cas 41332-24-5, 1-[4-(DiphenylMethyl)-1-piperazinyl]-3,3-diphenyl-1-propanone

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Structure-activity relationships of diphenylpiperazine N-type calcium channel inhibitors
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.
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.
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p. 1378 - 1383
(2010/07/06)

Scaffold-based design and synthesis of potent N-type calcium channel blockers
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
Zamponi, Gerald W.,Feng, Zhong-Ping,Zhang, Lingyun,Pajouhesh, Hossein,Ding, Yanbing,Belardetti, Francesco,Pajouhesh, Hassan,Dolphin, David,Mitscher, Lester A.,Snutch, Terrance P.
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p. 6467 - 6472
(2010/04/30)

METHOD FOR INCREASING THE BIOAVAILABILITY OF BENZHYDRYL PIPERAZINE CONTAINING COMPOUNDS
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:
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(2009/12/27)

Calcium channel blockers comprising two benzhydril moieties
Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.
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(2008/06/13)

CALCIUM CHANNEL BLOCKERS COMPRISING TWO BENZHYDRIL MOIETIES
Certain piperazine substituted compounds are described which are useful in altering calcium channel activity.
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(2008/06/13)

Chemical Properties

Boiling Point: 618.9±55.0 °C(Predicted)
Density: 1.142±0.06 g/cm3(Predicted)
Storage Temp.:Sealed in dry,Room Temperature
PKA: 5.99±0.10(Predicted)
PSA: 23.55000
LogP: 6.01820

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Chemical Properties

Boiling Point: 618.9±55.0 °C(Predicted)

Density: 1.142±0.06 g/cm3(Predicted)

Storage Temp.:Sealed in dry,Room Temperature

PKA: 5.99±0.10(Predicted)

PSA: 23.55000

LogP: 6.01820

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