{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2025,10,16]],"date-time":"2025-10-16T01:17:12Z","timestamp":1760577432100,"version":"3.37.3"},"reference-count":44,"publisher":"Oxford University Press (OUP)","issue":"7","license":[{"start":{"date-parts":[[2019,7,1]],"date-time":"2019-07-01T00:00:00Z","timestamp":1561939200000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/academic.oup.com\/journals\/pages\/open_access\/funder_policies\/chorus\/standard_publication_model"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":[],"published-print":{"date-parts":[[2019,7,1]]},"abstract":"<jats:title>Abstract<\/jats:title>\n               <jats:sec>\n                  <jats:title>Objectives<\/jats:title>\n                  <jats:p>Antidepressants need to penetrate the blood\u2013brain barrier (BBB) to exert their functions in the central nervous system. Breast cancer resistance protein (BCRP), an efflux transporter abundantly expressed in the BBB, prevents the accumulation of many drugs in the brain. This study aimed to identify whether five commonly used antidepressants (sertraline, duloxetine, fluoxetine, amitriptyline and mirtazapine) are BCRP substrates.<\/jats:p>\n               <\/jats:sec>\n               <jats:sec>\n                  <jats:title>Methods<\/jats:title>\n                  <jats:p>A combination of bidirectional transport and intracellular accumulation experiments was conducted on BCRP-overexpressing MDCKII and wild-type (WT) cells, and in situ brain perfusion was conducted in rats.<\/jats:p>\n               <\/jats:sec>\n               <jats:sec>\n                  <jats:title>Key findings<\/jats:title>\n                  <jats:p>The bidirectional transport study revealed that the net efflux ratio (NER) of sertraline reached 2.08 but decreased to 1.06 when co-incubated with Ko143, a selective BCRP inhibitor. Conversely, the other four antidepressants did not appear to be BCRP substrates, due to their low NER values (&amp;lt;1.5). The accumulation of sertraline in MDCKII-BCRP cells was significantly lower than that in MDCKII-WT cells. The presence of Ko143 significantly increased the sertraline accumulation in MDCKII-BCRP cells but not in MDCKII-WT cells. Brain perfusion showed that the permeability of 1 and 5 \u03bcm sertraline was significantly higher in the presence of Ko143.<\/jats:p>\n               <\/jats:sec>\n               <jats:sec>\n                  <jats:title>Conclusions<\/jats:title>\n                  <jats:p>Taken together, BCRP is involved in sertraline efflux.<\/jats:p>\n               <\/jats:sec>","DOI":"10.1111\/jphp.13100","type":"journal-article","created":{"date-parts":[[2019,5,1]],"date-time":"2019-05-01T01:44:23Z","timestamp":1556675063000},"page":"1133-1141","source":"Crossref","is-referenced-by-count":10,"title":["In-vitro and <i>in situ<\/i> assessment of the efflux of five antidepressants by breast cancer resistance protein"],"prefix":"10.1093","volume":"71","author":[{"given":"Suqin","family":"Feng","sequence":"first","affiliation":[{"name":"Department of Clinical Pharmacy and Pharmacy Administration, West China School of Pharmacy, Sichuan University , Chengdu,","place":["China"]}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Liang","family":"Zheng","sequence":"additional","affiliation":[{"name":"Department of Clinical Pharmacy and Pharmacy Administration, West China School of Pharmacy, Sichuan University , Chengdu,","place":["China"]}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Shiwei","family":"Tang","sequence":"additional","affiliation":[{"name":"Department of Pharmacy, People's Hospital of Dujiangyan City , Dujiangyan,","place":["China"]}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Juan","family":"Gu","sequence":"additional","affiliation":[{"name":"Department of Pharmacy, Affiliated Hospital of Zunyi Medical College , Zunyi,","place":["China"]}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Xuehua","family":"Jiang","sequence":"additional","affiliation":[{"name":"Department of Clinical Pharmacy and Pharmacy Administration, West China School of Pharmacy, Sichuan University , Chengdu,","place":["China"]}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-3220-6065","authenticated-orcid":false,"given":"Ling","family":"Wang","sequence":"additional","affiliation":[{"name":"Department of Clinical Pharmacy and Pharmacy Administration, West China School of Pharmacy, Sichuan University , Chengdu,","place":["China"]}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"286","published-online":{"date-parts":[[2019,7,1]]},"reference":[{"key":"2024103012352739200_jphp13100-cit-0001","doi-asserted-by":"crossref","first-page":"430","DOI":"10.1016\/j.jep.2015.07.011","article-title":"Aristolochic acid I is a substrate of BCRP but not P-glycoprotein or MRP2","volume":"172","author":"Liping","year":"2015","journal-title":"J Ethnopharmacol"},{"key":"2024103012352739200_jphp13100-cit-0002","first-page":"142","article-title":"Selective serotonin reuptake inhibitors (SSRIs) and routine specialist care with and 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