Structural hybridization of pyrrolidine-based T-type calcium channel inhibitors and exploration of their analgesic effects in a neuropathic pain model

Add time:08/27/2019    Source:sciencedirect.com

Highly effective and safe drugs for the treatment of neuropathic pain are urgently required and it was shown that blocking T-type calcium channels can be a promising strategy for drug development for neuropathic pain. We have developed pyrrolidine-based T-type calcium channel inhibitors by structural hybridization and subsequent assessment of in vitro activities against Cav3.1 and Cav3.2 channels. Profiling of in vitro ADME properties of compounds was also carried out. The representative compound 17h showed comparable in vivo efficacy to gabapentin in the SNL model, which indicates T-type calcium channel inhibitors can be developed as effective therapeutics for neuropathic pain.

We also recommend Trading Suppliers and Manufacturers of Pyrrolidine, 1-[4-(trifluoroMethyl)phenyl]- (cas 113845-68-4). Pls Click Website Link as below: cas 113845-68-4 suppliers

Prev:Synthesis and anticonvulsant activity of new 1-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]pyrrolidine-2,5-diones
Next:Synthesis of trifluoromethylated pyrrolidines via decarboxylative [3+2] cycloaddition of non-stabilized N-unsubstituted azomethine ylides)