Structural and biophysical determinants of single Ca(V)3.1 and Ca(V)3.2 T-type calcium channel inhibition by N(2)O

Cell Calcium. 2009 Oct;46(4):293-302. doi: 10.1016/j.ceca.2009.09.002. Epub 2009 Sep 26.

Abstract

We investigated the biophysical mechanism of inhibition of recombinant T-type calcium channels Ca(V)3.1 and Ca(V)3.2 by nitrous oxide (N(2)O). To identify functionally important channel structures, chimeras with reciprocal exchange of the N-terminal domains I and II and C-terminal domains III and IV were examined. In whole-cell recordings N(2)O significantly inhibited Ca(V)3.2, and - less pronounced - Ca(V)3.1. A Ca(V)3.2-prevalent inhibition of peak currents was also detected in cell-attached multi-channel patches. In cell-attached patches containing < or = 3 channels N(2)O reduced average peak current of Ca(V)3.2 by decreasing open probability and open time duration. Effects on Ca(V)3.1 were smaller and mediated by a reduced fraction of sweeps containing channel activity. Without drug, single Ca(V)3.1 channels were significantly less active than Ca(V)3.2. Chimeras revealed that domains III and IV control basal gating properties. Domains I and II, in particular a histidine residue within Ca(V)3.2 (H191), are responsible for the subtype-prevalent N(2)O inhibition. Our study demonstrates the biophysical (open times, open probability) and structural (domains I and II) basis of action of N(2)O on Ca(V)3.2. Such a fingerprint of single channels can help identifying the molecular nature of native channels. This is exemplified by a characterization of single channels expressed in human hMTC cells as functional homologues of recombinant Ca(V)3.1.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Calcium Channels, T-Type / chemistry
  • Calcium Channels, T-Type / drug effects
  • Calcium Channels, T-Type / genetics
  • Calcium Channels, T-Type / metabolism*
  • Cell Line, Transformed
  • Electrophysiology / methods
  • Humans
  • Ion Channel Gating / genetics
  • Ion Channel Gating / physiology*
  • Nitrous Oxide / metabolism
  • Nitrous Oxide / pharmacology*
  • Recombinant Fusion Proteins / chemistry
  • Recombinant Fusion Proteins / drug effects
  • Recombinant Fusion Proteins / metabolism

Substances

  • CACNA1G protein, human
  • CACNA1H protein, human
  • Calcium Channels, T-Type
  • Recombinant Fusion Proteins
  • Nitrous Oxide