Akins, Nicholas S.; Mishra, Nisha; Harris, Hannah M.; Dudhipala, Narendar; Kim, Seong Jong; Keasling, Adam W.; Majumdar, Soumyajit; Zjawiony, Jordan K.; Paris, Jason J.; Ashpole, Nicole M.; Le, Hoang V. published the artcile< C2-Salvinorin Ester 6,5-Fused Ring, Dual Kappa and Mu Opioid Receptor Agonists as Analgesics Devoid of Anxiogenic Effects>, Recommanded Product: 5-Fluoroindole-2-carboxylic acid, the main research area is methoxycarbonyl hydroxy dimethyl dioxobenzoisochromene aryl ester opioid receptor agonist.
Current common analgesics are mediated through the mu or kappa opioid receptor agonism. Unfortunately, selective mu or kappa receptor agonists often cause harmful side effects. However, ligands exhibiting dual agonism to the opioid receptors, such as to mu and kappa, or to mu and delta, have been suggested to temper undesirable adverse effects while retaining analgesic activity. Herein we report an introduction of various 6,5-fused rings to C2 of the salvinorin scaffold via an ester linker. In vitro studies showed that many of these compounds have dual agonism on kappa and mu opioid receptors. In vivo studies on the lead dual kappa and mu opioid receptor agonist demonstrated supraspinal thermal analgesic activity while avoiding anxiogenic effects in male mice, thus providing further strong evidence in support of the therapeutic advantages of dual opioid receptor agonists over selective opioid receptor agonists.
ChemMedChem published new progress about Analgesics. 399-76-8 belongs to class indole-building-block, and the molecular formula is C9H6FNO2, Recommanded Product: 5-Fluoroindole-2-carboxylic acid.
Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles