Sökning: WFRF:(Lundquist Patrik) > Cytochrome P450 Inh...
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000 | 03447naa a2200385 4500 | |
001 | oai:DiVA.org:uu-222384 | |
003 | SwePub | |
008 | 140410s2014 | |||||||||||000 ||eng| | |
009 | oai:prod.swepub.kib.ki.se:128378716 | |
024 | 7 | a https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-2223842 URI |
024 | 7 | a https://doi.org/10.1124/dmd.113.0549322 DOI |
024 | 7 | 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 | 7 | a ref2 swepub-contenttype |
072 | 7 | a art2 swepub-publicationtype |
100 | 1 | a Englund, Gunilla4 aut |
245 | 1 0 | a Cytochrome P450 Inhibitory Properties of Common Efflux Transporter Inhibitors |
264 | c 2014-01-06 | |
264 | 1 | b 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. | |
700 | 1 | a Lundquist, Patriku Uppsala universitet,Institutionen för farmaci4 aut0 (Swepub:uu)patlu774 |
700 | 1 | a Skogastierna, Cristine4 aut |
700 | 1 | a Johansson, Jenny4 aut |
700 | 1 | a Hoogstraate, Janet4 aut |
700 | 1 | a Afzelius, Lovisa4 aut |
700 | 1 | a Andersson, Tommy B.4 aut |
700 | 1 | a Projean, Denis4 aut |
710 | 2 | a Uppsala universitetb Institutionen för farmaci4 org |
773 | 0 | 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 |
856 | 4 8 | u https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-222384 |
856 | 4 8 | u https://doi.org/10.1124/dmd.113.054932 |
856 | 4 8 | u http://kipublications.ki.se/Default.aspx?queryparsed=id:128378716 |
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