《Novel TRPV1 Modulators with Reduced Pungency Induce Analgesic Effects in Mice》 was written by Treat, Anny; Henri, Vianie; Liu, Junke; Shen, Joyce; Gil-Silva, Mauricio; Morales, Alejandro; Rade, Avaneesh; Tidgewell, Kevin Joseph; Kolber, Benedict; Shen, Young. Application of 36016-38-3This research focused onTRPV1 agonists capsaicin analogs pungency reduction pain analgesics. The article conveys some information:
Capsaicin, the compound in hot chili peppers responsible for their pungency and an agonist of the transient receptor potential cation channel, subfamily V, member 1 (TRPV1), has long been known to promote the desensitization of nociceptors at high concentrations This has led to the utilization and implementation of topical capsaicin cream as an analgesic to treat acute and chronic pain. Critically, the application of capsaicin cream is limited due to capsaicin′s high pungency, which is experienced prior to analgesia. To combat this issue, novel capsaicin analogs were developed to provide analgesia with reduced pungency. Analogs reported in this paper add to and show some differences from previous structure-activity relationship (SAR) studies of capsaicin-like mols. against TRPV1, including the necessity of phenol in the aromatic “”A-region””, the secondary amide in the “”B-region””, and modifications in the hydrophobic “”C-region””. This provided a new framework for de novo small-mol. design using capsaicin as the starting point. In this study, we describe the synthesis of capsaicin analogs, their in vitro activity in Ca2+ assays, and initial in vivo pungency and feasibility studies of capsaicin analogs YB-11 and YB-16 as analgesics. Our results demonstrate that male and female mice treated with YB capsaicin analogs showed diminished pain-associated behavior in the spontaneous formalin assay as well as reduced thermal sensitivity in the hotplate assay. In the part of experimental materials, we found many familiar compounds, such as N-tert-Butoxycarbonylhydroxylamine(cas: 36016-38-3Application of 36016-38-3)
N-tert-Butoxycarbonylhydroxylamine(cas: 36016-38-3) belongs to anime. Examples of direct uses of amines and their salts are as corrosion inhibitors in boilers and in lubricating oils (morpholine), as antioxidants for rubber and roofing asphalt (diarylamines), as stabilizers for cellulose nitrate explosives (diphenylamine), as protectants against damage from gamma radiation (diarylamines), as developers in photography (aromatic diamines), as flotation agents in mining, as anticling and waterproofing agents for textiles, as fabric softeners, in paper coating, and for solubilizing herbicides.Application of 36016-38-3
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