Arylmethyloxyphenyl derivatives: small molecules displaying P-glycoprotein inhibition.
Article Details
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Colabufo NA, Berardi F, Perrone R, Rapposelli S, Digiacomo M, Balsamo A
Arylmethyloxyphenyl derivatives: small molecules displaying P-glycoprotein inhibition.
J Med Chem. 2006 Nov 2;49(22):6607-13.
- PubMed ID
- 17064079 [ View in PubMed]
- Abstract
Some arylmethyloxyphenyl derivatives were prepared as simplified structures of analogous arylpiperazines with high affinity toward dopaminergic D(2) and serotonergic 5-HT(1A) receptors and inhibiting P-glycoprotein (P-gp). The compounds 5b and 8b displayed good P-gp inhibition activity measured as [(3)H]vinblastine transport inhibition in the Caco-2 cell monolayer and intracellular doxorubicin accumulation in MCF7/Adr cells by flow cytometry. Compounds 5b and 8b also inhibited, dose-dependently, ATP-ase activation induced by P-gp substrate vinblastine.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Elacridar P-glycoprotein 1 EC 50 (nM) 2000 N/A N/A Details Verapamil P-glycoprotein 1 EC 50 (nM) 20000 N/A N/A Details