Effect of the putative 5-HT1A antagonists WAY100135 and SDZ 216-525 on 5-HT neuronal firing in the guinea-pig dorsal raphe nucleus
The selective 5-hydroxytryptamine1A (5-HT1A) agonist 8-hydroxy-2-(di-n-propylamino)tetralin (8-OHDPAT, 0.5-35 micrograms kg-1 i.v.) produces a dose related reversible inhibition (ED50 = 6.5 micrograms kg-1 i.v.) of the firing of serotonergic neurones in the dorsal raphe nucleus of the guinea-pig. Ad...
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| Veröffentlicht in: | Neuropharmacology 1994, Vol.33 (1), p.61-66 |
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| creator | MUNDEY, M. K FLETCHER, A MARSDEN, C. A |
| description | The selective 5-hydroxytryptamine1A (5-HT1A) agonist 8-hydroxy-2-(di-n-propylamino)tetralin (8-OHDPAT, 0.5-35 micrograms kg-1 i.v.) produces a dose related reversible inhibition (ED50 = 6.5 micrograms kg-1 i.v.) of the firing of serotonergic neurones in the dorsal raphe nucleus of the guinea-pig. Administration of N-tert-butyl-3- (4-(2-methoxyphenyl)piperazine-1-yl)-2phenylpropanamide dihydrochloride (WAY100135, 0.5 mg kg-1 i.v.), a specific 5-HT1A antagonist, antagonized the 8-OHDPAT induced inhibition of neuronal firing whilst methyl 4-(4-[4-(1,1,3-trioxo-2H-1,2-benzoisothiazol-2-yl)butyl]-1- piperazinyl) 1 H-indole-2-carboxylate (SDZ 216-525, 0.1-0.5 mg kg-1 i.v.) (also a putative 5-HT1A antagonist) reduced the basal firing of 5-HT neurones and furthermore failed to antagonize the inhibition produced by 8-OHDPAT. These results indicate that WAY 100135 is a silent and selective 5-HT1A antagonist whereas SDZ 216-525 demonstrates a partial agonist activity at the somatodendritic 5-HT1A autoreceptor in the guinea-pig DRN. |
| doi_str_mv | 10.1016/0028-3908(94)90097-3 |
| format | Article |
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Psychology ; Guinea Pigs ; In Vitro Techniques ; Indoles - pharmacology ; Male ; Neurons - drug effects ; Piperazines - pharmacology ; Raphe Nuclei - cytology ; Raphe Nuclei - drug effects ; Serotonin - physiology ; Serotonin Antagonists ; Serotonin Receptor Agonists - pharmacology ; Thiazoles - pharmacology ; Vertebrates: nervous system and sense organs</subject><ispartof>Neuropharmacology, 1994, Vol.33 (1), p.61-66</ispartof><rights>1994 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c331t-db075d83728ab8ebdee5f2ac4b286c6880cacacc253db1c5ce1052cf86550ee33</citedby><cites>FETCH-LOGICAL-c331t-db075d83728ab8ebdee5f2ac4b286c6880cacacc253db1c5ce1052cf86550ee33</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,4023,27922,27923,27924</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=3982285$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/8183439$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>MUNDEY, M. K</creatorcontrib><creatorcontrib>FLETCHER, A</creatorcontrib><creatorcontrib>MARSDEN, C. A</creatorcontrib><title>Effect of the putative 5-HT1A antagonists WAY100135 and SDZ 216-525 on 5-HT neuronal firing in the guinea-pig dorsal raphe nucleus</title><title>Neuropharmacology</title><addtitle>Neuropharmacology</addtitle><description>The selective 5-hydroxytryptamine1A (5-HT1A) agonist 8-hydroxy-2-(di-n-propylamino)tetralin (8-OHDPAT, 0.5-35 micrograms kg-1 i.v.) produces a dose related reversible inhibition (ED50 = 6.5 micrograms kg-1 i.v.) of the firing of serotonergic neurones in the dorsal raphe nucleus of the guinea-pig. Administration of N-tert-butyl-3- (4-(2-methoxyphenyl)piperazine-1-yl)-2phenylpropanamide dihydrochloride (WAY100135, 0.5 mg kg-1 i.v.), a specific 5-HT1A antagonist, antagonized the 8-OHDPAT induced inhibition of neuronal firing whilst methyl 4-(4-[4-(1,1,3-trioxo-2H-1,2-benzoisothiazol-2-yl)butyl]-1- piperazinyl) 1 H-indole-2-carboxylate (SDZ 216-525, 0.1-0.5 mg kg-1 i.v.) (also a putative 5-HT1A antagonist) reduced the basal firing of 5-HT neurones and furthermore failed to antagonize the inhibition produced by 8-OHDPAT. These results indicate that WAY 100135 is a silent and selective 5-HT1A antagonist whereas SDZ 216-525 demonstrates a partial agonist activity at the somatodendritic 5-HT1A autoreceptor in the guinea-pig DRN.</description><subject>8-Hydroxy-2-(di-n-propylamino)tetralin - antagonists & inhibitors</subject><subject>8-Hydroxy-2-(di-n-propylamino)tetralin - pharmacology</subject><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Central nervous system</subject><subject>Dose-Response Relationship, Drug</subject><subject>Electrophysiology</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>Guinea Pigs</subject><subject>In Vitro Techniques</subject><subject>Indoles - pharmacology</subject><subject>Male</subject><subject>Neurons - drug effects</subject><subject>Piperazines - pharmacology</subject><subject>Raphe Nuclei - cytology</subject><subject>Raphe Nuclei - drug effects</subject><subject>Serotonin - physiology</subject><subject>Serotonin Antagonists</subject><subject>Serotonin Receptor Agonists - pharmacology</subject><subject>Thiazoles - pharmacology</subject><subject>Vertebrates: nervous system and sense organs</subject><issn>0028-3908</issn><issn>1873-7064</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1994</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNo9kE9v1DAQxS1EVbYL3wAkHxAqB5fxv8Q5rkqhSJV6oAjBxXKc8WKUdYKdVOLKJye7Xa1GmpHee_MOP0Jec7jiwKsPAMIw2YC5bNT7BqCpmXxGVtzUktVQqedkdYq8IBel_AYAZbg5J-fLlko2K_LvJgT0Ex0CnX4hHefJTfERqWa3D3xDXZrcdkixTIV-3_zgAFzqRe3o148_qeAV00LTIR3yNOGch-R6GmKOaUtjOpRu55jQsTFuaTfksvjZjYueZt_jXF6Ss-D6gq-Od02-fbp5uL5ld_efv1xv7piXkk-sa6HWnZG1MK412HaIOgjnVStM5StjwLtlvNCya7nXHjlo4YOptAZEKdfk3VPvmIc_M5bJ7mLx2Pcu4TAXW1eqbtQCZk3UU9DnoZSMwY457lz-aznYPXq752r3XG2j7AG93fe_OfbP7Q6709OR9eK_PfqueNeH7JKP5RSTjRHCaPkfTh6JhA</recordid><startdate>1994</startdate><enddate>1994</enddate><creator>MUNDEY, M. K</creator><creator>FLETCHER, A</creator><creator>MARSDEN, C. A</creator><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>1994</creationdate><title>Effect of the putative 5-HT1A antagonists WAY100135 and SDZ 216-525 on 5-HT neuronal firing in the guinea-pig dorsal raphe nucleus</title><author>MUNDEY, M. K ; FLETCHER, A ; MARSDEN, C. A</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c331t-db075d83728ab8ebdee5f2ac4b286c6880cacacc253db1c5ce1052cf86550ee33</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1994</creationdate><topic>8-Hydroxy-2-(di-n-propylamino)tetralin - antagonists & inhibitors</topic><topic>8-Hydroxy-2-(di-n-propylamino)tetralin - pharmacology</topic><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Central nervous system</topic><topic>Dose-Response Relationship, Drug</topic><topic>Electrophysiology</topic><topic>Fundamental and applied biological sciences. Psychology</topic><topic>Guinea Pigs</topic><topic>In Vitro Techniques</topic><topic>Indoles - pharmacology</topic><topic>Male</topic><topic>Neurons - drug effects</topic><topic>Piperazines - pharmacology</topic><topic>Raphe Nuclei - cytology</topic><topic>Raphe Nuclei - drug effects</topic><topic>Serotonin - physiology</topic><topic>Serotonin Antagonists</topic><topic>Serotonin Receptor Agonists - pharmacology</topic><topic>Thiazoles - pharmacology</topic><topic>Vertebrates: nervous system and sense organs</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>MUNDEY, M. K</creatorcontrib><creatorcontrib>FLETCHER, A</creatorcontrib><creatorcontrib>MARSDEN, C. 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>Neuropharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>MUNDEY, M. K</au><au>FLETCHER, A</au><au>MARSDEN, C. A</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Effect of the putative 5-HT1A antagonists WAY100135 and SDZ 216-525 on 5-HT neuronal firing in the guinea-pig dorsal raphe nucleus</atitle><jtitle>Neuropharmacology</jtitle><addtitle>Neuropharmacology</addtitle><date>1994</date><risdate>1994</risdate><volume>33</volume><issue>1</issue><spage>61</spage><epage>66</epage><pages>61-66</pages><issn>0028-3908</issn><eissn>1873-7064</eissn><coden>NEPHBW</coden><abstract>The selective 5-hydroxytryptamine1A (5-HT1A) agonist 8-hydroxy-2-(di-n-propylamino)tetralin (8-OHDPAT, 0.5-35 micrograms kg-1 i.v.) produces a dose related reversible inhibition (ED50 = 6.5 micrograms kg-1 i.v.) of the firing of serotonergic neurones in the dorsal raphe nucleus of the guinea-pig. Administration of N-tert-butyl-3- (4-(2-methoxyphenyl)piperazine-1-yl)-2phenylpropanamide dihydrochloride (WAY100135, 0.5 mg kg-1 i.v.), a specific 5-HT1A antagonist, antagonized the 8-OHDPAT induced inhibition of neuronal firing whilst methyl 4-(4-[4-(1,1,3-trioxo-2H-1,2-benzoisothiazol-2-yl)butyl]-1- piperazinyl) 1 H-indole-2-carboxylate (SDZ 216-525, 0.1-0.5 mg kg-1 i.v.) (also a putative 5-HT1A antagonist) reduced the basal firing of 5-HT neurones and furthermore failed to antagonize the inhibition produced by 8-OHDPAT. These results indicate that WAY 100135 is a silent and selective 5-HT1A antagonist whereas SDZ 216-525 demonstrates a partial agonist activity at the somatodendritic 5-HT1A autoreceptor in the guinea-pig DRN.</abstract><cop>Oxford</cop><pub>Elsevier</pub><pmid>8183439</pmid><doi>10.1016/0028-3908(94)90097-3</doi><tpages>6</tpages></addata></record> |
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| subjects | 8-Hydroxy-2-(di-n-propylamino)tetralin - antagonists & inhibitors 8-Hydroxy-2-(di-n-propylamino)tetralin - pharmacology Animals Biological and medical sciences Central nervous system Dose-Response Relationship, Drug Electrophysiology Fundamental and applied biological sciences. Psychology Guinea Pigs In Vitro Techniques Indoles - pharmacology Male Neurons - drug effects Piperazines - pharmacology Raphe Nuclei - cytology Raphe Nuclei - drug effects Serotonin - physiology Serotonin Antagonists Serotonin Receptor Agonists - pharmacology Thiazoles - pharmacology Vertebrates: nervous system and sense organs |
| title | Effect of the putative 5-HT1A antagonists WAY100135 and SDZ 216-525 on 5-HT neuronal firing in the guinea-pig dorsal raphe nucleus |
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