Optimization of potency and pharmacokinetic properties of tetrahydroisoquinoline transient receptor potential melastatin 8 (TRPM8) Antagonists

…, MD Bartberger, Y Bo, J Clarine, CD Davis…

文献索引：Horne, Daniel B.; Tamayo, Nuria A.; Bartberger, Michael D.; Bo, Yunxin; Clarine, Jeffrey; Davis, Carl D.; Gore, Vijay K.; Kaller, Matthew R.; Lehto, Sonya G.; Ma, Vu V.; Nishimura, Nobuko; Nguyen, Thomas T.; Tang, Phi; Wang, Weiya; Youngblood, Beth D.; Zhang, Maosheng; Gavva, Narender R.; Monenschein, Holger; Norman, Mark H. Journal of Medicinal Chemistry, 2014 , vol. 57, # 7 p. 2989 - 3004

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被引用次数: 16

摘要

Transient receptor potential melastatin 8 (TRPM8) is a nonselective cation channel expressed in a subpopulation of sensory neurons in the peripheral nervous system. TRPM8 is the predominant mammalian cold temperature thermosensor and is activated by cold temperatures ranging from 8 to 25° C and cooling compounds such as menthol or icilin. TRPM8 antagonists are being pursued as potential therapeutics for treatment of pain and ...