41332-24-5Relevant articles and documents
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.
METHOD FOR INCREASING THE BIOAVAILABILITY OF BENZHYDRYL PIPERAZINE CONTAINING COMPOUNDS
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, (2009/12/27)
A method of increasing the bioavailability of a compound of formula 1 by orally administering to a patient a compound of formula 1, or a pharmaceutically acceptable salt thereof, with food:
CALCIUM CHANNEL BLOCKERS COMPRISING TWO BENZHYDRIL MOIETIES
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, (2008/06/13)
Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.
