PMID: 20645922Jul 22, 2010Paper

Substrates, inhibitors and activators of P-glycoprotein: candidates for radiolabeling and imaging perspectives

Current Topics in Medicinal Chemistry
Nicola Antonio ColabufoRoberto Perrone

Abstract

In recent years, several PET tracers for monitoring the activity and expression of P-gp at the BBB have been tested. P-gp substrates such as [(11)C]verapamil and [(11)C]loperamide can be employed to visualize P-gp activity, but they display a moderate baseline uptake in the brain and formation of radiolabeled metabolites which hamper the interpretation of PET data. P-gp inhibitors such as [(11)C]elacridar, [(11)C]laniquidar and [(11)C]tariquidar have been tested to investigate P-gp expression and the results need further investigation. Recently, we developed MC18, MC266 and MC80, that have been characterized as an inhibitor, substrate and inducer of P-gp both by in vitro assays and in the everted gut sac method. These compounds have been radiolabelled with (11)C and been evaluated in vivo. In the present review, we compare the outcome of biological in vitro assays and the corresponding in vivo PET data for the P-gp inhibitors [(11)C]MC18 and [(11)C]elacridar, the P-gp substrates [(11)C]MC266 and [(11)C]verapamil, the P-gp inducer [(11)C]MC80 and the P-gp modulator cyclosporin A. Since a satisfactory overlap was found comparing in vivo results and the corresponding in vitro findings, the proposed biological in vitro assays could...Continue Reading

Citations

Apr 2, 2013·Journal of Biological Inorganic Chemistry : JBIC : a Publication of the Society of Biological Inorganic Chemistry·Cristina BolzatiNicola Antonio Colabufo
Dec 14, 2012·Journal of Pharmacological and Toxicological Methods·Maria Grazia PerroneNicola Antonio Colabufo
Nov 26, 2015·Journal of Clinical Pharmacy and Therapeutics·Z R TanL S Wang
Aug 18, 2012·Nuclear Medicine and Biology·Xiaofeng BaoVictor W Pike
Nov 29, 2011·Drug Discovery Today·Lei ChenTingjun Hou
May 3, 2014·The International Journal of Biochemistry & Cell Biology·Jun-Feng ShiYu-Jie Sun
Sep 14, 2016·Expert Opinion on Therapeutic Patents·Inder Pal Singh, Purvi Shah
Apr 12, 2017·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Mariline GameiroFernando Remião
Feb 12, 2015·Clinical Pharmacology and Therapeutics·R M RaaphorstG Luurtsema
May 14, 2019·Expert Opinion on Therapeutic Patents·Marcello LeopoldoNicola Antonio Colabufo
Nov 26, 2011·Expert Review of Clinical Pharmacology·Andrea OrthmannReiner Zeisig
Dec 1, 2017·Current Medicinal Chemistry·Santiago VilarEugenio Uriarte
May 3, 2016·ChemMedChem·Maria Grazia PerroneAntonio Scilimati
Jan 7, 2021·Daru : Journal of Faculty of Pharmacy, Tehran University of Medical Sciences·Noor Safwah DamanhuriAhmad Hasnan Mansor
Oct 21, 2016·Physiological Research·M HrubýP Štěpánek

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