A nonclassical 5-hydroxytryptamine receptor positively coupled with adenylate cyclase in the central nervous system
A nonclassical 5-hydroxytryptamine (5-HT) receptor mediates the stimulation of adenylate cyclase activity in mouse embryo colliculi neurons in primary culture. The pharmacological profile characterized with agonists and antagonists suggests that this 5-HT receptor does not appear to correspond to a...
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| Veröffentlicht in: | Molecular pharmacology 1988-12, Vol.34 (6), p.880-887 |
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| description | A nonclassical 5-hydroxytryptamine (5-HT) receptor mediates the stimulation of adenylate cyclase activity in mouse embryo
colliculi neurons in primary culture. The pharmacological profile characterized with agonists and antagonists suggests that
this 5-HT receptor does not appear to correspond to a known 5-HT receptor. On this 5-HT receptor, 5-HT (EC50 = 109 +/- 17
nM) and 5-methoxytryptamine (5-MeOT) were equipotent agonists. The other tryptamine derivatives, 5-carboxamidotryptamine (5-CT)
and 5-methoxy-N,N-dimethyltryptamine (5-MeOT-N,N-DMT), were full potent agonists, whereas tryptamine, bufotenine, and 2-CH3-5-HT
were weak partial agonists. Two selective 5-HT1A agonists: 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT) and ipsapirone,
could not stimulate adenylate cyclase. RU 24969, a tetrahydropyridoindole derivative that is a potent 5-HT1A and 5-HT1B agonist
was also inactive, whereas RU 28253, another member of this series, could stimulate cAMP production. The action of antagonists
acting on 5-HT1 or 5-HT2 receptors, such as methiothepin (5-HT1 and 5-HT2), metergoline (5-HT1 and 5-HT2), spiperone (5-HT1A
and 5-HT2), (-)-pindolol (5-HT1B), mesulergine (5-HT1C), and ketanserin (5-HT2), were almost inactive in reversing the 5-HT
stimulating effect. The selective 5-HT3 antagonist ICS 205 930 was a full competitive antagonist at this receptor. Nevertheless,
MDL 72222, which is also a 5-HT3 antagonist, was very weak in antagonizing the 5-HT stimulatory effect. A receptor with similar
characteristics has also been found in guinea pig hippocampal membranes. In these membranes, the second receptor of low affinity
for 5-HT, termed RL, which is positively coupled to adenylate cyclase, was also antagonized by ICS 205 930. The relatively
low affinity of this hippocampal receptor for 5-CT, its stimulation by RU 28253 but not by RU 24969, and its previously reported
pharmacological characteristics support the contention that this 5-HT receptor and the 5-HT receptor of mouse embryo colliculi
neurons in primary culture (both positively coupled to cAMP formation) present great homologies. Inasmuch as none of the classical
specific 5-HT1 and 5-HT2 agonists or antagonists interact with these 5-HT receptors, it is unlikely that they belong to 5-HT1
or 5-HT2 receptor categories. |
| format | Article |
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colliculi neurons in primary culture. The pharmacological profile characterized with agonists and antagonists suggests that
this 5-HT receptor does not appear to correspond to a known 5-HT receptor. On this 5-HT receptor, 5-HT (EC50 = 109 +/- 17
nM) and 5-methoxytryptamine (5-MeOT) were equipotent agonists. The other tryptamine derivatives, 5-carboxamidotryptamine (5-CT)
and 5-methoxy-N,N-dimethyltryptamine (5-MeOT-N,N-DMT), were full potent agonists, whereas tryptamine, bufotenine, and 2-CH3-5-HT
were weak partial agonists. Two selective 5-HT1A agonists: 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT) and ipsapirone,
could not stimulate adenylate cyclase. RU 24969, a tetrahydropyridoindole derivative that is a potent 5-HT1A and 5-HT1B agonist
was also inactive, whereas RU 28253, another member of this series, could stimulate cAMP production. The action of antagonists
acting on 5-HT1 or 5-HT2 receptors, such as methiothepin (5-HT1 and 5-HT2), metergoline (5-HT1 and 5-HT2), spiperone (5-HT1A
and 5-HT2), (-)-pindolol (5-HT1B), mesulergine (5-HT1C), and ketanserin (5-HT2), were almost inactive in reversing the 5-HT
stimulating effect. The selective 5-HT3 antagonist ICS 205 930 was a full competitive antagonist at this receptor. Nevertheless,
MDL 72222, which is also a 5-HT3 antagonist, was very weak in antagonizing the 5-HT stimulatory effect. A receptor with similar
characteristics has also been found in guinea pig hippocampal membranes. In these membranes, the second receptor of low affinity
for 5-HT, termed RL, which is positively coupled to adenylate cyclase, was also antagonized by ICS 205 930. The relatively
low affinity of this hippocampal receptor for 5-CT, its stimulation by RU 28253 but not by RU 24969, and its previously reported
pharmacological characteristics support the contention that this 5-HT receptor and the 5-HT receptor of mouse embryo colliculi
neurons in primary culture (both positively coupled to cAMP formation) present great homologies. Inasmuch as none of the classical
specific 5-HT1 and 5-HT2 agonists or antagonists interact with these 5-HT receptors, it is unlikely that they belong to 5-HT1
or 5-HT2 receptor categories.</description><identifier>ISSN: 0026-895X</identifier><identifier>EISSN: 1521-0111</identifier><identifier>PMID: 2849052</identifier><identifier>CODEN: MOPMA3</identifier><language>eng</language><publisher>Bethesda, MD: American Society for Pharmacology and Experimental Therapeutics</publisher><subject>Adenylyl Cyclase Inhibitors ; Adenylyl Cyclases - metabolism ; Animals ; Biological and medical sciences ; Brain - metabolism ; Central nervous system ; Central neurotransmission. Neuromudulation. Pathways and receptors ; Cyclic AMP - biosynthesis ; Fundamental and applied biological sciences. Psychology ; Guinea Pigs ; Hippocampus - metabolism ; In Vitro Techniques ; Indoles - pharmacology ; Male ; Mice ; Receptors, Serotonin - drug effects ; Receptors, Serotonin - metabolism ; Serotonin - pharmacology ; Serotonin - physiology ; Serotonin Antagonists - pharmacology ; Superior Colliculi - metabolism ; Tryptamines - pharmacology ; Vertebrates: nervous system and sense organs</subject><ispartof>Molecular pharmacology, 1988-12, Vol.34 (6), p.880-887</ispartof><rights>1990 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=6682678$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/2849052$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>DUMUIS, A</creatorcontrib><creatorcontrib>BOUHELAL, R</creatorcontrib><creatorcontrib>SEBBEN, M</creatorcontrib><creatorcontrib>CORY, R</creatorcontrib><creatorcontrib>BOCKAERT, J</creatorcontrib><title>A nonclassical 5-hydroxytryptamine receptor positively coupled with adenylate cyclase in the central nervous system</title><title>Molecular pharmacology</title><addtitle>Mol Pharmacol</addtitle><description>A nonclassical 5-hydroxytryptamine (5-HT) receptor mediates the stimulation of adenylate cyclase activity in mouse embryo
colliculi neurons in primary culture. The pharmacological profile characterized with agonists and antagonists suggests that
this 5-HT receptor does not appear to correspond to a known 5-HT receptor. On this 5-HT receptor, 5-HT (EC50 = 109 +/- 17
nM) and 5-methoxytryptamine (5-MeOT) were equipotent agonists. The other tryptamine derivatives, 5-carboxamidotryptamine (5-CT)
and 5-methoxy-N,N-dimethyltryptamine (5-MeOT-N,N-DMT), were full potent agonists, whereas tryptamine, bufotenine, and 2-CH3-5-HT
were weak partial agonists. Two selective 5-HT1A agonists: 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT) and ipsapirone,
could not stimulate adenylate cyclase. RU 24969, a tetrahydropyridoindole derivative that is a potent 5-HT1A and 5-HT1B agonist
was also inactive, whereas RU 28253, another member of this series, could stimulate cAMP production. The action of antagonists
acting on 5-HT1 or 5-HT2 receptors, such as methiothepin (5-HT1 and 5-HT2), metergoline (5-HT1 and 5-HT2), spiperone (5-HT1A
and 5-HT2), (-)-pindolol (5-HT1B), mesulergine (5-HT1C), and ketanserin (5-HT2), were almost inactive in reversing the 5-HT
stimulating effect. The selective 5-HT3 antagonist ICS 205 930 was a full competitive antagonist at this receptor. Nevertheless,
MDL 72222, which is also a 5-HT3 antagonist, was very weak in antagonizing the 5-HT stimulatory effect. A receptor with similar
characteristics has also been found in guinea pig hippocampal membranes. In these membranes, the second receptor of low affinity
for 5-HT, termed RL, which is positively coupled to adenylate cyclase, was also antagonized by ICS 205 930. The relatively
low affinity of this hippocampal receptor for 5-CT, its stimulation by RU 28253 but not by RU 24969, and its previously reported
pharmacological characteristics support the contention that this 5-HT receptor and the 5-HT receptor of mouse embryo colliculi
neurons in primary culture (both positively coupled to cAMP formation) present great homologies. Inasmuch as none of the classical
specific 5-HT1 and 5-HT2 agonists or antagonists interact with these 5-HT receptors, it is unlikely that they belong to 5-HT1
or 5-HT2 receptor categories.</description><subject>Adenylyl Cyclase Inhibitors</subject><subject>Adenylyl Cyclases - metabolism</subject><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Brain - metabolism</subject><subject>Central nervous system</subject><subject>Central neurotransmission. Neuromudulation. Pathways and receptors</subject><subject>Cyclic AMP - biosynthesis</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>Guinea Pigs</subject><subject>Hippocampus - metabolism</subject><subject>In Vitro Techniques</subject><subject>Indoles - pharmacology</subject><subject>Male</subject><subject>Mice</subject><subject>Receptors, Serotonin - drug effects</subject><subject>Receptors, Serotonin - metabolism</subject><subject>Serotonin - pharmacology</subject><subject>Serotonin - physiology</subject><subject>Serotonin Antagonists - pharmacology</subject><subject>Superior Colliculi - metabolism</subject><subject>Tryptamines - pharmacology</subject><subject>Vertebrates: nervous system and sense organs</subject><issn>0026-895X</issn><issn>1521-0111</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1988</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkEFLHTEUhYdi0aftTxCyqN0NJJNJJlmKVFsQummhu-FO5j4nJZOMSZ6af9-Ij25dXS7fx-FwPjQ7JjrWUsbYSbOjtJOt0uLPWXOe0l9KWS8UPW1OO9VrKrpdk66JD944SMkacES0S5ljeCk5li3Daj2SiAa3HCLZQrLZPqErxITD5nAmzzYvBGb0xUFGYsprFBLrSV7qiz7HmuoxPoVDIqmkjOun5uMeXMLPx3vR_L799uvme3v_8-7HzfV9u3Ra5paz_ax7BJgkB6zF-aw0N3vOmTKUSQa0r2Tu-TTMoteqA02niXYagFI58Ivm61vuFsPjAVMeV5sMOgcea5txUGIYGH9fZIJJ0Q-6ipdH8TCtOI9btCvEMh7nrPzLkUOqa-4jeGPTf01K1clBVe3qTVvsw_JsI47bAnEFE1x4KCPvRzkqRfk_guyODQ</recordid><startdate>19881201</startdate><enddate>19881201</enddate><creator>DUMUIS, A</creator><creator>BOUHELAL, R</creator><creator>SEBBEN, M</creator><creator>CORY, R</creator><creator>BOCKAERT, J</creator><general>American Society for Pharmacology and Experimental Therapeutics</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>7TK</scope><scope>7X8</scope></search><sort><creationdate>19881201</creationdate><title>A nonclassical 5-hydroxytryptamine receptor positively coupled with adenylate cyclase in the central nervous system</title><author>DUMUIS, A ; BOUHELAL, R ; SEBBEN, M ; CORY, R ; BOCKAERT, J</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-h296t-31fd94eaab63ae4583d893cf3318c0161a0463ad43b7d54982a90bb029aa00673</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1988</creationdate><topic>Adenylyl Cyclase Inhibitors</topic><topic>Adenylyl Cyclases - metabolism</topic><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Brain - metabolism</topic><topic>Central nervous system</topic><topic>Central neurotransmission. Neuromudulation. Pathways and receptors</topic><topic>Cyclic AMP - biosynthesis</topic><topic>Fundamental and applied biological sciences. Psychology</topic><topic>Guinea Pigs</topic><topic>Hippocampus - metabolism</topic><topic>In Vitro Techniques</topic><topic>Indoles - pharmacology</topic><topic>Male</topic><topic>Mice</topic><topic>Receptors, Serotonin - drug effects</topic><topic>Receptors, Serotonin - metabolism</topic><topic>Serotonin - pharmacology</topic><topic>Serotonin - physiology</topic><topic>Serotonin Antagonists - pharmacology</topic><topic>Superior Colliculi - metabolism</topic><topic>Tryptamines - pharmacology</topic><topic>Vertebrates: nervous system and sense organs</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>DUMUIS, A</creatorcontrib><creatorcontrib>BOUHELAL, R</creatorcontrib><creatorcontrib>SEBBEN, M</creatorcontrib><creatorcontrib>CORY, R</creatorcontrib><creatorcontrib>BOCKAERT, J</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>Neurosciences Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Molecular pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>DUMUIS, A</au><au>BOUHELAL, R</au><au>SEBBEN, M</au><au>CORY, R</au><au>BOCKAERT, J</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>A nonclassical 5-hydroxytryptamine receptor positively coupled with adenylate cyclase in the central nervous system</atitle><jtitle>Molecular pharmacology</jtitle><addtitle>Mol Pharmacol</addtitle><date>1988-12-01</date><risdate>1988</risdate><volume>34</volume><issue>6</issue><spage>880</spage><epage>887</epage><pages>880-887</pages><issn>0026-895X</issn><eissn>1521-0111</eissn><coden>MOPMA3</coden><abstract>A nonclassical 5-hydroxytryptamine (5-HT) receptor mediates the stimulation of adenylate cyclase activity in mouse embryo
colliculi neurons in primary culture. The pharmacological profile characterized with agonists and antagonists suggests that
this 5-HT receptor does not appear to correspond to a known 5-HT receptor. On this 5-HT receptor, 5-HT (EC50 = 109 +/- 17
nM) and 5-methoxytryptamine (5-MeOT) were equipotent agonists. The other tryptamine derivatives, 5-carboxamidotryptamine (5-CT)
and 5-methoxy-N,N-dimethyltryptamine (5-MeOT-N,N-DMT), were full potent agonists, whereas tryptamine, bufotenine, and 2-CH3-5-HT
were weak partial agonists. Two selective 5-HT1A agonists: 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT) and ipsapirone,
could not stimulate adenylate cyclase. RU 24969, a tetrahydropyridoindole derivative that is a potent 5-HT1A and 5-HT1B agonist
was also inactive, whereas RU 28253, another member of this series, could stimulate cAMP production. The action of antagonists
acting on 5-HT1 or 5-HT2 receptors, such as methiothepin (5-HT1 and 5-HT2), metergoline (5-HT1 and 5-HT2), spiperone (5-HT1A
and 5-HT2), (-)-pindolol (5-HT1B), mesulergine (5-HT1C), and ketanserin (5-HT2), were almost inactive in reversing the 5-HT
stimulating effect. The selective 5-HT3 antagonist ICS 205 930 was a full competitive antagonist at this receptor. Nevertheless,
MDL 72222, which is also a 5-HT3 antagonist, was very weak in antagonizing the 5-HT stimulatory effect. A receptor with similar
characteristics has also been found in guinea pig hippocampal membranes. In these membranes, the second receptor of low affinity
for 5-HT, termed RL, which is positively coupled to adenylate cyclase, was also antagonized by ICS 205 930. The relatively
low affinity of this hippocampal receptor for 5-CT, its stimulation by RU 28253 but not by RU 24969, and its previously reported
pharmacological characteristics support the contention that this 5-HT receptor and the 5-HT receptor of mouse embryo colliculi
neurons in primary culture (both positively coupled to cAMP formation) present great homologies. Inasmuch as none of the classical
specific 5-HT1 and 5-HT2 agonists or antagonists interact with these 5-HT receptors, it is unlikely that they belong to 5-HT1
or 5-HT2 receptor categories.</abstract><cop>Bethesda, MD</cop><pub>American Society for Pharmacology and Experimental Therapeutics</pub><pmid>2849052</pmid><tpages>8</tpages></addata></record> |
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| ispartof | Molecular pharmacology, 1988-12, Vol.34 (6), p.880-887 |
| issn | 0026-895X 1521-0111 |
| language | eng |
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| source | MEDLINE; EZB-FREE-00999 freely available EZB journals |
| subjects | Adenylyl Cyclase Inhibitors Adenylyl Cyclases - metabolism Animals Biological and medical sciences Brain - metabolism Central nervous system Central neurotransmission. Neuromudulation. Pathways and receptors Cyclic AMP - biosynthesis Fundamental and applied biological sciences. Psychology Guinea Pigs Hippocampus - metabolism In Vitro Techniques Indoles - pharmacology Male Mice Receptors, Serotonin - drug effects Receptors, Serotonin - metabolism Serotonin - pharmacology Serotonin - physiology Serotonin Antagonists - pharmacology Superior Colliculi - metabolism Tryptamines - pharmacology Vertebrates: nervous system and sense organs |
| title | A nonclassical 5-hydroxytryptamine receptor positively coupled with adenylate cyclase in the central nervous system |
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