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Chemical Compound Review

Elacridar     N-[4-[2-(6,7-dimethoxy-3,4- dihydro-1H...

Synonyms: CHEMBL396298, SureCN536983, GG-918, GW-918, CS-1112, ...
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Disease relevance of Elacridar


High impact information on Elacridar


Anatomical context of Elacridar

  • 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 [7].

Associations of Elacridar with other chemical compounds

  • Brain uptake of drugs after intravenous pretreatment with P-gp reversal agents, (PSC 833, GF 120918, or (+/-)-verapamil), or vehicle also was studied in wild-type mice [8].

Analytical, diagnostic and therapeutic context of Elacridar


  1. HIV-1 viral envelope glycoprotein gp120 triggers an inflammatory response in cultured rat astrocytes and regulates the functional expression of P-glycoprotein. Ronaldson, P.T., Bendayan, R. Mol. Pharmacol. (2006) [Pubmed]
  2. Simultaneous delivery of doxorubicin and GG918 (Elacridar) by new Polymer-Lipid Hybrid Nanoparticles (PLN) for enhanced treatment of multidrug-resistant breast cancer. Wong, H.L., Bendayan, R., Rauth, A.M., Wu, X.Y. Journal of controlled release : official journal of the Controlled Release Society (2006) [Pubmed]
  3. The effect of Bcrp1 (Abcg2) on the in vivo pharmacokinetics and brain penetration of imatinib mesylate (Gleevec): implications for the use of breast cancer resistance protein and P-glycoprotein inhibitors to enable the brain penetration of imatinib in patients. Breedveld, P., Pluim, D., Cipriani, G., Wielinga, P., van Tellingen, O., Schinkel, A.H., Schellens, J.H. Cancer Res. (2005) [Pubmed]
  4. Evaluation of the permeation characteristics of a model opioid peptide, H-Tyr-D-Ala-Gly-Phe-D-Leu-OH (DADLE), and its cyclic prodrugs across the blood-brain barrier using an in situ perfused rat brain model. Chen, W., Yang, J.Z., Andersen, R., Nielsen, L.H., Borchardt, R.T. J. Pharmacol. Exp. Ther. (2002) [Pubmed]
  5. Quantitative analysis of the P-glycoprotein inhibitor Elacridar (GF120918) in human and dog plasma using liquid chromatography with tandem mass spectrometric detection. Stokvis, E., Rosing, H., Causon, R.C., Schellens, J.H., Beijnen, J.H. Journal of mass spectrometry : JMS. (2004) [Pubmed]
  6. Bidirectional transport of rhodamine 123 and Hoechst 33342, fluorescence probes of the binding sites on P-glycoprotein, across MDCK-MDR1 cell monolayers. Tang, F., Ouyang, H., Yang, J.Z., Borchardt, R.T. Journal of pharmaceutical sciences. (2004) [Pubmed]
  7. Development of a P-glycoprotein knockout model in rodents to define species differences in its functional effect at the blood-brain barrier. Cutler, L., Howes, C., Deeks, N.J., Buck, T.L., Jeffrey, P. Journal of pharmaceutical sciences. (2006) [Pubmed]
  8. Screening of multidrug-resistance sensitive drugs by in situ brain perfusion in P-glycoprotein-deficient mice. Cisternino, S., Rousselle, C., Dagenais, C., Scherrmann, J.M. Pharm. Res. (2001) [Pubmed]
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