Characterization of novel cannabinoid based T-type calcium channel blockers with analgesic effects.

ABSTRACT: Low-voltage-activated (T-type) calcium channels are important regulators of the transmission of nociceptive information in the primary afferent pathway and finding ligands that modulate these channels is a key focus of the drug discovery field. Recently, we characterized a set of novel compounds with mixed cannabinoid receptor/T-type channel blocking activity and examined their analgesic effects in animal models of pain. Here, we have built on these previous findings and synthesized a new series of small organic compounds. We then screened them using whole-cell voltage clamp techniques to identify the most potent T-type calcium channel inhibitors. The two most potent blockers (compounds 9 and 10) were then characterized using radioligand binding assays to determine their affinity for CB1 a

SUBMITTER: Bladen C 

PROVIDER: S-EPMC4372069 | biostudies-literature | 2015 Feb

REPOSITORIES: biostudies-literature