A β-carboline antagonizes benzodiazepine actions but does not precipitate the abstinence syndrome in cats
The beta-carbolines, which are potent ligands for benzodiazepine receptors, antagonize the pharmacological actions of benzodiazepines. In the cat, the stable beta-carboline derivative methylamide-beta-carboline-3-carboxylate, FG 7142, and the specific benzodiazepine antagonist Ro 15-1788 reversed be...
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Veröffentlicht in: | Psychopharmacologia 1985-01, Vol.86 (1-2), p.132-136 |
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description | The beta-carbolines, which are potent ligands for benzodiazepine receptors, antagonize the pharmacological actions of benzodiazepines. In the cat, the stable beta-carboline derivative methylamide-beta-carboline-3-carboxylate, FG 7142, and the specific benzodiazepine antagonist Ro 15-1788 reversed behavioral and electroencephalographic (EEG) changes produced by a single dose of diazepam. Surprisingly, the beta-carboline did not elicit signs of withdrawal when given after 22 days of a daily dose regimen of diazepam, while Ro 15-1788 precipitated an acute abstinence syndrome largely characterized by tremors, increased muscle tone, back arching, myoclonic jerks and pupil dilatation. Unlike Ro 15-1788, the beta-carboline produced effects of its own such as behavioral states of arousal and fearfulness. These findings indicate that the beta-carboline functionally interacts with benzodiazepine receptors in a manner unlike that seen with typical agonists and antagonists. |
doi_str_mv | 10.1007/BF00431697 |
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In the cat, the stable beta-carboline derivative methylamide-beta-carboline-3-carboxylate, FG 7142, and the specific benzodiazepine antagonist Ro 15-1788 reversed behavioral and electroencephalographic (EEG) changes produced by a single dose of diazepam. Surprisingly, the beta-carboline did not elicit signs of withdrawal when given after 22 days of a daily dose regimen of diazepam, while Ro 15-1788 precipitated an acute abstinence syndrome largely characterized by tremors, increased muscle tone, back arching, myoclonic jerks and pupil dilatation. Unlike Ro 15-1788, the beta-carboline produced effects of its own such as behavioral states of arousal and fearfulness. These findings indicate that the beta-carboline functionally interacts with benzodiazepine receptors in a manner unlike that seen with typical agonists and antagonists.</description><identifier>ISSN: 0033-3158</identifier><identifier>EISSN: 1432-2072</identifier><identifier>DOI: 10.1007/BF00431697</identifier><identifier>PMID: 2991962</identifier><identifier>CODEN: PSYPAG</identifier><language>eng</language><publisher>Berlin: Springer</publisher><subject>Animals ; Behavior, Animal - drug effects ; Benzodiazepinones - pharmacology ; Biological and medical sciences ; Brain - drug effects ; Carbolines - pharmacology ; Cats ; Diazepam - adverse effects ; Diazepam - antagonists & inhibitors ; Electroencephalography ; Flumazenil ; Humans ; Indoles - pharmacology ; Medical sciences ; Neuropharmacology ; Pharmacology. Drug treatments ; Psycholeptics: tranquillizer, neuroleptic ; Psychology. Psychoanalysis. 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In the cat, the stable beta-carboline derivative methylamide-beta-carboline-3-carboxylate, FG 7142, and the specific benzodiazepine antagonist Ro 15-1788 reversed behavioral and electroencephalographic (EEG) changes produced by a single dose of diazepam. Surprisingly, the beta-carboline did not elicit signs of withdrawal when given after 22 days of a daily dose regimen of diazepam, while Ro 15-1788 precipitated an acute abstinence syndrome largely characterized by tremors, increased muscle tone, back arching, myoclonic jerks and pupil dilatation. Unlike Ro 15-1788, the beta-carboline produced effects of its own such as behavioral states of arousal and fearfulness. These findings indicate that the beta-carboline functionally interacts with benzodiazepine receptors in a manner unlike that seen with typical agonists and antagonists.</description><subject>Animals</subject><subject>Behavior, Animal - drug effects</subject><subject>Benzodiazepinones - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Brain - drug effects</subject><subject>Carbolines - pharmacology</subject><subject>Cats</subject><subject>Diazepam - adverse effects</subject><subject>Diazepam - antagonists & inhibitors</subject><subject>Electroencephalography</subject><subject>Flumazenil</subject><subject>Humans</subject><subject>Indoles - pharmacology</subject><subject>Medical sciences</subject><subject>Neuropharmacology</subject><subject>Pharmacology. Drug treatments</subject><subject>Psycholeptics: tranquillizer, neuroleptic</subject><subject>Psychology. Psychoanalysis. Psychiatry</subject><subject>Psychopharmacology</subject><subject>Receptors, GABA-A - drug effects</subject><subject>Substance Withdrawal Syndrome - etiology</subject><issn>0033-3158</issn><issn>1432-2072</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1985</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNo90LtOwzAUgGELgUopLOxIHhBbwPfEY6koIFVigTmyHQdcJXaI3aF9LB6EZ8KCCC9HOv-nMxiAS4xuMULl3f0aIUaxkOURmGNGSUFQSY7BHCFKC4p5dQrOYtyi_FjFZmBGpMRSkDnYLuH3V2HUqEPnvIXKJ_UevDvYCLX1h9A4dbDDbzLJBZ_XuwSbkLsPCQ6jNW5wSSUL00dGOqaMvbEw7n0zht5C56FRKZ6Dk1Z10V5McwHe1g-vq6di8_L4vFpuioEIkQrSCC5L0SLWMoaEpFwIKRBpDFOGN0RyY4RGqNJWcUV0Wwqkq7a0HKkqK7oAN393hzF87mxMde-isV2nvA27WGNGuOREZHg1wZ3ubVMPo-vVuK-nz8n9euoqGtW1o_LGxX9WUYlpJegPUcB0Bg</recordid><startdate>19850101</startdate><enddate>19850101</enddate><creator>ONGINI, E</creator><creator>MARZANATTI, M</creator><creator>BAMONTE, F</creator><creator>MONOPOLI, A</creator><creator>GUZZON, V</creator><general>Springer</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></search><sort><creationdate>19850101</creationdate><title>A β-carboline antagonizes benzodiazepine actions but does not precipitate the abstinence syndrome in cats</title><author>ONGINI, E ; MARZANATTI, M ; BAMONTE, F ; MONOPOLI, A ; GUZZON, V</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-p266t-2d65976f04f4406935669602dc4ac5d295cc6b008bea5a2bf760b8f7e50a82dc3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1985</creationdate><topic>Animals</topic><topic>Behavior, Animal - drug effects</topic><topic>Benzodiazepinones - pharmacology</topic><topic>Biological and medical sciences</topic><topic>Brain - drug effects</topic><topic>Carbolines - pharmacology</topic><topic>Cats</topic><topic>Diazepam - adverse effects</topic><topic>Diazepam - antagonists & inhibitors</topic><topic>Electroencephalography</topic><topic>Flumazenil</topic><topic>Humans</topic><topic>Indoles - pharmacology</topic><topic>Medical sciences</topic><topic>Neuropharmacology</topic><topic>Pharmacology. Drug treatments</topic><topic>Psycholeptics: tranquillizer, neuroleptic</topic><topic>Psychology. Psychoanalysis. Psychiatry</topic><topic>Psychopharmacology</topic><topic>Receptors, GABA-A - drug effects</topic><topic>Substance Withdrawal Syndrome - etiology</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>ONGINI, E</creatorcontrib><creatorcontrib>MARZANATTI, M</creatorcontrib><creatorcontrib>BAMONTE, F</creatorcontrib><creatorcontrib>MONOPOLI, A</creatorcontrib><creatorcontrib>GUZZON, V</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><jtitle>Psychopharmacologia</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>ONGINI, E</au><au>MARZANATTI, M</au><au>BAMONTE, F</au><au>MONOPOLI, A</au><au>GUZZON, V</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>A β-carboline antagonizes benzodiazepine actions but does not precipitate the abstinence syndrome in cats</atitle><jtitle>Psychopharmacologia</jtitle><addtitle>Psychopharmacology (Berl)</addtitle><date>1985-01-01</date><risdate>1985</risdate><volume>86</volume><issue>1-2</issue><spage>132</spage><epage>136</epage><pages>132-136</pages><issn>0033-3158</issn><eissn>1432-2072</eissn><coden>PSYPAG</coden><abstract>The beta-carbolines, which are potent ligands for benzodiazepine receptors, antagonize the pharmacological actions of benzodiazepines. In the cat, the stable beta-carboline derivative methylamide-beta-carboline-3-carboxylate, FG 7142, and the specific benzodiazepine antagonist Ro 15-1788 reversed behavioral and electroencephalographic (EEG) changes produced by a single dose of diazepam. Surprisingly, the beta-carboline did not elicit signs of withdrawal when given after 22 days of a daily dose regimen of diazepam, while Ro 15-1788 precipitated an acute abstinence syndrome largely characterized by tremors, increased muscle tone, back arching, myoclonic jerks and pupil dilatation. Unlike Ro 15-1788, the beta-carboline produced effects of its own such as behavioral states of arousal and fearfulness. These findings indicate that the beta-carboline functionally interacts with benzodiazepine receptors in a manner unlike that seen with typical agonists and antagonists.</abstract><cop>Berlin</cop><pub>Springer</pub><pmid>2991962</pmid><doi>10.1007/BF00431697</doi><tpages>5</tpages></addata></record> |
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subjects | Animals Behavior, Animal - drug effects Benzodiazepinones - pharmacology Biological and medical sciences Brain - drug effects Carbolines - pharmacology Cats Diazepam - adverse effects Diazepam - antagonists & inhibitors Electroencephalography Flumazenil Humans Indoles - pharmacology Medical sciences Neuropharmacology Pharmacology. Drug treatments Psycholeptics: tranquillizer, neuroleptic Psychology. Psychoanalysis. Psychiatry Psychopharmacology Receptors, GABA-A - drug effects Substance Withdrawal Syndrome - etiology |
title | A β-carboline antagonizes benzodiazepine actions but does not precipitate the abstinence syndrome in cats |
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