Zobrazeno 1 - 10
of 24
pro vyhledávání: '"Mary Lou Lubin"'
Autor:
Ning Qin, Michael F.A. Finley, Christopher M. Flores, Michael P. Neeper, Michael P. Winters, Michael R. Brandt, Wall Mark, Nalin L. Subasinghe, Raymond W. Colburn, Zhihua Sui, Craig R. Schneider, Mary Lou Lubin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:3780-3783
A novel series of pyrazolyltetrahydropyran N-type calcium channel blockers are described. Structural modifications of the series led to potent compounds in both a cell-based fluorescent calcium influx assay and a patch clamp electrophysiology assay.
Autor:
Mark J, Wall, Nalin L, Subasinghe, Michael P, Winters, Mary Lou, Lubin, Michael F A, Finley, Ning, Qin, Michael R, Brandt, Michael P, Neeper, Craig R, Schneider, Raymond W, Colburn, Christopher M, Flores, Zhihua, Sui
Publikováno v:
Bioorganicmedicinal chemistry letters. 28(23-24)
A novel series of pyrazolyltetrahydropyran N-type calcium channel blockers are described. Structural modifications of the series led to potent compounds in both a cell-based fluorescent calcium influx assay and a patch clamp electrophysiology assay.
Autor:
Scott L. Dax, Mingde Xia, Dennis J. Stone, Xiaoqing Xu, Bin Zhu, Donald William Ludovici, Matthews Jay M, Mark A. Youngman, Tasha L. Hutchinson, Michael R. Brandt, Christopher M. Flores, Mary Lou Lubin, Mark J. Macielag, Raymond W. Colburn, Ning Qin, Manomi A. Tennakoon
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:2234-2237
A series of arylglycine-based analogs was synthesized and tested for TRPM8 antagonism in a cell-based functional assay. Following structure-activity relationship studies in vitro, a number of compounds were identified as potent TRPM8 antagonists and
Autor:
Michael R. Brandt, Michael F.A. Finley, Ning Qin, Michael P. Winters, Craig R. Schneider, Mary Lou Lubin, Michael P. Neeper, Nalin L. Subasinghe, Zhihua Sui, Raymond W. Colburn, Christopher M. Flores, Wall Mark
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:4080-4083
Selective blockers of the N-type calcium channel have proven to be effective in animal models of chronic pain. However, even though intrathecally delivered synthetic ω-conotoxin MVIIA from Conus magnus (ziconotide [Prialt®]) has been approved for t
Autor:
Shelley K. Ballentine, Mark R. Player, Mary Lou Lubin, Raul R. Calvo, Craig R. Schneider, William H. Parsons, Raymond W. Colburn, Parks Daniel J, Sanath K. Meegalla, Christopher M. Flores
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1903-1907
Thermosensitive transient receptor potential melastatin 8 (TRPM8) antagonists are considered to be potential therapeutic agents for the treatment of cold hypersensitivity. The discovery of a new class of TRPM8 antagonists that shows in vivo efficacy
Autor:
Yi Liu, Michael F.A. Finley, Mary Lou Lubin, Ning Qin, Michael P. Neeper, Christopher M. Flores, Edward J. Beck
Publikováno v:
ASSAY and Drug Development Technologies. 8:685-694
The N-type voltage-gated calcium channel (Cav2.2) has been intensively explored as a target for novel, small-molecule analgesic drugs because of its distribution in the pain pathway and its role in nociceptive processing. For example, Cav2.2 is local
Autor:
Mary Lou Lubin, Danielle Lawrence, Ning Qin, Yi Liu, Michael R. D'Andrea, Michael R. Brandt, Dennis J. Stone, Yan Wang, Christopher M. Flores, Raymond W. Colburn
Publikováno v:
Neuron. 54(3):379-386
Thermosensation is an essential sensory function that is subserved by a variety of transducer molecules, including those from the Transient Receptor Potential (TRP) ion channel superfamily. One of its members, TRPM8 (CMR1), a ligand-gated, nonselecti
Publikováno v:
European Journal of Biochemistry. 270:4762-4770
The voltage gated sodium channel comprises a pore-forming α subunit and regulatory β subunits. We report here the identification and characterization of a novel splicing variant of the human β1 subunit, termed β1B. The 807 bp open reading frame o
Autor:
Ning Qin, Mary Lou Lubin, Michael R. Brandt, Edward J. Beck, Zhihua Sui, Christopher M. Flores, Michael P. Winters, Yi Liu, Michael P. Neeper, Michael F.A. Finley, Wall Mark, Nalin L. Subasinghe
Publikováno v:
Bioorganicmedicinal chemistry letters. 24(9)
A novel series of substituted tetrahydropyrrolo[3,4-c]pyrazoles were investigated as blockers of the N-type calcium channel (Cav2.2 channels), a chronic pain target.
Autor:
Yi Liu, Mary Lou Lubin, Christopher M. Flores, Michael P. Winters, Michael F.A. Finley, Wall Mark, Ning Qin, Nalin L. Subasinghe, Michael R. Brandt, Michael P. Neeper, Zhihua Sui, Edward J. Beck
Publikováno v:
Bioorganicmedicinal chemistry letters. 24(9)
A novel series of substituted 2,4,5,6-tetrahydrocyclopenta[c]pyrazoles were investigated as N-type calcium channel blockers (Cav2.2 channels), a chronic pain target. One compound was active in vivo in the rat CFA pain model.