Referenced in: none

Automatically associated channels: Cav3.2

Title: T-type calcium channel blockers: spiro-piperidine azetidines and azetidinones-optimization, design and synthesis.

Authors: Elizabeth M Smith, Steve Sorota, Hyunjin M Kim, Brian A McKittrick, Terry L Nechuta, Chad Bennett, Chad Knutson, Duane A Burnett, Jane Kieselgof, Zheng Tan, Diane Rindgen, Terry Bridal, Xiaoping Zhou, Yu-Ping Jia, Zoe Dong, Debbie Mullins, Xiaoping Zhang, Tony Priestley, Craig C Correll, Deen Tulshian, Michael Czarniecki, William J Greenlee

Journal, date & volume: Bioorg. Med. Chem. Lett., 2010 Aug 1 , 20, 4602-6

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/20580233

Abstract
A series of spiro-azetidines and azetidinones has been evaluated as novel blockers of the T-type calcium channel (Ca(V)3.2) which is a new therapeutic target for the potential treatment of both inflammatory and neuropathic pain. Confirmation and optimization of the potency, selectivity and DMPK properties of leads will be described.