Xiong, Jiaying; Zhuang, Tao; Ma, Yurong; Xu, Junyi; Ye, Jiaqi; Ma, Ru; Zhang, Shuang; Liu, Xin; Liu, Bi-Feng; Hao, Chao; Zhang, Guisen; Chen, Yin published an article in 2021. The article was titled 《Optimization of bifunctional piperidinamide derivatives as σ1R Antagonists/MOR agonists for treating neuropathic pain》, and you may find the article in European Journal of Medicinal Chemistry.SDS of cas: 4755-77-5 The information in the text is summarized as follows:
Described the optimization, synthesis and associated pharmacol. analgesic activities of a new series of bifunctional piperidinamide derivatives I [R1 = H, Me; R2 = H, Me, Et; R3 = H, Me, Ph etc.; R4 = Et, acetyl, cyclopropanecarbonyl etc.; R5 = 1-ethylpropyl, cyclohexyl, 4-fluorophenyl] as sigma-1 receptor (σ1R) antagonists and mu opioid receptor (MOR) agonists. The new compounds I were evaluated in-vitro in σ1R and MOR binding assays. The most promising compound I [R1 = H; R2 = Me; R3 = benzyl; R4 = propanoyl; R5 = ph] (also called HKC-126), showed superior affinities for σ1R and MOR and good selectivity to addnl. receptors related to pain. Compound I [R1 = H; R2 = Me; R3 = benzyl; R4 = propanoyl; R5 = ph] showed powerful dose-dependent analgesic effects in the acetic acid writhing test, formalin test, hot plate test and chronic constriction injury (CCI) neuropathic pain model. In contrast to an equianalgesic dose of fentanyl, compound I [R1 = H; R2 = Me; R3 = benzyl; R4 = propanoyl; R5 = ph] produced fewer opioid-like side effects, such as reward liability, respiratory depression, phys. dependence and sedation. Lastly, the pharmacokinetic properties of this drug were also acceptable and these results suggested that compound I [R1 = H; R2 = Me; R3 = benzyl; R4 = propanoyl; R5 = ph] as a mixed σ1R/MOR ligand, was potential for treating neuropathic pain.Ethyl oxalyl monochloride(cas: 4755-77-5SDS of cas: 4755-77-5) was used in this study.
Ethyl oxalyl monochloride(cas: 4755-77-5) belongs to acyl chlorides. Lacking the ability to form hydrogen bonds, acyl chlorides have lower boiling and melting points than similar carboxylic acids. For example, acetic acid boils at 118 °C, whereas acetyl chloride boils at 51 °C. Like most carbonyl compounds, infrared spectroscopy reveals a band near 1750 cm−1.SDS of cas: 4755-77-5
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