1-Bromo-3-methoxybenzene(cas: 2398-37-0) can be used in chemical reaction as intermediates to obtain target materials such as dyes, pharmaceuticals, perfumes, photoinitiators and agrochemicals.Application of 2398-37-0
Huang, Huoming; Li, Xinwei; Guo, Wei; Zhu, Chen; Qian, Yuanyuan; Shen, Qing; Xu, Xuejun; Li, Wei; Wang, Yujun; Fu, Wei published an article in 2021. The article was titled 《Design, Synthesis, and Structure-Activity Relationship Exploration of Alkyl/Phenylalkyl Piperidine Analogues as Novel Highly Potent and Selective μ Opioid Receptor Agonists》, and you may find the article in ACS Chemical Neuroscience.Application of 2398-37-0 The information in the text is summarized as follows:
Pain was implicated in many diseases. Despite effectiveness to treat moderate to severe pain, opioid analgesics elicited many side effects, greatly limiting their prescription in clinics. Based on M1, an active metabolite of tramadol, 3-((dimethylamino)methyl)-4-(3-hydroxyphenyl)piperidin-4-ol analogs were designed, synthesized, and evaluated in vitro. Among all the compounds tested, compound 23 was found to be a novel, highly selective, and potent MOR agonist (Ki MOR = 0.0034 nM, EC50 MOR = 0.68 nM, Emax = 206.5%; Ki DOR = 41.67 nM; Ki KOR = 7.9 nM). Structure-activity relationship exploration showed that the linker between the piperidine ring and the Ph ring as well as substituent pattern of the Ph ring played a pivotal role in binding affinity and selectivity. (3R, 4S)-23(I) (Ki MOR = 0.0021 ± 0.0001 nM, EC50 MOR = 0.0013 ± 0.0001 nM, Emax = 209.1 ± 1.4%; Ki DOR = 18.4 ± 0.7 nM, EC50 DOR = 74.5 ± 2.8 nM, Emax = 267.1 ± 1.4%; Ki KOR = 25.8 ± 0.2 nM, EC50 DOR = 116.2 ± 4.4 nM, Emax = 209.5 ± 1.4%) had more potent activity for opioid receptors than its enantiomer (3S, 4R)-23 and was found to be a potent, highly selective MOR agonist with novel scaffold. High binding affinity and selectivity of (3R, 4S)-23 for MOR over KOR and DOR and its mechanism of activating MOR were proposed by docking and mol. dynamics simulations, resp. In the experiment, the researchers used many compounds, for example, 1-Bromo-3-methoxybenzene(cas: 2398-37-0Application of 2398-37-0)
1-Bromo-3-methoxybenzene(cas: 2398-37-0) can be used in chemical reaction as intermediates to obtain target materials such as dyes, pharmaceuticals, perfumes, photoinitiators and agrochemicals.Application of 2398-37-0
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