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

Title
Structural hybridization of pyrrolidine-based T-type calcium channel inhibitors and exploration of their analgesic effects in a neuropathic pain model
Authors
배애님임상민손우승정규성
Keywords
Neuropathic pain; T-type calcium channel
Issue Date
2019-05
Publisher
Bioorganic & medicinal chemistry letters
Citation
VOL 29, NO 10-1172
Abstract
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.
URI
http://pubs.kist.re.kr/handle/201004/70487
ISSN
0960-894X
Appears in Collections:
KIST Publication > Article
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