{"id":"https://openalex.org/W1998097979","doi":"https://doi.org/10.1021/jm00112a033","title":"3-Thienyl- and 3-furylaminobutyric acids. Synthesis and binding GABAB receptor studies","display_name":"3-Thienyl- and 3-furylaminobutyric acids. Synthesis and binding GABAB receptor studies","publication_year":1991,"publication_date":"1991-08-01","ids":{"openalex":"https://openalex.org/W1998097979","doi":"https://doi.org/10.1021/jm00112a033","mag":"1998097979","pmid":"https://pubmed.ncbi.nlm.nih.gov/1652022"},"language":"en","primary_location":{"id":"doi:10.1021/jm00112a033","doi":"https://doi.org/10.1021/jm00112a033","is_oa":false,"landing_page_url":"https://doi.org/10.1021/jm00112a033","pdf_url":null,"source":{"id":"https://openalex.org/S162030435","display_name":"Journal of Medicinal Chemistry","issn_l":"0022-2623","issn":["0022-2623","1520-4804"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["anvur-scientific","cwts-core","dongbi-a","jufo-3","ki-jl-2","medline","norway-2","poland-200","russia-white-list-1","vabb-shw"],"host_organization":"https://openalex.org/P4310320006","host_organization_name":"American Chemical Society","host_organization_lineage":["https://openalex.org/P4310320006"],"host_organization_lineage_names":["American Chemical Society"],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Journal of Medicinal Chemistry","raw_type":"journal-article"},"volume":null,"type":"article","is_traditional":true,"indexed_in":["crossref","pubmed"],"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/A5109956088","display_name":"Pascal Berthelot","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Pascal Berthelot","raw_affiliation_strings":["Laboratoire de Pharmacie Chimique, Facult\u00e9 de Pharmacie, Lille, France"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Laboratoire de Pharmacie Chimique, Facult\u00e9 de Pharmacie, Lille, France","institution_ids":[]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5105987040","display_name":"Claude Vaccher","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Claude Vaccher","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5062800640","display_name":"Nathalie Flouquet","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Nathalie Flouquet","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5079558090","display_name":"Michel Debaert","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Michel Debaert","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5109991141","display_name":"M. Luyckx","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Michel Luyckx","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"last","author":{"id":"https://openalex.org/A5109227140","display_name":"C. Brunet","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Claude Brunet","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]}],"institutions":[],"countries_distinct_count":0,"institutions_distinct_count":0,"corresponding_author_ids":[],"corresponding_institution_ids":[],"apc_list":{"value":4500,"currency":"USD","value_usd":4500},"apc_paid":null,"fwci":1.4207,"has_fulltext":false,"cited_by_count":72,"citation_normalized_percentile":{"value":0.8117769,"is_in_top_1_percent":false,"is_in_top_10_percent":false},"cited_by_percentile_year":{"min":88,"max":95},"biblio":{"volume":"34","issue":"8","first_page":"2557","last_page":"2560"},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T10077","display_name":"Neuroscience and Neuropharmacology Research","score":0.9667999744415283,"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/T10077","display_name":"Neuroscience and Neuropharmacology Research","score":0.9667999744415283,"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/T11178","display_name":"Receptor Mechanisms and Signaling","score":0.01600000075995922,"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"}},{"id":"https://openalex.org/T10274","display_name":"Heterocyclic Compound Synthesis and Bioactivity","score":0.00559999980032444,"subfield":{"id":"https://openalex.org/subfields/1605","display_name":"Organic Chemistry"},"field":{"id":"https://openalex.org/fields/16","display_name":"Chemistry"},"domain":{"id":"https://openalex.org/domains/3","display_name":"Physical Sciences"}}],"keywords":[{"id":"https://openalex.org/keywords/gabab-receptors","display_name":"GABAB receptors","score":0.9459999799728394},{"id":"https://openalex.org/keywords/baclofen","display_name":"baclofen","score":0.8460000157356262},{"id":"https://openalex.org/keywords/gaba-receptor-agonists","display_name":"GABA agonists","score":0.6159999966621399},{"id":"https://openalex.org/keywords/receptor-ligands","display_name":"receptor ligands","score":0.7039999961853027},{"id":"https://openalex.org/keywords/thienyl-derivatives","display_name":"thienyl compounds","score":0.5640000104904175},{"id":"https://openalex.org/keywords/receptor-binding-affinity","display_name":"receptor binding affinity","score":0.44999998807907104},{"id":"https://openalex.org/keywords/structure-activity-relationship","display_name":"structure-activity relationship","score":0.5580000281333923}],"concepts":[{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.9279272556304932},{"id":"https://openalex.org/C101027131","wikidata":"https://www.wikidata.org/wiki/Q305671","display_name":"GABAB receptor","level":4,"score":0.6769682765007019},{"id":"https://openalex.org/C71240020","wikidata":"https://www.wikidata.org/wiki/Q186011","display_name":"Stereochemistry","level":1,"score":0.38008326292037964},{"id":"https://openalex.org/C21951064","wikidata":"https://www.wikidata.org/wiki/Q899212","display_name":"Combinatorial chemistry","level":1,"score":0.3667558431625366},{"id":"https://openalex.org/C170493617","wikidata":"https://www.wikidata.org/wiki/Q208467","display_name":"Receptor","level":2,"score":0.3586235046386719},{"id":"https://openalex.org/C98274493","wikidata":"https://www.wikidata.org/wiki/Q128406","display_name":"Pharmacology","level":1,"score":0.32384541630744934},{"id":"https://openalex.org/C55493867","wikidata":"https://www.wikidata.org/wiki/Q7094","display_name":"Biochemistry","level":1,"score":0.31290262937545776},{"id":"https://openalex.org/C2778938600","wikidata":"https://www.wikidata.org/wiki/Q389934","display_name":"Agonist","level":3,"score":0.1834094524383545},{"id":"https://openalex.org/C71924100","wikidata":"https://www.wikidata.org/wiki/Q11190","display_name":"Medicine","level":0,"score":0.0}],"mesh":[{"descriptor_ui":"D000818","descriptor_name":"Animals","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D001418","descriptor_name":"Baclofen","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false},{"descriptor_ui":"D001667","descriptor_name":"Binding, Competitive","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D001921","descriptor_name":"Brain","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false},{"descriptor_ui":"D002621","descriptor_name":"Chemistry","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D005663","descriptor_name":"Furans","qualifier_ui":"Q000138","qualifier_name":"chemical synthesis","is_major_topic":true},{"descriptor_ui":"D005663","descriptor_name":"Furans","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false},{"descriptor_ui":"D005680","descriptor_name":"gamma-Aminobutyric Acid","qualifier_ui":"Q000031","qualifier_name":"analogs & derivatives","is_major_topic":true},{"descriptor_ui":"D005680","descriptor_name":"gamma-Aminobutyric Acid","qualifier_ui":"Q000138","qualifier_name":"chemical synthesis","is_major_topic":false},{"descriptor_ui":"D005680","descriptor_name":"gamma-Aminobutyric Acid","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false},{"descriptor_ui":"D009118","descriptor_name":"Muscimol","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false},{"descriptor_ui":"D011963","descriptor_name":"Receptors, GABA-A","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":true},{"descriptor_ui":"D013570","descriptor_name":"Synaptic Membranes","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false},{"descriptor_ui":"D013876","descriptor_name":"Thiophenes","qualifier_ui":"Q000138","qualifier_name":"chemical synthesis","is_major_topic":true},{"descriptor_ui":"D013876","descriptor_name":"Thiophenes","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false},{"descriptor_ui":"D015394","descriptor_name":"Molecular Structure","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D051381","descriptor_name":"Rats","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D055598","descriptor_name":"Chemical Phenomena","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false}],"locations_count":2,"locations":[{"id":"doi:10.1021/jm00112a033","doi":"https://doi.org/10.1021/jm00112a033","is_oa":false,"landing_page_url":"https://doi.org/10.1021/jm00112a033","pdf_url":null,"source":{"id":"https://openalex.org/S162030435","display_name":"Journal of Medicinal Chemistry","issn_l":"0022-2623","issn":["0022-2623","1520-4804"],"is_oa":false,"is_in_doaj":false,"is_core":true,"listed_in":["anvur-scientific","cwts-core","dongbi-a","jufo-3","ki-jl-2","medline","norway-2","poland-200","russia-white-list-1","vabb-shw"],"host_organization":"https://openalex.org/P4310320006","host_organization_name":"American Chemical Society","host_organization_lineage":["https://openalex.org/P4310320006"],"host_organization_lineage_names":["American Chemical Society"],"type":"journal"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Journal of Medicinal Chemistry","raw_type":"journal-article"},{"id":"pmid:1652022","doi":null,"is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/1652022","pdf_url":null,"source":{"id":"https://openalex.org/S4306525036","display_name":"PubMed","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I1299303238","host_organization_name":"National Institutes of Health","host_organization_lineage":["https://openalex.org/I1299303238"],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":"publishedVersion","is_accepted":true,"is_published":true,"raw_source_name":"Journal of medicinal chemistry","raw_type":"Comparative Study"}],"best_oa_location":null,"sustainable_development_goals":[{"id":"https://metadata.un.org/sdg/3","score":0.504800021648407,"display_name":"Good health and well-being"}],"study_designs":[],"awards":[],"funders":[],"has_content":{"pdf":false,"grobid_xml":false},"content_urls":null,"referenced_works_count":0,"referenced_works":[],"related_works":["https://openalex.org/W1974927854","https://openalex.org/W2005135546","https://openalex.org/W2415181284","https://openalex.org/W2950945213","https://openalex.org/W1986033342","https://openalex.org/W2951908880","https://openalex.org/W2007312469","https://openalex.org/W4412252583","https://openalex.org/W2017774566","https://openalex.org/W2951010610"],"abstract_inverted_index":{"Baclofen":[0],"(beta-(p-chlorophenyl)-GABA)":[1],"is":[2,22],"a":[3],"selective":[4],"agonist":[5],"for":[6,13,57,63,73,83],"the":[7,19,32,35,64],"bicuculline-insensitive":[8],"GABAB":[9,20,58],"receptor.":[10,59],"The":[11,60],"search":[12],"new":[14],"compounds":[15],"that":[16],"bind":[17],"to":[18,25,80],"receptor":[21],"very":[23],"important":[24],"clarify":[26],"structural":[27],"requirements.":[28],"We":[29],"report":[30],"herein":[31],"synthesis":[33],"and":[34,42,48,54,70,75],"binding":[36],"studies":[37],"of":[38,66],"variously":[39],"substituted":[40],"3-thienyl-":[41],"3-furylaminobutyric":[43],"acids.":[44],"4-Amino-3-(5-methyl-2-thienyl)butyric":[45],"acid":[46,50],"(5d)":[47],"4-amino-3-(5-chloro-2-thienyl)butyric":[49],"(5h)":[51],"are":[52,68],"potent":[53],"specific":[55],"ligands":[56],"IC50":[61],"values":[62],"displacement":[65],"(R)-(-)-[3H]baclofen":[67],"1.34":[69],"0.61":[71],"microM":[72,82],"5d":[74],"5h,":[76],"respectively,":[77],"as":[78],"compared":[79],"0.33":[81],"baclofen.":[84]},"counts_by_year":[{"year":2026,"cited_by_count":1},{"year":2025,"cited_by_count":1},{"year":2024,"cited_by_count":2},{"year":2020,"cited_by_count":1},{"year":2019,"cited_by_count":1},{"year":2018,"cited_by_count":1},{"year":2016,"cited_by_count":1},{"year":2015,"cited_by_count":2},{"year":2014,"cited_by_count":2},{"year":2013,"cited_by_count":1}],"updated_date":"2026-11-04T10:54:05.112534","created_date":"2016-06-24T00:00:00"}
