Pub. Date : 2003 May
PMID : 12751631
9 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Midazolam exhibits characteristics of a highly permeable P-glycoprotein substrate. | Midazolam | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 2 | PURPOSE: The purpose of this study was to investigate whether midazolam exhibits characteristics of a highly permeable P-glycoprotein (P-gp) substrate and to evaluate the potential influence of P-gp inhibition on 1-OH midazolam formation during midazolam transport. | Midazolam | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 3 | PURPOSE: The purpose of this study was to investigate whether midazolam exhibits characteristics of a highly permeable P-glycoprotein (P-gp) substrate and to evaluate the potential influence of P-gp inhibition on 1-OH midazolam formation during midazolam transport. | Midazolam | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 4 | METHODS: P-gp interaction was investigated by P-gp ATPase assay, efflux inhibition studies, and transport studies of midazolam across MDR1-MDCK and 1-alpha,25-dihydroxy vitamin D3-induced Caco-2 monolayers with and without the P-gp inhibitor GF120918. | Midazolam | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 5 | METHODS: P-gp interaction was investigated by P-gp ATPase assay, efflux inhibition studies, and transport studies of midazolam across MDR1-MDCK and 1-alpha,25-dihydroxy vitamin D3-induced Caco-2 monolayers with and without the P-gp inhibitor GF120918. | Midazolam | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 6 | P-gp ATPase activation by midazolam was dose-dependent and saturable [Km = 11.5(+/- 4.0) microM; Vmax = 41.1(+/- 7.4) nmol/mg/min]. | Midazolam | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 7 | P-gp inhibition increased 1-OH midazolam formation in A-to-B studies 1.3-fold when midazolam donor > or = 10 microM (p < 0.03). | Midazolam | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 8 | CONCLUSION: The results indicate that midazolam exhibited characteristics of a highly permeable P-gp substrate. | Midazolam | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 9 | 1-OH midazolam formation during A-to-B midazolam transport increased slightly when P-gp was inhibited. | Midazolam | ATP binding cassette subfamily B member 1 | Homo sapiens |