Discovery and SAR of a novel series of 2,4,5,6-tetrahydrocyclopenta[c]pyrazoles as N-type calcium channel inhibitors |
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| Affiliation: | 1. Drug Discovery Research, Astellas Pharma Inc., 21, Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan;2. Pharmacovigilance, Astellas Pharma Inc., 2-5-1, Nihonbashi-Honcho, Chuo-ku, Tokyo 103-8411, Japan;1. Department of Biology, University of Southern Denmark, Campusvej 55, DK-5230 Odense M, Denmark;2. Department of Bioscience, Aarhus University, Frederiksborgvej 399, DK-4000 Roskilde, Denmark;1. Departamento de Ecología Evolutiva, Estación Biológica de Doñana—CSIC, C/Américo Vespucio s/n, 41092 Sevilla, Spain;2. Department of Chemistry, Fujita Health University School of Health Sciences, Toyoake, Aichi 470-1192, Japan;3. Instituto de Investigación en Recursos Cinegéticos (IREC)—CSIC-UCLM-JCCM, Ronda de Toledo s/n, 13005 Ciudad Real, Spain;4. Departamento de Bioquímica y Biología Molecular B e Inmunología, Facultad de Medicina, Universidad de Murcia, 30100 Murcia, Spain |
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| Abstract: | 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. |
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| Keywords: | N-type calcium channel Pain Rat CFA model |
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