{"id":"https://openalex.org/W2043780424","doi":"https://doi.org/10.1021/jm970417o","title":"Effect of Plasma Protein Binding on in Vivo Activity and Brain Penetration of Glycine/NMDA Receptor Antagonists","display_name":"Effect of Plasma Protein Binding on in Vivo Activity and Brain Penetration of Glycine/NMDA Receptor Antagonists","publication_year":1997,"publication_date":"1997-12-01","ids":{"openalex":"https://openalex.org/W2043780424","doi":"https://doi.org/10.1021/jm970417o","mag":"2043780424","pmid":"https://pubmed.ncbi.nlm.nih.gov/9406596"},"language":"en","primary_location":{"id":"doi:10.1021/jm970417o","doi":"https://doi.org/10.1021/jm970417o","is_oa":false,"landing_page_url":"https://doi.org/10.1021/jm970417o","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/A5060422552","display_name":"Michael Rowley","orcid":"https://orcid.org/0000-0003-2672-1255","observed_orcids":["https://orcid.org/0000-0003-2672-1255"]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":true,"raw_author_name":"Michael Rowley","raw_affiliation_strings":["Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5071924682","display_name":"Janusz J. Kulagowski","orcid":"https://orcid.org/0000-0002-8155-9919","observed_orcids":["https://orcid.org/0000-0002-8155-9919"]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Janusz J. Kulagowski","raw_affiliation_strings":["Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5111714417","display_name":"Alan P. Watt","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Alan P. Watt","raw_affiliation_strings":["Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5081102454","display_name":"Denise Rathbone","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Denise Rathbone","raw_affiliation_strings":["Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5009342141","display_name":"Graeme I. Stevenson","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Graeme I. Stevenson","raw_affiliation_strings":["Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5080950417","display_name":"Robert W. Carling","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Robert W. Carling","raw_affiliation_strings":["Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5103551292","display_name":"Raymond Baker","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Raymond Baker","raw_affiliation_strings":["Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5104305302","display_name":"George R. Marshall","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"George R. Marshall","raw_affiliation_strings":["Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5111559911","display_name":"John A. Kemp","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"John A. Kemp","raw_affiliation_strings":["Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5056598194","display_name":"Alan C. Foster","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Alan C. Foster","raw_affiliation_strings":["Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5108377409","display_name":"Sarah Grimwood","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Sarah Grimwood","raw_affiliation_strings":["Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5110221578","display_name":"Richard J Hargreaves","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Richard Hargreaves","raw_affiliation_strings":["Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":null,"display_name":"Catherine Hurley","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Catherine Hurley","raw_affiliation_strings":["Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5054684782","display_name":"Kay L. Saywell","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Kay L. Saywell","raw_affiliation_strings":["Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5067902930","display_name":"Mark David Tricklebank","orcid":"https://orcid.org/0000-0002-9949-6290","observed_orcids":["https://orcid.org/0000-0002-9949-6290"]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Mark D. Tricklebank","raw_affiliation_strings":["Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom","institution_ids":["https://openalex.org/I4210087189"]}]},{"author_position":"last","author":{"id":"https://openalex.org/A5037689001","display_name":"Paul D. Leeson","orcid":"https://orcid.org/0000-0003-0212-3437","observed_orcids":["https://orcid.org/0000-0003-0212-3437"]},"institutions":[{"id":"https://openalex.org/I4210087189","display_name":"MSD (UK) Limited (United Kingdom)","ror":"https://ror.org/004nn4n27","country_code":"GB","type":"company","lineage":["https://openalex.org/I1285764155","https://openalex.org/I4210087189"]}],"countries":["GB"],"is_corresponding":false,"raw_author_name":"Paul D. Leeson","raw_affiliation_strings":["Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, United Kingdom","institution_ids":["https://openalex.org/I4210087189"]}]}],"institutions":[],"countries_distinct_count":1,"institutions_distinct_count":1,"corresponding_author_ids":["https://openalex.org/A5060422552"],"corresponding_institution_ids":["https://openalex.org/I4210087189"],"apc_list":{"value":4500,"currency":"USD","value_usd":4500},"apc_paid":null,"fwci":1.4884,"has_fulltext":false,"cited_by_count":130,"citation_normalized_percentile":{"value":0.81816304,"is_in_top_1_percent":false,"is_in_top_10_percent":false},"cited_by_percentile_year":{"min":87,"max":99},"biblio":{"volume":"40","issue":"25","first_page":"4053","last_page":"4068"},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T11908","display_name":"Protein Interaction Studies and Fluorescence Analysis","score":0.4779999852180481,"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"}},"topics":[{"id":"https://openalex.org/T11908","display_name":"Protein Interaction Studies and Fluorescence Analysis","score":0.4779999852180481,"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/T10077","display_name":"Neuroscience and Neuropharmacology Research","score":0.2572999894618988,"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/T11872","display_name":"Barrier Structure and Function Studies","score":0.06520000100135803,"subfield":{"id":"https://openalex.org/subfields/2808","display_name":"Neurology"},"field":{"id":"https://openalex.org/fields/28","display_name":"Neuroscience"},"domain":{"id":"https://openalex.org/domains/1","display_name":"Life Sciences"}}],"keywords":[{"id":"https://openalex.org/keywords/plasma-protein-binding","display_name":"plasma protein binding","score":0.949999988079071},{"id":"https://openalex.org/keywords/albumin-binding","display_name":"albumin binding","score":0.9620000123977661},{"id":"https://openalex.org/keywords/brain-penetration","display_name":"brain penetration","score":0.8519999980926514},{"id":"https://openalex.org/keywords/blood-brain-barrier","display_name":"blood-brain barrier","score":0.968999981880188},{"id":"https://openalex.org/keywords/anticonvulsant-activity","display_name":"anticonvulsant activity","score":0.9150000214576721},{"id":"https://openalex.org/keywords/lipophilicity","display_name":"lipophilicity","score":0.8489999771118164},{"id":"https://openalex.org/keywords/octanol-water-partition-coefficient","display_name":"octanol-water partition coefficient","score":0.6399999856948853},{"id":"https://openalex.org/keywords/drug-design","display_name":"drug design","score":0.38600000739097595},{"id":"https://openalex.org/keywords/in-situ-brain-perfusion","display_name":"in situ brain perfusion","score":0.8339999914169312},{"id":"https://openalex.org/keywords/nmda-receptor-glycine-site","display_name":"NMDA receptor glycine site","score":0.6179999709129333},{"id":"https://openalex.org/keywords/seizures","display_name":"seizures","score":0.3019999861717224},{"id":"https://openalex.org/keywords/brain-to-blood-ratio","display_name":"brain-to-blood ratio","score":0.7089999914169312},{"id":"https://openalex.org/keywords/in-vitro-in-vivo-correlation","display_name":"in vitro-in vivo correlation","score":0.5400000214576721},{"id":"https://openalex.org/keywords/drug-metabolism-and-pharmacokinetics","display_name":"drug metabolism and pharmacokinetics","score":0.35899999737739563},{"id":"https://openalex.org/keywords/drug-drug-interactions","display_name":"drug-drug interactions","score":0.40400001406669617}],"concepts":[{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.8688068985939026},{"id":"https://openalex.org/C207001950","wikidata":"https://www.wikidata.org/wiki/Q141124","display_name":"In vivo","level":2,"score":0.6424567699432373},{"id":"https://openalex.org/C67018056","wikidata":"https://www.wikidata.org/wiki/Q414896","display_name":"NMDA receptor","level":3,"score":0.5949087142944336},{"id":"https://openalex.org/C2775858608","wikidata":"https://www.wikidata.org/wiki/Q576618","display_name":"Anticonvulsant","level":3,"score":0.5877605676651001},{"id":"https://openalex.org/C51639874","wikidata":"https://www.wikidata.org/wiki/Q167149","display_name":"Plasma protein binding","level":2,"score":0.5541919469833374},{"id":"https://openalex.org/C2776125364","wikidata":"https://www.wikidata.org/wiki/Q169219","display_name":"Albumin","level":2,"score":0.5050655007362366},{"id":"https://openalex.org/C146543888","wikidata":"https://www.wikidata.org/wiki/Q425056","display_name":"Blood proteins","level":2,"score":0.47268372774124146},{"id":"https://openalex.org/C107824862","wikidata":"https://www.wikidata.org/wiki/Q616005","display_name":"Binding site","level":2,"score":0.46351683139801025},{"id":"https://openalex.org/C2777756961","wikidata":"https://www.wikidata.org/wiki/Q620730","display_name":"Glycine","level":3,"score":0.4596744179725647},{"id":"https://openalex.org/C112705442","wikidata":"https://www.wikidata.org/wiki/Q323936","display_name":"Pharmacokinetics","level":2,"score":0.4276256859302521},{"id":"https://openalex.org/C2776575606","wikidata":"https://www.wikidata.org/wiki/Q79749","display_name":"Blood plasma","level":2,"score":0.4248339533805847},{"id":"https://openalex.org/C165616093","wikidata":"https://www.wikidata.org/wiki/Q424232","display_name":"Serum albumin","level":2,"score":0.42018061876296997},{"id":"https://openalex.org/C67847695","wikidata":"https://www.wikidata.org/wiki/Q626478","display_name":"Radioligand","level":3,"score":0.4142743647098541},{"id":"https://openalex.org/C43617362","wikidata":"https://www.wikidata.org/wiki/Q170050","display_name":"Chromatography","level":1,"score":0.34954315423965454},{"id":"https://openalex.org/C170493617","wikidata":"https://www.wikidata.org/wiki/Q208467","display_name":"Receptor","level":2,"score":0.3436187505722046},{"id":"https://openalex.org/C55493867","wikidata":"https://www.wikidata.org/wiki/Q7094","display_name":"Biochemistry","level":1,"score":0.3354450464248657},{"id":"https://openalex.org/C98274493","wikidata":"https://www.wikidata.org/wiki/Q128406","display_name":"Pharmacology","level":1,"score":0.28673964738845825},{"id":"https://openalex.org/C515207424","wikidata":"https://www.wikidata.org/wiki/Q8066","display_name":"Amino acid","level":2,"score":0.18043190240859985},{"id":"https://openalex.org/C2778186239","wikidata":"https://www.wikidata.org/wiki/Q41571","display_name":"Epilepsy","level":2,"score":0.06002873182296753},{"id":"https://openalex.org/C71924100","wikidata":"https://www.wikidata.org/wiki/Q11190","display_name":"Medicine","level":0,"score":0.0},{"id":"https://openalex.org/C150903083","wikidata":"https://www.wikidata.org/wiki/Q7108","display_name":"Biotechnology","level":1,"score":0.0},{"id":"https://openalex.org/C169760540","wikidata":"https://www.wikidata.org/wiki/Q207011","display_name":"Neuroscience","level":1,"score":0.0},{"id":"https://openalex.org/C86803240","wikidata":"https://www.wikidata.org/wiki/Q420","display_name":"Biology","level":0,"score":0.0}],"mesh":[{"descriptor_ui":"D000818","descriptor_name":"Animals","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D001798","descriptor_name":"Blood Proteins","qualifier_ui":"Q000378","qualifier_name":"metabolism","is_major_topic":true},{"descriptor_ui":"D001812","descriptor_name":"Blood-Brain Barrier","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":true},{"descriptor_ui":"D008297","descriptor_name":"Male","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D011485","descriptor_name":"Protein Binding","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D016194","descriptor_name":"Receptors, N-Methyl-D-Aspartate","qualifier_ui":"Q000037","qualifier_name":"antagonists & inhibitors","is_major_topic":true},{"descriptor_ui":"D018009","descriptor_name":"Receptors, Glycine","qualifier_ui":"Q000037","qualifier_name":"antagonists & inhibitors","is_major_topic":true},{"descriptor_ui":"D018691","descriptor_name":"Excitatory Amino Acid Antagonists","qualifier_ui":"Q000138","qualifier_name":"chemical synthesis","is_major_topic":false},{"descriptor_ui":"D018691","descriptor_name":"Excitatory Amino Acid Antagonists","qualifier_ui":"Q000493","qualifier_name":"pharmacokinetics","is_major_topic":true},{"descriptor_ui":"D051379","descriptor_name":"Mice","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}],"locations_count":2,"locations":[{"id":"doi:10.1021/jm970417o","doi":"https://doi.org/10.1021/jm970417o","is_oa":false,"landing_page_url":"https://doi.org/10.1021/jm970417o","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:9406596","doi":null,"is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/9406596","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"}],"best_oa_location":null,"sustainable_development_goals":[{"id":"https://metadata.un.org/sdg/3","score":0.9391000270843506,"display_name":"Good health and well-being"}],"study_designs":[],"awards":[],"funders":[],"has_content":{"grobid_xml":false,"pdf":false},"content_urls":null,"referenced_works_count":33,"referenced_works":["https://openalex.org/W262895456","https://openalex.org/W591403642","https://openalex.org/W1963895697","https://openalex.org/W1981964376","https://openalex.org/W1997495339","https://openalex.org/W2002060837","https://openalex.org/W2028365439","https://openalex.org/W2029093606","https://openalex.org/W2030463961","https://openalex.org/W2030557362","https://openalex.org/W2030950703","https://openalex.org/W2034473936","https://openalex.org/W2038134571","https://openalex.org/W2038284932","https://openalex.org/W2040524342","https://openalex.org/W2067577545","https://openalex.org/W2071870159","https://openalex.org/W2075345533","https://openalex.org/W2076831847","https://openalex.org/W2076959752","https://openalex.org/W2082214060","https://openalex.org/W2083637127","https://openalex.org/W2083810819","https://openalex.org/W2085354202","https://openalex.org/W2086106390","https://openalex.org/W2086593457","https://openalex.org/W2093248888","https://openalex.org/W2094126290","https://openalex.org/W2106722078","https://openalex.org/W2114890056","https://openalex.org/W2312618570","https://openalex.org/W2949660215","https://openalex.org/W2952792068"],"related_works":["https://openalex.org/W2036068251","https://openalex.org/W7053041601","https://openalex.org/W2075345533","https://openalex.org/W2002589410","https://openalex.org/W2023657406","https://openalex.org/W1963895697","https://openalex.org/W2952055270","https://openalex.org/W6982369912","https://openalex.org/W1799745768","https://openalex.org/W2049565541"],"abstract_inverted_index":{"A":[0,24],"major":[1,75],"issue":[2],"in":[3,21,35,43,44,53,81,162,184,198,268,273,296,312,355],"designing":[4],"drugs":[5],"as":[6],"antagonists":[7,29],"at":[8,331],"the":[9,13,36,62,74,116,129,166,188,201,209,232,249,277,282,293,297,308,315,325,370,401,415],"glycine":[10,28,317,382,419],"site":[11,102,318,383,420],"of":[12,26,61,100,106,149,168,171,203,222,251,263,279,299,324,367,381,417],"NMDA":[14],"receptor":[15],"has":[16,119],"been":[17,120,376],"to":[18,32,64,73,123,133,155,190,196,206,275,328,378,400,430,439],"achieve":[19],"good":[20,441],"vivo":[22,356],"activity.":[23,55,445],"series":[25,380],"4-hydroxyquinolone":[27,130],"was":[30,79],"found":[31],"be":[33],"active":[34],"DBA/2":[37],"mouse":[38],"anticonvulsant":[39,54,158],"assay,":[40,94],"but":[41,165,302],"improvements":[42],"vitro":[45,163],"affinity":[46,320],"were":[47],"not":[48,339,408],"mirrored":[49],"by":[50,85,258],"corresponding":[51],"increases":[52,160,187,321],"Here":[56],"we":[57],"show":[58,231],"that":[59,194,286,389,406,426],"binding":[60,72,88,109,132,181,195,245,319,373,399],"compounds":[63,227,287,405],"plasma":[65,76,107,125,134,179,199,300,371],"protein":[66,108,126,135,180,346,372,398],"limits":[67],"their":[68],"brain":[69,264,270,294],"penetration.":[70],"Relative":[71],"protein,":[77,301],"albumin,":[78],"measured":[80],"two":[82],"different":[83],"ways:":[84],"a":[86,96,147,169,329,332,350,362,391],"radioligand":[87],"experiment":[89],"or":[90,436],"using":[91,266],"an":[92,267],"HPLC":[93,117],"for":[95,225,243,253,390,404,414],"wide":[97],"structural":[98],"range":[99,148],"glycine/NMDA":[101],"ligands.":[103],"These":[104],"measures":[105],"correlate":[110],"well":[111,295],"(r":[112,137],"=":[113,138],"0.84),":[114],"and":[115,290,358,385,422],"assay":[118],"used":[121],"extensively":[122],"quantify":[124],"binding.":[127],"For":[128],"series,":[131],"correlates":[136],"0.92)":[139],"with":[140,161,235,322,344,361],"log":[141,150,237,333,359,364,393,433],"P":[142,151,334,365,394,434],"(octanol/pH":[143],"7.4":[144],"buffer)":[145],"over":[146],"values":[152],"from":[153,215],"0":[154],"5.":[156],"The":[157,410],"activity":[159,357],"affinity,":[164],"slope":[167,189],"plot":[170,186],"pED50":[172],"versus":[173],"pIC50":[174],"is":[175,304,310,387,424,428],"low":[176,435],"(0.40);":[177],"taking":[178],"into":[182],"account":[183],"this":[185,303,348],"0.60.":[191],"This":[192],"shows":[193],"albumin":[197,244],"reduces":[200],"amount":[202,278],"compound":[204],"free":[205],"diffuse":[207],"across":[208],"blood-brain":[210,283],"barrier.":[211],"Further":[212],"evidence":[213],"comes":[214],"three":[216,226],"other":[217,379],"experiments:":[218],"(a)":[219],"Direct":[220,261],"measurements":[221,262],"brain/blood":[223],"ratios":[224],"(2,":[228],"16,":[229],"26)":[230],"ratio":[233],"decreases":[234],"increasing":[236,345],"R.":[238],"(b)":[239],"Warfarin,":[240],"which":[241],"competes":[242],"sites":[246],"dose-dependently,":[247],"decreased":[248],"ED50":[250],"26":[252],"protection":[254],"against":[255],"seizures":[256],"induced":[257],"NMDLA.":[259],"(c)":[260],"penetration":[265],"situ":[269],"perfusion":[271],"model":[272],"rat":[274],"measure":[276],"drug":[280,309],"crossing":[281],"barrier":[284],"showed":[285],"2,":[288],"26,":[289],"32":[291],"penetrate":[292],"absence":[298],"greatly":[305],"reduced":[306],"when":[307],"delivered":[311],"plasma.":[313],"In":[314],"4-hydroxyquinolones":[316],"lipophilicity":[323],"3-substituent":[326],"up":[327],"maximum":[330,363],"around":[335],"3,":[336],"then":[337],"does":[338],"improve":[340],"further.":[341],"When":[342],"combined":[343],"binding,":[347],"gives":[349],"parabolic":[351],"relationship":[352],"between":[353],"predicted":[354],"P,":[360],"value":[366],"2.39.":[368],"Finally,":[369],"studies":[374],"have":[375,396,412],"extended":[377],"antagonists,":[384,421],"its":[386],"shown":[388],"given":[392],"these":[395],"similar":[397],"4-hydroxyquinolones,":[402],"except":[403],"are":[407],"acidic.":[409],"results":[411],"implications":[413],"design":[416],"novel":[418],"it":[423,427],"suggested":[425],"necessary":[429],"either":[431],"keep":[432],"pKa":[437],"high":[438],"obtain":[440],"central":[442],"nervous":[443],"system":[444]},"counts_by_year":[{"year":2025,"cited_by_count":2},{"year":2024,"cited_by_count":5},{"year":2023,"cited_by_count":2},{"year":2022,"cited_by_count":5},{"year":2021,"cited_by_count":1},{"year":2020,"cited_by_count":6},{"year":2019,"cited_by_count":3},{"year":2018,"cited_by_count":3},{"year":2017,"cited_by_count":5},{"year":2016,"cited_by_count":13},{"year":2015,"cited_by_count":3},{"year":2014,"cited_by_count":4},{"year":2013,"cited_by_count":7},{"year":2012,"cited_by_count":5}],"updated_date":"2026-10-31T12:09:11.096373","created_date":"2016-06-24T00:00:00"}