Zhang, Mengna published the artcileDevelopment of Multifunctional and Orally Active Cyclic Peptide Agonists of Opioid/Neuropeptide FF Receptors that Produce Potent, Long-Lasting, and Peripherally Restricted Antinociception with Diminished Side Effects, Application In Synthesis of 77128-73-5, the publication is Journal of Medicinal Chemistry (2021), 64(18), 13394-13409, database is CAplus and MEDLINE.
We previously reported that a multifunctional opioid/neuropeptide FF receptor agonist, DN-9, achieved peripherally restricted analgesia with reduced side effects. To develop stable and orally bioavailable analogs of DN-9, eight lactam-bridged cyclic analogs of DN-9 between positions 2 and 5 were designed, synthesized, and biol. evaluated. In vitro cAMP assays revealed that these analogs, except 7, were multifunctional ligands that activated opioid and neuropeptide FF receptors. Analog 1 exhibited improved potency for κ-opioid and NPFF2 receptors. All analogs exhibited potent, long-lasting, and peripherally restricted antinociception in the tail-flick test without tolerance development after s.c. administration and produced oral analgesia. Oral administration of the optimized compound analog 1 exhibited powerful, peripherally restricted antinociceptive effects in mouse models of acute, inflammatory, and neuropathic pain. Remarkably, orally administered analog 1 had no significant side effects, such as tolerance, dependence, constipation, or respiratory depression, at effective analgesic doses.
Journal of Medicinal Chemistry published new progress about 77128-73-5. 77128-73-5 belongs to ethers-buliding-blocks, auxiliary class Inhibitor, name is (S)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)(methyl)amino)-3-phenylpropanoic acid, and the molecular formula is C7H5Br2F, Application In Synthesis of 77128-73-5.
Referemce:
https://en.wikipedia.org/wiki/Ether,
Ether | (C2H5)2O – PubChem