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dc.contributor.authorKumar, Vinod
dc.contributor.authorPolgar, Willma E.
dc.contributor.authorCami-Kobeci, Gerta
dc.contributor.authorThomas, Mark P.
dc.contributor.authorKhroyan, Taline V.
dc.contributor.authorToll, Lawrence
dc.contributor.authorHusbands, Stephen M.
dc.contributor.illustrator
dc.date.accessioned2020-11-26T12:23:31Z
dc.date.available2018-09-19T00:00:00Z
dc.date.available2020-11-26T12:23:31Z
dc.date.issued2018-09-19
dc.identifier.citationKumar V, Polgar WE, Cami-Kobeci G, Thomas MP, Khroyan TV, Toll L, Husbands SM (2018) 'Synthesis, biological evaluation, and SAR studies of 14β-phenylacetyl substituted 17-cyclopropylmethyl-7, 8-dihydronoroxymorphinones derivatives: Ligands with mixed NOP and opioid receptor profile', Frontiers in Psychiatry, 9, pp.430-.en_US
dc.identifier.issn1664-0640
dc.identifier.pmid30283364
dc.identifier.doi10.3389/fpsyt.2018.00430
dc.identifier.urihttp://hdl.handle.net/10547/624678
dc.description.abstractA series of 14β-acyl substituted 17-cyclopropylmethyl-7,8-dihydronoroxymorphinone compounds has been synthesized and evaluated for affinity and efficacy for mu (MOP), kappa (KOP), and delta (DOP) opioid receptors and nociceptin/orphanin FQ peptide (NOP) receptors. The majority of the new ligands displayed high binding affinities for the three opioid receptors, and moderate affinity for NOP receptors. The affinities for NOP receptors are of particular interest as most classical opioid ligands do not bind to NOP receptors. The predominant activity in the [35S]GTPγS assay was partial agonism at each receptor. The results are consistent with our prediction that an appropriate 14β side chain would access a binding site within the NOP receptor and result in substantially higher affinity than displayed by the parent compound naltrexone. Molecular modeling studies, utilizing the recently reported structure of the NOP receptor, are also consistent with this interpretation.en_US
dc.language.isoenen_US
dc.publisherFrontiers Media S.A.en_US
dc.relation.urlhttps://www.frontiersin.org/articles/10.3389/fpsyt.2018.00430/fullen_US
dc.rightsAttribution-NonCommercial-NoDerivatives 4.0 International*
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/4.0/*
dc.subjectMu opioid receptorsen_US
dc.subjectnociceptinen_US
dc.subjectKappa opioid receptor,en_US
dc.subjectanalgesicsen_US
dc.subjectORL-1en_US
dc.subjectopioiden_US
dc.subjectSubject Categories::B200 Pharmacology, Toxicology and Pharmacyen_US
dc.titleSynthesis, biological evaluation, and SAR studies of 14β-phenylacetyl substituted 17-cyclopropylmethyl-7, 8-dihydronoroxymorphinones derivatives: Ligands with mixed NOP and opioid receptor profileen_US
dc.typeArticleen_US
dc.identifier.eissn1664-0640
dc.contributor.departmentCentral University of Punjaben_US
dc.contributor.departmentSRI Internationalen_US
dc.contributor.departmentUniversity of Bathen_US
dc.contributor.departmentFlorida Atlantic Universityen_US
dc.identifier.journalFrontiers in Psychiatryen_US
dc.identifier.pmcidPMC6156383
dc.date.updated2020-11-26T11:54:19Z
dc.description.noteopen access


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