1228029-89-7Relevant academic research and scientific papers
Synthesis and SAR of 4-aminocyclopentapyrrolidines as N-type Ca 2+ channel blockers with analgesic activity
Beebe, Xenia,Darczak, Daria,Henry, Rodger F.,Vortherms, Timothy,Janis, Richard,Namovic, Marian,Donnelly-Roberts, Diana,Kage, Karen L.,Surowy, Carol,Milicic, Ivan,Niforatos, Wende,Swensen, Andrew,Marsh, Kennan C.,Wetter, Jill M.,Franklin, Pamela,Baker, Scott,Zhong, Chengmin,Simler, Gricelda,Gomez, Erica,Boyce-Rustay, Janel M.,Zhu, Chang Z.,Stewart, Andrew O.,Jarvis, Michael F.,Scott, Victoria E.
, p. 4128 - 4139 (2012/09/22)
A novel 4-aminocyclopentapyrrolidine series of N-type Ca2+ channel blockers have been discovered. Enantioselective synthesis of the 4-aminocyclopentapyrrolidines was enabled using N-tert-butyl sulfinamide chemistry. SAR studies demonstrate selectivity over L-type Ca2+ channels. N-type Ca2+ channel blockade was confirmed using electrophysiological recording techniques. Compound 25 is an N-type Ca 2+ channel blocker that produces antinociception in inflammatory and nociceptive pain models without exhibiting cardiovascular or motor liabilities.
