Pub. Date : 2012 Dec
PMID : 22975888
6 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Respiratory toxicity of buprenorphine results from the blockage of P-glycoprotein-mediated efflux of norbuprenorphine at the blood-brain barrier in mice. | Buprenorphine | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 2 | Recently, norbuprenorphine, in contrast to buprenorphine, was shown in vitro to be a substrate of human P-glycoprotein, a drug-transporter involved in all steps of pharmacokinetics including transport at the blood-brain barrier. | Buprenorphine | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 3 | Our objectives were to assess P-glycoprotein involvement in norbuprenorphine transport in vivo and study its role in the modulation of buprenorphine-related respiratory effects in mice. | Buprenorphine | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 4 | In P-glycoprotein-knockout mice, buprenorphine-related effects on VE (p < .01), TE (p < .001), and TI (p < .05) and norbuprenorphine-related effects on VE (p < .05) and TI (p < .001) were significantly enhanced. | Buprenorphine | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 5 | CONCLUSIONS: P-glycoprotein plays a key-protective role in buprenorphine-related respiratory effects, by allowing norbuprenorphine efflux at the blood-brain barrier. | Buprenorphine | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 6 | Our findings suggest a major role for drug-drug interactions that lead to P-glycoprotein inhibition in buprenorphine-associated fatalities and respiratory depression. | Buprenorphine | ATP binding cassette subfamily B member 1 | Homo sapiens |