866562-65-4Relevant academic research and scientific papers
Scaffold-based design and synthesis of potent N-type calcium channel blockers
Zamponi, Gerald W.,Feng, Zhong-Ping,Zhang, Lingyun,Pajouhesh, Hossein,Ding, Yanbing,Belardetti, Francesco,Pajouhesh, Hassan,Dolphin, David,Mitscher, Lester A.,Snutch, Terrance P.
, p. 6467 - 6472 (2009)
The therapeutic agents flunarizine and lomerizine exhibit inhibitory activities against a variety of ion channels and neurotransmitter receptors. We have optimized their scaffolds to obtain more selective N-type calcium channel blockers. During this optim
Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors
Pajouhesh, Hassan,Feng, Zhong-Ping,Ding, Yanbing,Zhang, Lingyun,Pajouhesh, Hossein,Morrison, Jerrie-Lynn,Belardetti, Francesco,Tringham, Elizabeth,Simonson, Eric,Vanderah, Todd W.,Porreca, Frank,Zamponi, Gerald W.,Mitscher, Lester A.,Snutch, Terrance P.
scheme or table, p. 1378 - 1383 (2010/07/06)
A novel series of compounds derived from the previously reported N-type calcium channel blocker NP118809 (1-(4-benzhydrylpiperazin-1-yl)-3,3-diphenylpropan-1-one) is described. Extensive SAR studies resulted in compounds with IC50 values in the range of 10-150 nM and selectivity over the L-type channels up to nearly 1200-fold. Orally administered compounds 5 and 21 exhibited both anti-allodynic and anti-hyperalgesic activity in the spinal nerve ligation model of neuropathic pain.
Diarylamine derivatives as calcium channel blockers
-
, (2008/06/13)
Compounds which are derivatives of diarylamine substituted piperazine and amino-piperidine are useful in treating conditions mediated by calcium ion channel activity.
