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The ABC membrane transporter ABCG2 prevents access of FAAH inhibitor URB937 to the central nervous system.

Moreno-Sanz G, Barrera B, Guijarro A, d'Elia I, Otero JA, Alvarez AI, Bandiera T, Merino G, Piomelli D.

Pharmacol Res. 2011 Oct;64(4):359-63. doi: 10.1016/j.phrs.2011.07.001. Epub 2011 Jul 7.


Structural determinants of peripheral O-arylcarbamate FAAH inhibitors render them dual substrates for Abcb1 and Abcg2 and restrict their access to the brain.

Moreno-Sanz G, Barrera B, Armirotti A, Bertozzi SM, Scarpelli R, Bandiera T, Prieto JG, Duranti A, Tarzia G, Merino G, Piomelli D.

Pharmacol Res. 2014 Sep;87:87-93. doi: 10.1016/j.phrs.2014.06.004. Epub 2014 Jun 30.


Pharmacological characterization of the peripheral FAAH inhibitor URB937 in female rodents: interaction with the Abcg2 transporter in the blood-placenta barrier.

Moreno-Sanz G, Sasso O, Guijarro A, Oluyemi O, Bertorelli R, Reggiani A, Piomelli D.

Br J Pharmacol. 2012 Dec;167(8):1620-8. doi: 10.1111/j.1476-5381.2012.02098.x.


Peripheral FAAH inhibition causes profound antinociception and protects against indomethacin-induced gastric lesions.

Sasso O, Bertorelli R, Bandiera T, Scarpelli R, Colombano G, Armirotti A, Moreno-Sanz G, Reggiani A, Piomelli D.

Pharmacol Res. 2012 May;65(5):553-63. doi: 10.1016/j.phrs.2012.02.012. Epub 2012 Mar 7.


Dinaciclib, a cyclin-dependent kinase inhibitor, is a substrate of human ABCB1 and ABCG2 and an inhibitor of human ABCC1 in vitro.

Cihalova D, Ceckova M, Kucera R, Klimes J, Staud F.

Biochem Pharmacol. 2015 Dec 1;98(3):465-72. doi: 10.1016/j.bcp.2015.08.099. Epub 2015 Aug 20.


ABC transporter (P-gp/ABCB1, MRP1/ABCC1, BCRP/ABCG2) expression in the developing human CNS.

Daood M, Tsai C, Ahdab-Barmada M, Watchko JF.

Neuropediatrics. 2008 Aug;39(4):211-8. doi: 10.1055/s-0028-1103272. Epub 2009 Jan 22.


Breast cancer resistance protein (BCRP/ABCG2) and P-glycoprotein (P-GP/ABCB1) restrict oral availability and brain accumulation of the PARP inhibitor rucaparib (AG-014699).

Durmus S, Sparidans RW, van Esch A, Wagenaar E, Beijnen JH, Schinkel AH.

Pharm Res. 2015 Jan;32(1):37-46. doi: 10.1007/s11095-014-1442-z. Epub 2014 Jun 25.


Synthesis and structure-activity relationship studies of O-biphenyl-3-yl carbamates as peripherally restricted fatty acid amide hydrolase inhibitors.

Moreno-Sanz G, Duranti A, Melzig L, Fiorelli C, Ruda GF, Colombano G, Mestichelli P, Sanchini S, Tontini A, Mor M, Bandiera T, Scarpelli R, Tarzia G, Piomelli D.

J Med Chem. 2013 Jul 25;56(14):5917-30. doi: 10.1021/jm4007017. Epub 2013 Jul 3.


The gut microbiota ellagic acid-derived metabolite urolithin A and its sulfate conjugate are substrates for the drug efflux transporter breast cancer resistance protein (ABCG2/BCRP).

González-Sarrías A, Miguel V, Merino G, Lucas R, Morales JC, Tomás-Barberán F, Alvarez AI, Espín JC.

J Agric Food Chem. 2013 May 8;61(18):4352-9. doi: 10.1021/jf4007505. Epub 2013 Apr 24.


Brain and Testis Accumulation of Regorafenib is Restricted by Breast Cancer Resistance Protein (BCRP/ABCG2) and P-glycoprotein (P-GP/ABCB1).

Kort A, Durmus S, Sparidans RW, Wagenaar E, Beijnen JH, Schinkel AH.

Pharm Res. 2015 Jul;32(7):2205-16. doi: 10.1007/s11095-014-1609-7. Epub 2015 Jan 8.


Anandamide suppresses pain initiation through a peripheral endocannabinoid mechanism.

Clapper JR, Moreno-Sanz G, Russo R, Guijarro A, Vacondio F, Duranti A, Tontini A, Sanchini S, Sciolino NR, Spradley JM, Hohmann AG, Calignano A, Mor M, Tarzia G, Piomelli D.

Nat Neurosci. 2010 Oct;13(10):1265-70. doi: 10.1038/nn.2632. Epub 2010 Sep 19.


In vitro and in vivo evidence for the importance of breast cancer resistance protein transporters (BCRP/MXR/ABCP/ABCG2).

Meyer zu Schwabedissen HE, Kroemer HK.

Handb Exp Pharmacol. 2011;(201):325-71. doi: 10.1007/978-3-642-14541-4_9. Review.


Novel understanding of ABC transporters ABCB1/MDR/P-glycoprotein, ABCC2/MRP2, and ABCG2/BCRP in colorectal pathophysiology.

Andersen V, Svenningsen K, Knudsen LA, Hansen AK, Holmskov U, Stensballe A, Vogel U.

World J Gastroenterol. 2015 Nov 7;21(41):11862-76. doi: 10.3748/wjg.v21.i41.11862.


Increased oral availability and brain accumulation of the ALK inhibitor crizotinib by coadministration of the P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) inhibitor elacridar.

Tang SC, Nguyen LN, Sparidans RW, Wagenaar E, Beijnen JH, Schinkel AH.

Int J Cancer. 2014 Mar 15;134(6):1484-94. doi: 10.1002/ijc.28475. Epub 2013 Oct 3.


URB937, a peripherally restricted inhibitor for fatty acid amide hydrolase, reduces prostaglandin E2 -induced bladder overactivity and hyperactivity of bladder mechano-afferent nerve fibres in rats.

Aizawa N, Gandaglia G, Hedlund P, Fujimura T, Fukuhara H, Montorsi F, Homma Y, Igawa Y.

BJU Int. 2016 May;117(5):821-8. doi: 10.1111/bju.13223. Epub 2015 Aug 19.


Stereoselective interaction of pantoprazole with ABCG2. II. In vitro flux analysis.

Wang L, Leggas M, Empey PE, McNamara PJ.

Drug Metab Dispos. 2012 May;40(5):1024-31. doi: 10.1124/dmd.111.041616. Epub 2012 Feb 21.


"Effect of the drug transporters ABCB1, ABCC2, and ABCG2 on the disposition and brain accumulation of the taxane analog BMS-275,183".

Marchetti S, Pluim D, Beijnen JH, Mazzanti R, van Tellingen O, Schellens JH.

Invest New Drugs. 2014 Dec;32(6):1083-95. doi: 10.1007/s10637-014-0143-0. Epub 2014 Jul 31.


Impact of P-glycoprotein (ABCB1) and breast cancer resistance protein (ABCG2) on the brain distribution of a novel BRAF inhibitor: vemurafenib (PLX4032).

Mittapalli RK, Vaidhyanathan S, Sane R, Elmquist WF.

J Pharmacol Exp Ther. 2012 Jul;342(1):33-40. doi: 10.1124/jpet.112.192195. Epub 2012 Mar 27.

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