Preclinical Pharmacokinetics of GZK-111, a Dipeptide with Neuroprotective Activity

We studied the pharmacokinetics of GZK-111 (N-phenylacetyl-glycyl-L-proline ethyl ether), a compound with neuroprotective activity, and its metabolite CPG (cyclo-L-prolylglycine) in rat blood plasma after single intravenous and intragastric administration in a dose of 20 mg/kg. It was found that the...

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Published inBulletin of experimental biology and medicine Vol. 172; no. 3; pp. 310 - 313
Main Authors Litvin, A. A., Kolyvanov, G. B., Bochkov, P. O., Shevchenko, R. V., Podol’ko, A. L., Kolyasnikova, K. N., Zherdev, V. P.
Format Journal Article
LanguageEnglish
Published New York Springer US 2022
Springer
Springer Nature B.V
Subjects
Animal experimentation
Animals
Biomedical and Life Sciences
Biomedicine
Biotransformation
Cell Biology
Dipeptides - chemistry
Internal Medicine
Intravenous administration
L-Proline
Laboratory Medicine
Metabolites
Neuroprotection
Pathology
Pharmacokinetics
Pharmacology and Toxicology
Proline
Rats
GZK-111
pharmacokinetics
HPLCmass spectrometry
cyclo-L-prolylglycine
neuroprotector
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Summary:We studied the pharmacokinetics of GZK-111 (N-phenylacetyl-glycyl-L-proline ethyl ether), a compound with neuroprotective activity, and its metabolite CPG (cyclo-L-prolylglycine) in rat blood plasma after single intravenous and intragastric administration in a dose of 20 mg/kg. It was found that the parent drug undergoes intensive biotransformation; its metabolite CPG persists in the circulation more than twice as long as GZK-111 and its plasma concentrations were higher by 50-70 times than the concentrations of the parent compound.
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ISSN:0007-4888
1573-8221
DOI:10.1007/s10517-022-05400-x