type channels, flunarizine, have been investigated. Endogenous basal acetylcholine release and electrically (1 Hz, 1 ms, 450 mA)-evoked overflow in the presence of cholinesterase inhibitor were studied. omega-Conotoxin (1-10 nM) and nifedipine (0.03-3 microM) dose-dependently inhibited basal and electrically-evoked acetylcholine release. Maximal inhibition of basal or electrically-evoked acetylcholine release was about 40% for nifedipine and about 75% for omega-conotoxin. The potency of nifedipine was inversely related to the external calcium concentration: its EC50 value in low-calcium medium (0.5 mM) was as low as 12 nM. Flunarizine inhibited acetylcholine release only at concentrations higher than 0.2 microM. Our results are consistent with an involvement of N- and L-type calcium channels in the control of the endogenous acetylcholine release from the guinea-pig colon.

Publication types

  • Comparative Study

MeSH terms

  • Acetylcholine / antagonists & inhibitors
  • Acetylcholine / metabolism*
  • Animals
  • Calcium / pharmacology
  • Calcium Channel Blockers / pharmacology*
  • Calcium Channels / drug effects
  • Calcium Channels / physiology*
  • Colon / drug effects
  • Colon / innervation
  • Colon / metabolism*
  • Electric Stimulation
  • Electrophysiology
  • Flunarizine / pharmacology
  • Guinea Pigs
  • In Vitro Techniques
  • Male
  • Neurons / drug effects
  • Neurons / metabolism*
  • Nifedipine / pharmacology
  • Peptides, Cyclic / pharmacology
  • omega-Conotoxin GVIA

Substances

  • Calcium Channel Blockers
  • Calcium Channels
  • Peptides, Cyclic
  • omega-Conotoxin GVIA
  • Nifedipine
  • Acetylcholine
  • Flunarizine
  • Calcium