The effects of non-medically used psychoactive drugs on monoamine neurotransmission in rat brain
We developed a reproducible, simple, and small-scale method for determining the re-uptake and release of monoamines (dopamine, serotonin (5-HT) and norepinephrine) using rat brain synaptosomes. These assays were then applied to study the effects of different kinds of non-medically used psychoactive...
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| Veröffentlicht in: | European journal of pharmacology 2007-03, Vol.559 (2), p.132-137 |
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| creator | Nagai, Fumiko Nonaka, Ryouichi Satoh Hisashi Kamimura, Kanako |
| description | We developed a reproducible, simple, and small-scale method for determining the re-uptake and release of monoamines (dopamine, serotonin (5-HT) and norepinephrine) using rat brain synaptosomes. These assays were then applied to study the effects of different kinds of non-medically used psychoactive drugs on monoamine re-uptake and release. The phenethylamine derivatives, 4-fluoroamphetamine, 2-methylamino-3,4-methylene-dioxy-propiophenone (methylone), 1-(1,3-benzodioxol-5-yl)-2-butanamine (BDB), and
N-methyl-1-(1,3-benzodioxol-5-yl)-2-butanamine (MBDB), had strong inhibitory effects on the re-uptake of dopamine, 5-HT and norepinephrine. 4-Fluoroamphetamine, methylone and BDB also strongly increased the release of the three monoamines, but MBDB increased 5-HT and norepinephrine release, but had little effect on dopamine release. However, 2,5-dimethoxy-4-iodophenethylamine (2C-I), 2,5-dimethoxy-4-ethylphenethylamine (2C-E), 2,5-dimethoxy-4-chlorophenethylamine (2C-C), 2,4,5-trimethoxyamphetamine (TMA-2) and 2,4,6-trimethoxyamphetamine (TMA-6), which are methoxylated phenethylamine derivatives, slightly influenced the re-uptake and release of monoamines. α-Metyltryptamine (AMT), a tryptamine derivative, was one of the strongest re-uptake inhibitors and releasers of the three monoamines. The tryptamine derivative, 5-methoxy-α-methyltryptamine (5-MeO-AMT), also strongly inhibited re-uptake and increased the release of the three monoamines.
N,
N-dipropyltryptamine (DPT), 5-methoxy-
N,
N-diisopropyltryptamine (5-MeO-DIPT), 5-methoxy-
N,
N-methylisopropyltryptamine (5-MeO-MIPT), and 5-methoxy-
N,
N-dimethyltryptamine (5-MeO-DMT) inhibited monoamine re-uptake, but had a few effects on monoamine release. 1-(3-Chlorophenyl)piperazine (3CPP) and 1-(methoxyphenyl)piperazine (4MPP), which are piperazine derivatives, inhibited monoamine re-uptake and accelerated their release. The results suggest that some designer drugs strongly act on the central nerve system to the same extent as restricted drugs. |
| doi_str_mv | 10.1016/j.ejphar.2006.11.075 |
| format | Article |
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N-methyl-1-(1,3-benzodioxol-5-yl)-2-butanamine (MBDB), had strong inhibitory effects on the re-uptake of dopamine, 5-HT and norepinephrine. 4-Fluoroamphetamine, methylone and BDB also strongly increased the release of the three monoamines, but MBDB increased 5-HT and norepinephrine release, but had little effect on dopamine release. However, 2,5-dimethoxy-4-iodophenethylamine (2C-I), 2,5-dimethoxy-4-ethylphenethylamine (2C-E), 2,5-dimethoxy-4-chlorophenethylamine (2C-C), 2,4,5-trimethoxyamphetamine (TMA-2) and 2,4,6-trimethoxyamphetamine (TMA-6), which are methoxylated phenethylamine derivatives, slightly influenced the re-uptake and release of monoamines. α-Metyltryptamine (AMT), a tryptamine derivative, was one of the strongest re-uptake inhibitors and releasers of the three monoamines. The tryptamine derivative, 5-methoxy-α-methyltryptamine (5-MeO-AMT), also strongly inhibited re-uptake and increased the release of the three monoamines.
N,
N-dipropyltryptamine (DPT), 5-methoxy-
N,
N-diisopropyltryptamine (5-MeO-DIPT), 5-methoxy-
N,
N-methylisopropyltryptamine (5-MeO-MIPT), and 5-methoxy-
N,
N-dimethyltryptamine (5-MeO-DMT) inhibited monoamine re-uptake, but had a few effects on monoamine release. 1-(3-Chlorophenyl)piperazine (3CPP) and 1-(methoxyphenyl)piperazine (4MPP), which are piperazine derivatives, inhibited monoamine re-uptake and accelerated their release. The results suggest that some designer drugs strongly act on the central nerve system to the same extent as restricted drugs.</description><identifier>ISSN: 0014-2999</identifier><identifier>EISSN: 1879-0712</identifier><identifier>DOI: 10.1016/j.ejphar.2006.11.075</identifier><identifier>PMID: 17223101</identifier><identifier>CODEN: EJPHAZ</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>5-MeO-AMT ; 5-MeO-DIPT ; 5-MeO-MIPT ; Adrenergic Uptake Inhibitors - pharmacology ; AMT ; Animals ; Biogenic Monoamines - metabolism ; Biological and medical sciences ; Biological Assay - methods ; Brain - drug effects ; Brain - metabolism ; Designer Drugs - pharmacology ; Dopamine - metabolism ; Dopamine Uptake Inhibitors - pharmacology ; Dose-Response Relationship, Drug ; In Vitro Techniques ; Male ; MBDB ; Medical sciences ; Methylone ; Monoamines ; Norepinephrine - metabolism ; Pharmacology. Drug treatments ; Phenethylamine ; Piperazine ; Psychoactive drug ; Psychotropic Drugs - pharmacology ; Rats ; Rats, Sprague-Dawley ; Reproducibility of Results ; Serotonin - metabolism ; Serotonin Uptake Inhibitors - pharmacology ; Synaptic Transmission - drug effects ; Synaptosomes - drug effects ; Synaptosomes - metabolism ; Tryptamine</subject><ispartof>European journal of pharmacology, 2007-03, Vol.559 (2), p.132-137</ispartof><rights>2006 Elsevier B.V.</rights><rights>2007 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c507t-2fc54656a7f99e398272b069b01c121920d5162bce83766a4712917123e0ab8c3</citedby><cites>FETCH-LOGICAL-c507t-2fc54656a7f99e398272b069b01c121920d5162bce83766a4712917123e0ab8c3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0014299906013811$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=18583542$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/17223101$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Nagai, Fumiko</creatorcontrib><creatorcontrib>Nonaka, Ryouichi</creatorcontrib><creatorcontrib>Satoh Hisashi Kamimura, Kanako</creatorcontrib><title>The effects of non-medically used psychoactive drugs on monoamine neurotransmission in rat brain</title><title>European journal of pharmacology</title><addtitle>Eur J Pharmacol</addtitle><description>We developed a reproducible, simple, and small-scale method for determining the re-uptake and release of monoamines (dopamine, serotonin (5-HT) and norepinephrine) using rat brain synaptosomes. These assays were then applied to study the effects of different kinds of non-medically used psychoactive drugs on monoamine re-uptake and release. The phenethylamine derivatives, 4-fluoroamphetamine, 2-methylamino-3,4-methylene-dioxy-propiophenone (methylone), 1-(1,3-benzodioxol-5-yl)-2-butanamine (BDB), and
N-methyl-1-(1,3-benzodioxol-5-yl)-2-butanamine (MBDB), had strong inhibitory effects on the re-uptake of dopamine, 5-HT and norepinephrine. 4-Fluoroamphetamine, methylone and BDB also strongly increased the release of the three monoamines, but MBDB increased 5-HT and norepinephrine release, but had little effect on dopamine release. However, 2,5-dimethoxy-4-iodophenethylamine (2C-I), 2,5-dimethoxy-4-ethylphenethylamine (2C-E), 2,5-dimethoxy-4-chlorophenethylamine (2C-C), 2,4,5-trimethoxyamphetamine (TMA-2) and 2,4,6-trimethoxyamphetamine (TMA-6), which are methoxylated phenethylamine derivatives, slightly influenced the re-uptake and release of monoamines. α-Metyltryptamine (AMT), a tryptamine derivative, was one of the strongest re-uptake inhibitors and releasers of the three monoamines. The tryptamine derivative, 5-methoxy-α-methyltryptamine (5-MeO-AMT), also strongly inhibited re-uptake and increased the release of the three monoamines.
N,
N-dipropyltryptamine (DPT), 5-methoxy-
N,
N-diisopropyltryptamine (5-MeO-DIPT), 5-methoxy-
N,
N-methylisopropyltryptamine (5-MeO-MIPT), and 5-methoxy-
N,
N-dimethyltryptamine (5-MeO-DMT) inhibited monoamine re-uptake, but had a few effects on monoamine release. 1-(3-Chlorophenyl)piperazine (3CPP) and 1-(methoxyphenyl)piperazine (4MPP), which are piperazine derivatives, inhibited monoamine re-uptake and accelerated their release. The results suggest that some designer drugs strongly act on the central nerve system to the same extent as restricted drugs.</description><subject>5-MeO-AMT</subject><subject>5-MeO-DIPT</subject><subject>5-MeO-MIPT</subject><subject>Adrenergic Uptake Inhibitors - pharmacology</subject><subject>AMT</subject><subject>Animals</subject><subject>Biogenic Monoamines - metabolism</subject><subject>Biological and medical sciences</subject><subject>Biological Assay - methods</subject><subject>Brain - drug effects</subject><subject>Brain - metabolism</subject><subject>Designer Drugs - pharmacology</subject><subject>Dopamine - metabolism</subject><subject>Dopamine Uptake Inhibitors - pharmacology</subject><subject>Dose-Response Relationship, Drug</subject><subject>In Vitro Techniques</subject><subject>Male</subject><subject>MBDB</subject><subject>Medical sciences</subject><subject>Methylone</subject><subject>Monoamines</subject><subject>Norepinephrine - metabolism</subject><subject>Pharmacology. Drug treatments</subject><subject>Phenethylamine</subject><subject>Piperazine</subject><subject>Psychoactive drug</subject><subject>Psychotropic Drugs - pharmacology</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>Reproducibility of Results</subject><subject>Serotonin - metabolism</subject><subject>Serotonin Uptake Inhibitors - pharmacology</subject><subject>Synaptic Transmission - drug effects</subject><subject>Synaptosomes - drug effects</subject><subject>Synaptosomes - metabolism</subject><subject>Tryptamine</subject><issn>0014-2999</issn><issn>1879-0712</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2007</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kcFu1DAQhi0EotvCG1SVL3BLGDuxHV-Q0Kq0lSpxKWfjOBPWq8Re7KTSvj0uu1JvXMaH-ebXzGdCrhnUDJj8sq9xf9jZVHMAWTNWgxJvyIZ1SlegGH9LNgCsrbjW-oJc5rwHAKG5eE8umOK8KSkb8utphxTHEd2SaRxpiKGacfDOTtORrhkHeshHt4vWLf4Z6ZDW3wUMdI4h2tkHpAHXFJdkQ559zr70fKDJLrRP1ocP5N1op4wfz-8V-fn99ml7Xz3-uHvYfnusnAC1VHx0opVCWjVqjY3uuOI9SN0Dc4wzzWEQTPLeYdcoKW1bLtSslAbB9p1rrsjnU-4hxT8r5sWUbRxOkw0Y12wUcC4bJQrYnkCXYs4JR3NIfrbpaBiYF7Nmb05mzYtZw5iBf2M35_y1L4Jeh84qC_DpDNhc7I1FiPP5letE14iWF-7ricNi49ljMtl5DK5IT-UXzBD9_zf5C53GmKk</recordid><startdate>20070322</startdate><enddate>20070322</enddate><creator>Nagai, Fumiko</creator><creator>Nonaka, Ryouichi</creator><creator>Satoh Hisashi Kamimura, Kanako</creator><general>Elsevier B.V</general><general>Elsevier</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>20070322</creationdate><title>The effects of non-medically used psychoactive drugs on monoamine neurotransmission in rat brain</title><author>Nagai, Fumiko ; Nonaka, Ryouichi ; Satoh Hisashi Kamimura, Kanako</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c507t-2fc54656a7f99e398272b069b01c121920d5162bce83766a4712917123e0ab8c3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2007</creationdate><topic>5-MeO-AMT</topic><topic>5-MeO-DIPT</topic><topic>5-MeO-MIPT</topic><topic>Adrenergic Uptake Inhibitors - pharmacology</topic><topic>AMT</topic><topic>Animals</topic><topic>Biogenic Monoamines - metabolism</topic><topic>Biological and medical sciences</topic><topic>Biological Assay - methods</topic><topic>Brain - drug effects</topic><topic>Brain - metabolism</topic><topic>Designer Drugs - pharmacology</topic><topic>Dopamine - metabolism</topic><topic>Dopamine Uptake Inhibitors - pharmacology</topic><topic>Dose-Response Relationship, Drug</topic><topic>In Vitro Techniques</topic><topic>Male</topic><topic>MBDB</topic><topic>Medical sciences</topic><topic>Methylone</topic><topic>Monoamines</topic><topic>Norepinephrine - metabolism</topic><topic>Pharmacology. Drug treatments</topic><topic>Phenethylamine</topic><topic>Piperazine</topic><topic>Psychoactive drug</topic><topic>Psychotropic Drugs - pharmacology</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>Reproducibility of Results</topic><topic>Serotonin - metabolism</topic><topic>Serotonin Uptake Inhibitors - pharmacology</topic><topic>Synaptic Transmission - drug effects</topic><topic>Synaptosomes - drug effects</topic><topic>Synaptosomes - metabolism</topic><topic>Tryptamine</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Nagai, Fumiko</creatorcontrib><creatorcontrib>Nonaka, Ryouichi</creatorcontrib><creatorcontrib>Satoh Hisashi Kamimura, Kanako</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>European journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Nagai, Fumiko</au><au>Nonaka, Ryouichi</au><au>Satoh Hisashi Kamimura, Kanako</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>The effects of non-medically used psychoactive drugs on monoamine neurotransmission in rat brain</atitle><jtitle>European journal of pharmacology</jtitle><addtitle>Eur J Pharmacol</addtitle><date>2007-03-22</date><risdate>2007</risdate><volume>559</volume><issue>2</issue><spage>132</spage><epage>137</epage><pages>132-137</pages><issn>0014-2999</issn><eissn>1879-0712</eissn><coden>EJPHAZ</coden><abstract>We developed a reproducible, simple, and small-scale method for determining the re-uptake and release of monoamines (dopamine, serotonin (5-HT) and norepinephrine) using rat brain synaptosomes. These assays were then applied to study the effects of different kinds of non-medically used psychoactive drugs on monoamine re-uptake and release. The phenethylamine derivatives, 4-fluoroamphetamine, 2-methylamino-3,4-methylene-dioxy-propiophenone (methylone), 1-(1,3-benzodioxol-5-yl)-2-butanamine (BDB), and
N-methyl-1-(1,3-benzodioxol-5-yl)-2-butanamine (MBDB), had strong inhibitory effects on the re-uptake of dopamine, 5-HT and norepinephrine. 4-Fluoroamphetamine, methylone and BDB also strongly increased the release of the three monoamines, but MBDB increased 5-HT and norepinephrine release, but had little effect on dopamine release. However, 2,5-dimethoxy-4-iodophenethylamine (2C-I), 2,5-dimethoxy-4-ethylphenethylamine (2C-E), 2,5-dimethoxy-4-chlorophenethylamine (2C-C), 2,4,5-trimethoxyamphetamine (TMA-2) and 2,4,6-trimethoxyamphetamine (TMA-6), which are methoxylated phenethylamine derivatives, slightly influenced the re-uptake and release of monoamines. α-Metyltryptamine (AMT), a tryptamine derivative, was one of the strongest re-uptake inhibitors and releasers of the three monoamines. The tryptamine derivative, 5-methoxy-α-methyltryptamine (5-MeO-AMT), also strongly inhibited re-uptake and increased the release of the three monoamines.
N,
N-dipropyltryptamine (DPT), 5-methoxy-
N,
N-diisopropyltryptamine (5-MeO-DIPT), 5-methoxy-
N,
N-methylisopropyltryptamine (5-MeO-MIPT), and 5-methoxy-
N,
N-dimethyltryptamine (5-MeO-DMT) inhibited monoamine re-uptake, but had a few effects on monoamine release. 1-(3-Chlorophenyl)piperazine (3CPP) and 1-(methoxyphenyl)piperazine (4MPP), which are piperazine derivatives, inhibited monoamine re-uptake and accelerated their release. The results suggest that some designer drugs strongly act on the central nerve system to the same extent as restricted drugs.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>17223101</pmid><doi>10.1016/j.ejphar.2006.11.075</doi><tpages>6</tpages></addata></record> |
| fulltext | fulltext |
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| ispartof | European journal of pharmacology, 2007-03, Vol.559 (2), p.132-137 |
| issn | 0014-2999 1879-0712 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | 5-MeO-AMT 5-MeO-DIPT 5-MeO-MIPT Adrenergic Uptake Inhibitors - pharmacology AMT Animals Biogenic Monoamines - metabolism Biological and medical sciences Biological Assay - methods Brain - drug effects Brain - metabolism Designer Drugs - pharmacology Dopamine - metabolism Dopamine Uptake Inhibitors - pharmacology Dose-Response Relationship, Drug In Vitro Techniques Male MBDB Medical sciences Methylone Monoamines Norepinephrine - metabolism Pharmacology. Drug treatments Phenethylamine Piperazine Psychoactive drug Psychotropic Drugs - pharmacology Rats Rats, Sprague-Dawley Reproducibility of Results Serotonin - metabolism Serotonin Uptake Inhibitors - pharmacology Synaptic Transmission - drug effects Synaptosomes - drug effects Synaptosomes - metabolism Tryptamine |
| title | The effects of non-medically used psychoactive drugs on monoamine neurotransmission in rat brain |
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