Huang, Huoming; Li, Xueping; Xie, Peng; Li, Xinwei; Xu, XueJun; Qian, Yuanyuan; Yuan, Congmin; Meng, Xiangguo; Chai, JingRui; Chen, Jing; Liu, Jing; Wang, Wenli; Li, Wei; Wang, YuJun; Fu, Wei; Liu, Jinggen published their research in Journal of Medicinal Chemistry in 2021. The article was titled 《Discovery, Structure-Activity Relationship, and Mechanistic Studies of 1-((3R,4S)-3-((Dimethylamino)methyl)-4-hydroxy-4-(3-methoxyphenyl)piperidin-1-yl)-2-(2,4,5-trifluorophenyl)ethan-1-one as a Novel Potent Analgesic》.Synthetic Route of C7H7BrO The article contains the following contents:
Management of moderate to severe pain relies heavily on opioid analgesics such as morphine, oxycodone, and fentanyl in clinics. However, their prolonged use was associated with undesirable side effects. Many new strategies to reduce side effects have been proposed, but not without disadvantages. Using a hot plate model as a phenotypic screening method, our studies identified (3R,4S)-9d (I) with a new scaffold as a potent analgesic with ED50 values of 0.54 mg/kg and 0.021 mg/kg in hot plate and antiwrithing models, resp. Mechanistic studies showed that it elicited its analgesic effect via the active metabolite (3R,4S)-10a (II). The mechanism of (3R,4S)-10a-induced activation of the μ opioid receptor (MOR) was proposed by means of mol. dynamics (MD) simulation. In the part of experimental materials, we found many familiar compounds, such as 1-Bromo-3-methoxybenzene(cas: 2398-37-0Synthetic Route of C7H7BrO)
1-Bromo-3-methoxybenzene(cas: 2398-37-0) is a compound useful in organic synthesis and other chemical processes. It is an intermediate used for pharmaceuticals, perfumes and agrochemicals.Synthetic Route of C7H7BrO
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