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Imaging techniques to study drug transporter function in vivo.
Tournier N, Stieger B, Langer O. Tournier N, et al. Pharmacol Ther. 2018 Sep;189:104-122. doi: 10.1016/j.pharmthera.2018.04.006. Epub 2018 Apr 22. Pharmacol Ther. 2018. PMID: 29684469 Free article. Review.
We conclude that despite certain methodological limitations, imaging has a great potential to study transporters at work in humans and that imaging will become an important tool, not only in drug development but also in medicine. Imaging
We conclude that despite certain methodological limitations, imaging has a great potential to study transporters at wor …
Imaging Probes and Modalities for the Study of Solute Carrier O (SLCO)-Transport Function In Vivo.
Marie S, Cisternino S, Buvat I, Declèves X, Tournier N. Marie S, et al. Among authors: tournier n. J Pharm Sci. 2017 Sep;106(9):2335-2344. doi: 10.1016/j.xphs.2017.04.031. Epub 2017 Apr 25. J Pharm Sci. 2017. PMID: 28454744 Review.
Transporters of the solute carrier O (SLCO) family, former organic anion-transporting polypeptides, are now recognized as key players in pharmacokinetics. ...All these approaches rely on the use of SLCO substrates that are detected using corresponding modalities. Th
Transporters of the solute carrier O (SLCO) family, former organic anion-transporting polypeptides, are now recognized as key
[PET imaging to study the functional impact of P-glycoprotein in neuropharmacokinetics].
Marie S, Tournier N. Marie S, et al. Among authors: tournier n. Therapie. 2020 Nov-Dec;75(6):623-632. doi: 10.1016/j.therap.2020.02.018. Epub 2020 Feb 22. Therapie. 2020. PMID: 32200996 French.
Positron emission tomography (PET) is an imaging technique allowing for the determination of the tissue kinetics of microdose of radiolabeled compounds. ...This approach is also useful to predict the risk for drug-drug interaction caused by P-gp inhibi …
Positron emission tomography (PET) is an imaging technique allowing for the determination of the tissue kinetics of microdose …
Imaging the impact of cyclosporin A and dipyridamole on P-glycoprotein (ABCB1) function at the blood-brain barrier: A [(11)C]-N-desmethyl-loperamide PET study in nonhuman primates.
Damont A, Goutal S, Auvity S, Valette H, Kuhnast B, Saba W, Tournier N. Damont A, et al. Among authors: tournier n. Eur J Pharm Sci. 2016 Aug 25;91:98-104. doi: 10.1016/j.ejps.2016.06.005. Epub 2016 Jun 7. Eur J Pharm Sci. 2016. PMID: 27283486
Injection of pharmacologic dose of DPy did not enhance [(11)C]dLop brain distribution with AUCR being 1.2, 0.9 and 1.1 after administration of 0.56, 0.96 and 2mg/kg DPy doses, respectively. We used [(11)C]dLop PET imaging in baboons, a relevant in vivo model of P-gp …
Injection of pharmacologic dose of DPy did not enhance [(11)C]dLop brain distribution with AUCR being 1.2, 0.9 and 1.1 after administration …
Imaging the neuroimmune response to alcohol exposure in adolescent baboons: a TSPO PET study using (18) F-DPA-714.
Saba W, Goutal S, Auvity S, Kuhnast B, Coulon C, Kouyoumdjian V, Buvat I, Leroy C, Tournier N. Saba W, et al. Among authors: tournier n. Addict Biol. 2018 Sep;23(5):1000-1009. doi: 10.1111/adb.12548. Epub 2017 Sep 25. Addict Biol. 2018. PMID: 28944558
The brain distribution of (18) F-DPA-714 (V(T) ; in ml/cm(3) ) was estimated in several brain regions using the Logan plot analysis and the metabolite-corrected arterial input function. Compared with alcohol-naive animals (V(Tbrain) = 3.7 0.7 ml/cm(3) ), the regional V(T) …
The brain distribution of (18) F-DPA-714 (V(T) ; in ml/cm(3) ) was estimated in several brain regions using the Logan plot analysis and the …
Diphenhydramine as a selective probe to study H(+)-antiporter function at the blood-brain barrier: Application to [(11)C]diphenhydramine positron emission tomography imaging.
Auvity S, Chapy H, Goutal S, Caillé F, Hosten B, Smirnova M, Declèves X, Tournier N, Cisternino S. Auvity S, et al. Among authors: tournier n. J Cereb Blood Flow Metab. 2017 Jun;37(6):2185-2195. doi: 10.1177/0271678X16662042. Epub 2016 Jan 1. J Cereb Blood Flow Metab. 2017. PMID: 27488910 Free PMC article.
Diphenhydramine, a sedative histamine H(1)-receptor (H(1)R) antagonist, was evaluated as a probe to measure drug/H(+)-antiporter function at the blood-brain barrier. In situ brain perfusion experiments in mice and rats showed that diphenhydramine transport at …
Diphenhydramine, a sedative histamine H(1)-receptor (H(1)R) antagonist, was evaluated as a probe to measure drug/H(+)-antiporter f
Strategies to Inhibit ABCB1- and ABCG2-Mediated Efflux Transport of Erlotinib at the Blood-Brain Barrier: A PET Study on Nonhuman Primates.
Tournier N, Goutal S, Auvity S, Traxl A, Mairinger S, Wanek T, Helal OB, Buvat I, Soussan M, Caillé F, Langer O. Tournier N, et al. J Nucl Med. 2017 Jan;58(1):117-122. doi: 10.2967/jnumed.116.178665. Epub 2016 Aug 4. J Nucl Med. 2017. PMID: 27493269 Free article.
The tyrosine kinase inhibitor erlotinib poorly penetrates the blood-brain barrier (BBB) because of efflux transport by P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2), thereby limiting its utility in the treatment of non-small cell lung cancer metastase …
The tyrosine kinase inhibitor erlotinib poorly penetrates the blood-brain barrier (BBB) because of efflux transport by P-glycoprotein …
Inhibition of ABCB1 and ABCG2 at the Mouse Blood-Brain Barrier with Marketed Drugs To Improve Brain Delivery of the Model ABCB1/ABCG2 Substrate [11C]erlotinib.
Traxl A, Mairinger S, Filip T, Sauberer M, Stanek J, Poschner S, Jäger W, Zoufal V, Novarino G, Tournier N, Bauer M, Wanek T, Langer O. Traxl A, et al. Among authors: tournier n. Mol Pharm. 2019 Mar 4;16(3):1282-1293. doi: 10.1021/acs.molpharmaceut.8b01217. Epub 2019 Feb 11. Mol Pharm. 2019. PMID: 30694684
There is a crucial need for pharmacological ABCB1 and ABCG2 inhibition protocols for a more effective treatment of brain diseases. In the present study, seven marketed drugs (osimertinib, erlotinib, nilotinib, imatinib, lapatinib, pazopanib, and cyclosporine A) and one non …
There is a crucial need for pharmacological ABCB1 and ABCG2 inhibition protocols for a more effective treatment of brain diseases. In the pr …