The metabolism of [14C]N-ethoxycarbonyl-3-morpholinosydnonimine (molsidomine) in man
1. [14C]-N-Ethoxycarbonyl-3-morpholinosydnonimine (molsidomine, Corvaton®) was administered orally at a dose of 2 mg per subject to eight healthy male volunteers. 2. Maximal plasma concentrations of total radioactivity of 32.4±6.4ng equiv./ml (mean ± S.D.) were detected compared with maximum plasma...
Gespeichert in:
| Veröffentlicht in: | Xenobiotica 1987, Vol.17 (1), p.93-104 |
|---|---|
| Hauptverfasser: | , , , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 104 |
|---|---|
| container_issue | 1 |
| container_start_page | 93 |
| container_title | Xenobiotica |
| container_volume | 17 |
| creator | Wilson, I. D. Fromson, J. M. Illing, H. P. A. Schraven, E. |
| description | 1. [14C]-N-Ethoxycarbonyl-3-morpholinosydnonimine (molsidomine, Corvaton®)
was administered orally at a dose of 2 mg per subject to eight healthy male volunteers.
2. Maximal plasma concentrations of total radioactivity of 32.4±6.4ng equiv./ml
(mean ± S.D.) were detected compared with maximum plasma concentrations of
141 ± 5.9ng/ml (mean±S.D.) of molsidomine. In both cases these were attained at 0.5 h
after dosing. From the peak, concentrations of parent drug fell rapidly with a half-life of 1.25
± 0.38 h (mean ± S.D.). In contrast, total radioactivity declined more slowly with a terminal
half-life of 138 ± 42.7 h (mean ± S.D.).
3. The bulk of the radiolabel was rapidly excreted as metabolites in the urine, with over
85% of the dose recovered in the first 24 h. The main urinary radiolabelled metabolites
appeared, from chromatographic evidence, to be similar to those previously identified
in animals, namely N-morpholinosydnonimine, N-cyanomethylamino-N-(2'-
hydroxyethy1)glycine and (N-cyanomethylenamino-2-aminoethyoxy)-acetic acid. |
| doi_str_mv | 10.3109/00498258709047179 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_pasca</sourceid><recordid>TN_cdi_proquest_miscellaneous_77432066</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>77432066</sourcerecordid><originalsourceid>FETCH-LOGICAL-c430t-4a8f21ec197f62b8a72869a24606ef3e108f47e47e1a52b350b6891ad33563693</originalsourceid><addsrcrecordid>eNp9kUtr3DAUhUVISadpfkAWAS9CaBdu9bIskWzK0BeEdjNdlWKubQkr6DGVPLT-99Uw00ApBARC93zncu8RQpcEv2EEq7cYcyVpI1usMG9Jq07QijAh6kZReYpWe70uAH-OXuT8gDEWhNIzdMZKseArtNlMuvJ6hj46m30VTfWd8PWPL7Wep_h7GSD1MSyuZrWPaTsVKsS8jCEG623Q1SsfXbZj3D9eVzZUHsJL9MyAy_rieJ-jbx_eb9af6vuvHz-v393XA2d4rjlIQ4keiGqNoL2ElkqhgHKBhTZMEywNb3U5BBraswb3QioCI2ONYEKxc3Rz6LtN8edO57nzNg_aOQg67nLXtpxRLEQByQEcUsw5adNtk_WQlo7gbp9k91-SxXN1bL7rvR4fHcfoin591CEP4EyCMNj8iEkqpOCkYHcHzAYTk4dfMbmxm2FxMf31sKemuP3HPmlw81R-RXcPcZdCifeJHf4AVVafQg</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>77432066</pqid></control><display><type>article</type><title>The metabolism of [14C]N-ethoxycarbonyl-3-morpholinosydnonimine (molsidomine) in man</title><source>MEDLINE</source><source>Taylor & Francis:Master (3349 titles)</source><source>Taylor & Francis Medical Library - CRKN</source><creator>Wilson, I. D. ; Fromson, J. M. ; Illing, H. P. A. ; Schraven, E.</creator><creatorcontrib>Wilson, I. D. ; Fromson, J. M. ; Illing, H. P. A. ; Schraven, E.</creatorcontrib><description>1. [14C]-N-Ethoxycarbonyl-3-morpholinosydnonimine (molsidomine, Corvaton®)
was administered orally at a dose of 2 mg per subject to eight healthy male volunteers.
2. Maximal plasma concentrations of total radioactivity of 32.4±6.4ng equiv./ml
(mean ± S.D.) were detected compared with maximum plasma concentrations of
141 ± 5.9ng/ml (mean±S.D.) of molsidomine. In both cases these were attained at 0.5 h
after dosing. From the peak, concentrations of parent drug fell rapidly with a half-life of 1.25
± 0.38 h (mean ± S.D.). In contrast, total radioactivity declined more slowly with a terminal
half-life of 138 ± 42.7 h (mean ± S.D.).
3. The bulk of the radiolabel was rapidly excreted as metabolites in the urine, with over
85% of the dose recovered in the first 24 h. The main urinary radiolabelled metabolites
appeared, from chromatographic evidence, to be similar to those previously identified
in animals, namely N-morpholinosydnonimine, N-cyanomethylamino-N-(2'-
hydroxyethy1)glycine and (N-cyanomethylenamino-2-aminoethyoxy)-acetic acid.</description><identifier>ISSN: 0049-8254</identifier><identifier>EISSN: 1366-5928</identifier><identifier>DOI: 10.3109/00498258709047179</identifier><identifier>PMID: 3825179</identifier><identifier>CODEN: XENOBH</identifier><language>eng</language><publisher>London: Informa UK Ltd</publisher><subject>Administration, Oral ; Adult ; Antianginal agents. Coronary vasodilator agents ; Biological and medical sciences ; Biotransformation ; Cardiovascular system ; Humans ; Kinetics ; Medical sciences ; Metabolic Clearance Rate ; Middle Aged ; Molsidomine - metabolism ; Molsidomine - urine ; Pharmacology. Drug treatments</subject><ispartof>Xenobiotica, 1987, Vol.17 (1), p.93-104</ispartof><rights>1987 Informa UK Ltd All rights reserved: reproduction in whole or part not permitted 1987</rights><rights>1987 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c430t-4a8f21ec197f62b8a72869a24606ef3e108f47e47e1a52b350b6891ad33563693</citedby><cites>FETCH-LOGICAL-c430t-4a8f21ec197f62b8a72869a24606ef3e108f47e47e1a52b350b6891ad33563693</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.tandfonline.com/doi/pdf/10.3109/00498258709047179$$EPDF$$P50$$Ginformaworld$$H</linktopdf><linktohtml>$$Uhttps://www.tandfonline.com/doi/full/10.3109/00498258709047179$$EHTML$$P50$$Ginformaworld$$H</linktohtml><link.rule.ids>314,780,784,4024,27923,27924,27925,59647,59753,60436,60542,61221,61256,61402,61437</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=8268641$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/3825179$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Wilson, I. D.</creatorcontrib><creatorcontrib>Fromson, J. M.</creatorcontrib><creatorcontrib>Illing, H. P. A.</creatorcontrib><creatorcontrib>Schraven, E.</creatorcontrib><title>The metabolism of [14C]N-ethoxycarbonyl-3-morpholinosydnonimine (molsidomine) in man</title><title>Xenobiotica</title><addtitle>Xenobiotica</addtitle><description>1. [14C]-N-Ethoxycarbonyl-3-morpholinosydnonimine (molsidomine, Corvaton®)
was administered orally at a dose of 2 mg per subject to eight healthy male volunteers.
2. Maximal plasma concentrations of total radioactivity of 32.4±6.4ng equiv./ml
(mean ± S.D.) were detected compared with maximum plasma concentrations of
141 ± 5.9ng/ml (mean±S.D.) of molsidomine. In both cases these were attained at 0.5 h
after dosing. From the peak, concentrations of parent drug fell rapidly with a half-life of 1.25
± 0.38 h (mean ± S.D.). In contrast, total radioactivity declined more slowly with a terminal
half-life of 138 ± 42.7 h (mean ± S.D.).
3. The bulk of the radiolabel was rapidly excreted as metabolites in the urine, with over
85% of the dose recovered in the first 24 h. The main urinary radiolabelled metabolites
appeared, from chromatographic evidence, to be similar to those previously identified
in animals, namely N-morpholinosydnonimine, N-cyanomethylamino-N-(2'-
hydroxyethy1)glycine and (N-cyanomethylenamino-2-aminoethyoxy)-acetic acid.</description><subject>Administration, Oral</subject><subject>Adult</subject><subject>Antianginal agents. Coronary vasodilator agents</subject><subject>Biological and medical sciences</subject><subject>Biotransformation</subject><subject>Cardiovascular system</subject><subject>Humans</subject><subject>Kinetics</subject><subject>Medical sciences</subject><subject>Metabolic Clearance Rate</subject><subject>Middle Aged</subject><subject>Molsidomine - metabolism</subject><subject>Molsidomine - urine</subject><subject>Pharmacology. Drug treatments</subject><issn>0049-8254</issn><issn>1366-5928</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1987</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kUtr3DAUhUVISadpfkAWAS9CaBdu9bIskWzK0BeEdjNdlWKubQkr6DGVPLT-99Uw00ApBARC93zncu8RQpcEv2EEq7cYcyVpI1usMG9Jq07QijAh6kZReYpWe70uAH-OXuT8gDEWhNIzdMZKseArtNlMuvJ6hj46m30VTfWd8PWPL7Wep_h7GSD1MSyuZrWPaTsVKsS8jCEG623Q1SsfXbZj3D9eVzZUHsJL9MyAy_rieJ-jbx_eb9af6vuvHz-v393XA2d4rjlIQ4keiGqNoL2ElkqhgHKBhTZMEywNb3U5BBraswb3QioCI2ONYEKxc3Rz6LtN8edO57nzNg_aOQg67nLXtpxRLEQByQEcUsw5adNtk_WQlo7gbp9k91-SxXN1bL7rvR4fHcfoin591CEP4EyCMNj8iEkqpOCkYHcHzAYTk4dfMbmxm2FxMf31sKemuP3HPmlw81R-RXcPcZdCifeJHf4AVVafQg</recordid><startdate>1987</startdate><enddate>1987</enddate><creator>Wilson, I. D.</creator><creator>Fromson, J. M.</creator><creator>Illing, H. P. A.</creator><creator>Schraven, E.</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>7X8</scope></search><sort><creationdate>1987</creationdate><title>The metabolism of [14C]N-ethoxycarbonyl-3-morpholinosydnonimine (molsidomine) in man</title><author>Wilson, I. D. ; Fromson, J. M. ; Illing, H. P. A. ; Schraven, E.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c430t-4a8f21ec197f62b8a72869a24606ef3e108f47e47e1a52b350b6891ad33563693</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1987</creationdate><topic>Administration, Oral</topic><topic>Adult</topic><topic>Antianginal agents. Coronary vasodilator agents</topic><topic>Biological and medical sciences</topic><topic>Biotransformation</topic><topic>Cardiovascular system</topic><topic>Humans</topic><topic>Kinetics</topic><topic>Medical sciences</topic><topic>Metabolic Clearance Rate</topic><topic>Middle Aged</topic><topic>Molsidomine - metabolism</topic><topic>Molsidomine - urine</topic><topic>Pharmacology. Drug treatments</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Wilson, I. D.</creatorcontrib><creatorcontrib>Fromson, J. M.</creatorcontrib><creatorcontrib>Illing, H. P. A.</creatorcontrib><creatorcontrib>Schraven, E.</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>MEDLINE - Academic</collection><jtitle>Xenobiotica</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Wilson, I. D.</au><au>Fromson, J. M.</au><au>Illing, H. P. A.</au><au>Schraven, E.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>The metabolism of [14C]N-ethoxycarbonyl-3-morpholinosydnonimine (molsidomine) in man</atitle><jtitle>Xenobiotica</jtitle><addtitle>Xenobiotica</addtitle><date>1987</date><risdate>1987</risdate><volume>17</volume><issue>1</issue><spage>93</spage><epage>104</epage><pages>93-104</pages><issn>0049-8254</issn><eissn>1366-5928</eissn><coden>XENOBH</coden><abstract>1. [14C]-N-Ethoxycarbonyl-3-morpholinosydnonimine (molsidomine, Corvaton®)
was administered orally at a dose of 2 mg per subject to eight healthy male volunteers.
2. Maximal plasma concentrations of total radioactivity of 32.4±6.4ng equiv./ml
(mean ± S.D.) were detected compared with maximum plasma concentrations of
141 ± 5.9ng/ml (mean±S.D.) of molsidomine. In both cases these were attained at 0.5 h
after dosing. From the peak, concentrations of parent drug fell rapidly with a half-life of 1.25
± 0.38 h (mean ± S.D.). In contrast, total radioactivity declined more slowly with a terminal
half-life of 138 ± 42.7 h (mean ± S.D.).
3. The bulk of the radiolabel was rapidly excreted as metabolites in the urine, with over
85% of the dose recovered in the first 24 h. The main urinary radiolabelled metabolites
appeared, from chromatographic evidence, to be similar to those previously identified
in animals, namely N-morpholinosydnonimine, N-cyanomethylamino-N-(2'-
hydroxyethy1)glycine and (N-cyanomethylenamino-2-aminoethyoxy)-acetic acid.</abstract><cop>London</cop><pub>Informa UK Ltd</pub><pmid>3825179</pmid><doi>10.3109/00498258709047179</doi><tpages>12</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0049-8254 |
| ispartof | Xenobiotica, 1987, Vol.17 (1), p.93-104 |
| issn | 0049-8254 1366-5928 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_77432066 |
| source | MEDLINE; Taylor & Francis:Master (3349 titles); Taylor & Francis Medical Library - CRKN |
| subjects | Administration, Oral Adult Antianginal agents. Coronary vasodilator agents Biological and medical sciences Biotransformation Cardiovascular system Humans Kinetics Medical sciences Metabolic Clearance Rate Middle Aged Molsidomine - metabolism Molsidomine - urine Pharmacology. Drug treatments |
| title | The metabolism of [14C]N-ethoxycarbonyl-3-morpholinosydnonimine (molsidomine) in man |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2024-12-26T18%3A43%3A37IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_pasca&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=The%20metabolism%20of%20%5B14C%5DN-ethoxycarbonyl-3-morpholinosydnonimine%20(molsidomine)%20in%20man&rft.jtitle=Xenobiotica&rft.au=Wilson,%20I.%20D.&rft.date=1987&rft.volume=17&rft.issue=1&rft.spage=93&rft.epage=104&rft.pages=93-104&rft.issn=0049-8254&rft.eissn=1366-5928&rft.coden=XENOBH&rft_id=info:doi/10.3109/00498258709047179&rft_dat=%3Cproquest_pasca%3E77432066%3C/proquest_pasca%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_pqid=77432066&rft_id=info:pmid/3825179&rfr_iscdi=true |