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N-(3,4-dimethoxyphenethyl)-4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2[1H]-yl)-6,7-dimethoxyquinazolin-2-amine (CP-100,356) as a "chemical knock-out equivalent" to assess the impact of efflux transporters on oral drug absorption in the rat.
Kalgutkar AS, Frederick KS, Chupka J, Feng B, Kempshall S, Mireles RJ, Fenner KS, Troutman MD. Kalgutkar AS, et al. Among authors: mireles rj. J Pharm Sci. 2009 Dec;98(12):4914-27. doi: 10.1002/jps.21756. J Pharm Sci. 2009. PMID: 19373887
Role of transporters in the disposition of the selective phosphodiesterase-4 inhibitor (+)-2-[4-({[2-(benzo[1,3]dioxol-5-yloxy)-pyridine-3-carbonyl]-amino}-methyl)-3-fluoro-phenoxy]-propionic acid in rat and human.
Kalgutkar AS, Feng B, Nguyen HT, Frederick KS, Campbell SD, Hatch HL, Bi YA, Kazolias DC, Davidson RE, Mireles RJ, Duignan DB, Choo EF, Zhao SX. Kalgutkar AS, et al. Among authors: mireles rj. Drug Metab Dispos. 2007 Nov;35(11):2111-8. doi: 10.1124/dmd.107.016162. Epub 2007 Aug 8. Drug Metab Dispos. 2007. PMID: 17686907