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Sökning: onr:"swepub:oai:DiVA.org:uu-222384" > Cytochrome P450 Inh...

LIBRIS Formathandbok  (Information om MARC21)
FältnamnIndikatorerMetadata
00003447naa a2200385 4500
001oai:DiVA.org:uu-222384
003SwePub
008140410s2014 | |||||||||||000 ||eng|
009oai:prod.swepub.kib.ki.se:128378716
0247 a https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-2223842 URI
0247 a https://doi.org/10.1124/dmd.113.0549322 DOI
0247 a http://kipublications.ki.se/Default.aspx?queryparsed=id:1283787162 URI
040 a (SwePub)uud (SwePub)ki
041 a engb eng
042 9 SwePub
072 7a ref2 swepub-contenttype
072 7a art2 swepub-publicationtype
1001 a Englund, Gunilla4 aut
2451 0a Cytochrome P450 Inhibitory Properties of Common Efflux Transporter Inhibitors
264 c 2014-01-06
264 1b American Society for Pharmacology & Experimental Therapeutics (ASPET),c 2014
338 a print2 rdacarrier
520 a Drug transporter inhibitors are important tools to elucidate the contribution of transporters to drug disposition both in vitro and in vivo. These inhibitors are often unselective and affect several transporters as well as drug metabolizing enzymes, which can make experimental results difficult to interpret with confidence. We therefore tested 14 commonly used P-glycoprotein (P-gp), breast cancer resistance protein (BCRP), and multidrug-resistance associated protein (MRP) inhibitors as inhibitors of cytochrome P450 (P450) enzyme activities using recombinant enzymes. A subset of P-gp and/or CYP3A inhibitors were selected (cyclosporin A, elacridar, ketoconazole, quinidine, reserpine, and tacrolimus) for a comparison of P450 inhibition in human microsomes and hepatocytes. Most P-gp inhibitors showed CYP3A4 inhibition, with potencies often in a similar range as their P-gp inhibition, as well as less potent CYP2C19 inhibition. Other P450 enzymes were not strongly inhibited except a few cases of CYP2D6 inhibition. MRP and BCRP inhibitors showed limited P450 inhibition. Some inhibitors showed less P450 inhibition in human hepatocytes than human liver microsomes, for example, elacridar, probably due to differences in binding, permeability limitations, or active, P-gp mediated efflux of the inhibitor from the hepatocytes. Quinidine was a potent P450 inhibitor in hepatocytes but only showed weak inhibition in microsomes. Quinidine shows an extensive cellular uptake, which may potentiate intracellular P450 inhibition. Elacridar, described as a potent and selective P-gp inhibitor, displayed modest P450 inhibition in this study and is thus a useful model inhibitor to define the role of P-gp in drug disposition without interference with other processes.
7001 a Lundquist, Patriku Uppsala universitet,Institutionen för farmaci4 aut0 (Swepub:uu)patlu774
7001 a Skogastierna, Cristine4 aut
7001 a Johansson, Jenny4 aut
7001 a Hoogstraate, Janet4 aut
7001 a Afzelius, Lovisa4 aut
7001 a Andersson, Tommy B.4 aut
7001 a Projean, Denis4 aut
7102 a Uppsala universitetb Institutionen för farmaci4 org
7730 t Drug Metabolism And Dispositiond : American Society for Pharmacology & Experimental Therapeutics (ASPET)g 42:3, s. 441-447q 42:3<441-447x 0090-9556x 1521-009X
8564 8u https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-222384
8564 8u https://doi.org/10.1124/dmd.113.054932
8564 8u http://kipublications.ki.se/Default.aspx?queryparsed=id:128378716

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