Structural requirements of steroidal agonists of transient receptor potential melastatin 3 (TRPM3) cation channels.

ABSTRACT:

Background and purpose

Transient receptor potential melastatin 3 (TRPM3) proteins form non-selective but calcium-permeable membrane channels, rapidly activated by extracellular application of the steroid pregnenolone sulphate and the dihydropyridine nifedipine. Our aim was to characterize the steroid binding site by analysing the structural chemical requirements for TRPM3 activation.

Experimental approach

Whole-cell patch-clamp recordings and measurements of intracellular calcium concentrations were performed on HEK293 cells transfected with TRPM3 (or untransfected controls) during superfusion with pharmacological substances.

Key results

Pregnenolone sulphate and nifedipine activated TRPM3 channels supra-additively over a wide concentration range. Other dihydropyridin

SUBMITTER: Drews A 

PROVIDER: S-EPMC3925040 | biostudies-literature | 2014 Feb

REPOSITORIES: biostudies-literature