{"doi":"10.1016/j.bmcl.2013.03.101","title":"Designing bifunctional NOP receptor–mu opioid receptor ligands from NOP receptor-selective scaffolds. Part I.","abstract":null,"journal":"Bioorganic &amp; Medicinal Chemistry Letters","year":2013,"id":620775,"datarank":0.5495342469194471,"base_score":3.6635616461296463,"endowment":3.6635616461296463,"self_citation_contribution":0.5495342469194471,"citation_network_contribution":0.0,"self_endowment_contribution":0.5495342469194471,"citer_contribution":0.0,"corpus_percentile":null,"corpus_rank":null,"citation_count":38,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":1,"is_dataset":false,"is_dataset_confidence":null,"is_data_producer":false,"deposit_databanks":null,"is_oa":false,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":null,"fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":1585560,"name":"Faming Jiang","orcid":null,"position":1,"is_corresponding":false},{"id":1585561,"name":"Cris Olsen","orcid":null,"position":2,"is_corresponding":false},{"id":793548,"name":"Willma E. Polgar","orcid":null,"position":3,"is_corresponding":false},{"id":443580,"name":"Lawrence Toll","orcid":"0000-0002-4501-7573","position":4,"is_corresponding":false},{"id":792996,"name":"Nurulain T. Zaveri","orcid":"0000-0002-6850-6732","position":0,"is_corresponding":false}],"reference_count":0,"raw_metadata":{"has_enrichment":true,"resolved":true,"title":"Designing bifunctional NOP receptor–mu opioid receptor ligands from NOP receptor-selective scaffolds. Part I.","abstract":"The nociceptin receptor (NOP) and its endogenous agonist, nociceptin/orphanin FQ (N/OFQ), members of the opioid receptor and peptide families respectively, modulate the pharmacological effects of classical opioids, particularly opioid-induced reward and nociception. We hypothesized that compounds containing both NOP and opioid receptor activity in a single molecule may have useful pharmacological profiles as non-addicting analgesics or as drug abuse medications. We report here our forays into the structure-activity relationships for discovering 'bifunctional' NOP-mu opioid receptor (MOP) ligands, starting from our NOP-selective scaffolds. This initial SAR suggests pharmacophoric elements that may be modified to modulate/increase opioid affinity, while maintaining high affinity for the NOP receptor, to result in potent bifunctional small-molecule NOP/MOP ligands.","is_dataset_classified":null,"base_score":3.6635616461296463,"endowment":3.6635616461296463,"datacite_reuse_total":1,"file_count":0,"downloads":0,"views":0,"has_version_chain":false,"is_dataset":false,"is_oa":false,"pmid":"23623415","pmcid":"PMC3651809","openalex_id":"https://openalex.org/W2009644683","authors":[],"funders":[{"funder_name":"NIDA NIH HHS","grant_id":"R01 DA027811","title":null},{"funder_name":"NIDA NIH HHS","grant_id":"R01 DA014026","title":null},{"funder_name":"NIDA NIH HHS","grant_id":"R01DA14026","title":null},{"funder_name":"NIDA NIH HHS","grant_id":"R01 DA023281","title":null}],"total_grants":4,"fwci":1.557,"citation_percentile":0.79663015,"influential_citations":0,"citation_trend":[{"year":2013,"count":1},{"year":2014,"count":3},{"year":2015,"count":3},{"year":2016,"count":5},{"year":2017,"count":5},{"year":2018,"count":4},{"year":2019,"count":7},{"year":2020,"count":2},{"year":2021,"count":1},{"year":2022,"count":1},{"year":2023,"count":2},{"year":2024,"count":3},{"year":2026,"count":1}],"oa_status":"green","license":"https://www.elsevier.com/legal/tdmrep-license","oa_locations":[{"url":"https://www.ncbi.nlm.nih.gov/pmc/articles/3651809","host_type":"repository"},{"url":"https://www.ncbi.nlm.nih.gov/pmc/articles/3651809","host_type":"repository"},{"url":"https://api.elsevier.com/content/article/PII:S0960894X13004290?httpAccept=text/xml","host_type":"publisher"},{"url":"https://api.elsevier.com/content/article/PII:S0960894X13004290?httpAccept=text/plain","host_type":"publisher"},{"url":"https://doi.org/10.1016/j.bmcl.2013.03.101","host_type":"journal"},{"url":"https://pubmed.ncbi.nlm.nih.gov/23623415","host_type":"repository"},{"url":"http://europepmc.org/articles/PMC3651809","host_type":"repository"},{"url":"https://doi.org/10.7270/q2t43vhn","host_type":"repository"}],"fields_of_study":["Neuropeptides and Animal Physiology","Receptor Mechanisms and Signaling","Pharmacological Receptor Mechanisms and Effects"],"mesh_terms":["Nociceptin Receptor","Piperidines","Protein Binding","Receptors, Opioid","Structure-Activity Relationship","Drug Design","Receptors, Opioid, mu"],"keywords":["NOP","Nociceptin receptor","Chemistry","Opioid receptor","Opioid","Receptor","Pharmacology","Agonist","Bifunctional","Opioid peptide","Stereochemistry","Biochemistry","Medicine"],"sdg_mappings":[{"sdg_number":0,"sdg_label":"Good health and well-being"}],"linked_datasets":[{"doi":"10.7270/q2t43vhn","title":"BindingDB Entry 50043020: Designing bifunctional NOP receptor-mu opioid receptor ligands from NOP receptor-selective scaffolds. 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