发现乙烯基环烷基取代苯并咪唑 TRPM8 拮抗剂可有效治疗冷感觉异常。
Discovery of vinylcycloalkyl-substituted benzimidazole TRPM8 antagonists effective in the treatment of cold allodynia.
机构信息
Janssen Research & Development, Welsh and McKean Roads, Spring House, PA 19477-0776, USA.
出版信息
Bioorg Med Chem Lett. 2012 Mar 1;22(5):1903-7. doi: 10.1016/j.bmcl.2012.01.060. Epub 2012 Jan 28.
PMID:22330635
Abstract
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 in the rat chronic constriction injury (CCI)-induced model of neuropathic pain is described.
摘要
热敏瞬时受体电位 melastatin 8（TRPM8）拮抗剂被认为是治疗冷感觉过敏的潜在治疗剂。本文描述了一类新的 TRPM8 拮抗剂的发现，该拮抗剂在大鼠慢性缩窄性损伤（CCI）诱导的神经病理性疼痛模型中显示出体内疗效。
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