PMC:7796052 / 15348-16071 JSONTXT

{"target":"https://pubannotation.org/docs/sourcedb/PMC/sourceid/7796052","sourcedb":"PMC","sourceid":"7796052","source_url":"https://www.ncbi.nlm.nih.gov/pmc/7796052","text":"The aim of the present study was to characterize the pharmacological profile of raloxifene towards the bradykinin receptors. The compound was identified as a micromolar ligand of the B2 receptor by virtual screening in a drug repurposing campaign. Results showed that raloxifene is a weak partial agonist toward the B2 receptor, with a 19% efficacy compared to bradykinin, with an apparent dissociation constant KB ~ 21 µM. The discovery of the bradykinin pharmacodynamics profile of raloxidene explains in part its observed vascular beneficial effects, although they could also be due to activation of the GPR30 receptor signaling pathway. On the other hand, it acts as a bradykinin antagonist for B2 with an IC50 ~ 21 µM.","tracks":[{"project":"LitCovid-PubTator","denotations":[{"id":"397","span":{"begin":183,"end":194},"obj":"Gene"},{"id":"398","span":{"begin":316,"end":327},"obj":"Gene"},{"id":"399","span":{"begin":361,"end":371},"obj":"Gene"},{"id":"400","span":{"begin":445,"end":455},"obj":"Gene"},{"id":"401","span":{"begin":607,"end":612},"obj":"Gene"},{"id":"402","span":{"begin":673,"end":683},"obj":"Gene"},{"id":"403","span":{"begin":80,"end":90},"obj":"Chemical"},{"id":"404","span":{"begin":268,"end":278},"obj":"Chemical"},{"id":"405","span":{"begin":484,"end":494},"obj":"Chemical"}],"attributes":[{"id":"A397","pred":"tao:has_database_id","subj":"397","obj":"Gene:624"},{"id":"A398","pred":"tao:has_database_id","subj":"398","obj":"Gene:624"},{"id":"A399","pred":"tao:has_database_id","subj":"399","obj":"Gene:3827"},{"id":"A400","pred":"tao:has_database_id","subj":"400","obj":"Gene:3827"},{"id":"A401","pred":"tao:has_database_id","subj":"401","obj":"Gene:2852"},{"id":"A402","pred":"tao:has_database_id","subj":"402","obj":"Gene:3827"},{"id":"A403","pred":"tao:has_database_id","subj":"403","obj":"MESH:D020849"},{"id":"A404","pred":"tao:has_database_id","subj":"404","obj":"MESH:D020849"},{"subj":"397","pred":"source","obj":"LitCovid-PubTator"},{"subj":"398","pred":"source","obj":"LitCovid-PubTator"},{"subj":"399","pred":"source","obj":"LitCovid-PubTator"},{"subj":"400","pred":"source","obj":"LitCovid-PubTator"},{"subj":"401","pred":"source","obj":"LitCovid-PubTator"},{"subj":"402","pred":"source","obj":"LitCovid-PubTator"},{"subj":"403","pred":"source","obj":"LitCovid-PubTator"},{"subj":"404","pred":"source","obj":"LitCovid-PubTator"},{"subj":"405","pred":"source","obj":"LitCovid-PubTator"}],"namespaces":[{"prefix":"Tax","uri":"https://www.ncbi.nlm.nih.gov/taxonomy/"},{"prefix":"MESH","uri":"https://id.nlm.nih.gov/mesh/"},{"prefix":"Gene","uri":"https://www.ncbi.nlm.nih.gov/gene/"},{"prefix":"CVCL","uri":"https://web.expasy.org/cellosaurus/CVCL_"}]},{"project":"LitCovid-sentences","denotations":[{"id":"T107","span":{"begin":0,"end":124},"obj":"Sentence"},{"id":"T108","span":{"begin":125,"end":247},"obj":"Sentence"},{"id":"T109","span":{"begin":248,"end":423},"obj":"Sentence"},{"id":"T110","span":{"begin":424,"end":640},"obj":"Sentence"},{"id":"T111","span":{"begin":641,"end":723},"obj":"Sentence"}],"namespaces":[{"prefix":"_base","uri":"http://pubannotation.org/ontology/tao.owl#"}],"attributes":[{"subj":"T107","pred":"source","obj":"LitCovid-sentences"},{"subj":"T108","pred":"source","obj":"LitCovid-sentences"},{"subj":"T109","pred":"source","obj":"LitCovid-sentences"},{"subj":"T110","pred":"source","obj":"LitCovid-sentences"},{"subj":"T111","pred":"source","obj":"LitCovid-sentences"}]}],"config":{"attribute types":[{"pred":"source","value type":"selection","values":[{"id":"LitCovid-PubTator","color":"#da93ec","default":true},{"id":"LitCovid-sentences","color":"#93ecc0"}]}]}}