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Pharmacokinetics of a New Neuroprotector — Indenoquinoxalinone Derivative after Intravenous Administration in Rabbits and Rats

  • PHARMACOLOGY AND TOXICOLOGY
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Bulletin of Experimental Biology and Medicine Aims and scope

The specific JNK inhibitor and NO donor 11H-indeno[1,2-b]quinoxalin-11-one oxime (IQ-1) demonstrated pronounced neuroprotective properties in an in vivo model of ischemic stroke in rats. The pharmacokinetic behavior of IQ-1 was studied in two animal species (rats, rabbits) after intravenous administration in a dose of 1 mg/kg. IQ-1 concentrations in venous blood plasma were measured by the liquid chromatography—tandem mass spectrometry method. The pharmacokinetics of IQ-1 was adequately described by the two-compartmental model. The calculated C0 for IQ-1 in rabbit and rat plasma were 2239.83±1229.55 and 1552.50±182.23 ng/ml, respectively. Two animal species are characterized by extensive tissue distribution of IQ-1 (Vss exceeded the total body water in rabbits and rats by 3.6 and 5.6 times, respectively) and high clearance values (88-94% of hepatic blood flow).

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Authors and Affiliations

  1. E. D. Goldberg Research Institute of Pharmacology and Regenerative Medicine, Tomsk National Research Medical Center, Russian Academy of Sciences, Tomsk, Russia

    E. A. Yanovskaya, G. A. Frelikh, A. P. Lakeev, G. A. Chernysheva & V. I. Smol’yakova

  2. National Research Tomsk Polytechnic University, Tomsk, Russia

    A. R. Kovrizhina

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  1. E. A. Yanovskaya
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  2. G. A. Frelikh
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  3. A. P. Lakeev
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  4. G. A. Chernysheva
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  5. V. I. Smol’yakova
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  6. A. R. Kovrizhina
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Corresponding author

Correspondence to E. A. Yanovskaya.

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Translated from Byulleten’ Eksperimental’noi Biologii i Meditsiny, Vol. 175, No. 6, pp. 725-729, June, 2023

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Yanovskaya, E.A., Frelikh, G.A., Lakeev, A.P. et al. Pharmacokinetics of a New Neuroprotector — Indenoquinoxalinone Derivative after Intravenous Administration in Rabbits and Rats. Bull Exp Biol Med 175, 770–773 (2023). https://doi.org/10.1007/s10517-023-05943-7

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  • DOI: https://doi.org/10.1007/s10517-023-05943-7

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