Zobrazeno 1 - 10
of 29
pro vyhledávání: '"Francesco Belardetti"'
Autor:
Sian D. Spacey, Francesco Belardetti
Publikováno v:
Wiley Interdisciplinary Reviews: Membrane Transport and Signaling. 1:433-451
Voltage gated calcium channels regulate numerous physiological functions, across a wide range of organ systems including heart, muscle, and brain. Different calcium channel subtypes have evolved to mediate specific cellular functions in these tissues
Autor:
Lina Chen, Hassan Pajouhesh, Cyrus Eduljee, Michael E. Hildebrand, Yongbao Zhu, Stephen P. Arneric, Molly Fee-Maki, Frank Porreca, Terrance P. Snutch, Paula L. Smith, Manjeet Parmar, Francesco Belardetti, Chris Bladen, David Parker, Clint J. Doering, Janette Mezeyova, Gerald W. Zamponi, Elizabeth Tringham, Jennifer Y. Xie
Publikováno v:
Pain. 152:833-843
Voltage-gated ion channels are implicated in pain sensation and transmission signaling mechanisms within both peripheral nociceptors and the spinal cord. Genetic knockdown and knockout experiments have shown that specific channel isoforms, including
Autor:
Francesco Belardetti
Publikováno v:
Future Medicinal Chemistry. 2:791-802
Clinical exploitation of the therapeutic potential of calcium channels has long been limited to L-type blockers for cardiovascular diseases. Recently, N-type blockers have been fully validated for the treatment of chronic pain, following approval of
Autor:
Terrance P. Snutch, Hossein Pajouhesh, Lingyun Zhang, Zhong-Ping Feng, Lester A. Mitscher, David Dolphin, Francesco Belardetti, Hassan Pajouhesh, Gerald W. Zamponi, Yanbing Ding
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:6467-6472
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
Autor:
Diana Janke, Haiheng Dong, David Parker, Hassan Pajouhesh, Francesco Belardetti, Afsheen Khawaja, Stephen P. Arneric, Terrance P. Snutch, Cyrus Eduljee, Robert A. Fraser, Adam Hendricson, Elizabeth Tringham, Yoko Shimizu, Xinpo Jiang, Janette Mezeyova
Publikováno v:
ASSAY and Drug Development Technologies. 7:266-280
T-type voltage-gated Ca(2+) channels have been implicated in contributing to a broad variety of human disorders, including pain, epilepsy, sleep disturbances, cardiac arrhythmias, and certain types of cancer. However, potent and selective T-type Ca(2
Publikováno v:
Neuropharmacology. 56:984-993
Dopamine (DA) efflux from terminals of the mesocorticolimbic system is linked to incentive motivation, drug dependency and schizophrenia. Strategies for modulating dopaminergic activity have focused on transmitter receptors or the DA transporter, not
Publikováno v:
Journal of Neurophysiology. 76:3559-3562
1. In NG108-15 cells dialyzed with 10 mM ethylene glycolbis (beta-aminoethyl ether)-N,N,N',N'-tetraacetic acid (EGTA) or bis (o-aminophenoxy)-N,N,N',N'-tetraacetic acid (BAPTA), bradykinin (BK) selectively inhibited the N-type calcium current. This e
Autor:
Soyon Ahn, Jordan J. Hynd, Cassie M. Macrae, James J. Miller, Anthony G. Phillips, Francesco Belardetti, Donovan M. Ashby, Kelly A. Butts, Christopher C. Lapish, Kitty So
Publikováno v:
The international journal of neuropsychopharmacology. 15(10)
Tetrahydroprotoberberines (THPBs) are compounds derived from traditional Chinese medicine and increasing preclinical evidence suggests efficacy in treatment of a wide range of symptoms observed in schizophrenia. A receptor-binding profile of the THPB
Autor:
Francesco Belardetti, Terrance P. Snutch, Zhong-Ping Feng, David Dolphin, Lester A. Mitscher, Gerald W. Zamponi, Hassan Pajouhesh, Lingyun Zhang, Hossein Pajouhesh, Yanbing Ding
Publikováno v:
ChemInform. 41
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
Autor:
Jerrie Lynn Morrison, Gerald W. Zamponi, Frank Porreca, Todd W. Vanderah, Elizabeth Tringham, Lester A. Mitscher, Eric Simonson, Terrance P. Snutch, Hossein Pajouhesh, Hassan Pajouhesh, Francesco Belardetti, Zhong Ping Feng, Lingyun Zhang, Yanbing Ding
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(4)
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 IC(50) values in the ran