Pub. Date : 2014 Feb 3
PMID : 24364805
4 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Using positron emission tomography (PET), (11)C-verapamil as the P-gp substrate, and cyclosporine A (CsA) as the P-gp inhibitor, we showed that the magnitude of P-gp-based drug interactions at the human blood-brain barrier (BBB) is modest. | Cyclosporine | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 2 | Using positron emission tomography (PET), (11)C-verapamil as the P-gp substrate, and cyclosporine A (CsA) as the P-gp inhibitor, we showed that the magnitude of P-gp-based drug interactions at the human blood-brain barrier (BBB) is modest. | Cyclosporine | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 3 | However, such interactions at clinically relevant CsA blood concentrations may be greater for substrates where P-gp plays an even larger role (fractional contribution of P-gp, ft > 0.97) in preventing the CNS entry of the drug (e.g., nelfinavir). | Cyclosporine | ATP binding cassette subfamily B member 1 | Homo sapiens |
| 4 | Then, using these data, as well as in vitro data in LLCPK1 cells expressing the human P-gp, we predicted that CsA (at clinically relevant blood concentration of 1.5 muM) will increase the distribution of nelfinavir into the human brain by 236%. | Cyclosporine | ATP binding cassette subfamily B member 1 | Homo sapiens |