Analgesic transient receptor potential vanilloid-1-active compounds inhibit native and recombinant T-type calcium channels.

ABSTRACT:

Background and purpose

T-type calcium (Ca_v 3) and transient receptor potential vanilloid-1 (TRPV1) channels play central roles in the control of excitability in the peripheral nervous system and are regarded as potential therapeutic pain targets. Modulators that either activate or inhibit TRPV1-mediated currents display analgesic properties in various pain models despite opposing effects on their connate target, TRPV1. We explored the effects of TRPV1-active compounds on Ca_v 3-mediated currents.

Experimental approach

Whole-cell patch clamp recordings were used to examine the effects of TRPV1-active compounds on rat dorsal root ganglion low voltage-activated calcium currents and recombinant Ca_v 3 isoforms in expression systems.

Key results<

SUBMITTER: McArthur JR 

PROVIDER: S-EPMC6555866 | biostudies-literature | 2019 Jul

REPOSITORIES: biostudies-literature