Opioids and Their Receptors Present and Emerging Concepts in Opioid Drug Discovery

• Andere auteurs: Spetea, Mariana (Redacteur), Schmidhammer, Helmut (Redacteur)
• Formaat: Elektronisch Hoofdstuk
• Taal: Engels
• Gepubliceerd in: Basel, Switzerland MDPI - Multidisciplinary Digital Publishing Institute 2020
• Onderwerpen: Medicine; opioid receptors; neurokinin-1 receptor; peptide synthesis; receptor binding studies; functional assay; writhing test; tolerance; Leu-enkephalin; beta-arrestin; mu opioid receptor; delta opioid receptor; biased signaling; DADLE; ischemia; plasma stability; morphinan; BNTX; δ opioid receptor antagonist; 1H-NMR experiments; mechanism elucidation; peripheral antinociception; 14-methoxycodeine-6-O-sulfate; codeine-6-O-sulfate; opioid peptides and peptidomimetics; DAMGO; DALDA; [Dmt1]DALDA; KGOP01; binding; molecular docking; structure-activity relationships; β2-amino acids; β2-Homo-amino acids; µ-opioid receptor; opioid peptides; TAPP; racemic synthesis of β2-amino acids; peripheral µ-opioid receptors; analgesia; peripheral analgesic tolerance; dysbiosis; opioid; bifunctional ligands; (−)-N-phenethylnorhydromorphone analogs; [35S]GTPgammaS assay; forskolin-induced cAMP accumulation assays; β-arrestin recruitment assays; MOR and DOR agonists; respiratory depression; bias factor; molecular modeling & simulation; δ opioid receptor; NTI derivative; sulfonamide; inverse agonist; neutral antagonist; agonist; opioids; mu receptor; opioid side effects; biased agonism; partial agonism; zerumbone; chronic constriction injury (CCI); allodynia; hyperalgesia; potassium channels; over-the-counter drugs; misuse; abuse; opioid drugs; pharmacology; codeine; dihydrocodeine; loperamide; opioid peptide; macrocyclic tetrapeptide; multifunctional ligands; kappa opioid receptor; analgesics; opioid liabilities; μ opioid receptor; receptor model; biased ligands; dependence; pain therapy; neonatal opioid withdrawal syndrome; naltrexone; 6β-naltrexol; buprenorphine; G-protein bias; arrestin recruitment; respiration; mitragynine; heteromer; internalization; primary hippocampal culture; lysosomes; µ opioid receptor; molecular dynamics; docking; interaction fingerprints; biased agonists; SR-17018; PZM21; morphine; fentanyl; diphenethylamines; design and synthesis; partial agonist; biased agonist; antagonist; binding affinity; selectivity; n/a
• Online toegang: DOAB: download the publication; DOAB: description of the publication

The interest in opioids such as morphine, the prototypical opioid ligand, has been maintained through the years. The identification of endogenous opioids and their receptors (mu, delta, kappa, and nociceptin), molecular cloning, and the elucidation of the crystal structures of opioid receptors repre...