{"id":"https://openalex.org/W84643873","doi":null,"title":"BAY X1005, a new selective inhibitor of leukotriene synthesis: pharmacology and pharmacokinetics.","display_name":"BAY X1005, a new selective inhibitor of leukotriene synthesis: pharmacology and pharmacokinetics.","publication_year":1993,"publication_date":"1993-03-01","ids":{"openalex":"https://openalex.org/W84643873","mag":"84643873","pmid":"https://pubmed.ncbi.nlm.nih.gov/8395246"},"language":"en","primary_location":{"id":"pmid:8395246","doi":null,"is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/8395246","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 lipid mediators","raw_type":"Journal Article"},"volume":null,"type":"article","is_traditional":true,"indexed_in":["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/A5068439786","display_name":"Reiner M\u00fcller-Peddinghaus","orcid":null,"observed_orcids":[]},"institutions":[{"id":"https://openalex.org/I67348948","display_name":"Bayer (Germany)","ror":"https://ror.org/04hmn8g73","country_code":"DE","type":"company","lineage":["https://openalex.org/I67348948"]}],"countries":["DE"],"is_corresponding":false,"raw_author_name":"R M\u00fcller-Peddinghaus","raw_affiliation_strings":["Pharma Research Center, Bayer AG, Wuppertal, Germany"],"raw_orcid":null,"affiliations":[{"raw_affiliation_string":"Pharma Research Center, Bayer AG, Wuppertal, Germany","institution_ids":["https://openalex.org/I67348948"]}]},{"author_position":"middle","author":{"id":"https://openalex.org/A5079870410","display_name":"Romanis Fruchtmann","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"R Fruchtmann","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5111406353","display_name":"H J Ahr","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"H J Ahr","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":null,"display_name":"B Beckermann","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"B Beckermann","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5002689810","display_name":"Klaus B\u00fchner","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"K B\u00fchner","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5021141292","display_name":"Burkhard Fugmann","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"B Fugmann","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5000251005","display_name":"Bodo Junge","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"B Junge","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":null,"display_name":"M Matzke","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"M Matzke","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"middle","author":{"id":"https://openalex.org/A5081918713","display_name":"Christian Kohlsdorfer","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"C Kohlsdorfer","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]},{"author_position":"last","author":{"id":"https://openalex.org/A5040038065","display_name":"Siegfried Raddatz","orcid":null,"observed_orcids":[]},"institutions":[],"countries":[],"is_corresponding":false,"raw_author_name":"S Raddatz","raw_affiliation_strings":[],"raw_orcid":null,"affiliations":[]}],"institutions":[],"countries_distinct_count":1,"institutions_distinct_count":1,"corresponding_author_ids":[],"corresponding_institution_ids":[],"apc_list":null,"apc_paid":null,"fwci":0.6259,"has_fulltext":false,"cited_by_count":15,"citation_normalized_percentile":{"value":0.64428234,"is_in_top_1_percent":false,"is_in_top_10_percent":false},"cited_by_percentile_year":{"min":88,"max":97},"biblio":{"volume":"6","issue":"1-3","first_page":"245","last_page":"8"},"is_retracted":false,"is_paratext":false,"is_xpac":false,"primary_topic":{"id":"https://openalex.org/T10678","display_name":"Inflammatory mediators and NSAID effects","score":0.9276999831199646,"subfield":{"id":"https://openalex.org/subfields/2736","display_name":"Pharmacology (medical)"},"field":{"id":"https://openalex.org/fields/27","display_name":"Medicine"},"domain":{"id":"https://openalex.org/domains/4","display_name":"Health Sciences"}},"topics":[{"id":"https://openalex.org/T10678","display_name":"Inflammatory mediators and NSAID effects","score":0.9276999831199646,"subfield":{"id":"https://openalex.org/subfields/2736","display_name":"Pharmacology (medical)"},"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/T12910","display_name":"Eicosanoids and Hypertension Pharmacology","score":0.06549999862909317,"subfield":{"id":"https://openalex.org/subfields/1303","display_name":"Biochemistry"},"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/T10387","display_name":"Fatty Acid Research and Health","score":0.0007999999797903001,"subfield":{"id":"https://openalex.org/subfields/2916","display_name":"Nutrition and Dietetics"},"field":{"id":"https://openalex.org/fields/29","display_name":"Nursing"},"domain":{"id":"https://openalex.org/domains/4","display_name":"Health Sciences"}}],"keywords":[{"id":"https://openalex.org/keywords/leukotriene-synthesis-inhibitors","display_name":"leukotriene synthesis inhibitors","score":0.8949999809265137},{"id":"https://openalex.org/keywords/5-lipoxygenase-inhibition","display_name":"5-lipoxygenase inhibition","score":0.8679999709129333},{"id":"https://openalex.org/keywords/leukotriene-b4","display_name":"leukotriene B4","score":0.9100000262260437},{"id":"https://openalex.org/keywords/leukotriene-c4","display_name":"leukotriene C4","score":0.9940000176429749},{"id":"https://openalex.org/keywords/neutrophils","display_name":"neutrophils","score":0.5849999785423279},{"id":"https://openalex.org/keywords/macrophages","display_name":"macrophages","score":0.9909999966621399},{"id":"https://openalex.org/keywords/pharmacokinetics","display_name":"pharmacokinetics","score":0.8109999895095825},{"id":"https://openalex.org/keywords/bioavailability","display_name":"bioavailability","score":0.847000002861023},{"id":"https://openalex.org/keywords/oral-bioavailability","display_name":"oral bioavailability","score":0.6449999809265137},{"id":"https://openalex.org/keywords/anti-inflammatory-activity","display_name":"anti-inflammatory activity","score":0.6340000033378601},{"id":"https://openalex.org/keywords/ear-edema","display_name":"ear edema","score":0.7300000190734863},{"id":"https://openalex.org/keywords/myeloperoxidase","display_name":"myeloperoxidase","score":0.9449999928474426},{"id":"https://openalex.org/keywords/arachidonic-acid-metabolism","display_name":"arachidonic acid metabolism","score":0.7120000123977661},{"id":"https://openalex.org/keywords/quinoline-derivatives","display_name":"quinoline derivatives","score":0.5120000243186951},{"id":"https://openalex.org/keywords/enantiomers","display_name":"enantiomers","score":0.5130000114440918},{"id":"https://openalex.org/keywords/allergic-diseases","display_name":"allergic diseases","score":0.4180000126361847}],"concepts":[{"id":"https://openalex.org/C98274493","wikidata":"https://www.wikidata.org/wiki/Q128406","display_name":"Pharmacology","level":1,"score":0.7461129426956177},{"id":"https://openalex.org/C112705442","wikidata":"https://www.wikidata.org/wiki/Q323936","display_name":"Pharmacokinetics","level":2,"score":0.6218414306640625},{"id":"https://openalex.org/C207001950","wikidata":"https://www.wikidata.org/wiki/Q141124","display_name":"In vivo","level":2,"score":0.5886422991752625},{"id":"https://openalex.org/C2777752497","wikidata":"https://www.wikidata.org/wiki/Q286779","display_name":"IC50","level":3,"score":0.544363796710968},{"id":"https://openalex.org/C22979827","wikidata":"https://www.wikidata.org/wiki/Q5137311","display_name":"Cmax","level":3,"score":0.5110965371131897},{"id":"https://openalex.org/C57992300","wikidata":"https://www.wikidata.org/wiki/Q2066956","display_name":"Potency","level":3,"score":0.4750005006790161},{"id":"https://openalex.org/C181389837","wikidata":"https://www.wikidata.org/wiki/Q461809","display_name":"Bioavailability","level":2,"score":0.4745771884918213},{"id":"https://openalex.org/C2776452501","wikidata":"https://www.wikidata.org/wiki/Q424190","display_name":"Leukotriene","level":3,"score":0.4563674330711365},{"id":"https://openalex.org/C185592680","wikidata":"https://www.wikidata.org/wiki/Q2329","display_name":"Chemistry","level":0,"score":0.4486010670661926},{"id":"https://openalex.org/C203565725","wikidata":"https://www.wikidata.org/wiki/Q420012","display_name":"Myeloperoxidase","level":3,"score":0.43095847964286804},{"id":"https://openalex.org/C42533223","wikidata":"https://www.wikidata.org/wiki/Q1378064","display_name":"ED50","level":3,"score":0.4270167946815491},{"id":"https://openalex.org/C202751555","wikidata":"https://www.wikidata.org/wiki/Q221681","display_name":"In vitro","level":2,"score":0.35179173946380615},{"id":"https://openalex.org/C86803240","wikidata":"https://www.wikidata.org/wiki/Q420","display_name":"Biology","level":0,"score":0.305084764957428},{"id":"https://openalex.org/C2776914184","wikidata":"https://www.wikidata.org/wiki/Q101991","display_name":"Inflammation","level":2,"score":0.3016452491283417},{"id":"https://openalex.org/C55493867","wikidata":"https://www.wikidata.org/wiki/Q7094","display_name":"Biochemistry","level":1,"score":0.27549904584884644},{"id":"https://openalex.org/C203014093","wikidata":"https://www.wikidata.org/wiki/Q101929","display_name":"Immunology","level":1,"score":0.15083715319633484},{"id":"https://openalex.org/C2776042228","wikidata":"https://www.wikidata.org/wiki/Q35869","display_name":"Asthma","level":2,"score":0.0},{"id":"https://openalex.org/C150903083","wikidata":"https://www.wikidata.org/wiki/Q7108","display_name":"Biotechnology","level":1,"score":0.0}],"mesh":[{"descriptor_ui":"D000284","descriptor_name":"Administration, Oral","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D000818","descriptor_name":"Animals","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D006801","descriptor_name":"Humans","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"descriptor_ui":"D007975","descriptor_name":"Leukotriene B4","qualifier_ui":"Q000037","qualifier_name":"antagonists & inhibitors","is_major_topic":true},{"descriptor_ui":"D007975","descriptor_name":"Leukotriene B4","qualifier_ui":"Q000096","qualifier_name":"biosynthesis","is_major_topic":false},{"descriptor_ui":"D009504","descriptor_name":"Neutrophils","qualifier_ui":"Q000201","qualifier_name":"enzymology","is_major_topic":false},{"descriptor_ui":"D011804","descriptor_name":"Quinolines","qualifier_ui":"Q000008","qualifier_name":"administration & dosage","is_major_topic":false},{"descriptor_ui":"D011804","descriptor_name":"Quinolines","qualifier_ui":"Q000493","qualifier_name":"pharmacokinetics","is_major_topic":true},{"descriptor_ui":"D011804","descriptor_name":"Quinolines","qualifier_ui":"Q000494","qualifier_name":"pharmacology","is_major_topic":true},{"descriptor_ui":"D016859","descriptor_name":"Lipoxygenase Inhibitors","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false},{"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},{"descriptor_ui":"D066298","descriptor_name":"In Vitro Techniques","qualifier_ui":null,"qualifier_name":null,"is_major_topic":false}],"locations_count":2,"locations":[{"id":"pmid:8395246","doi":null,"is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/8395246","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 lipid mediators","raw_type":"Journal Article"},{"id":"mag:84643873","doi":null,"is_oa":false,"landing_page_url":"https://pubmed.ncbi.nlm.nih.gov/8395246","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":null,"is_accepted":false,"is_published":false,"raw_source_name":"PubMed","raw_type":null}],"best_oa_location":null,"sustainable_development_goals":[{"score":0.9391000270843506,"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":0,"referenced_works":[],"related_works":["https://openalex.org/W2051010723","https://openalex.org/W2252978673","https://openalex.org/W1999783546","https://openalex.org/W2062947688","https://openalex.org/W272373211","https://openalex.org/W3159565964","https://openalex.org/W2335169562","https://openalex.org/W762928327","https://openalex.org/W2065246975","https://openalex.org/W2089338169"],"abstract_inverted_index":{"The":[0],"enantiomer":[1],"BAY":[2,59,81,121,160],"X1005":[3,60,82,122,161],"[(R)-2-[4-(quinolin-2-yl-methoxy)phenyl]-2-cyclopentyl":[4],"acetic":[5],"acid]":[6],"potently":[7],"inhibits":[8,83],"LTB4":[9,44,114],"synthesis":[10,27,45,115,158],"in":[11,28,40,47,74,89,103,110,140,164,170],"isolated":[12],"PMNL":[13],"of":[14,132,137,155],"various":[15],"species":[16],"(IC50":[17,31],"mumol/l,":[18],"human":[19,75],"0.22,":[20],"rat":[21,105,142],"0.026,":[22],"mouse":[23,29,92],"0.039)":[24],"and":[25,69,86,98,135,152,172],"LTC4":[26],"macrophages":[30],"0.021":[32],"mumol/l).":[33],"Due":[34],"to":[35,52],"high":[36,125],"protein":[37],"binding":[38],"the":[39,64,90,104,141,148,156],"vitro":[41],"potency":[42],"for":[43,63,113,166],"inhibition":[46,116],"whole":[48,76,111],"blood":[49,112],"is":[50,61,108],"lowered":[51],"17":[53],"mumol/l":[54],"as":[55,72],"determined":[56,73],"by":[57],"RIA.":[58],"selective":[62],"5-lipoxygenase":[65],"pathway":[66],"leaving":[67],"12-HETE":[68],"HHT":[70],"unaltered,":[71],"blood.":[77],"After":[78],"oral":[79],"application":[80],"edema":[84],"formation":[85],"myeloperoxidase":[87],"activity":[88,102],"arachidonate-induced":[91],"ear":[93],"inflammation":[94],"test":[95],"(ED50":[96,117],"48.7":[97],"7.9,":[99],"respectively).":[100],"Oral":[101],"ex":[106],"vivo":[107],"found":[109],"11.8":[118],"mg/kg":[119,145],"p.o.).":[120],"demonstrates":[123],"a":[124,130],"bioavailability":[126],"(f":[127],"86%)":[128],"with":[129],"Cmax":[131],"13":[133],"mg/l":[134],"t1/2":[136],"3.5":[138],"h":[139],"at":[143],"10":[144],"p.o.":[146],"Thus,":[147],"pharmacodynamic,":[149],"pharmacokinetic":[150],"profile":[151],"safety":[153],"aspects":[154],"leukotriene":[157],"inhibitor":[159],"allow":[162],"testing":[163],"man":[165],"its":[167],"therapeutic":[168],"potential":[169],"inflammatory":[171],"allergic":[173],"diseases.":[174]},"counts_by_year":[{"year":2019,"cited_by_count":1},{"year":2017,"cited_by_count":3},{"year":2016,"cited_by_count":2},{"year":2015,"cited_by_count":1}],"updated_date":"2026-11-04T10:54:05.112534","created_date":"2016-06-24T00:00:00"}