{"id":"https://openalex.org/W2013299143","doi":"https://doi.org/10.1021/jm000371q","title":"A Novel Class of Potent 3-Isoxazolol GABAAAntagonists: Design, Synthesis, and Pharmacology","display_name":"A Novel Class of Potent 3-Isoxazolol GABAAAntagonists: Design, Synthesis, and Pharmacology","publication_year":2000,"publication_date":"2000-11-23","ids":{"openalex":"https://openalex.org/W2013299143","doi":"https://doi.org/10.1021/jm000371q","mag":"2013299143","pmid":"https://pubmed.ncbi.nlm.nih.gov/11150163"},"language":"en","primary_location":{"id":"doi:10.1021/jm000371q","doi":"https://doi.org/10.1021/jm000371q","is_oa":false,"landing_page_url":"https://doi.org/10.1021/jm000371q","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"},"parent_works":[],"lineage":["https://openalex.org/W2013299143"],"child_works_count":0,"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/A5001593002","display_name":"Bente Fr\u00f8lund","orcid":"https://orcid.org/0000-0001-5476-6288","observed_orcids":["https://orcid.org/0000-0001-5476-6288"]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Bente Fr\u00f8lund","raw_affiliation_strings":["Departments of Medicinal Chemistry and Pharmacology, Centre for Drug Design and Transport, The Royal Danish School of Pharmacy, 2 Universitetsparken, DK 2100 Copenhagen, Denmark"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Departments of Medicinal Chemistry and Pharmacology, Centre for Drug Design and Transport, The Royal Danish School of Pharmacy, 2 Universitetsparken, DK 2100 Copenhagen, Denmark","institution_ids":[]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5058687195","display_name":"Lena Tagmose","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Lena Tagmose","raw_affiliation_strings":["Departments of Medicinal Chemistry and Pharmacology, Centre for Drug Design and Transport, The Royal Danish School of Pharmacy, 2 Universitetsparken, DK 2100 Copenhagen, Denmark"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Departments of Medicinal Chemistry and Pharmacology, Centre for Drug Design and Transport, The Royal Danish School of Pharmacy, 2 Universitetsparken, DK 2100 Copenhagen, Denmark","institution_ids":[]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5071791987","display_name":"Tommy Liljefors","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Tommy Liljefors","raw_affiliation_strings":["Departments of Medicinal Chemistry and Pharmacology, Centre for Drug Design and Transport, The Royal Danish School of Pharmacy, 2 Universitetsparken, DK 2100 Copenhagen, Denmark"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Departments of Medicinal Chemistry and Pharmacology, Centre for Drug Design and Transport, The Royal Danish School of Pharmacy, 2 Universitetsparken, DK 2100 Copenhagen, Denmark","institution_ids":[]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5110191635","display_name":"Tine B. Stensb\u00f8l","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Tine Bryan Stensb\u00f8l","raw_affiliation_strings":["Departments of Medicinal Chemistry and Pharmacology, Centre for Drug Design and Transport, The Royal Danish School of Pharmacy, 2 Universitetsparken, DK 2100 Copenhagen, Denmark"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Departments of Medicinal Chemistry and Pharmacology, Centre for Drug Design and Transport, The Royal Danish School of Pharmacy, 2 Universitetsparken, DK 2100 Copenhagen, Denmark","institution_ids":[]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5084256115","display_name":"Christine Engblom","orcid":"https://orcid.org/0000-0001-7545-2026","observed_orcids":["https://orcid.org/0000-0001-7545-2026"]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Christine Engblom","raw_affiliation_strings":["Departments of Medicinal Chemistry and Pharmacology, Centre for Drug Design and Transport, The Royal Danish School of Pharmacy, 2 Universitetsparken, DK 2100 Copenhagen, Denmark"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Departments of Medicinal Chemistry and Pharmacology, Centre for Drug Design and Transport, The Royal Danish School of Pharmacy, 2 Universitetsparken, DK 2100 Copenhagen, Denmark","institution_ids":[]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5043236966","display_name":"Uffe Kristiansen","orcid":"https://orcid.org/0000-0001-9050-7806","observed_orcids":["https://orcid.org/0000-0001-9050-7806"]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Uffe Kristiansen","raw_affiliation_strings":["Departments of Medicinal Chemistry and Pharmacology, Centre for Drug Design and Transport, The Royal Danish School of Pharmacy, 2 Universitetsparken, DK 2100 Copenhagen, Denmark"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Departments of Medicinal Chemistry and Pharmacology, Centre for Drug Design and Transport, The Royal Danish School of Pharmacy, 2 Universitetsparken, DK 2100 Copenhagen, Denmark","institution_ids":[]}]},{"author_position":"last","author":{"id":"https://openalex.org/A5110162997","display_name":"Povl Krogsgaard\u2010Larsen","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"Povl Krogsgaard-Larsen","raw_affiliation_strings":["Departments of Medicinal Chemistry and Pharmacology, Centre for Drug Design and Transport, The Royal Danish School of Pharmacy, 2 Universitetsparken, DK 2100 Copenhagen, Denmark"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Departments of Medicinal Chemistry and Pharmacology, Centre for Drug Design and Transport, The Royal Danish School of Pharmacy, 2 Universitetsparken, DK 2100 Copenhagen, Denmark","institution_ids":[]}]}],"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":0.6986,"has_fulltext":false,"cited_by_count":37,"citation_normalized_percentile":{"value":0.61623816,"is_in_top_1_percent":false,"is_in_top_10_percent":false},"cited_by_percentile_year":{"min":88,"max":97},"biblio":{"volume":"43","issue":"26","first_page":"4930","last_page":"4933"},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T10077","display_name":"Neuroscience and Neuropharmacology Research","score":0.9911999702453613,"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":0.9911999702453613,"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/T10274","display_name":"Heterocyclic Compound Synthesis and Bioactivity","score":0.002099999925121665,"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"}},{"id":"https://openalex.org/T11178","display_name":"Receptor Mechanisms and Signaling","score":0.0017999999690800905,"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/gaba-a-receptor-antagonists","display_name":"GABA-A receptor antagonists","score":0.8849999904632568},{"id":"https://openalex.org/keywords/benzodiazepine-receptor","display_name":"benzodiazepine receptor","score":0.7049999833106995},{"id":"https://openalex.org/keywords/ligand-design","display_name":"ligand design","score":0.5090000033378601},{"id":"https://openalex.org/keywords/heterocycle-synthesis","display_name":"heterocyclic synthesis","score":0.6510000228881836},{"id":"https://openalex.org/keywords/receptor-binding-affinity","display_name":"receptor binding affinity","score":0.47999998927116394},{"id":"https://openalex.org/keywords/conformational-analysis","display_name":"conformational analysis","score":0.4580000042915344},{"id":"https://openalex.org/keywords/antiepileptic-drugs","display_name":"antiepileptic drugs","score":0.5860000252723694},{"id":"https://openalex.org/keywords/anxiolytics","display_name":"anxiolytics","score":0.824999988079071},{"id":"https://openalex.org/keywords/sedatives","display_name":"sedatives","score":0.47999998927116394},{"id":"https://openalex.org/keywords/muscle-relaxants","display_name":"muscle relaxants","score":0.8119999766349792},{"id":"https://openalex.org/keywords/antispasmodic-agents","display_name":"antispasmodic agents","score":0.4339999854564667}],"concepts":[{"id":"https://openalex.org/C2778805511","wikidata":"https://www.wikidata.org/wiki/Q1713","display_name":"Citation","level":2,"score":0.568343997001648},{"id":"https://openalex.org/C161191863","wikidata":"https://www.wikidata.org/wiki/Q199655","display_name":"Library science","level":1,"score":0.48965054750442505},{"id":"https://openalex.org/C2777212361","wikidata":"https://www.wikidata.org/wiki/Q5127848","display_name":"Class (philosophy)","level":2,"score":0.4523027539253235},{"id":"https://openalex.org/C104863432","wikidata":"https://www.wikidata.org/wiki/Q614304","display_name":"Pharmacy","level":2,"score":0.4441143274307251},{"id":"https://openalex.org/C41008148","wikidata":"https://www.wikidata.org/wiki/Q21198","display_name":"Computer science","level":0,"score":0.42672330141067505},{"id":"https://openalex.org/C136764020","wikidata":"https://www.wikidata.org/wiki/Q466","display_name":"World Wide Web","level":1,"score":0.349337637424469},{"id":"https://openalex.org/C71924100","wikidata":"https://www.wikidata.org/wiki/Q11190","display_name":"Medicine","level":0,"score":0.3352847695350647},{"id":"https://openalex.org/C154945302","wikidata":"https://www.wikidata.org/wiki/Q11660","display_name":"Artificial intelligence","level":1,"score":0.1730918288230896},{"id":"https://openalex.org/C512399662","wikidata":"https://www.wikidata.org/wiki/Q3505712","display_name":"Family medicine","level":1,"score":0.13594689965248108}],"mesh":[{"descriptor_ui":"D000818","descriptor_name":"Animals","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D001921","descriptor_name":"Brain","qualifier_ui":"Q000166","qualifier_name":"cytology","is_major_topic":false},{"descriptor_ui":"D001921","descriptor_name":"Brain","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false},{"descriptor_ui":"D001921","descriptor_name":"Brain","qualifier_ui":"Q000648","qualifier_name":"ultrastructure","is_major_topic":false},{"descriptor_ui":"D002478","descriptor_name":"Cells, Cultured","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D007555","descriptor_name":"Isoxazoles","qualifier_ui":"Q000138","qualifier_name":"chemical synthesis","is_major_topic":true},{"descriptor_ui":"D007555","descriptor_name":"Isoxazoles","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false},{"descriptor_ui":"D007555","descriptor_name":"Isoxazoles","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":false},{"descriptor_ui":"D007555","descriptor_name":"Isoxazoles","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":false},{"descriptor_ui":"D008958","descriptor_name":"Models, Molecular","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D009118","descriptor_name":"Muscimol","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false},{"descriptor_ui":"D009474","descriptor_name":"Neurons","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false},{"descriptor_ui":"D009474","descriptor_name":"Neurons","qualifier_ui":"Q000502","qualifier_name":"physiology","is_major_topic":false},{"descriptor_ui":"D010880","descriptor_name":"Piperidines","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false},{"descriptor_ui":"D010880","descriptor_name":"Piperidines","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":false},{"descriptor_ui":"D011869","descriptor_name":"Radioligand Assay","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D011963","descriptor_name":"Receptors, GABA-A","qualifier_ui":"Q000187","qualifier_name":"drug effects","is_major_topic":true},{"descriptor_ui":"D011963","descriptor_name":"Receptors, GABA-A","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false},{"descriptor_ui":"D013329","descriptor_name":"Structure-Activity Relationship","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D013570","descriptor_name":"Synaptic Membranes","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false},{"descriptor_ui":"D018408","descriptor_name":"Patch-Clamp Techniques","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D018756","descriptor_name":"GABA Antagonists","qualifier_ui":"Q000138","qualifier_name":"chemical synthesis","is_major_topic":true},{"descriptor_ui":"D018756","descriptor_name":"GABA Antagonists","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":false},{"descriptor_ui":"D018756","descriptor_name":"GABA Antagonists","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":false},{"descriptor_ui":"D018756","descriptor_name":"GABA Antagonists","qualifier_ui":"Q000737","qualifier_name":"chemistry","is_major_topic":false},{"descriptor_ui":"D051381","descriptor_name":"Rats","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false}],"locations_count":4,"locations":[{"id":"doi:10.1021/jm000371q","doi":"https://doi.org/10.1021/jm000371q","is_oa":false,"landing_page_url":"https://doi.org/10.1021/jm000371q","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:11150163","doi":null,"is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/11150163","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":"Journal Article"},{"id":"pmh:oai:pure.atira.dk:openaire_cris_publications/91ce2d93-fd16-4ef6-8b00-cdbc453d4f31","doi":null,"is_oa":false,"landing_page_url":"https://researchprofiles.ku.dk/da/publications/91ce2d93-fd16-4ef6-8b00-cdbc453d4f31","pdf_url":null,"source":{"id":"https://openalex.org/S4306401983","display_name":"Research at the University of Copenhagen (University of Copenhagen)","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I124055696","host_organization_name":"University of Copenhagen","host_organization_lineage":["https://openalex.org/I124055696"],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":"submittedVersion","is_accepted":false,"is_published":false,"raw_source_name":"Fr\u00f8lund , B , Tagmose , L , Liljefors , T , Stensb\u00f8l , T B , Engblom , C , Kristiansen , U & Krogsgaard-Larsen , P 2000 , ' A Novel Class of Potent 3-Isoxazolol GABA A Antagonists: Design, Synthesis, and Pharmacology ' , Journal of Medicinal Chemistry , vol. 43 , pp. 4930\u20134933 .","raw_type":"article"},{"id":"pmh:oai:pure.atira.dk:openaire_cris_publications/eddea572-e8c8-4305-b9df-1db7963d6e9e","doi":null,"is_oa":false,"landing_page_url":"https://researchprofiles.ku.dk/da/publications/eddea572-e8c8-4305-b9df-1db7963d6e9e","pdf_url":null,"source":{"id":"https://openalex.org/S4306401983","display_name":"Research at the University of Copenhagen (University of Copenhagen)","issn_l":null,"issn":null,"is_oa":false,"is_in_doaj":false,"is_core":false,"listed_in":[],"host_organization":"https://openalex.org/I124055696","host_organization_name":"University of Copenhagen","host_organization_lineage":["https://openalex.org/I124055696"],"host_organization_lineage_names":[],"type":"repository"},"license":null,"license_id":null,"version":"submittedVersion","is_accepted":false,"is_published":false,"raw_source_name":"Fr\u00f8lund, B, Tagmose, L, Liljefors, T, Stensb\u00f8l, T B, Engblom, C, Kristiansen, U & Krogsgaard-Larsen, P 2000, 'A novel class of potent 3-isoxazolol GABA A antagonists : Design, systhesis, and pharmacology [3]', Journal of Medicinal Chemistry, vol. 43, no. 26, pp. 4930-4933. https://doi.org/10.1021/jm000371q","raw_type":"info:eu-repo/semantics/publishedVersion"}],"best_oa_location":null,"sustainable_development_goals":[],"study_designs":[],"awards":[],"funders":[],"has_content":{"pdf":false,"grobid_xml":false},"content_urls":null,"referenced_works_count":25,"referenced_works":["https://openalex.org/W1514573559","https://openalex.org/W1518033152","https://openalex.org/W1965019394","https://openalex.org/W1966837740","https://openalex.org/W1971643138","https://openalex.org/W1983621709","https://openalex.org/W2008935536","https://openalex.org/W2014635182","https://openalex.org/W2021139758","https://openalex.org/W2027646804","https://openalex.org/W2033281125","https://openalex.org/W2035983200","https://openalex.org/W2039789476","https://openalex.org/W2040674328","https://openalex.org/W2042485333","https://openalex.org/W2043763965","https://openalex.org/W2072792060","https://openalex.org/W2074216375","https://openalex.org/W2076436731","https://openalex.org/W2078051297","https://openalex.org/W2078698570","https://openalex.org/W2078902355","https://openalex.org/W2131124255","https://openalex.org/W2949401139","https://openalex.org/W4251224408"],"related_works":["https://openalex.org/W2951173731","https://openalex.org/W7071748795","https://openalex.org/W2468740529","https://openalex.org/W1977741529","https://openalex.org/W2006225190","https://openalex.org/W1988932718","https://openalex.org/W2016099601","https://openalex.org/W2012480383","https://openalex.org/W2002305402","https://openalex.org/W2006052244"],"abstract_inverted_index":null,"counts_by_year":[{"year":2026,"cited_by_count":1},{"year":2024,"cited_by_count":1},{"year":2023,"cited_by_count":1},{"year":2021,"cited_by_count":3},{"year":2018,"cited_by_count":1},{"year":2016,"cited_by_count":1},{"year":2014,"cited_by_count":3},{"year":2013,"cited_by_count":4}],"updated_date":"2026-11-13T13:42:25.865203","created_date":"2016-06-24T00:00:00"}
