用于治疗疼痛的新型吡唑基四氢吡喃N型钙通道（Ca 2.2）阻滞剂的发现与优化。
Discovery and optimization of a novel series of pyrazolyltetrahydropyran N-type calcium channel (Ca 2.2) blockers for the treatment of pain.
作者信息
Wall Mark J, Subasinghe Nalin L, Winters Michael P, Lubin Mary Lou, Finley Michael F A, Qin Ning, Brandt Michael R, Neeper Michael P, Schneider Craig R, Colburn Raymond W, Flores Christopher M, Sui Zhihua
机构信息
Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA.
Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA.
出版信息
Bioorg Med Chem Lett. 2018 Dec 15;28(23-24):3780-3783. doi: 10.1016/j.bmcl.2018.10.007. Epub 2018 Oct 12.
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. Representative compounds from the series were bioavailable and showed efficacy in the rat CFA and CCI models of inflammatory and neuropathic pain.
描述了一系列新型的吡唑基四氢吡喃N型钙通道阻滞剂。该系列的结构修饰在基于细胞的荧光钙内流测定和膜片钳电生理测定中均产生了强效化合物。该系列的代表性化合物具有生物利用度，并在大鼠CFA和CCI炎症性和神经性疼痛模型中显示出疗效。
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