The effect of 5-HT receptor ligands on the uptake of [ 3H]5-hydroxytryptamine into rat cortical synaptosomes
The effect of 5-HT receptor agonists and antagonists to inhibit [ 3H]5-HT uptake was investigated in rat cortical synaptosomes. The 5-HT (5-hydroxytryptamine) uptake inhibitors paroxetine and fluoxetine yielded pK i values of 8.41 ± 0.12 and 7.43 ± 0.06 respectively. The 5-HT 3/5-HT 4 receptor antag...
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| Veröffentlicht in: | European journal of pharmacology 1993-08, Vol.239 (1), p.211-214 |
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| creator | Cheng, Celine H.K. Costall, Brenda Naylor, Robert J. Rudd, John A. |
| description | The effect of 5-HT receptor agonists and antagonists to inhibit [
3H]5-HT uptake was investigated in rat cortical synaptosomes. The 5-HT (5-hydroxytryptamine) uptake inhibitors paroxetine and fluoxetine yielded pK
i values of 8.41 ± 0.12 and 7.43 ± 0.06 respectively. The 5-HT
3/5-HT
4 receptor antagonist tropisetron and the 5-HT
1A agonist 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) had similar inhibitory potencies to cocaine (pK
i values of 6.58 ± 0.04, 6.47 ± 0.14 and 6.45 ± 0.12 respectively). The dopamine and noradrenaline uptake inhibitors GBR12909 and desipramine had comparable values of 6.5 ± 0.05 and 6.13 ± 0.07. Other 5-HT receptor ligands had pK
i values less than 6.0 (R(+)-zacopride, MDL72222, R(+)/S(−)-zacopride) or 5.0 (5-methoxytryptamine, m-chlorophenylbiguanide, S(−)-zacopride, SDZ205–557, ondansetron and renzapride). It is concluded, with the possible exception of tropisetron and 8-OH-DPAT, that it is unlikely that the effects of the 5-HT receptor ligands to inhibit 5-HT uptake contribute to their effects in vivo. |
| doi_str_mv | 10.1016/0014-2999(93)90996-U |
| format | Article |
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3H]5-HT uptake was investigated in rat cortical synaptosomes. The 5-HT (5-hydroxytryptamine) uptake inhibitors paroxetine and fluoxetine yielded pK
i values of 8.41 ± 0.12 and 7.43 ± 0.06 respectively. The 5-HT
3/5-HT
4 receptor antagonist tropisetron and the 5-HT
1A agonist 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) had similar inhibitory potencies to cocaine (pK
i values of 6.58 ± 0.04, 6.47 ± 0.14 and 6.45 ± 0.12 respectively). The dopamine and noradrenaline uptake inhibitors GBR12909 and desipramine had comparable values of 6.5 ± 0.05 and 6.13 ± 0.07. Other 5-HT receptor ligands had pK
i values less than 6.0 (R(+)-zacopride, MDL72222, R(+)/S(−)-zacopride) or 5.0 (5-methoxytryptamine, m-chlorophenylbiguanide, S(−)-zacopride, SDZ205–557, ondansetron and renzapride). It is concluded, with the possible exception of tropisetron and 8-OH-DPAT, that it is unlikely that the effects of the 5-HT receptor ligands to inhibit 5-HT uptake contribute to their effects in vivo.</description><identifier>ISSN: 0014-2999</identifier><identifier>EISSN: 1879-0712</identifier><identifier>DOI: 10.1016/0014-2999(93)90996-U</identifier><identifier>PMID: 8223895</identifier><identifier>CODEN: EJPHAZ</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>5-HT (5-hydroxytryptamine, serotonin) ; 5-HT receptor ligands ; 8-Hydroxy-2-(di-n-propylamino)tetralin - pharmacology ; [ 3H]5-HT uptake ; Animals ; Biological and medical sciences ; Cerebral Cortex - drug effects ; Cerebral Cortex - metabolism ; Cocaine ; Cocaine - pharmacology ; Cortical synaptosomes (rat) ; Desipramine - pharmacology ; Female ; Fluoxetine - pharmacology ; In Vitro Techniques ; Indoles - pharmacology ; Medical sciences ; Neuropharmacology ; Neurotransmitter Uptake Inhibitors - pharmacology ; Neurotransmitters. Neurotransmission. Receptors ; Paroxetine - pharmacology ; Pharmacology. Drug treatments ; Piperazines - pharmacology ; Rats ; Serotonin - metabolism ; Serotonin Antagonists - pharmacology ; Serotonin Receptor Agonists - pharmacology ; Serotonin Uptake Inhibitors - pharmacology ; Serotoninergic system ; Synaptosomes - drug effects ; Synaptosomes - metabolism ; Tropisetron</subject><ispartof>European journal of pharmacology, 1993-08, Vol.239 (1), p.211-214</ispartof><rights>1993</rights><rights>1993 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c386t-e39730c1725c668f536e7773cb5edcb8006d91e2bb26f8d483cb43594021716e3</citedby><cites>FETCH-LOGICAL-c386t-e39730c1725c668f536e7773cb5edcb8006d91e2bb26f8d483cb43594021716e3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/001429999390996U$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=4862606$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/8223895$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Cheng, Celine H.K.</creatorcontrib><creatorcontrib>Costall, Brenda</creatorcontrib><creatorcontrib>Naylor, Robert J.</creatorcontrib><creatorcontrib>Rudd, John A.</creatorcontrib><title>The effect of 5-HT receptor ligands on the uptake of [ 3H]5-hydroxytryptamine into rat cortical synaptosomes</title><title>European journal of pharmacology</title><addtitle>Eur J Pharmacol</addtitle><description>The effect of 5-HT receptor agonists and antagonists to inhibit [
3H]5-HT uptake was investigated in rat cortical synaptosomes. The 5-HT (5-hydroxytryptamine) uptake inhibitors paroxetine and fluoxetine yielded pK
i values of 8.41 ± 0.12 and 7.43 ± 0.06 respectively. The 5-HT
3/5-HT
4 receptor antagonist tropisetron and the 5-HT
1A agonist 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) had similar inhibitory potencies to cocaine (pK
i values of 6.58 ± 0.04, 6.47 ± 0.14 and 6.45 ± 0.12 respectively). The dopamine and noradrenaline uptake inhibitors GBR12909 and desipramine had comparable values of 6.5 ± 0.05 and 6.13 ± 0.07. Other 5-HT receptor ligands had pK
i values less than 6.0 (R(+)-zacopride, MDL72222, R(+)/S(−)-zacopride) or 5.0 (5-methoxytryptamine, m-chlorophenylbiguanide, S(−)-zacopride, SDZ205–557, ondansetron and renzapride). It is concluded, with the possible exception of tropisetron and 8-OH-DPAT, that it is unlikely that the effects of the 5-HT receptor ligands to inhibit 5-HT uptake contribute to their effects in vivo.</description><subject>5-HT (5-hydroxytryptamine, serotonin)</subject><subject>5-HT receptor ligands</subject><subject>8-Hydroxy-2-(di-n-propylamino)tetralin - pharmacology</subject><subject>[ 3H]5-HT uptake</subject><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Cerebral Cortex - drug effects</subject><subject>Cerebral Cortex - metabolism</subject><subject>Cocaine</subject><subject>Cocaine - pharmacology</subject><subject>Cortical synaptosomes (rat)</subject><subject>Desipramine - pharmacology</subject><subject>Female</subject><subject>Fluoxetine - pharmacology</subject><subject>In Vitro Techniques</subject><subject>Indoles - pharmacology</subject><subject>Medical sciences</subject><subject>Neuropharmacology</subject><subject>Neurotransmitter Uptake Inhibitors - pharmacology</subject><subject>Neurotransmitters. Neurotransmission. Receptors</subject><subject>Paroxetine - pharmacology</subject><subject>Pharmacology. Drug treatments</subject><subject>Piperazines - pharmacology</subject><subject>Rats</subject><subject>Serotonin - metabolism</subject><subject>Serotonin Antagonists - pharmacology</subject><subject>Serotonin Receptor Agonists - pharmacology</subject><subject>Serotonin Uptake Inhibitors - pharmacology</subject><subject>Serotoninergic system</subject><subject>Synaptosomes - drug effects</subject><subject>Synaptosomes - metabolism</subject><subject>Tropisetron</subject><issn>0014-2999</issn><issn>1879-0712</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1993</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kU2LFDEQhoO4rOPqP1DIQUQPrfnofF0WZFFnYWEvMyeRkE5Xu9HuzphkFvvfm3GGOXqqw_vUS_EUQq8o-UAJlR8JoW3DjDHvDH9viDGy2T5BK6qVaYii7ClanZFn6HnOPwkhwjBxiS41Y1wbsULj5gEwDAP4guOARbPe4AQediUmPIYfbu4zjjMuFdvvivsFB-wb5uvvonlY-hT_LCUtNZnCDDjMJeLkCvYxleDdiPMyu1qW4wT5BboY3Jjh5Wleoe2Xz5ubdXN3__X25tNd47mWpQFuFCeeKia8lHoQXIJSivtOQO87TYjsDQXWdUwOum91TVouTEsYVVQCv0Jvj727FH_vIRc7hexhHN0McZ-tkoQJTmgF2yPoU8w5wWB3KUwuLZYSe5BsDwbtwaA13P6TbLd17fWpf99N0J-XTlZr_uaUu1wdDMnNPuQz1mrJJJEVuz5iUF08Bkg2-wCzhz7UFxTbx_D_O_4CkJKYMA</recordid><startdate>19930803</startdate><enddate>19930803</enddate><creator>Cheng, Celine H.K.</creator><creator>Costall, Brenda</creator><creator>Naylor, Robert J.</creator><creator>Rudd, John A.</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>19930803</creationdate><title>The effect of 5-HT receptor ligands on the uptake of [ 3H]5-hydroxytryptamine into rat cortical synaptosomes</title><author>Cheng, Celine H.K. ; Costall, Brenda ; Naylor, Robert J. ; Rudd, John A.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c386t-e39730c1725c668f536e7773cb5edcb8006d91e2bb26f8d483cb43594021716e3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1993</creationdate><topic>5-HT (5-hydroxytryptamine, serotonin)</topic><topic>5-HT receptor ligands</topic><topic>8-Hydroxy-2-(di-n-propylamino)tetralin - pharmacology</topic><topic>[ 3H]5-HT uptake</topic><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Cerebral Cortex - drug effects</topic><topic>Cerebral Cortex - metabolism</topic><topic>Cocaine</topic><topic>Cocaine - pharmacology</topic><topic>Cortical synaptosomes (rat)</topic><topic>Desipramine - pharmacology</topic><topic>Female</topic><topic>Fluoxetine - pharmacology</topic><topic>In Vitro Techniques</topic><topic>Indoles - pharmacology</topic><topic>Medical sciences</topic><topic>Neuropharmacology</topic><topic>Neurotransmitter Uptake Inhibitors - pharmacology</topic><topic>Neurotransmitters. Neurotransmission. Receptors</topic><topic>Paroxetine - pharmacology</topic><topic>Pharmacology. Drug treatments</topic><topic>Piperazines - pharmacology</topic><topic>Rats</topic><topic>Serotonin - metabolism</topic><topic>Serotonin Antagonists - pharmacology</topic><topic>Serotonin Receptor Agonists - pharmacology</topic><topic>Serotonin Uptake Inhibitors - pharmacology</topic><topic>Serotoninergic system</topic><topic>Synaptosomes - drug effects</topic><topic>Synaptosomes - metabolism</topic><topic>Tropisetron</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Cheng, Celine H.K.</creatorcontrib><creatorcontrib>Costall, Brenda</creatorcontrib><creatorcontrib>Naylor, Robert J.</creatorcontrib><creatorcontrib>Rudd, John 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>European journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Cheng, Celine H.K.</au><au>Costall, Brenda</au><au>Naylor, Robert J.</au><au>Rudd, John A.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>The effect of 5-HT receptor ligands on the uptake of [ 3H]5-hydroxytryptamine into rat cortical synaptosomes</atitle><jtitle>European journal of pharmacology</jtitle><addtitle>Eur J Pharmacol</addtitle><date>1993-08-03</date><risdate>1993</risdate><volume>239</volume><issue>1</issue><spage>211</spage><epage>214</epage><pages>211-214</pages><issn>0014-2999</issn><eissn>1879-0712</eissn><coden>EJPHAZ</coden><abstract>The effect of 5-HT receptor agonists and antagonists to inhibit [
3H]5-HT uptake was investigated in rat cortical synaptosomes. The 5-HT (5-hydroxytryptamine) uptake inhibitors paroxetine and fluoxetine yielded pK
i values of 8.41 ± 0.12 and 7.43 ± 0.06 respectively. The 5-HT
3/5-HT
4 receptor antagonist tropisetron and the 5-HT
1A agonist 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) had similar inhibitory potencies to cocaine (pK
i values of 6.58 ± 0.04, 6.47 ± 0.14 and 6.45 ± 0.12 respectively). The dopamine and noradrenaline uptake inhibitors GBR12909 and desipramine had comparable values of 6.5 ± 0.05 and 6.13 ± 0.07. Other 5-HT receptor ligands had pK
i values less than 6.0 (R(+)-zacopride, MDL72222, R(+)/S(−)-zacopride) or 5.0 (5-methoxytryptamine, m-chlorophenylbiguanide, S(−)-zacopride, SDZ205–557, ondansetron and renzapride). It is concluded, with the possible exception of tropisetron and 8-OH-DPAT, that it is unlikely that the effects of the 5-HT receptor ligands to inhibit 5-HT uptake contribute to their effects in vivo.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>8223895</pmid><doi>10.1016/0014-2999(93)90996-U</doi><tpages>4</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0014-2999 |
| ispartof | European journal of pharmacology, 1993-08, Vol.239 (1), p.211-214 |
| issn | 0014-2999 1879-0712 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_76025301 |
| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | 5-HT (5-hydroxytryptamine, serotonin) 5-HT receptor ligands 8-Hydroxy-2-(di-n-propylamino)tetralin - pharmacology [ 3H]5-HT uptake Animals Biological and medical sciences Cerebral Cortex - drug effects Cerebral Cortex - metabolism Cocaine Cocaine - pharmacology Cortical synaptosomes (rat) Desipramine - pharmacology Female Fluoxetine - pharmacology In Vitro Techniques Indoles - pharmacology Medical sciences Neuropharmacology Neurotransmitter Uptake Inhibitors - pharmacology Neurotransmitters. Neurotransmission. Receptors Paroxetine - pharmacology Pharmacology. Drug treatments Piperazines - pharmacology Rats Serotonin - metabolism Serotonin Antagonists - pharmacology Serotonin Receptor Agonists - pharmacology Serotonin Uptake Inhibitors - pharmacology Serotoninergic system Synaptosomes - drug effects Synaptosomes - metabolism Tropisetron |
| title | The effect of 5-HT receptor ligands on the uptake of [ 3H]5-hydroxytryptamine into rat cortical synaptosomes |
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