Dihydropyridine block of omega-agatoxin IVA- and omega-conotoxin GVIA-sensitive Ca2+ channels in rat pituitary melanotropic cells

Eur J Pharmacol. 1996 Sep 12;311(2-3):293-304. doi: 10.1016/0014-2999(96)00432-3.

Abstract

High voltage-activated Ca2+ currents in rat melanotropic cells consist of a sustained and an inactivating component. In this study the pharmacological properties of the high voltage-activated Ca2+ channels underlying these components are investigated with whole-cell recordings. We report that melanotropes express four pharmacologically distinct high voltage-activated Ca2+ channels. Non-inactivating L-type channels account for 35% of the total high voltage-activated channel population. These channels have a very high affinity for the dihydropyridine nimodipine (EC50 approximately 3 pM). The cone snail toxin omega-conotoxin GVIA irreversibly blocked an inactivating high voltage-activated component which accounted for 26% of the total whole-cell high voltage-activated Ca2+ current. The spider toxin omega-agatoxin IVA reversibly blocked an additional 31% of the total high voltage-activated current. The current blocked by omega-agatoxin IVA was not homogenous and consisted of a sustained component with a high affinity for omega-agatoxin IVA (< 10 nM) and an inactivating current with a low affinity for omega-agatoxin IVA (> 100 nM). Both the omega-agatoxin IVA and omega-conotoxin GVIA-blocked currents were very sensitive to nimodipine and nitrendipine with a half maximal block at 200-500 nM. 10 microM nimodipine blocked 70% of the omega-conotoxin GVIA-sensitive current and 90% of the omega-agatoxin IVA-sensitive current. Thus, omega-conotoxin GVIA- and omega-agatoxin IVA-sensitive high voltage-activated Ca2+ channels in melanotropes have an unusual high affinity for dihydropyridines compared to N-, P-, and Q-type channels in other preparations.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Calcium Channel Blockers / pharmacology*
  • Calcium Channels / metabolism
  • Cells, Cultured / drug effects
  • Dihydropyridines / pharmacology*
  • Dose-Response Relationship, Drug
  • Male
  • Melanophores / drug effects*
  • Melanophores / metabolism
  • Nimodipine / pharmacology*
  • Patch-Clamp Techniques
  • Peptides / antagonists & inhibitors*
  • Pituitary Gland / cytology
  • Pituitary Gland / drug effects
  • Rats
  • Rats, Wistar
  • Spider Venoms / antagonists & inhibitors*
  • omega-Agatoxin IVA
  • omega-Conotoxin GVIA

Substances

  • Calcium Channel Blockers
  • Calcium Channels
  • Dihydropyridines
  • Peptides
  • Spider Venoms
  • omega-Agatoxin IVA
  • Nimodipine
  • 1,4-dihydropyridine
  • omega-Conotoxin GVIA