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2 protocols using eletriptan

1

Evaluation of P-gp Substrate Compounds

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Radiolabelled [14C]- or [3H]-mannitol and the P-gp substrate [3H]-digoxin were purchased from American RadioChemicals (St. Louis, MO). The P-gp substrates GSK-1,-2 and −3, and indacaterol were supplied by GlaxoSmithKline (Stevenage, UK). Unlabelled P-gp substrates also contributing to the test panel of compounds included: acrivastine, erythromycin, mitoxantrone, monensin, puromycin, saquinavir, chloroquine, colchicine, domperidone, eletriptan, rhodamine-123 (Rh-123), salbutamol and salmeterol, all obtained from Sigma Aldrich (Poole, UK). All other chemicals and solvents were obtained from Sigma-Aldrich or Fisher Scientific at the highest available purities.
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2

Liver Microsome Preparation and Characterization

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Midazolam, rizatriptan, phenylephrine and sertraline were purchased from Wako Pure Chemical Industries (Osaka, Japan). Sumatriptan and S-citalopram were purchased from Tokyo Chemical Industry (Tokyo, Japan). Imipramine was purchased from Nakalai Tesque (Kyoto, Japan). Eletriptan and fatty acid-free human serum albumin (HSA) were obtained from Sigma-Aldrich (St. Louis, MO). All other chemicals and reagents were analytical-grade products from commercial sources. Pooled HLMs (50 donors, #PLo50BA), CD-1 mouse liver microsomes, SD rat liver microsomes and beagle dog liver microsomes were purchased from Thermo Fisher Scientific (Waltham, MA). Pooled HLMt (5 donors, #1110152) was purchased from Sekisui XenoTech.
(Kansas City, KS). An MAO expression system (Supersomes: MAO-A, MAO-B and control) was purchased from Corning (Corning, NY). Individual HLMs and HLMt were prepared according to the previously reported method (13) . Human liver blocks were obtained from Human and Animal Bridging Research Organization (Chiba, Japan). The study protocol was approved by the ethical committees of the School of Medicine in Kanazawa University. Individual HLMs and HLMt were independently prepared to prevent loss derived from sequential purification.
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