Circulating and brain metabolites of minaprine in the baboon
1. A mixture of 15N-labelled, 14C-labelled and unlabelled minaprine was administered orally to three baboons, and metabolites in blood, urine and brain investigated. 2. Biological samples were extracted with dichloromethane and the radioactive components extracted were analysed by t.l.c. and autorad...
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| Veröffentlicht in: | Xenobiotica 1985-01, Vol.15 (2), p.97-106 |
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| creator | Davi, H. Carayon, A. Marti, E. Sales, Y. Cautreels, W. |
| description | 1. A mixture of 15N-labelled, 14C-labelled and unlabelled minaprine was administered orally to three baboons, and metabolites in blood, urine and brain investigated.
2. Biological samples were extracted with dichloromethane and the radioactive components extracted were analysed by t.l.c. and autoradiography. Compounds identified by comparing their physicochemical properties with those of synthetic standards and by g.l.c.-mass spectrometry were minaprine, 3-[2-(3-oxo)morpholino-ethylamino]-4-methyl-6-phenylpyridazine, 3-amino-4-methyl-6-phenylpyridazine, 3-[2-(aminoethyl) ethylamino]-4-methyl-6-phenylpyridazine, p-hydroxyminaprine and minaprine N-oxide.
3. In addition to the urinary metabolites, two circulating metabolites were detected: metabolite A, 3-[2-(3-oxo)morpholino-ethylamino]-4-methyl-6-phenylpyridazine, and metabolite B (unidentified).
4. All circulating metabolites appeared very early in blood, confirming the rapid and extensive metabolism of the drug. Metabolites A, B and 3 (p-hydroxyminaprine) were the major metabolites present in plasma. The parent drug was not the major circulating form, and was present in a higher concentration in erythrocytes than in plasma. Erythrocytes might act as a reservoir of the drug and could explain the relatively slow blood clearance of minaprine despite its rapid metabolism.
5. The qualitative metabolic profile in brain tissue was similar to that in blood. |
| doi_str_mv | 10.3109/00498258509045339 |
| format | Article |
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2. Biological samples were extracted with dichloromethane and the radioactive components extracted were analysed by t.l.c. and autoradiography. Compounds identified by comparing their physicochemical properties with those of synthetic standards and by g.l.c.-mass spectrometry were minaprine, 3-[2-(3-oxo)morpholino-ethylamino]-4-methyl-6-phenylpyridazine, 3-amino-4-methyl-6-phenylpyridazine, 3-[2-(aminoethyl) ethylamino]-4-methyl-6-phenylpyridazine, p-hydroxyminaprine and minaprine N-oxide.
3. In addition to the urinary metabolites, two circulating metabolites were detected: metabolite A, 3-[2-(3-oxo)morpholino-ethylamino]-4-methyl-6-phenylpyridazine, and metabolite B (unidentified).
4. All circulating metabolites appeared very early in blood, confirming the rapid and extensive metabolism of the drug. Metabolites A, B and 3 (p-hydroxyminaprine) were the major metabolites present in plasma. The parent drug was not the major circulating form, and was present in a higher concentration in erythrocytes than in plasma. Erythrocytes might act as a reservoir of the drug and could explain the relatively slow blood clearance of minaprine despite its rapid metabolism.
5. The qualitative metabolic profile in brain tissue was similar to that in blood.</description><identifier>ISSN: 0049-8254</identifier><identifier>EISSN: 1366-5928</identifier><identifier>DOI: 10.3109/00498258509045339</identifier><identifier>PMID: 4002739</identifier><identifier>CODEN: XENOBH</identifier><language>eng</language><publisher>London: Informa UK Ltd</publisher><subject>Animals ; Autoradiography ; Biological and medical sciences ; Brain - metabolism ; Chromatography, Thin Layer ; Female ; Gas Chromatography-Mass Spectrometry ; Kinetics ; Male ; Medical sciences ; Neuropharmacology ; Papio ; Papio papio ; Pharmacology. Drug treatments ; Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease) ; Psychology. Psychoanalysis. Psychiatry ; Psychopharmacology ; Pyridazines - blood ; Pyridazines - metabolism ; Pyridazines - urine</subject><ispartof>Xenobiotica, 1985-01, Vol.15 (2), p.97-106</ispartof><rights>1985 Informa UK Ltd All rights reserved: reproduction in whole or part not permitted 1985</rights><rights>1985 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c461t-49ea076afc6322115f40b8331be2c872b805f92baaf01821d1d9f704a7db8f943</citedby><cites>FETCH-LOGICAL-c461t-49ea076afc6322115f40b8331be2c872b805f92baaf01821d1d9f704a7db8f943</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.tandfonline.com/doi/pdf/10.3109/00498258509045339$$EPDF$$P50$$Ginformahealthcare$$H</linktopdf><linktohtml>$$Uhttps://www.tandfonline.com/doi/full/10.3109/00498258509045339$$EHTML$$P50$$Ginformahealthcare$$H</linktohtml><link.rule.ids>314,776,780,27901,27902,59620,59726,60409,60515,61194,61229,61375,61410</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=9255819$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/4002739$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Davi, H.</creatorcontrib><creatorcontrib>Carayon, A.</creatorcontrib><creatorcontrib>Marti, E.</creatorcontrib><creatorcontrib>Sales, Y.</creatorcontrib><creatorcontrib>Cautreels, W.</creatorcontrib><title>Circulating and brain metabolites of minaprine in the baboon</title><title>Xenobiotica</title><addtitle>Xenobiotica</addtitle><description>1. A mixture of 15N-labelled, 14C-labelled and unlabelled minaprine was administered orally to three baboons, and metabolites in blood, urine and brain investigated.
2. Biological samples were extracted with dichloromethane and the radioactive components extracted were analysed by t.l.c. and autoradiography. Compounds identified by comparing their physicochemical properties with those of synthetic standards and by g.l.c.-mass spectrometry were minaprine, 3-[2-(3-oxo)morpholino-ethylamino]-4-methyl-6-phenylpyridazine, 3-amino-4-methyl-6-phenylpyridazine, 3-[2-(aminoethyl) ethylamino]-4-methyl-6-phenylpyridazine, p-hydroxyminaprine and minaprine N-oxide.
3. In addition to the urinary metabolites, two circulating metabolites were detected: metabolite A, 3-[2-(3-oxo)morpholino-ethylamino]-4-methyl-6-phenylpyridazine, and metabolite B (unidentified).
4. All circulating metabolites appeared very early in blood, confirming the rapid and extensive metabolism of the drug. Metabolites A, B and 3 (p-hydroxyminaprine) were the major metabolites present in plasma. The parent drug was not the major circulating form, and was present in a higher concentration in erythrocytes than in plasma. Erythrocytes might act as a reservoir of the drug and could explain the relatively slow blood clearance of minaprine despite its rapid metabolism.
5. The qualitative metabolic profile in brain tissue was similar to that in blood.</description><subject>Animals</subject><subject>Autoradiography</subject><subject>Biological and medical sciences</subject><subject>Brain - metabolism</subject><subject>Chromatography, Thin Layer</subject><subject>Female</subject><subject>Gas Chromatography-Mass Spectrometry</subject><subject>Kinetics</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Neuropharmacology</subject><subject>Papio</subject><subject>Papio papio</subject><subject>Pharmacology. Drug treatments</subject><subject>Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease)</subject><subject>Psychology. Psychoanalysis. Psychiatry</subject><subject>Psychopharmacology</subject><subject>Pyridazines - blood</subject><subject>Pyridazines - metabolism</subject><subject>Pyridazines - urine</subject><issn>0049-8254</issn><issn>1366-5928</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1985</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkU1r3DAQhkVpSTZpf0APBR9Kb05HH7YlkktYmg8I5JKezUiWugqylEg2If--XnYbKIHkpMPzvIPmHUK-UjjhFNRPAKEka2QDCkTDufpAVpS3bd0oJj-S1ZbXiyAOyVEp9wDQUsYOyIEAYB1XK3K29tnMAScf_1QYh0pn9LEa7YQ6BT_ZUiVXjT7iQ_bRVgubNrbSC03xM_nkMBT7Zf8ek98Xv-7WV_XN7eX1-vymNqKlUy2URehadKbljFHaOAFack61ZUZ2TEtonGIa0QGVjA50UK4Dgd2gpVOCH5Mfu7kPOT3Otkz96IuxIWC0aS5911Ihuq59V6SCMQaSLiLdiSanUrJ1_bLeiPm5p9Bvq-1fVbtkvu2Hz3q0w0ti3-XCv-85FoPBZYzGlxdNsaaRdKud7TQfXcojPqUchn7C55Dyvwx_6xen_8U3FsO0MZhtf5_mHJc7vLHDX7-KpCc</recordid><startdate>19850101</startdate><enddate>19850101</enddate><creator>Davi, H.</creator><creator>Carayon, A.</creator><creator>Marti, E.</creator><creator>Sales, Y.</creator><creator>Cautreels, W.</creator><general>Informa UK Ltd</general><general>Taylor & Francis</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7TK</scope><scope>7X8</scope></search><sort><creationdate>19850101</creationdate><title>Circulating and brain metabolites of minaprine in the baboon</title><author>Davi, H. ; Carayon, A. ; Marti, E. ; Sales, Y. ; Cautreels, W.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c461t-49ea076afc6322115f40b8331be2c872b805f92baaf01821d1d9f704a7db8f943</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1985</creationdate><topic>Animals</topic><topic>Autoradiography</topic><topic>Biological and medical sciences</topic><topic>Brain - metabolism</topic><topic>Chromatography, Thin Layer</topic><topic>Female</topic><topic>Gas Chromatography-Mass Spectrometry</topic><topic>Kinetics</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Neuropharmacology</topic><topic>Papio</topic><topic>Papio papio</topic><topic>Pharmacology. Drug treatments</topic><topic>Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease)</topic><topic>Psychology. Psychoanalysis. Psychiatry</topic><topic>Psychopharmacology</topic><topic>Pyridazines - blood</topic><topic>Pyridazines - metabolism</topic><topic>Pyridazines - urine</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Davi, H.</creatorcontrib><creatorcontrib>Carayon, A.</creatorcontrib><creatorcontrib>Marti, E.</creatorcontrib><creatorcontrib>Sales, Y.</creatorcontrib><creatorcontrib>Cautreels, W.</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Neurosciences Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Xenobiotica</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Davi, H.</au><au>Carayon, A.</au><au>Marti, E.</au><au>Sales, Y.</au><au>Cautreels, W.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Circulating and brain metabolites of minaprine in the baboon</atitle><jtitle>Xenobiotica</jtitle><addtitle>Xenobiotica</addtitle><date>1985-01-01</date><risdate>1985</risdate><volume>15</volume><issue>2</issue><spage>97</spage><epage>106</epage><pages>97-106</pages><issn>0049-8254</issn><eissn>1366-5928</eissn><coden>XENOBH</coden><abstract>1. A mixture of 15N-labelled, 14C-labelled and unlabelled minaprine was administered orally to three baboons, and metabolites in blood, urine and brain investigated.
2. Biological samples were extracted with dichloromethane and the radioactive components extracted were analysed by t.l.c. and autoradiography. Compounds identified by comparing their physicochemical properties with those of synthetic standards and by g.l.c.-mass spectrometry were minaprine, 3-[2-(3-oxo)morpholino-ethylamino]-4-methyl-6-phenylpyridazine, 3-amino-4-methyl-6-phenylpyridazine, 3-[2-(aminoethyl) ethylamino]-4-methyl-6-phenylpyridazine, p-hydroxyminaprine and minaprine N-oxide.
3. In addition to the urinary metabolites, two circulating metabolites were detected: metabolite A, 3-[2-(3-oxo)morpholino-ethylamino]-4-methyl-6-phenylpyridazine, and metabolite B (unidentified).
4. All circulating metabolites appeared very early in blood, confirming the rapid and extensive metabolism of the drug. Metabolites A, B and 3 (p-hydroxyminaprine) were the major metabolites present in plasma. The parent drug was not the major circulating form, and was present in a higher concentration in erythrocytes than in plasma. Erythrocytes might act as a reservoir of the drug and could explain the relatively slow blood clearance of minaprine despite its rapid metabolism.
5. The qualitative metabolic profile in brain tissue was similar to that in blood.</abstract><cop>London</cop><pub>Informa UK Ltd</pub><pmid>4002739</pmid><doi>10.3109/00498258509045339</doi><tpages>10</tpages></addata></record> |
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| subjects | Animals Autoradiography Biological and medical sciences Brain - metabolism Chromatography, Thin Layer Female Gas Chromatography-Mass Spectrometry Kinetics Male Medical sciences Neuropharmacology Papio Papio papio Pharmacology. Drug treatments Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease) Psychology. Psychoanalysis. Psychiatry Psychopharmacology Pyridazines - blood Pyridazines - metabolism Pyridazines - urine |
| title | Circulating and brain metabolites of minaprine in the baboon |
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