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Determination of in vitro metabolism of new non-imidazole histamine H3 receptor antagonist 1-[3-(4-tert-butylphenoxy)propyl]piperidine

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Kryczyk-Poprawa A., Szafarz M., Palak A. P., Łażewska D., Kuś K., Opoka W., Szymura-Oleksiak J.

Acta Poloniae Pharmaceutica - Drug Research

2019

vol. 76

issue 5

877-884

Early understanding of the pharmacokinetics of drug candidates is essential during the evaluation of drug development process. DL76 1-[3-(4-tert-butylphenoxy)propyl]piperidine is a novel promising non-imidazole H3 receptor antagonist. Presented study was undertaken to compare with each other the predicted hepatic clearance values of DL76 calculated, using two most common mathematical models “well-stirred” and “parallel tube”, based on the data obtained in in vitro experiments. The metabolic intrinsic clearance of DL76 equaled to 0.4848 mL/min/mg protein was scaled up and the values of hepatic clearance estimated from "well-stirred" and "parallel tube" models were 55.47 mL/min/kg and 58.80 mL/min/kg, respectively. They were further compared with pharmacokinetic parameters calculated based on the concentration-time profile obtained following intravenous administration of DL76 to rats at the dose of 6 mg/kg. The estimated systemic serum clearance value of 144.5 mL/h/kg and blood clearance value of 81.17 mL/min/kg indicate the potential extrahepatic metabolism of the investigated compound. This study demonstrates the utility of rat liver microsomes for the prediction of DL76 hepatic clearance.

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1 Acta Poloniae Pharmaceutica - Drug Research

1 2019

1 Kryczyk-Poprawa A.

1 Kuś K.

1 Opoka W.

1 Palak A. P.

1 Szafarz M.

1 Szymura-Oleksiak J.

1 Łażewska D.

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Determination of in vitro metabolism of new non-imidazole histamine H3 receptor antagonist 1-[3-(4-tert-butylphenoxy)propyl]piperidine