Discovery and optimization of a novel series of pyrazolyltetrahydropyran N-type calcium channel (Cav 2.2) blockers for the treatment of pain
| 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 |
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| Rok vydání: | 2018 |
| Předmět: |
010405 organic chemistry
Chemistry Calcium channel Organic Chemistry Clinical Biochemistry Patch clamp electrophysiology Cell Pharmaceutical Science Pharmacology N-type calcium channel 010402 general chemistry 01 natural sciences Biochemistry 0104 chemical sciences medicine.anatomical_structure Drug Discovery Neuropathic pain medicine Molecular Medicine Molecular Biology Calcium influx |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 28:3780-3783 |
| ISSN: | 0960-894X |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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