Cocaethylene: A Unique Cocaine Metabolite Displays High Affinity for the Dopamine Transporter
: Concurrent cocaine and alcohol use is common practice in the general population, as indicated by recent prevalence studies. In the presence of ethyl alcohol, cocaine is metabolized to its ethyl homolog, cocaethylene. The transesterification of cocaine and ethanol to cocaethylene takes place in the...
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| Veröffentlicht in: | Journal of neurochemistry 1991-02, Vol.56 (2), p.698-701 |
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| container_end_page | 701 |
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| container_issue | 2 |
| container_start_page | 698 |
| container_title | Journal of neurochemistry |
| container_volume | 56 |
| creator | Hearn, W. Lee Flynn, Donna D. Hime, George W. Rose, Stefan Cofino, Julio C. Mantero‐Atienza, Emilio Wetli, Charles V. Mash, Deborah C. |
| description | : Concurrent cocaine and alcohol use is common practice in the general population, as indicated by recent prevalence studies. In the presence of ethyl alcohol, cocaine is metabolized to its ethyl homolog, cocaethylene. The transesterification of cocaine and ethanol to cocaethylene takes place in the liver and represents a novel metabolic reaction. Cocaethylene was detected in postmortem blood, liver, and neurological tissues in concentrations equal to and sometimes exceeding those of cocaine. In vitro binding studies demonstrate that cocaethylene has a pharmacological profile similar but not identical to that of cocaine at monoamine transport sites assayed in the human brain. Cocaethylene was equipotent to cocaine at inhibiting [3H]mazindol binding to the dopamine transporter. The blockade of dopamine reuptake in the synaptic cleft by cocaethylene may account for the enhanced euphoria associated with combined alcohol and cocaine abuse. |
| doi_str_mv | 10.1111/j.1471-4159.1991.tb08205.x |
| format | Article |
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Lee ; Flynn, Donna D. ; Hime, George W. ; Rose, Stefan ; Cofino, Julio C. ; Mantero‐Atienza, Emilio ; Wetli, Charles V. ; Mash, Deborah C.</creator><creatorcontrib>Hearn, W. Lee ; Flynn, Donna D. ; Hime, George W. ; Rose, Stefan ; Cofino, Julio C. ; Mantero‐Atienza, Emilio ; Wetli, Charles V. ; Mash, Deborah C.</creatorcontrib><description>: Concurrent cocaine and alcohol use is common practice in the general population, as indicated by recent prevalence studies. In the presence of ethyl alcohol, cocaine is metabolized to its ethyl homolog, cocaethylene. The transesterification of cocaine and ethanol to cocaethylene takes place in the liver and represents a novel metabolic reaction. Cocaethylene was detected in postmortem blood, liver, and neurological tissues in concentrations equal to and sometimes exceeding those of cocaine. In vitro binding studies demonstrate that cocaethylene has a pharmacological profile similar but not identical to that of cocaine at monoamine transport sites assayed in the human brain. Cocaethylene was equipotent to cocaine at inhibiting [3H]mazindol binding to the dopamine transporter. The blockade of dopamine reuptake in the synaptic cleft by cocaethylene may account for the enhanced euphoria associated with combined alcohol and cocaine abuse.</description><identifier>ISSN: 0022-3042</identifier><identifier>EISSN: 1471-4159</identifier><identifier>DOI: 10.1111/j.1471-4159.1991.tb08205.x</identifier><identifier>PMID: 1988563</identifier><identifier>CODEN: JONRA9</identifier><language>eng</language><publisher>Oxford, UK: Blackwell Publishing Ltd</publisher><subject>Adult ; Biological and medical sciences ; Brain - metabolism ; Carrier Proteins - metabolism ; CNS ; Cocaine ; Cocaine - analogs & derivatives ; Cocaine - blood ; Cocaine - metabolism ; Dopamine Plasma Membrane Transport Proteins ; Drug addictions ; Esterification ; Ethanol ; Ethanol - blood ; Ethanol - metabolism ; Female ; Humans ; Liver - metabolism ; Male ; Mazindol - metabolism ; Medical sciences ; Membrane Glycoproteins ; Membrane Transport Proteins ; Monoamine uptake sites ; Nerve Tissue Proteins ; Toxicology</subject><ispartof>Journal of neurochemistry, 1991-02, Vol.56 (2), p.698-701</ispartof><rights>1991 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c4658-25382d7e78b5dec2dfaf55eec2e46e9a7db3c87dc749f2461ce6b8c122a868813</citedby><cites>FETCH-LOGICAL-c4658-25382d7e78b5dec2dfaf55eec2e46e9a7db3c87dc749f2461ce6b8c122a868813</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1111%2Fj.1471-4159.1991.tb08205.x$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1111%2Fj.1471-4159.1991.tb08205.x$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>314,780,784,1417,27924,27925,45574,45575</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=19661884$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/1988563$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Hearn, W. Lee</creatorcontrib><creatorcontrib>Flynn, Donna D.</creatorcontrib><creatorcontrib>Hime, George W.</creatorcontrib><creatorcontrib>Rose, Stefan</creatorcontrib><creatorcontrib>Cofino, Julio C.</creatorcontrib><creatorcontrib>Mantero‐Atienza, Emilio</creatorcontrib><creatorcontrib>Wetli, Charles V.</creatorcontrib><creatorcontrib>Mash, Deborah C.</creatorcontrib><title>Cocaethylene: A Unique Cocaine Metabolite Displays High Affinity for the Dopamine Transporter</title><title>Journal of neurochemistry</title><addtitle>J Neurochem</addtitle><description>: Concurrent cocaine and alcohol use is common practice in the general population, as indicated by recent prevalence studies. In the presence of ethyl alcohol, cocaine is metabolized to its ethyl homolog, cocaethylene. The transesterification of cocaine and ethanol to cocaethylene takes place in the liver and represents a novel metabolic reaction. Cocaethylene was detected in postmortem blood, liver, and neurological tissues in concentrations equal to and sometimes exceeding those of cocaine. In vitro binding studies demonstrate that cocaethylene has a pharmacological profile similar but not identical to that of cocaine at monoamine transport sites assayed in the human brain. Cocaethylene was equipotent to cocaine at inhibiting [3H]mazindol binding to the dopamine transporter. The blockade of dopamine reuptake in the synaptic cleft by cocaethylene may account for the enhanced euphoria associated with combined alcohol and cocaine abuse.</description><subject>Adult</subject><subject>Biological and medical sciences</subject><subject>Brain - metabolism</subject><subject>Carrier Proteins - metabolism</subject><subject>CNS</subject><subject>Cocaine</subject><subject>Cocaine - analogs & derivatives</subject><subject>Cocaine - blood</subject><subject>Cocaine - metabolism</subject><subject>Dopamine Plasma Membrane Transport Proteins</subject><subject>Drug addictions</subject><subject>Esterification</subject><subject>Ethanol</subject><subject>Ethanol - blood</subject><subject>Ethanol - metabolism</subject><subject>Female</subject><subject>Humans</subject><subject>Liver - metabolism</subject><subject>Male</subject><subject>Mazindol - metabolism</subject><subject>Medical sciences</subject><subject>Membrane Glycoproteins</subject><subject>Membrane Transport Proteins</subject><subject>Monoamine uptake sites</subject><subject>Nerve Tissue Proteins</subject><subject>Toxicology</subject><issn>0022-3042</issn><issn>1471-4159</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1991</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqVkE9P3DAQxS3UCrbAR6hkIbW3pLZjOw4HpNX2D0VAL3CsLMcZd73KJsHOquTb42hXpVd8GcvvvfHMD6ELSnKazpdNTnlJM05FldOqovlYE8WIyJ-P0OKf9A4tCGEsKwhnJ-hDjBtCqOSSHqNjWiklZLFAv1e9NTCupxY6uMRL_Nj5px3g-dl3gO9gNHXf-hHwVx-H1kwRX_s_a7x0znd-nLDrAx7XSe4Hs50jD8F0cejDCOEMvXemjXB-qKfo8fu3h9V1dvvrx8_V8jazXAqVMVEo1pRQqlo0YFnjjBMC0g24hMqUTV1YVTa25JVjaQMLslaWMmaUVIoWp-jzvu8Q-jR9HPXWRwttazrod1GrhEDxUiTj5d5oQx9jAKeH4LcmTJoSPbPVGz0D1DNAPbPVB7b6OYU_Hn7Z1VtoXqN7mEn_dNBNtKZ1iYP18T-blFQpnnxXe99f38L0hgn0zf1KVqp4Ab6Glwo</recordid><startdate>199102</startdate><enddate>199102</enddate><creator>Hearn, W. Lee</creator><creator>Flynn, Donna D.</creator><creator>Hime, George W.</creator><creator>Rose, Stefan</creator><creator>Cofino, Julio C.</creator><creator>Mantero‐Atienza, Emilio</creator><creator>Wetli, Charles V.</creator><creator>Mash, Deborah C.</creator><general>Blackwell Publishing Ltd</general><general>Blackwell</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>199102</creationdate><title>Cocaethylene: A Unique Cocaine Metabolite Displays High Affinity for the Dopamine Transporter</title><author>Hearn, W. Lee ; Flynn, Donna D. ; Hime, George W. ; Rose, Stefan ; Cofino, Julio C. ; Mantero‐Atienza, Emilio ; Wetli, Charles V. ; Mash, Deborah C.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c4658-25382d7e78b5dec2dfaf55eec2e46e9a7db3c87dc749f2461ce6b8c122a868813</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1991</creationdate><topic>Adult</topic><topic>Biological and medical sciences</topic><topic>Brain - metabolism</topic><topic>Carrier Proteins - metabolism</topic><topic>CNS</topic><topic>Cocaine</topic><topic>Cocaine - analogs & derivatives</topic><topic>Cocaine - blood</topic><topic>Cocaine - metabolism</topic><topic>Dopamine Plasma Membrane Transport Proteins</topic><topic>Drug addictions</topic><topic>Esterification</topic><topic>Ethanol</topic><topic>Ethanol - blood</topic><topic>Ethanol - metabolism</topic><topic>Female</topic><topic>Humans</topic><topic>Liver - metabolism</topic><topic>Male</topic><topic>Mazindol - metabolism</topic><topic>Medical sciences</topic><topic>Membrane Glycoproteins</topic><topic>Membrane Transport Proteins</topic><topic>Monoamine uptake sites</topic><topic>Nerve Tissue Proteins</topic><topic>Toxicology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Hearn, W. 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The transesterification of cocaine and ethanol to cocaethylene takes place in the liver and represents a novel metabolic reaction. Cocaethylene was detected in postmortem blood, liver, and neurological tissues in concentrations equal to and sometimes exceeding those of cocaine. In vitro binding studies demonstrate that cocaethylene has a pharmacological profile similar but not identical to that of cocaine at monoamine transport sites assayed in the human brain. Cocaethylene was equipotent to cocaine at inhibiting [3H]mazindol binding to the dopamine transporter. The blockade of dopamine reuptake in the synaptic cleft by cocaethylene may account for the enhanced euphoria associated with combined alcohol and cocaine abuse.</abstract><cop>Oxford, UK</cop><pub>Blackwell Publishing Ltd</pub><pmid>1988563</pmid><doi>10.1111/j.1471-4159.1991.tb08205.x</doi><tpages>4</tpages></addata></record> |
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| subjects | Adult Biological and medical sciences Brain - metabolism Carrier Proteins - metabolism CNS Cocaine Cocaine - analogs & derivatives Cocaine - blood Cocaine - metabolism Dopamine Plasma Membrane Transport Proteins Drug addictions Esterification Ethanol Ethanol - blood Ethanol - metabolism Female Humans Liver - metabolism Male Mazindol - metabolism Medical sciences Membrane Glycoproteins Membrane Transport Proteins Monoamine uptake sites Nerve Tissue Proteins Toxicology |
| title | Cocaethylene: A Unique Cocaine Metabolite Displays High Affinity for the Dopamine Transporter |
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