In vitro metabolism of chlorpheniramine in the rabbit
The in vitro metabolism of 3-( p-chloiophenyl)-3-(2-pyridyl)- N, N-dimethylpropylamine (chlorpheniramine, I) by rabbit liver microsomes was examined. The metabolites, tentatively identified by gas-liquid chromatography-mass spectrometry, included the mono- and didemethyl metabolites, the aldehyde th...
Gespeichert in:
| Veröffentlicht in: | Biochemical pharmacology 1987-10, Vol.36 (20), p.3445-3452 |
|---|---|
| Hauptverfasser: | , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 3452 |
|---|---|
| container_issue | 20 |
| container_start_page | 3445 |
| container_title | Biochemical pharmacology |
| container_volume | 36 |
| creator | Kammerer, R.Craig Lampe, Marilyn A. |
| description | The
in vitro metabolism of 3-(
p-chloiophenyl)-3-(2-pyridyl)-
N,
N-dimethylpropylamine (chlorpheniramine, I) by rabbit liver microsomes was examined. The metabolites, tentatively identified by gas-liquid chromatography-mass spectrometry, included the mono- and didemethyl metabolites, the aldehyde that results from deamination, and further metabolites of this aldehyde including its intramolecular cyclization product, an indolizine, and its reduction product, the alcohol. Inhibition of metabolism of I by N
2, CO, SKF-525A, 2,4-dichloro-6-phenylphenoxyethylamine (DPEA), or deletion of NADPH implies some involvement of cytochrome P-450 in the metabolic reactions. Quantitation of metabolism in these studies accounted for only 69% of the dose, so that binding and/or other undetected metabolic pathways were operative. |
| doi_str_mv | 10.1016/0006-2952(87)90324-8 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_81105608</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><els_id>0006295287903248</els_id><sourcerecordid>81105608</sourcerecordid><originalsourceid>FETCH-LOGICAL-c301t-2307b4a4bcfe4c97f265c4a8bbd0f8ffd83ef8466ea8e3915f14edaec6391e9e3</originalsourceid><addsrcrecordid>eNp9kE1LAzEQQIMotVb_gcIeRPSwmmyySfYiSPGjUPCi55BkJzSyu6nJtuC_d9eWHj0NM_NmmHkIXRJ8TzDhDxhjnhdVWdxKcVdhWrBcHqEpkYIOZS6P0fSAnKKzlL7GVHIyQRPKRcmxmKJy0WVb38eQtdBrExqf2iy4zK6aENcr6HzUre8g813WryCL2hjfn6MTp5sEF_s4Q58vzx_zt3z5_rqYPy1zSzHp84JiYZhmxjpgthKu4KVlWhpTYyedqyUFJxnnoCXQipSOMKg1WD4kUAGdoZvd3nUM3xtIvWp9stA0uoOwSUoSgoc_5ACyHWhjSCmCU-voWx1_FMFqtKXG39WoQkmh_mypcexqv39jWqgPQ3s9Q_9639fJ6sZF3VmfDpgQshC4GrDHHQaDi62HqJL10FmofQTbqzr4_-_4BQYohcI</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>81105608</pqid></control><display><type>article</type><title>In vitro metabolism of chlorpheniramine in the rabbit</title><source>Elsevier ScienceDirect Journals Complete - AutoHoldings</source><source>MEDLINE</source><creator>Kammerer, R.Craig ; Lampe, Marilyn A.</creator><creatorcontrib>Kammerer, R.Craig ; Lampe, Marilyn A.</creatorcontrib><description>The
in vitro metabolism of 3-(
p-chloiophenyl)-3-(2-pyridyl)-
N,
N-dimethylpropylamine (chlorpheniramine, I) by rabbit liver microsomes was examined. The metabolites, tentatively identified by gas-liquid chromatography-mass spectrometry, included the mono- and didemethyl metabolites, the aldehyde that results from deamination, and further metabolites of this aldehyde including its intramolecular cyclization product, an indolizine, and its reduction product, the alcohol. Inhibition of metabolism of I by N
2, CO, SKF-525A, 2,4-dichloro-6-phenylphenoxyethylamine (DPEA), or deletion of NADPH implies some involvement of cytochrome P-450 in the metabolic reactions. Quantitation of metabolism in these studies accounted for only 69% of the dose, so that binding and/or other undetected metabolic pathways were operative.</description><identifier>ISSN: 0006-2952</identifier><identifier>EISSN: 1873-2968</identifier><identifier>DOI: 10.1016/0006-2952(87)90324-8</identifier><identifier>PMID: 3675607</identifier><identifier>CODEN: BCPCA6</identifier><language>eng</language><publisher>New York, NY: Elsevier Inc</publisher><subject>Acylation ; Animals ; Biological and medical sciences ; Chlorpheniramine - metabolism ; Gas Chromatography-Mass Spectrometry ; Histamine and antagonists. Allergy ; In Vitro Techniques ; Male ; Medical sciences ; Microsomes, Liver - metabolism ; Pharmacology. Drug treatments ; Proadifen - pharmacology ; Rabbits</subject><ispartof>Biochemical pharmacology, 1987-10, Vol.36 (20), p.3445-3452</ispartof><rights>1987</rights><rights>1988 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c301t-2307b4a4bcfe4c97f265c4a8bbd0f8ffd83ef8466ea8e3915f14edaec6391e9e3</citedby><cites>FETCH-LOGICAL-c301t-2307b4a4bcfe4c97f265c4a8bbd0f8ffd83ef8466ea8e3915f14edaec6391e9e3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/0006-2952(87)90324-8$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3549,27923,27924,45994</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=7782709$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/3675607$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Kammerer, R.Craig</creatorcontrib><creatorcontrib>Lampe, Marilyn A.</creatorcontrib><title>In vitro metabolism of chlorpheniramine in the rabbit</title><title>Biochemical pharmacology</title><addtitle>Biochem Pharmacol</addtitle><description>The
in vitro metabolism of 3-(
p-chloiophenyl)-3-(2-pyridyl)-
N,
N-dimethylpropylamine (chlorpheniramine, I) by rabbit liver microsomes was examined. The metabolites, tentatively identified by gas-liquid chromatography-mass spectrometry, included the mono- and didemethyl metabolites, the aldehyde that results from deamination, and further metabolites of this aldehyde including its intramolecular cyclization product, an indolizine, and its reduction product, the alcohol. Inhibition of metabolism of I by N
2, CO, SKF-525A, 2,4-dichloro-6-phenylphenoxyethylamine (DPEA), or deletion of NADPH implies some involvement of cytochrome P-450 in the metabolic reactions. Quantitation of metabolism in these studies accounted for only 69% of the dose, so that binding and/or other undetected metabolic pathways were operative.</description><subject>Acylation</subject><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Chlorpheniramine - metabolism</subject><subject>Gas Chromatography-Mass Spectrometry</subject><subject>Histamine and antagonists. Allergy</subject><subject>In Vitro Techniques</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Microsomes, Liver - metabolism</subject><subject>Pharmacology. Drug treatments</subject><subject>Proadifen - pharmacology</subject><subject>Rabbits</subject><issn>0006-2952</issn><issn>1873-2968</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1987</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kE1LAzEQQIMotVb_gcIeRPSwmmyySfYiSPGjUPCi55BkJzSyu6nJtuC_d9eWHj0NM_NmmHkIXRJ8TzDhDxhjnhdVWdxKcVdhWrBcHqEpkYIOZS6P0fSAnKKzlL7GVHIyQRPKRcmxmKJy0WVb38eQtdBrExqf2iy4zK6aENcr6HzUre8g813WryCL2hjfn6MTp5sEF_s4Q58vzx_zt3z5_rqYPy1zSzHp84JiYZhmxjpgthKu4KVlWhpTYyedqyUFJxnnoCXQipSOMKg1WD4kUAGdoZvd3nUM3xtIvWp9stA0uoOwSUoSgoc_5ACyHWhjSCmCU-voWx1_FMFqtKXG39WoQkmh_mypcexqv39jWqgPQ3s9Q_9639fJ6sZF3VmfDpgQshC4GrDHHQaDi62HqJL10FmofQTbqzr4_-_4BQYohcI</recordid><startdate>19871015</startdate><enddate>19871015</enddate><creator>Kammerer, R.Craig</creator><creator>Lampe, Marilyn A.</creator><general>Elsevier Inc</general><general>Elsevier Science</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>19871015</creationdate><title>In vitro metabolism of chlorpheniramine in the rabbit</title><author>Kammerer, R.Craig ; Lampe, Marilyn A.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c301t-2307b4a4bcfe4c97f265c4a8bbd0f8ffd83ef8466ea8e3915f14edaec6391e9e3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1987</creationdate><topic>Acylation</topic><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Chlorpheniramine - metabolism</topic><topic>Gas Chromatography-Mass Spectrometry</topic><topic>Histamine and antagonists. Allergy</topic><topic>In Vitro Techniques</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Microsomes, Liver - metabolism</topic><topic>Pharmacology. Drug treatments</topic><topic>Proadifen - pharmacology</topic><topic>Rabbits</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kammerer, R.Craig</creatorcontrib><creatorcontrib>Lampe, Marilyn A.</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>Biochemical pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kammerer, R.Craig</au><au>Lampe, Marilyn A.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>In vitro metabolism of chlorpheniramine in the rabbit</atitle><jtitle>Biochemical pharmacology</jtitle><addtitle>Biochem Pharmacol</addtitle><date>1987-10-15</date><risdate>1987</risdate><volume>36</volume><issue>20</issue><spage>3445</spage><epage>3452</epage><pages>3445-3452</pages><issn>0006-2952</issn><eissn>1873-2968</eissn><coden>BCPCA6</coden><abstract>The
in vitro metabolism of 3-(
p-chloiophenyl)-3-(2-pyridyl)-
N,
N-dimethylpropylamine (chlorpheniramine, I) by rabbit liver microsomes was examined. The metabolites, tentatively identified by gas-liquid chromatography-mass spectrometry, included the mono- and didemethyl metabolites, the aldehyde that results from deamination, and further metabolites of this aldehyde including its intramolecular cyclization product, an indolizine, and its reduction product, the alcohol. Inhibition of metabolism of I by N
2, CO, SKF-525A, 2,4-dichloro-6-phenylphenoxyethylamine (DPEA), or deletion of NADPH implies some involvement of cytochrome P-450 in the metabolic reactions. Quantitation of metabolism in these studies accounted for only 69% of the dose, so that binding and/or other undetected metabolic pathways were operative.</abstract><cop>New York, NY</cop><pub>Elsevier Inc</pub><pmid>3675607</pmid><doi>10.1016/0006-2952(87)90324-8</doi><tpages>8</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0006-2952 |
| ispartof | Biochemical pharmacology, 1987-10, Vol.36 (20), p.3445-3452 |
| issn | 0006-2952 1873-2968 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_81105608 |
| source | Elsevier ScienceDirect Journals Complete - AutoHoldings; MEDLINE |
| subjects | Acylation Animals Biological and medical sciences Chlorpheniramine - metabolism Gas Chromatography-Mass Spectrometry Histamine and antagonists. Allergy In Vitro Techniques Male Medical sciences Microsomes, Liver - metabolism Pharmacology. Drug treatments Proadifen - pharmacology Rabbits |
| title | In vitro metabolism of chlorpheniramine in the rabbit |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-09T04%3A58%3A30IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_cross&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=In%20vitro%20metabolism%20of%20chlorpheniramine%20in%20the%20rabbit&rft.jtitle=Biochemical%20pharmacology&rft.au=Kammerer,%20R.Craig&rft.date=1987-10-15&rft.volume=36&rft.issue=20&rft.spage=3445&rft.epage=3452&rft.pages=3445-3452&rft.issn=0006-2952&rft.eissn=1873-2968&rft.coden=BCPCA6&rft_id=info:doi/10.1016/0006-2952(87)90324-8&rft_dat=%3Cproquest_cross%3E81105608%3C/proquest_cross%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_pqid=81105608&rft_id=info:pmid/3675607&rft_els_id=0006295287903248&rfr_iscdi=true |