LEADER 06569nam 2201753z- 450 001 9910557108003321 005 20231214132947.0 035 $a(CKB)5400000000040967 035 $a(oapen)https://directory.doabooks.org/handle/20.500.12854/69428 035 $a(EXLCZ)995400000000040967 100 $a20202105d2020 |y 0 101 0 $aeng 135 $aurmn|---annan 181 $ctxt$2rdacontent 182 $cc$2rdamedia 183 $acr$2rdacarrier 200 10$aOpioids and Their Receptors$ePresent and Emerging Concepts in Opioid Drug Discovery 210 $aBasel, Switzerland$cMDPI - Multidisciplinary Digital Publishing Institute$d2020 215 $a1 electronic resource (358 p.) 311 $a3-0365-0046-4 311 $a3-0365-0047-2 330 $aThe 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 represent key milestones in opioid research. The opioid system modulates numerous pharmacological responses, with therapeutic (i.e., analgesia) and detrimental side effects (i.e., addiction). The medical use and misuse of opioids have dramatically increased, leading to the 21st century opioid crisis. This book presents recent developments in opioid drug discovery, specifically in the medicinal chemistry and pharmacology of new ligands targeting the opioid receptors as effective and safe therapeutics for human diseases. Furthermore, it draws a special attention to advancing concepts and strategies in opioid drug discovery to mitigate opioid liabilities. The diversity among the discussed topics is a testimony to the complexity of the opioid system, which results from the expression, regulation, and functional role of ligands and receptors. The array of multidisciplinary research areas illustrates the rapidly developing basic research and translational activities in opioid drug discovery. This book will serve as a useful reference while also stimulating continued research in the chemistry and pharmacology of opioids and their receptors, with the prospect of developing improved therapies for human diseases, but also improving health and quality of life in general. 517 $aOpioids and Their Receptors 606 $aMedicine$2bicssc 610 $aopioid receptors 610 $aneurokinin-1 receptor 610 $apeptide synthesis 610 $areceptor binding studies 610 $afunctional assay 610 $awrithing test 610 $atolerance 610 $aLeu-enkephalin 610 $abeta-arrestin 610 $amu opioid receptor 610 $adelta opioid receptor 610 $abiased signaling 610 $aDADLE 610 $aischemia 610 $aplasma stability 610 $amorphinan 610 $aBNTX 610 $a? opioid receptor antagonist 610 $a1H-NMR experiments 610 $amechanism elucidation 610 $aperipheral antinociception 610 $a14-methoxycodeine-6-O-sulfate 610 $acodeine-6-O-sulfate 610 $aopioid peptides and peptidomimetics 610 $aDAMGO 610 $aDALDA 610 $a[Dmt1]DALDA 610 $aKGOP01 610 $abinding 610 $amolecular docking 610 $astructure-activity relationships 610 $a?2-amino acids 610 $a?2-Homo-amino acids 610 $aµ-opioid receptor 610 $aopioid peptides 610 $aTAPP 610 $aracemic synthesis of ?2-amino acids 610 $aperipheral µ-opioid receptors 610 $aanalgesia 610 $aperipheral analgesic tolerance 610 $adysbiosis 610 $aopioid 610 $abifunctional ligands 610 $a(?)-N-phenethylnorhydromorphone analogs 610 $a[35S]GTPgammaS assay 610 $aforskolin-induced cAMP accumulation assays 610 $a?-arrestin recruitment assays 610 $aMOR and DOR agonists 610 $arespiratory depression 610 $abias factor 610 $amolecular modeling & 610 $asimulation 610 $a? opioid receptor 610 $aNTI derivative 610 $asulfonamide 610 $ainverse agonist 610 $aneutral antagonist 610 $aagonist 610 $aopioids 610 $amu receptor 610 $aopioid side effects 610 $abiased agonism 610 $apartial agonism 610 $azerumbone 610 $achronic constriction injury (CCI) 610 $aallodynia 610 $ahyperalgesia 610 $apotassium channels 610 $aover-the-counter drugs 610 $amisuse 610 $aabuse 610 $aopioid drugs 610 $apharmacology 610 $acodeine 610 $adihydrocodeine 610 $aloperamide 610 $aopioid peptide 610 $amacrocyclic tetrapeptide 610 $amultifunctional ligands 610 $akappa opioid receptor 610 $aanalgesics 610 $aopioid liabilities 610 $a? opioid receptor 610 $areceptor model 610 $abiased ligands 610 $adependence 610 $apain therapy 610 $aneonatal opioid withdrawal syndrome 610 $analtrexone 610 $a6?-naltrexol 610 $abuprenorphine 610 $aG-protein bias 610 $aarrestin recruitment 610 $arespiration 610 $amitragynine 610 $aheteromer 610 $ainternalization 610 $aprimary hippocampal culture 610 $alysosomes 610 $aµ opioid receptor 610 $amolecular dynamics 610 $adocking 610 $ainteraction fingerprints 610 $abiased agonists 610 $aSR-17018 610 $aPZM21 610 $amorphine 610 $afentanyl 610 $adiphenethylamines 610 $adesign and synthesis 610 $astructure-activity relationships 610 $apartial agonist 610 $abiased agonist 610 $aantagonist 610 $abinding affinity 610 $aselectivity 615 7$aMedicine 700 $aSpetea$b Mariana$4edt$01304705 702 $aSchmidhammer$b Helmut$4edt 702 $aSpetea$b Mariana$4oth 702 $aSchmidhammer$b Helmut$4oth 906 $aBOOK 912 $a9910557108003321 996 $aOpioids and Their Receptors$93027635 997 $aUNINA