Functional characterization and analgesic effects of mixed cannabinoid receptor/T-type channel ligands.

ABSTRACT:

Background

Both T-type calcium channels and cannabinoid receptors modulate signalling in the primary afferent pain pathway. Here, we investigate the analgesics activities of a series of novel cannabinoid receptor ligands with T-type calcium channel blocking activity.

Results

Novel compounds were characterized in radioligand binding assays and in vitro functional assays at human and rat CB1 and CB2 receptors. The inhibitory effects of these compounds on transient expressed human T-type calcium channels were examined in tsA-201 cells using standard whole-cell voltage clamp techniques, and their analgesic effects in response to various administration routes (intrathecally, intraplantarly, intraperitoneally) assessed in the formalin model. A series of compounds were synthesized

SUBMITTER: You H 

PROVIDER: S-EPMC3250956 | biostudies-literature | 2011 Nov

REPOSITORIES: biostudies-literature