Pharmacological characterisation of Ca2+ channels of the L-type in human peripheral blood lymphocytes

Eur J Pharmacol. 1996 Apr 22;301(1-3):189-94. doi: 10.1016/0014-2999(96)00016-7.

Abstract

Ca2+ channels of the L-type were characterised in intact human peripheral blood lymphocytes using a radioligand binding technique and the dihydropyridine-type Ca2+ channel antagonist [3H](+)-PN 200-110 (isopropyl-4-(2,1,3-benzoxadiazol-4-yl)1,4-dihydro-5-methoxycarbon yl-2, 6-dimethyl-3-pyridine carboxylate) as a ligand. [3H](+)-PN 200-110 binding to human peripheral blood lymphocytes was time-, temperature-, concentration-dependent and of high affinity. The dissociation constant (Kd) value was 0.4 +/- 0.02 nM and the maximum binding capacity (Bmax) was 33.5 +/- 1.6 fmol/10(6) cells. Pharmacological analysis of [3H](+)-PN 200-110 binding to human peripheral blood lymphocytes was consistent with the labelling of a Ca2+ channel of the L-type. In fact, dihydropyridine derivatives were the most potent competitors of [3H](+)-PN 200-110 binding, whereas phenylalkylamine and benzothiazepine compounds or non-selective Ca2+ channel modulators were weak or ineffective displacers. These findings are the first observation that human peripheral blood lymphocytes express Ca2+ channels of the L-type. The possibility that Ca2+ channel antagonists may interfere with immune system function is discussed.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Binding, Competitive / drug effects
  • Calcium Channel Blockers / pharmacokinetics
  • Calcium Channels / drug effects
  • Calcium Channels / metabolism*
  • Humans
  • In Vitro Techniques
  • Isradipine / pharmacokinetics
  • Kinetics
  • Lymphocytes / drug effects
  • Lymphocytes / metabolism*
  • Radioligand Assay
  • Regression Analysis
  • Temperature

Substances

  • Calcium Channel Blockers
  • Calcium Channels
  • Isradipine