Pharmacological aspects of R-(+)-7-OH-DPAT, a putative dopamine D3 receptor ligand
The R-(+)-isomer of 7-hydroxy-2-(N,N-di-n-propylamino)tetralin (7-OH-DPAT) bound with a more than 200-fold higher affinity to cloned human dopamine D3 receptors (Ki = 0.57 nM) than to dopamine D2 receptors; the corresponding S-(-)-enantiomer had considerably less affinity for both dopamine receptor...
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| Veröffentlicht in: | European journal of pharmacology 1993-11, Vol.249 (3), p.R9-R10 |
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| container_issue | 3 |
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| container_title | European journal of pharmacology |
| container_volume | 249 |
| creator | DAMSMA, G BOTTEMA, T WESTERINK, B. H. C TEPPER, P. G DIJKSTRA, D PUGSLEY, T. A MACKENZIE, R. G HEFFNER, T. G WIKSTRÖM, H |
| description | The R-(+)-isomer of 7-hydroxy-2-(N,N-di-n-propylamino)tetralin (7-OH-DPAT) bound with a more than 200-fold higher affinity to cloned human dopamine D3 receptors (Ki = 0.57 nM) than to dopamine D2 receptors; the corresponding S-(-)-enantiomer had considerably less affinity for both dopamine receptor subtypes, indicating that the known enantiomer selectivity of 7-OH-DPAT for the 'classical' dopamine D2 receptor subtype extends to the recently discovered dopamine D3 receptor subtype. In rats R-(+)-7-OH-DPAT dose dependently (10-1000 nmol/kg) decreased dopamine release and induced yawning, while sniffing behaviour occurred at the highest dose tested (1000 nmol/kg). The possibility that the inhibition of dopamine release and the elicitation of yawning are mediated by dopamine D3 receptors is considered. |
| doi_str_mv | 10.1016/0014-2999(93)90533-n |
| format | Article |
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The possibility that the inhibition of dopamine release and the elicitation of yawning are mediated by dopamine D3 receptors is considered.</description><identifier>ISSN: 0014-2999</identifier><identifier>EISSN: 1879-0712</identifier><identifier>DOI: 10.1016/0014-2999(93)90533-n</identifier><identifier>PMID: 8287911</identifier><identifier>CODEN: EJPHAZ</identifier><language>eng</language><publisher>Amsterdam: Elsevier</publisher><subject>Animals ; Behavior, Animal - drug effects ; Biological and medical sciences ; Catecholaminergic system ; Dopamine - metabolism ; Dose-Response Relationship, Drug ; Male ; Medical sciences ; Neuropharmacology ; Neurotransmitters. Neurotransmission. Receptors ; Pharmacology. Drug treatments ; Rats ; Rats, Wistar ; Receptors, Dopamine - drug effects ; Receptors, Dopamine - metabolism ; Receptors, Dopamine D2 ; Receptors, Dopamine D3 ; Stereoisomerism ; Tetrahydronaphthalenes - metabolism ; Tetrahydronaphthalenes - pharmacology ; Yawning - drug effects</subject><ispartof>European journal of pharmacology, 1993-11, Vol.249 (3), p.R9-R10</ispartof><rights>1994 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c312t-3e8544454c00e654c0e78be013b3ee37aa269174dcaff47a4f9def378e0f345b3</citedby><cites>FETCH-LOGICAL-c312t-3e8544454c00e654c0e78be013b3ee37aa269174dcaff47a4f9def378e0f345b3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=3807167$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/8287911$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>DAMSMA, G</creatorcontrib><creatorcontrib>BOTTEMA, T</creatorcontrib><creatorcontrib>WESTERINK, B. H. C</creatorcontrib><creatorcontrib>TEPPER, P. G</creatorcontrib><creatorcontrib>DIJKSTRA, D</creatorcontrib><creatorcontrib>PUGSLEY, T. A</creatorcontrib><creatorcontrib>MACKENZIE, R. G</creatorcontrib><creatorcontrib>HEFFNER, T. G</creatorcontrib><creatorcontrib>WIKSTRÖM, H</creatorcontrib><title>Pharmacological aspects of R-(+)-7-OH-DPAT, a putative dopamine D3 receptor ligand</title><title>European journal of pharmacology</title><addtitle>Eur J Pharmacol</addtitle><description>The R-(+)-isomer of 7-hydroxy-2-(N,N-di-n-propylamino)tetralin (7-OH-DPAT) bound with a more than 200-fold higher affinity to cloned human dopamine D3 receptors (Ki = 0.57 nM) than to dopamine D2 receptors; the corresponding S-(-)-enantiomer had considerably less affinity for both dopamine receptor subtypes, indicating that the known enantiomer selectivity of 7-OH-DPAT for the 'classical' dopamine D2 receptor subtype extends to the recently discovered dopamine D3 receptor subtype. In rats R-(+)-7-OH-DPAT dose dependently (10-1000 nmol/kg) decreased dopamine release and induced yawning, while sniffing behaviour occurred at the highest dose tested (1000 nmol/kg). The possibility that the inhibition of dopamine release and the elicitation of yawning are mediated by dopamine D3 receptors is considered.</description><subject>Animals</subject><subject>Behavior, Animal - drug effects</subject><subject>Biological and medical sciences</subject><subject>Catecholaminergic system</subject><subject>Dopamine - metabolism</subject><subject>Dose-Response Relationship, Drug</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Neuropharmacology</subject><subject>Neurotransmitters. Neurotransmission. Receptors</subject><subject>Pharmacology. Drug treatments</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>Receptors, Dopamine - drug effects</subject><subject>Receptors, Dopamine - metabolism</subject><subject>Receptors, Dopamine D2</subject><subject>Receptors, Dopamine D3</subject><subject>Stereoisomerism</subject><subject>Tetrahydronaphthalenes - metabolism</subject><subject>Tetrahydronaphthalenes - pharmacology</subject><subject>Yawning - drug effects</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>eNo9kUtLAzEUhYMoWh__QCELEUWjySQzmSyLbxBbSl2H28yNjszLZCr4751q6eouznfO4ruEHAt-LbjIbjgXiiXGmHMjLwxPpWTNFhmJXBvGtUi2yWiD7JH9GD8556lJ0l2ymycDJcSIzKYfEGpwbdW-lw4qCrFD10faejpj55cXTLPJE7ubjudXFGi37KEvv5EWbQd12SC9kzSgw65vA63Kd2iKQ7LjoYp4tL4H5O3hfn77xF4mj8-34xfmpEh6JjFPlVKpcpxjtjqo8wVyIRcSUWqAJDNCq8KB90qD8qZAL3WO3EuVLuQBOfvf7UL7tcTY27qMDqsKGmyX0epM6CRN8wFU_6ALbYwBve1CWUP4sYLblUq78mRXnqyR9k-lfR1qJ-v95aLGYlNauxvy03UOcTDnAzSujBtM5sMTMi1_AZKheXs</recordid><startdate>19931116</startdate><enddate>19931116</enddate><creator>DAMSMA, G</creator><creator>BOTTEMA, T</creator><creator>WESTERINK, B. 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G ; WIKSTRÖM, H</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c312t-3e8544454c00e654c0e78be013b3ee37aa269174dcaff47a4f9def378e0f345b3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1993</creationdate><topic>Animals</topic><topic>Behavior, Animal - drug effects</topic><topic>Biological and medical sciences</topic><topic>Catecholaminergic system</topic><topic>Dopamine - metabolism</topic><topic>Dose-Response Relationship, Drug</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Neuropharmacology</topic><topic>Neurotransmitters. Neurotransmission. Receptors</topic><topic>Pharmacology. 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G</creatorcontrib><creatorcontrib>WIKSTRÖM, H</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>DAMSMA, G</au><au>BOTTEMA, T</au><au>WESTERINK, B. H. C</au><au>TEPPER, P. G</au><au>DIJKSTRA, D</au><au>PUGSLEY, T. A</au><au>MACKENZIE, R. G</au><au>HEFFNER, T. G</au><au>WIKSTRÖM, H</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Pharmacological aspects of R-(+)-7-OH-DPAT, a putative dopamine D3 receptor ligand</atitle><jtitle>European journal of pharmacology</jtitle><addtitle>Eur J Pharmacol</addtitle><date>1993-11-16</date><risdate>1993</risdate><volume>249</volume><issue>3</issue><spage>R9</spage><epage>R10</epage><pages>R9-R10</pages><issn>0014-2999</issn><eissn>1879-0712</eissn><coden>EJPHAZ</coden><abstract>The R-(+)-isomer of 7-hydroxy-2-(N,N-di-n-propylamino)tetralin (7-OH-DPAT) bound with a more than 200-fold higher affinity to cloned human dopamine D3 receptors (Ki = 0.57 nM) than to dopamine D2 receptors; the corresponding S-(-)-enantiomer had considerably less affinity for both dopamine receptor subtypes, indicating that the known enantiomer selectivity of 7-OH-DPAT for the 'classical' dopamine D2 receptor subtype extends to the recently discovered dopamine D3 receptor subtype. In rats R-(+)-7-OH-DPAT dose dependently (10-1000 nmol/kg) decreased dopamine release and induced yawning, while sniffing behaviour occurred at the highest dose tested (1000 nmol/kg). The possibility that the inhibition of dopamine release and the elicitation of yawning are mediated by dopamine D3 receptors is considered.</abstract><cop>Amsterdam</cop><pub>Elsevier</pub><pmid>8287911</pmid><doi>10.1016/0014-2999(93)90533-n</doi></addata></record> |
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| ispartof | European journal of pharmacology, 1993-11, Vol.249 (3), p.R9-R10 |
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| language | eng |
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| source | MEDLINE; Access via ScienceDirect (Elsevier) |
| subjects | Animals Behavior, Animal - drug effects Biological and medical sciences Catecholaminergic system Dopamine - metabolism Dose-Response Relationship, Drug Male Medical sciences Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Rats Rats, Wistar Receptors, Dopamine - drug effects Receptors, Dopamine - metabolism Receptors, Dopamine D2 Receptors, Dopamine D3 Stereoisomerism Tetrahydronaphthalenes - metabolism Tetrahydronaphthalenes - pharmacology Yawning - drug effects |
| title | Pharmacological aspects of R-(+)-7-OH-DPAT, a putative dopamine D3 receptor ligand |
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