T-type calcium channel blockers - new and notable

Gen Physiol Biophys. 2011 Dec;30(4):403-9. doi: 10.4149/gpb_2011_04_403.

Abstract

Since cloning of the T-type or Ca(V)3.n calcium channel family in 1998-1999 much progress was made in investigation of their regulation. Most effective metal Ca(V)3 channel blockers are trivalent cations from lanthanide group together with transition metals La(3+) and Y(3+). Divalent cations Zn(2+), Cu(2+) and Ni(2+) inhibit Ca(V)3.2 channels more efficiently than Ca(V)3.1 and Ca(V)3.3 channels via second high-affinity binding site including histidine H191 specific for the Ca(V)3.2 channel. Dihydropyridines and phenylalkylamines in addition to block of L-type calcium channel can inhibit Ca(V)3 channels in clinically relevant concentration.

Publication types

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

MeSH terms

  • Animals
  • Calcium Channel Blockers / pharmacology*
  • Calcium Channels, T-Type / chemistry
  • Calcium Channels, T-Type / metabolism*
  • Cations
  • Copper / chemistry
  • Humans
  • Inhibitory Concentration 50
  • Kinetics
  • Nickel / chemistry
  • Zinc / chemistry

Substances

  • CACNA1G protein, human
  • CACNA1H protein, human
  • CACNA1I protein, human
  • Calcium Channel Blockers
  • Calcium Channels, T-Type
  • Cations
  • Copper
  • Nickel
  • Zinc