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Permeability of the Blood-Brain Barrier for Dilept and Its Active Metabolite
Experiments on rats with measurements by HPLC-MS/MS showed that antipsychotic preparation dilept (N-caproyl-L-prolyl-L-tyrosine methyl ester) administered per os in doses of 40 and 200 mg/kg crossed the blood-brain barrier and was detected in rat brain (unchanged drug and its active metabolite N-cap...
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| Published in: | Bulletin of experimental biology and medicine 2011-07, Vol.151 (3), p.330-332 |
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| container_end_page | 332 |
| container_issue | 3 |
| container_start_page | 330 |
| container_title | Bulletin of experimental biology and medicine |
| container_volume | 151 |
| creator | Zherdev, V. P. Boyko, S. S. Mesonzhnik, N. V. Bastrygin, D. V. |
| description | Experiments on rats with measurements by HPLC-MS/MS showed that antipsychotic preparation dilept (N-caproyl-L-prolyl-L-tyrosine methyl ester) administered
per os
in doses of 40 and 200 mg/kg crossed the blood-brain barrier and was detected in rat brain (unchanged drug and its active metabolite N-caproyl-L-prolyl-L-tyrosine). The brain/plasma distribution coefficient for dilept was 2.0, for metabolite 0.5. No dose-concentration relationship was found, presumably because of the high dose of the drug transported from the blood to the brain not only by free diffusion, but also with participation of active carriers, whose number was limited. |
| doi_str_mv | 10.1007/s10517-011-1322-z |
| format | article |
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per os
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per os
in doses of 40 and 200 mg/kg crossed the blood-brain barrier and was detected in rat brain (unchanged drug and its active metabolite N-caproyl-L-prolyl-L-tyrosine). The brain/plasma distribution coefficient for dilept was 2.0, for metabolite 0.5. No dose-concentration relationship was found, presumably because of the high dose of the drug transported from the blood to the brain not only by free diffusion, but also with participation of active carriers, whose number was limited.</description><subject>Animals</subject><subject>Antipsychotic Agents - metabolism</subject><subject>Antipsychotic Agents - pharmacokinetics</subject><subject>Biological Transport</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedicine</subject><subject>Blood-brain barrier</subject><subject>Blood-Brain Barrier - drug effects</subject><subject>Blood-Brain Barrier - metabolism</subject><subject>Brain</subject><subject>Brain - blood supply</subject><subject>Brain - metabolism</subject><subject>Cell Biology</subject><subject>Chromatography, High Pressure Liquid</subject><subject>Diffusion</subject><subject>Drugs</subject><subject>Internal Medicine</subject><subject>Laboratory Medicine</subject><subject>Male</subject><subject>Membrane permeability</subject><subject>Metabolites</subject><subject>Neuroleptics</subject><subject>Pathology</subject><subject>Peptides</subject><subject>Permeability</subject><subject>Pharmacology and Toxicology</subject><subject>Proline - analogs & derivatives</subject><subject>Proline - metabolism</subject><subject>Proline - pharmacokinetics</subject><subject>Rats</subject><subject>Tandem Mass Spectrometry</subject><subject>Tyrosine - analogs & derivatives</subject><subject>Tyrosine - metabolism</subject><subject>Tyrosine - pharmacokinetics</subject><issn>0007-4888</issn><issn>1573-8221</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2011</creationdate><recordtype>article</recordtype><recordid>eNp9kktv1DAUhS0EokPhB7BBFkiUTYofcewsZ_qglQbBAtaW49x0XCXxYDtI7a_HUcqjFSDLsq78nSOdq4PQS0qOKSHyfaREUFkQSgvKGStuH6EVFZIXijH6GK1IhopSKXWAnsV4PY-kok_RAWOloErWK7T9DGEA07jepRvsO5x2gDe9922xCcaNeGNCcBBw5wM-dT3sEzZjiy9TxGub3HfAHyGZxmc9PEdPOtNHeHH3HqKv52dfTi6K7acPlyfrbWFLwVPBKsM4q6E0SlrWSt40trKqbqpGNjWz0vLSABeSiHzzQEvSyo60tWK1aCg_REeL7z74bxPEpAcXLfS9GcFPUdeCM1JVZZXJd_8lKeFK1Lwks-nrB-i1n8KYc2glVSVrLmbozQJdmR60GzufgrGzp15zUXHBJWeZOv4LlU8Lg7N-hC4v8r7g7R-CHZg-7aLvp-T8GO-DdAFt8DEG6PQ-uMGEm5xEz53QSyd07oSeO6Fvs-bVXbCpGaD9pfhZggywBYj5a7yC8Dv5v11_AD22vIg</recordid><startdate>20110701</startdate><enddate>20110701</enddate><creator>Zherdev, V. 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P. ; Boyko, S. S. ; Mesonzhnik, N. V. ; Bastrygin, D. 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per os
in doses of 40 and 200 mg/kg crossed the blood-brain barrier and was detected in rat brain (unchanged drug and its active metabolite N-caproyl-L-prolyl-L-tyrosine). The brain/plasma distribution coefficient for dilept was 2.0, for metabolite 0.5. No dose-concentration relationship was found, presumably because of the high dose of the drug transported from the blood to the brain not only by free diffusion, but also with participation of active carriers, whose number was limited.</abstract><cop>Boston</cop><pub>Springer US</pub><pmid>22451879</pmid><doi>10.1007/s10517-011-1322-z</doi><tpages>3</tpages></addata></record> |
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| ispartof | Bulletin of experimental biology and medicine, 2011-07, Vol.151 (3), p.330-332 |
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| source | Springer Nature |
| subjects | Animals Antipsychotic Agents - metabolism Antipsychotic Agents - pharmacokinetics Biological Transport Biomedical and Life Sciences Biomedicine Blood-brain barrier Blood-Brain Barrier - drug effects Blood-Brain Barrier - metabolism Brain Brain - blood supply Brain - metabolism Cell Biology Chromatography, High Pressure Liquid Diffusion Drugs Internal Medicine Laboratory Medicine Male Membrane permeability Metabolites Neuroleptics Pathology Peptides Permeability Pharmacology and Toxicology Proline - analogs & derivatives Proline - metabolism Proline - pharmacokinetics Rats Tandem Mass Spectrometry Tyrosine - analogs & derivatives Tyrosine - metabolism Tyrosine - pharmacokinetics |
| title | Permeability of the Blood-Brain Barrier for Dilept and Its Active Metabolite |
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