Neuropharmacology of a new potential anxiolytic compound, F 2692, 1-(3'-trifluoromethyl phenyl) 1,4-dihydro 3-amino 4-oxo 6-methyl pyridazine. 1. Acute and in vitro effects
F 2692 [1-(3'-trifluoromethyl phenyl) 1,4-dihydro 3-amino 4-oxo 6-methyl pyridazine] exhibited dose-dependent "anxiolytic" properties in the elevated plus-maze and the punished drinking tests in rats. It was also active in the two-compartment test in mice. The "anxiolytic" e...
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| Veröffentlicht in: | Psychopharmacology 1993, Vol.110 (1-2), p.13-18 |
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| creator | Assié, M B Chopin, P Stenger, A Palmier, C Briley, M |
| description | F 2692 [1-(3'-trifluoromethyl phenyl) 1,4-dihydro 3-amino 4-oxo 6-methyl pyridazine] exhibited dose-dependent "anxiolytic" properties in the elevated plus-maze and the punished drinking tests in rats. It was also active in the two-compartment test in mice. The "anxiolytic" effects were antagonised by the benzodiazepine antagonists, flumazenil and ZK 93426. The compound exhibited anticonvulsant, sedative, myorelaxant and amnesic effects at doses 3-30 times higher than those required for "anxiolytic" activity. F 2692 has a very low affinity for benzodiazepine binding sites in vitro and in vivo (about 1000 and 160 fold lower than diazepam respectively). In addition it displayed no affinity for GABAA, alpha 2-adrenergic, 5-HT1A or 5-HT2 receptors. These data suggest that F 2692 may be a potential anxiolytic compound with an unusual mechanism of action. |
| doi_str_mv | 10.1007/BF02246945 |
| format | Article |
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Acute and in vitro effects</title><source>MEDLINE</source><source>SpringerLink Journals - AutoHoldings</source><creator>Assié, M B ; Chopin, P ; Stenger, A ; Palmier, C ; Briley, M</creator><creatorcontrib>Assié, M B ; Chopin, P ; Stenger, A ; Palmier, C ; Briley, M</creatorcontrib><description>F 2692 [1-(3'-trifluoromethyl phenyl) 1,4-dihydro 3-amino 4-oxo 6-methyl pyridazine] exhibited dose-dependent "anxiolytic" properties in the elevated plus-maze and the punished drinking tests in rats. It was also active in the two-compartment test in mice. The "anxiolytic" effects were antagonised by the benzodiazepine antagonists, flumazenil and ZK 93426. The compound exhibited anticonvulsant, sedative, myorelaxant and amnesic effects at doses 3-30 times higher than those required for "anxiolytic" activity. F 2692 has a very low affinity for benzodiazepine binding sites in vitro and in vivo (about 1000 and 160 fold lower than diazepam respectively). In addition it displayed no affinity for GABAA, alpha 2-adrenergic, 5-HT1A or 5-HT2 receptors. These data suggest that F 2692 may be a potential anxiolytic compound with an unusual mechanism of action.</description><identifier>ISSN: 0033-3158</identifier><identifier>EISSN: 1432-2072</identifier><identifier>DOI: 10.1007/BF02246945</identifier><identifier>PMID: 7870872</identifier><language>eng</language><publisher>Germany</publisher><subject>Animals ; Anti-Anxiety Agents - antagonists & inhibitors ; Anti-Anxiety Agents - pharmacokinetics ; Anti-Anxiety Agents - pharmacology ; Anticonvulsants - pharmacology ; Anxiety - drug therapy ; Anxiety - psychology ; Binding, Competitive - drug effects ; Drinking Behavior - drug effects ; Exploratory Behavior - drug effects ; Flunitrazepam - pharmacokinetics ; Male ; Memory - drug effects ; Motor Activity - drug effects ; Muscle Relaxants, Central - pharmacology ; Postural Balance - drug effects ; Prosencephalon - metabolism ; Pyridazines - antagonists & inhibitors ; Pyridazines - pharmacokinetics ; Pyridazines - pharmacology ; Rats ; Rats, Sprague-Dawley ; Reinforcement (Psychology) ; Sleep - drug effects</subject><ispartof>Psychopharmacology, 1993, Vol.110 (1-2), p.13-18</ispartof><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><cites>FETCH-LOGICAL-c187t-fa43baefd1ec4354468a4010eb4979f7ef226ae1d5ab04adbda5bc332602277f3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,4010,27902,27903,27904</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/7870872$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Assié, M B</creatorcontrib><creatorcontrib>Chopin, P</creatorcontrib><creatorcontrib>Stenger, A</creatorcontrib><creatorcontrib>Palmier, C</creatorcontrib><creatorcontrib>Briley, M</creatorcontrib><title>Neuropharmacology of a new potential anxiolytic compound, F 2692, 1-(3'-trifluoromethyl phenyl) 1,4-dihydro 3-amino 4-oxo 6-methyl pyridazine. 1. Acute and in vitro effects</title><title>Psychopharmacology</title><addtitle>Psychopharmacology (Berl)</addtitle><description>F 2692 [1-(3'-trifluoromethyl phenyl) 1,4-dihydro 3-amino 4-oxo 6-methyl pyridazine] exhibited dose-dependent "anxiolytic" properties in the elevated plus-maze and the punished drinking tests in rats. It was also active in the two-compartment test in mice. The "anxiolytic" effects were antagonised by the benzodiazepine antagonists, flumazenil and ZK 93426. The compound exhibited anticonvulsant, sedative, myorelaxant and amnesic effects at doses 3-30 times higher than those required for "anxiolytic" activity. F 2692 has a very low affinity for benzodiazepine binding sites in vitro and in vivo (about 1000 and 160 fold lower than diazepam respectively). In addition it displayed no affinity for GABAA, alpha 2-adrenergic, 5-HT1A or 5-HT2 receptors. These data suggest that F 2692 may be a potential anxiolytic compound with an unusual mechanism of action.</description><subject>Animals</subject><subject>Anti-Anxiety Agents - antagonists & inhibitors</subject><subject>Anti-Anxiety Agents - pharmacokinetics</subject><subject>Anti-Anxiety Agents - pharmacology</subject><subject>Anticonvulsants - pharmacology</subject><subject>Anxiety - drug therapy</subject><subject>Anxiety - psychology</subject><subject>Binding, Competitive - drug effects</subject><subject>Drinking Behavior - drug effects</subject><subject>Exploratory Behavior - drug effects</subject><subject>Flunitrazepam - pharmacokinetics</subject><subject>Male</subject><subject>Memory - drug effects</subject><subject>Motor Activity - drug effects</subject><subject>Muscle Relaxants, Central - pharmacology</subject><subject>Postural Balance - drug effects</subject><subject>Prosencephalon - metabolism</subject><subject>Pyridazines - antagonists & inhibitors</subject><subject>Pyridazines - pharmacokinetics</subject><subject>Pyridazines - pharmacology</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>Reinforcement (Psychology)</subject><subject>Sleep - drug effects</subject><issn>0033-3158</issn><issn>1432-2072</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1993</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkU1v1DAQhi0EKkvhwh3JJwpovfgrdnIsFQtIFVzgHDn2mDVK7OA40PQ38SNJ1S0cO5e5PO870jwIPWd0xyjVb9_tKedSNbJ6gDZMCk441fwh2lAqBBGsqh-jJ9P0g64ja3mCTnStaa35Bv35DHNO48HkwdjUp-8LTh4bHOE3HlOBWILpsYlXIfVLCRbbNIxpjm6L95irhm8xI6_EGSk5-H5OOQ1QDkuPxwPEpX-N2VYSFw6LywkLYoYQE5YkXSWsyB265ODMdYiww2yHz-1cYD3pcIj4VyhrELwHW6an6JE3_QTPjvsUfdu__3rxkVx--fDp4vySWFbrQryRojPgHQMrRSWlqo2kjEInG914DZ5zZYC5ynRUGtc5U3VWCK7WN2rtxSl6eds75vRzhqm0Q5gs9L2JkOap1UowoWp5L8hU1TSi5iv45ha0OU1TBt-OOQwmLy2j7Y3D9r_DFX5xbJ27Adw_9ChN_AUOlJZK</recordid><startdate>1993</startdate><enddate>1993</enddate><creator>Assié, M B</creator><creator>Chopin, P</creator><creator>Stenger, A</creator><creator>Palmier, C</creator><creator>Briley, M</creator><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>7TK</scope><scope>7X8</scope></search><sort><creationdate>1993</creationdate><title>Neuropharmacology of a new potential anxiolytic compound, F 2692, 1-(3'-trifluoromethyl phenyl) 1,4-dihydro 3-amino 4-oxo 6-methyl pyridazine. 1. Acute and in vitro effects</title><author>Assié, M B ; Chopin, P ; Stenger, A ; Palmier, C ; Briley, M</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c187t-fa43baefd1ec4354468a4010eb4979f7ef226ae1d5ab04adbda5bc332602277f3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1993</creationdate><topic>Animals</topic><topic>Anti-Anxiety Agents - antagonists & inhibitors</topic><topic>Anti-Anxiety Agents - pharmacokinetics</topic><topic>Anti-Anxiety Agents - pharmacology</topic><topic>Anticonvulsants - pharmacology</topic><topic>Anxiety - drug therapy</topic><topic>Anxiety - psychology</topic><topic>Binding, Competitive - drug effects</topic><topic>Drinking Behavior - drug effects</topic><topic>Exploratory Behavior - drug effects</topic><topic>Flunitrazepam - pharmacokinetics</topic><topic>Male</topic><topic>Memory - drug effects</topic><topic>Motor Activity - drug effects</topic><topic>Muscle Relaxants, Central - pharmacology</topic><topic>Postural Balance - drug effects</topic><topic>Prosencephalon - metabolism</topic><topic>Pyridazines - antagonists & inhibitors</topic><topic>Pyridazines - pharmacokinetics</topic><topic>Pyridazines - pharmacology</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>Reinforcement (Psychology)</topic><topic>Sleep - drug effects</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Assié, M B</creatorcontrib><creatorcontrib>Chopin, P</creatorcontrib><creatorcontrib>Stenger, A</creatorcontrib><creatorcontrib>Palmier, C</creatorcontrib><creatorcontrib>Briley, M</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Neurosciences Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Psychopharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Assié, M B</au><au>Chopin, P</au><au>Stenger, A</au><au>Palmier, C</au><au>Briley, M</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Neuropharmacology of a new potential anxiolytic compound, F 2692, 1-(3'-trifluoromethyl phenyl) 1,4-dihydro 3-amino 4-oxo 6-methyl pyridazine. 1. Acute and in vitro effects</atitle><jtitle>Psychopharmacology</jtitle><addtitle>Psychopharmacology (Berl)</addtitle><date>1993</date><risdate>1993</risdate><volume>110</volume><issue>1-2</issue><spage>13</spage><epage>18</epage><pages>13-18</pages><issn>0033-3158</issn><eissn>1432-2072</eissn><abstract>F 2692 [1-(3'-trifluoromethyl phenyl) 1,4-dihydro 3-amino 4-oxo 6-methyl pyridazine] exhibited dose-dependent "anxiolytic" properties in the elevated plus-maze and the punished drinking tests in rats. It was also active in the two-compartment test in mice. The "anxiolytic" effects were antagonised by the benzodiazepine antagonists, flumazenil and ZK 93426. The compound exhibited anticonvulsant, sedative, myorelaxant and amnesic effects at doses 3-30 times higher than those required for "anxiolytic" activity. F 2692 has a very low affinity for benzodiazepine binding sites in vitro and in vivo (about 1000 and 160 fold lower than diazepam respectively). In addition it displayed no affinity for GABAA, alpha 2-adrenergic, 5-HT1A or 5-HT2 receptors. These data suggest that F 2692 may be a potential anxiolytic compound with an unusual mechanism of action.</abstract><cop>Germany</cop><pmid>7870872</pmid><doi>10.1007/BF02246945</doi><tpages>6</tpages></addata></record> |
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| ispartof | Psychopharmacology, 1993, Vol.110 (1-2), p.13-18 |
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| subjects | Animals Anti-Anxiety Agents - antagonists & inhibitors Anti-Anxiety Agents - pharmacokinetics Anti-Anxiety Agents - pharmacology Anticonvulsants - pharmacology Anxiety - drug therapy Anxiety - psychology Binding, Competitive - drug effects Drinking Behavior - drug effects Exploratory Behavior - drug effects Flunitrazepam - pharmacokinetics Male Memory - drug effects Motor Activity - drug effects Muscle Relaxants, Central - pharmacology Postural Balance - drug effects Prosencephalon - metabolism Pyridazines - antagonists & inhibitors Pyridazines - pharmacokinetics Pyridazines - pharmacology Rats Rats, Sprague-Dawley Reinforcement (Psychology) Sleep - drug effects |
| title | Neuropharmacology of a new potential anxiolytic compound, F 2692, 1-(3'-trifluoromethyl phenyl) 1,4-dihydro 3-amino 4-oxo 6-methyl pyridazine. 1. Acute and in vitro effects |
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