Zheng, Yi; Obeng, Samuel; Wang, Huiqun; Jali, Abdulmajeed M.; Peddibhotla, Bharath; Williams, Dwight A.; Zou, Chuanchun; Stevens, David L.; Dewey, William L.; Akbarali, Hamid I.; Selley, Dana E.; Zhang, Yan published an article on January 24 ,2019. The article was titled 《Design, Synthesis, and Biological Evaluation of the Third Generation 17-Cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6β-[(4′-pyridyl)carboxamido]morphinan (NAP) Derivatives as μ/κ Opioid Receptor Dual Selective Ligands》, and you may find the article in Journal of Medicinal Chemistry.Recommanded Product: 59290-82-3 The information in the text is summarized as follows:
μ Opioid receptor (MOR) agonists have been widely applied for treating moderate to severe pain. However, numerous adverse effects have been associated with their application, including opioid-induced constipation (OIC), respiratory depression, and addiction. On the basis of previous work in our laboratory, NAP, a 6β-N-4′-pyridyl substituted naltrexamine derivative, was identified as a peripheral MOR antagonist that may be used to treat OIC. To further explore its structure-activity relationship, a new series of NAP derivatives were designed, synthesized, and biol. evaluated. Among these derivatives, NFP and NYP significantly antagonized the antinociception effect of morphine. Whereas NAP acted mainly peripherally, its derivatives NFP and NYP actually can act centrally. Furthermore, NFP produced significantly lesser withdrawal symptoms than naloxone at similar doses. These results suggest that NFP has the potential to be a lead compound to treat opioid abuse and addiction. The experimental part of the paper was very detailed, including the reaction process of 3-Nitroisonicotinic acid(cas: 59290-82-3Recommanded Product: 59290-82-3)
3-Nitroisonicotinic acid(cas: 59290-82-3) belongs to pyridine. Pyridine, its benzo and pyridine-based compounds play diverse roles in organic chemistry. As ligands, solvents, and catalysts they facilitate reactions; thus descriptions of these new ligands and their applications abound each year.Recommanded Product: 59290-82-3