{"id":"https://openalex.org/W2030596402","doi":"https://doi.org/10.1039/c0md00249f","title":"Discovery and pharmacological characterization of a selective delta opiate receptor antagonist (CP-646,777)","display_name":"Discovery and pharmacological characterization of a selective delta opiate receptor antagonist (CP-646,777)","publication_year":2011,"publication_date":"2011-01-01","ids":{"openalex":"https://openalex.org/W2030596402","doi":"https://doi.org/10.1039/c0md00249f","mag":"2030596402"},"language":"en","primary_location":{"id":"doi:10.1039/c0md00249f","doi":"https://doi.org/10.1039/c0md00249f","is_oa":false,"landing_page_url":"https://doi.org/10.1039/c0md00249f","pdf_url":null,"source":{"id":"https://openalex.org/S191926780","display_name":"MedChemComm","issn_l":"2040-2503","issn":["2040-2503","2040-2511"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["cwts-core","ki-jl-1","norway-1","poland-70"],"host_organization":"https://openalex.org/P4310320556","host_organization_name":"Royal Society of Chemistry","host_organization_lineage":["https://openalex.org/P4310320556"],"host_organization_lineage_names":["Royal Society of Chemistry"],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"MedChemComm","raw_type":"journal-article"},"volume":null,"type":"article","indexed_in":["crossref"],"open_access":{"is_oa":false,"oa_status":"closed","oa_url":null,"any_repository_has_fulltext":false},"authorships":[{"author_position":"first","author":{"id":"https://openalex.org/A5072802372","display_name":"Spiros I. Liras","orcid":"https://orcid.org/0000-0002-0334-2095","observed_orcids":["https://orcid.org/0000-0002-0334-2095"]},"institutions":[{"id":"https://openalex.org/I180857899","display_name":"Pfizer (United States)","ror":"https://ror.org/01xdqrp08","country_code":"US","type":"company","lineage":["https://openalex.org/I180857899"]}],"countries":["US"],"is_corresponding":true,"raw_author_name":"Spiros Liras","raw_affiliation_strings":["Neuroscience Medicinal Chemistry, Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT, USA","Neuroscience Medicinal Chemistry, Pfizer Worldwide Research and Development, Eastern Point Road,Groton,USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Neuroscience Medicinal Chemistry, Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT, USA","institution_ids":["https://openalex.org/I180857899"]},{"raw_affiliation_string":"Neuroscience Medicinal Chemistry, Pfizer Worldwide Research and Development, Eastern Point Road,Groton,USA","institution_ids":["https://openalex.org/I180857899"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5010689843","display_name":"Stanton F. McHardy","orcid":"https://orcid.org/0000-0003-0070-4924","observed_orcids":["https://orcid.org/0000-0003-0070-4924"]},"institutions":[{"id":"https://openalex.org/I180857899","display_name":"Pfizer (United States)","ror":"https://ror.org/01xdqrp08","country_code":"US","type":"company","lineage":["https://openalex.org/I180857899"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Stanton F. McHardy","raw_affiliation_strings":["Neuroscience Medicinal Chemistry, Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT, USA","Neuroscience Medicinal Chemistry, Pfizer Worldwide Research and Development, Eastern Point Road,Groton,USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Neuroscience Medicinal Chemistry, Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT, USA","institution_ids":["https://openalex.org/I180857899"]},{"raw_affiliation_string":"Neuroscience Medicinal Chemistry, Pfizer Worldwide Research and Development, Eastern Point Road,Groton,USA","institution_ids":["https://openalex.org/I180857899"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5103855187","display_name":"Martin P. Allen","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I180857899","display_name":"Pfizer (United States)","ror":"https://ror.org/01xdqrp08","country_code":"US","type":"company","lineage":["https://openalex.org/I180857899"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Martin P. Allen","raw_affiliation_strings":["Neuroscience Medicinal Chemistry, Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT, USA","Neuroscience Medicinal Chemistry, Pfizer Worldwide Research and Development, Eastern Point Road,Groton,USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Neuroscience Medicinal Chemistry, Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT, USA","institution_ids":["https://openalex.org/I180857899"]},{"raw_affiliation_string":"Neuroscience Medicinal Chemistry, Pfizer Worldwide Research and Development, Eastern Point Road,Groton,USA","institution_ids":["https://openalex.org/I180857899"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5032532705","display_name":"Barb E. Segelstein","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I180857899","display_name":"Pfizer (United States)","ror":"https://ror.org/01xdqrp08","country_code":"US","type":"company","lineage":["https://openalex.org/I180857899"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Barb E. Segelstein","raw_affiliation_strings":["Neuroscience Medicinal Chemistry, Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT, USA","Neuroscience Medicinal Chemistry, Pfizer Worldwide Research and Development, Eastern Point Road,Groton,USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Neuroscience Medicinal Chemistry, Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT, USA","institution_ids":["https://openalex.org/I180857899"]},{"raw_affiliation_string":"Neuroscience Medicinal Chemistry, Pfizer Worldwide Research and Development, Eastern Point Road,Groton,USA","institution_ids":["https://openalex.org/I180857899"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5109250608","display_name":"Steven D. Heck","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I180857899","display_name":"Pfizer (United States)","ror":"https://ror.org/01xdqrp08","country_code":"US","type":"company","lineage":["https://openalex.org/I180857899"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Steven D. Heck","raw_affiliation_strings":["Neuroscience Medicinal Chemistry, Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT, USA","Neuroscience Medicinal Chemistry, Pfizer Worldwide Research and Development, Eastern Point Road,Groton,USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Neuroscience Medicinal Chemistry, Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT, USA","institution_ids":["https://openalex.org/I180857899"]},{"raw_affiliation_string":"Neuroscience Medicinal Chemistry, Pfizer Worldwide Research and Development, Eastern Point Road,Groton,USA","institution_ids":["https://openalex.org/I180857899"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5045329484","display_name":"Dianne K. Bryce","orcid":"https://orcid.org/0000-0002-2249-2240","observed_orcids":["https://orcid.org/0000-0002-2249-2240"]},"institutions":[{"id":"https://openalex.org/I180857899","display_name":"Pfizer (United States)","ror":"https://ror.org/01xdqrp08","country_code":"US","type":"company","lineage":["https://openalex.org/I180857899"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Dianne K. Bryce","raw_affiliation_strings":["Neuroscience Biology, Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT, USA","Neuroscience Biology, Pfizer Worldwide Research and Development, Eastern Point Road,Groton,USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Neuroscience Biology, Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT, USA","institution_ids":["https://openalex.org/I180857899"]},{"raw_affiliation_string":"Neuroscience Biology, Pfizer Worldwide Research and Development, Eastern Point Road,Groton,USA","institution_ids":["https://openalex.org/I180857899"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5037158935","display_name":"Anne W. Schmidt","orcid":"https://orcid.org/0000-0003-3222-5661","observed_orcids":["https://orcid.org/0000-0003-3222-5661"]},"institutions":[{"id":"https://openalex.org/I180857899","display_name":"Pfizer (United States)","ror":"https://ror.org/01xdqrp08","country_code":"US","type":"company","lineage":["https://openalex.org/I180857899"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Anne W. Schmidt","raw_affiliation_strings":["Neuroscience Biology, Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT, USA","Neuroscience Biology, Pfizer Worldwide Research and Development, Eastern Point Road,Groton,USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Neuroscience Biology, Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT, USA","institution_ids":["https://openalex.org/I180857899"]},{"raw_affiliation_string":"Neuroscience Biology, Pfizer Worldwide Research and Development, Eastern Point Road,Groton,USA","institution_ids":["https://openalex.org/I180857899"]}]},{"author_position":"middle","author":{"id":null,"display_name":"Rebecca O'Connor","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I180857899","display_name":"Pfizer (United States)","ror":"https://ror.org/01xdqrp08","country_code":"US","type":"company","lineage":["https://openalex.org/I180857899"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Rebecca O'Connor","raw_affiliation_strings":["Neuroscience Biology, Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT, USA","Neuroscience Biology, Pfizer Worldwide Research and Development, Eastern Point Road,Groton,USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Neuroscience Biology, Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT, USA","institution_ids":["https://openalex.org/I180857899"]},{"raw_affiliation_string":"Neuroscience Biology, Pfizer Worldwide Research and Development, Eastern Point Road,Groton,USA","institution_ids":["https://openalex.org/I180857899"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5060972429","display_name":"Michelle A. Vanase-Frawley","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I180857899","display_name":"Pfizer (United States)","ror":"https://ror.org/01xdqrp08","country_code":"US","type":"company","lineage":["https://openalex.org/I180857899"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Michelle Vanase-Frawley","raw_affiliation_strings":["Neuroscience Biology, Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT, USA","Neuroscience Biology, Pfizer Worldwide Research and Development, Eastern Point Road,Groton,USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Neuroscience Biology, Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT, USA","institution_ids":["https://openalex.org/I180857899"]},{"raw_affiliation_string":"Neuroscience Biology, Pfizer Worldwide Research and Development, Eastern Point Road,Groton,USA","institution_ids":["https://openalex.org/I180857899"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5089103959","display_name":"Ernesto Callegari","orcid":"https://orcid.org/0000-0002-8429-0724","observed_orcids":["https://orcid.org/0000-0002-8429-0724"]},"institutions":[{"id":"https://openalex.org/I180857899","display_name":"Pfizer (United States)","ror":"https://ror.org/01xdqrp08","country_code":"US","type":"company","lineage":["https://openalex.org/I180857899"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Ernesto Callegari","raw_affiliation_strings":["Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT, USA","Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research and Development, Eastern Point Road,Groton,USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT, USA","institution_ids":["https://openalex.org/I180857899"]},{"raw_affiliation_string":"Pharmacokinetics, Dynamics and Metabolism, Pfizer Worldwide Research and Development, Eastern Point Road,Groton,USA","institution_ids":["https://openalex.org/I180857899"]}]},{"author_position":"last","author":{"id":"https://openalex.org/A5110618940","display_name":"Stafford McLean","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I180857899","display_name":"Pfizer (United States)","ror":"https://ror.org/01xdqrp08","country_code":"US","type":"company","lineage":["https://openalex.org/I180857899"]}],"countries":["US"],"is_corresponding":false,"raw_author_name":"Stafford McLean","raw_affiliation_strings":["Neuroscience Biology, Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT, USA","Neuroscience Biology, Pfizer Worldwide Research and Development, Eastern Point Road,Groton,USA"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Neuroscience Biology, Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT, USA","institution_ids":["https://openalex.org/I180857899"]},{"raw_affiliation_string":"Neuroscience Biology, Pfizer Worldwide Research and Development, Eastern Point Road,Groton,USA","institution_ids":["https://openalex.org/I180857899"]}]}],"institutions":[],"countries_distinct_count":1,"institutions_distinct_count":1,"corresponding_author_ids":["https://openalex.org/A5072802372"],"corresponding_institution_ids":["https://openalex.org/I180857899"],"apc_list":null,"apc_paid":null,"fwci":0.2642,"has_fulltext":false,"cited_by_count":3,"citation_normalized_percentile":{"value":0.51113461,"is_in_top_1_percent":false,"is_in_top_10_percent":false},"cited_by_percentile_year":{"min":89,"max":94},"biblio":{"volume":"2","issue":"5","first_page":"413","last_page":"413"},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T10814","display_name":"Neuropeptides and Animal Physiology","score":0.6074000000953674,"subfield":{"id":"https://openalex.org/subfields/2804","display_name":"Cellular and Molecular Neuroscience"},"field":{"id":"https://openalex.org/fields/28","display_name":"Neuroscience"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}},"topics":[{"id":"https://openalex.org/T10814","display_name":"Neuropeptides and Animal Physiology","score":0.6074000000953674,"subfield":{"id":"https://openalex.org/subfields/2804","display_name":"Cellular and Molecular Neuroscience"},"field":{"id":"https://openalex.org/fields/28","display_name":"Neuroscience"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}},{"id":"https://openalex.org/T11199","display_name":"Pain Management and Opioid Use","score":0.07909999787807465,"subfield":{"id":"https://openalex.org/subfields/2703","display_name":"Anesthesiology and Pain Medicine"},"field":{"id":"https://openalex.org/fields/27","display_name":"Medicine"},"domain":{"id":"https://openalex.org/domains/4","display_name":"Health Sciences"}},{"id":"https://openalex.org/T11178","display_name":"Receptor Mechanisms and Signaling","score":0.07460000365972519,"subfield":{"id":"https://openalex.org/subfields/1312","display_name":"Molecular Biology"},"field":{"id":"https://openalex.org/fields/13","display_name":"Biochemistry, Genetics and Molecular Biology"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}}],"keywords":[{"id":"https://openalex.org/keywords/delta-opioid-receptor-antagonists","display_name":"delta-opioid receptor antagonists","score":0.8339999914169312},{"id":"https://openalex.org/keywords/drug-synthesis","display_name":"drug synthesis","score":0.550000011920929},{"id":"https://openalex.org/keywords/pharmacokinetics","display_name":"pharmacokinetics","score":0.9800000190734863},{"id":"https://openalex.org/keywords/pharmacological-characterization","display_name":"pharmacological characterization","score":0.5329999923706055},{"id":"https://openalex.org/keywords/human-liver-microsomes","display_name":"human liver microsomes","score":0.7200000286102295},{"id":"https://openalex.org/keywords/drug-clearance","display_name":"drug clearance","score":0.6990000009536743},{"id":"https://openalex.org/keywords/p-glycoprotein-efflux","display_name":"P-glycoprotein efflux","score":0.9240000247955322}],"concepts":[{"id":"https://openalex.org/C2776885963","wikidata":"https://www.wikidata.org/wiki/Q245204","display_name":"Antagonist","level":3,"score":0.7138262987136841},{"id":"https://openalex.org/C98274493","wikidata":"https://www.wikidata.org/wiki/Q128406","display_name":"Pharmacology","level":1,"score":0.6932616829872131},{"id":"https://openalex.org/C38022665","wikidata":"https://www.wikidata.org/wiki/Q1149305","display_name":"Disposition","level":2,"score":0.6565731167793274},{"id":"https://openalex.org/C2778140631","wikidata":"https://www.wikidata.org/wiki/Q2026938","display_name":"Opiate","level":3,"score":0.5190954208374023},{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.49727633595466614},{"id":"https://openalex.org/C200082930","wikidata":"https://www.wikidata.org/wiki/Q22327148","display_name":"Efflux","level":2,"score":0.4903535842895508},{"id":"https://openalex.org/C2778122271","wikidata":"https://www.wikidata.org/wiki/Q410943","display_name":"Receptor antagonist","level":4,"score":0.4612514078617096},{"id":"https://openalex.org/C112705442","wikidata":"https://www.wikidata.org/wiki/Q323936","display_name":"Pharmacokinetics","level":2,"score":0.4194461405277252},{"id":"https://openalex.org/C2781063702","wikidata":"https://www.wikidata.org/wiki/Q427523","display_name":"Opioid","level":3,"score":0.4162524342536926},{"id":"https://openalex.org/C170493617","wikidata":"https://www.wikidata.org/wiki/Q208467","display_name":"Receptor","level":2,"score":0.39641496539115906},{"id":"https://openalex.org/C71924100","wikidata":"https://www.wikidata.org/wiki/Q11190","display_name":"Medicine","level":0,"score":0.30285802483558655},{"id":"https://openalex.org/C55493867","wikidata":"https://www.wikidata.org/wiki/Q7094","display_name":"Biochemistry","level":1,"score":0.14131808280944824},{"id":"https://openalex.org/C15744967","wikidata":"https://www.wikidata.org/wiki/Q9418","display_name":"Psychology","level":0,"score":0.09194600582122803},{"id":"https://openalex.org/C77805123","wikidata":"https://www.wikidata.org/wiki/Q161272","display_name":"Social psychology","level":1,"score":0.0}],"mesh":[],"locations_count":1,"locations":[{"id":"doi:10.1039/c0md00249f","doi":"https://doi.org/10.1039/c0md00249f","is_oa":false,"landing_page_url":"https://doi.org/10.1039/c0md00249f","pdf_url":null,"source":{"id":"https://openalex.org/S191926780","display_name":"MedChemComm","issn_l":"2040-2503","issn":["2040-2503","2040-2511"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["cwts-core","ki-jl-1","norway-1","poland-70"],"host_organization":"https://openalex.org/P4310320556","host_organization_name":"Royal Society of Chemistry","host_organization_lineage":["https://openalex.org/P4310320556"],"host_organization_lineage_names":["Royal Society of Chemistry"],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"MedChemComm","raw_type":"journal-article"}],"best_oa_location":null,"sustainable_development_goals":[{"score":0.9537000060081482,"id":"https://metadata.un.org/sdg/3","display_name":"Good health and well-being"}],"study_designs":[],"awards":[],"funders":[],"has_content":{"pdf":false,"grobid_xml":false},"content_urls":null,"referenced_works_count":22,"referenced_works":["https://openalex.org/W1966834285","https://openalex.org/W1972617674","https://openalex.org/W1979532264","https://openalex.org/W1985341525","https://openalex.org/W1995735458","https://openalex.org/W2000074306","https://openalex.org/W2009005630","https://openalex.org/W2013785959","https://openalex.org/W2016081029","https://openalex.org/W2042013533","https://openalex.org/W2065716899","https://openalex.org/W2068904721","https://openalex.org/W2074115024","https://openalex.org/W2079197876","https://openalex.org/W2081965953","https://openalex.org/W2108982217","https://openalex.org/W2124622759","https://openalex.org/W2148366489","https://openalex.org/W2162194843","https://openalex.org/W2166631226","https://openalex.org/W2206881671","https://openalex.org/W2949529216"],"related_works":["https://openalex.org/W1967198484","https://openalex.org/W2012192563","https://openalex.org/W2006916500","https://openalex.org/W4396744886","https://openalex.org/W1562990382","https://openalex.org/W2115743942","https://openalex.org/W1994264183","https://openalex.org/W2162637520","https://openalex.org/W2056132478","https://openalex.org/W2885136394"],"abstract_inverted_index":{"CP-646,777":[0,56],"(compound":[1],"2a)":[2],"is":[3,40,57],"identified":[4],"as":[5,34],"a":[6],"potent":[7],"and":[8,20,50],"selective":[9],"delta":[10],"opioid":[11],"receptor":[12],"antagonist.":[13],"The":[14,42],"synthesis,":[15],"pharmacological":[16,53],"evaluation,":[17],"disposition":[18,49],"characteristics":[19],"pharmacokinetic":[21],"properties":[22],"of":[23,44,55],"this":[24],"compound":[25],"are":[26],"reported":[27],"herein.":[28],"An":[29],"approach":[30],"for":[31],"reducing":[32],"clearance":[33],"measured":[35],"by":[36],"human":[37],"liver":[38],"microsomes":[39],"demonstrated.":[41],"significance":[43],"p-glycoprotein":[45],"efflux":[46],"on":[47,51],"CNS":[48],"the":[52],"action":[54],"also":[58],"discussed.":[59]},"counts_by_year":[{"year":2019,"cited_by_count":1},{"year":2013,"cited_by_count":1}],"updated_date":"2026-10-14T16:39:01.820549","created_date":"2016-06-24T00:00:00"}
