| http://purl.uniprot.org/citations/16850390 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/16850390 | http://www.w3.org/2000/01/rdf-schema#comment | "The objective of this study was to establish the optimal blood concentrations of the potent P-glycoprotein (P-gp) inhibitor GF120918 (Elacridar) required to achieve maximal knockout of this efflux transporter in the blood-brain barrier (BBB) of mice, rats, and guinea pigs. Genetic mdr1a/b(-/-) knockout mice and "chemical" P-gp knockout mice, rats, and guinea pigs, generated by 24 h continuous infusion of GF120918, were used to investigate the effects of P-gp modulation on the brain penetration of SB-487946. Genetic mdr1a/b(-/-) knockout mice demonstrated a >70-fold increase in brain:blood ratio of SB-487946 compared to mdr1a/b(+/+) wild-type mice. There was a similar increase in SB-487946 brain:blood ratio in GF120918-treated mice (ca. >67-fold) and rats (ca. 95-fold) but a significantly smaller increase (ca. 10-fold) in guinea pigs treated with GF120918. An appreciable difference was found in the BBB functional effect of P-gp efflux in rodents. GF120918 blood EC90 in mice and rats were similar however, the EC90 in guinea pigs was ca. 10-fold higher, suggesting a species difference in the activity of P-gp at the BBB in some rodents. This study establishes the optimal blood concentrations of GF120918 in relation to SB-487946, to achieve chemically induced P-gp knockout in rodents."xsd:string |
| http://purl.uniprot.org/citations/16850390 | http://purl.org/dc/terms/identifier | "doi:10.1002/jps.20658"xsd:string |
| http://purl.uniprot.org/citations/16850390 | http://purl.uniprot.org/core/author | "Jeffrey P."xsd:string |
| http://purl.uniprot.org/citations/16850390 | http://purl.uniprot.org/core/author | "Buck T.L."xsd:string |
| http://purl.uniprot.org/citations/16850390 | http://purl.uniprot.org/core/author | "Cutler L."xsd:string |
| http://purl.uniprot.org/citations/16850390 | http://purl.uniprot.org/core/author | "Deeks N.J."xsd:string |
| http://purl.uniprot.org/citations/16850390 | http://purl.uniprot.org/core/author | "Howes C."xsd:string |
| http://purl.uniprot.org/citations/16850390 | http://purl.uniprot.org/core/date | "2006"xsd:gYear |
| http://purl.uniprot.org/citations/16850390 | http://purl.uniprot.org/core/name | "J Pharm Sci"xsd:string |
| http://purl.uniprot.org/citations/16850390 | http://purl.uniprot.org/core/pages | "1944-1953"xsd:string |
| http://purl.uniprot.org/citations/16850390 | http://purl.uniprot.org/core/title | "Development of a P-glycoprotein knockout model in rodents to define species differences in its functional effect at the blood-brain barrier."xsd:string |
| http://purl.uniprot.org/citations/16850390 | http://purl.uniprot.org/core/volume | "95"xsd:string |
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