Design and synthesis of peripherally restricted transient receptor potential vanilloid 1 (TRPV1) antagonists

…, H Liao, MM Stec, X Wang, P Chakrabarti…

文献索引：Tamayo, Nuria; Liao, Hongyu; Stec, Markian M.; Wang, Xianghong; Chakrabarti, Partha; Retz, Dan; Doherty, Elizabeth M.; Surapaneni, Sekhar; Tamir, Rami; Bannon, Anthony W.; Gavva, Narender R.; Norman, Mark H. Journal of Medicinal Chemistry, 2008 , vol. 51, # 9 p. 2744 - 2757

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被引用次数: 55

摘要

Transient receptor potential vanilloid 1 (TRPV1) channel antagonists may have clinical utility for the treatment of chronic nociceptive and neuropathic pain. We recently advanced a TRPV1 antagonist, 3 (AMG 517), into clinical trials as a new therapy for the treatment of pain. However, in addition to the desired analgesic effects, this TRPV1 antagonist significantly increased body core temperature following oral administration in rodents. Here, we report ...