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

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...

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Bibliographic Details
Other Authors:	Spetea, Mariana (Editor), Schmidhammer, Helmut (Editor)
Format:	Book Chapter
Published:	Basel, Switzerland MDPI - Multidisciplinary Digital Publishing Institute 2020
Subjects:	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 &amp 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
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Opioids and Their Receptors : Present and Emerging Concepts in Opioid Drug Discovery

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