Benzodiazepine antagonist Ro 15-1788: neurological and behavioral effects
In neurological and behavioral studies in mice, rats, dogs and squirrel monkeys, the imidazobenzodiazepinone Ro 15-1788 acted as a potent benzodiazepine antagonist. The antagonistic activity was both preventive and curative and seen at doses at which no intrinsic effects were detected. It was highly...
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| Veröffentlicht in: | Psychopharmacology 1982, Vol.78 (1), p.8-18 |
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| container_title | Psychopharmacology |
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| creator | Bonetti, E P Pieri, L Cumin, R Schaffner, R Pieri, M Gamzu, E R Müller, R K Haefely, W |
| description | In neurological and behavioral studies in mice, rats, dogs and squirrel monkeys, the imidazobenzodiazepinone Ro 15-1788 acted as a potent benzodiazepine antagonist. The antagonistic activity was both preventive and curative and seen at doses at which no intrinsic effects were detected. It was highly selective in that it acted against CNS effects induced by benzodiazepines but not against those produced by other depressants, such as phenobarbitone, meprobamate, ethanol, and valproate. The onset of action was rapid even after oral administration. Depending on the animal species studied, the antagonistic effects lasted from a few hours to 1 day. The acute and subacute toxicity of Ro 15-1788 was found to be very low. Benzodiazepine-like effects were not seen. |
| doi_str_mv | 10.1007/BF00470579 |
| format | Article |
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The antagonistic activity was both preventive and curative and seen at doses at which no intrinsic effects were detected. It was highly selective in that it acted against CNS effects induced by benzodiazepines but not against those produced by other depressants, such as phenobarbitone, meprobamate, ethanol, and valproate. The onset of action was rapid even after oral administration. Depending on the animal species studied, the antagonistic effects lasted from a few hours to 1 day. The acute and subacute toxicity of Ro 15-1788 was found to be very low. Benzodiazepine-like effects were not seen.</description><identifier>ISSN: 0033-3158</identifier><identifier>DOI: 10.1007/BF00470579</identifier><identifier>PMID: 6292984</identifier><language>eng</language><publisher>Germany</publisher><subject>Animals ; Avoidance Learning - drug effects ; Behavior, Animal - drug effects ; Benzodiazepinones - pharmacology ; Conditioning, Operant - drug effects ; Dogs ; Dose-Response Relationship, Drug ; Exploratory Behavior - drug effects ; Female ; Flumazenil ; Male ; Motor Activity - drug effects ; Motor Skills - drug effects ; Muridae ; Nervous System - drug effects ; Pentylenetetrazole - pharmacology ; Rabbits ; Rats ; Receptors, Drug - drug effects ; Receptors, GABA-A ; Reflex - drug effects ; Respiration - drug effects ; Saimiri ; Seizures - chemically induced</subject><ispartof>Psychopharmacology, 1982, Vol.78 (1), p.8-18</ispartof><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,778,782,4012,27906,27907,27908</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/6292984$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Bonetti, E P</creatorcontrib><creatorcontrib>Pieri, L</creatorcontrib><creatorcontrib>Cumin, R</creatorcontrib><creatorcontrib>Schaffner, R</creatorcontrib><creatorcontrib>Pieri, M</creatorcontrib><creatorcontrib>Gamzu, E R</creatorcontrib><creatorcontrib>Müller, R K</creatorcontrib><creatorcontrib>Haefely, W</creatorcontrib><title>Benzodiazepine antagonist Ro 15-1788: neurological and behavioral effects</title><title>Psychopharmacology</title><addtitle>Psychopharmacology (Berl)</addtitle><description>In neurological and behavioral studies in mice, rats, dogs and squirrel monkeys, the imidazobenzodiazepinone Ro 15-1788 acted as a potent benzodiazepine antagonist. 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Benzodiazepine-like effects were not seen.</description><subject>Animals</subject><subject>Avoidance Learning - drug effects</subject><subject>Behavior, Animal - drug effects</subject><subject>Benzodiazepinones - pharmacology</subject><subject>Conditioning, Operant - drug effects</subject><subject>Dogs</subject><subject>Dose-Response Relationship, Drug</subject><subject>Exploratory Behavior - drug effects</subject><subject>Female</subject><subject>Flumazenil</subject><subject>Male</subject><subject>Motor Activity - drug effects</subject><subject>Motor Skills - drug effects</subject><subject>Muridae</subject><subject>Nervous System - drug effects</subject><subject>Pentylenetetrazole - pharmacology</subject><subject>Rabbits</subject><subject>Rats</subject><subject>Receptors, Drug - drug effects</subject><subject>Receptors, GABA-A</subject><subject>Reflex - drug effects</subject><subject>Respiration - drug effects</subject><subject>Saimiri</subject><subject>Seizures - chemically induced</subject><issn>0033-3158</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1982</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNotj01Lw0AYhPeg1Fq9eBdy8hZ9N_vtzRarhYIgeg67yZu6kmRjNhHsrzdi5jIM8zAwhFxRuKUA6m69BeAKhDInZAnAWMqo0GfkPMZPmMQ1X5CFzExmNF-S3RrbYyi9PWLnW0xsO9hDaH0ckteQUJFSpfV90uLYhzocfGHriSkThx_224d-ilhVWAzxgpxWto54OfuKvG8f3zbP6f7labd52KcdlWZINa9kWRUCaEGFpCJzVlcCOTijXWap0w6EllYoAWqqjDWSZRQUMMGMpWxFbv53uz58jRiHvPGxwLq2LYYx5lQIzo38A69ncHQNlnnX-8b2P_n8nf0CuilWWg</recordid><startdate>1982</startdate><enddate>1982</enddate><creator>Bonetti, E P</creator><creator>Pieri, L</creator><creator>Cumin, R</creator><creator>Schaffner, R</creator><creator>Pieri, M</creator><creator>Gamzu, E R</creator><creator>Müller, R K</creator><creator>Haefely, W</creator><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>7TK</scope></search><sort><creationdate>1982</creationdate><title>Benzodiazepine antagonist Ro 15-1788: neurological and behavioral effects</title><author>Bonetti, E P ; Pieri, L ; Cumin, R ; Schaffner, R ; Pieri, M ; Gamzu, E R ; Müller, R K ; Haefely, W</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-p169t-84f6dfc501c156152ba8f5e40b98b2a1b8b0586a57507a8f9a963210703539a13</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1982</creationdate><topic>Animals</topic><topic>Avoidance Learning - drug effects</topic><topic>Behavior, Animal - drug effects</topic><topic>Benzodiazepinones - pharmacology</topic><topic>Conditioning, Operant - drug effects</topic><topic>Dogs</topic><topic>Dose-Response Relationship, Drug</topic><topic>Exploratory Behavior - drug effects</topic><topic>Female</topic><topic>Flumazenil</topic><topic>Male</topic><topic>Motor Activity - drug effects</topic><topic>Motor Skills - drug effects</topic><topic>Muridae</topic><topic>Nervous System - drug effects</topic><topic>Pentylenetetrazole - pharmacology</topic><topic>Rabbits</topic><topic>Rats</topic><topic>Receptors, Drug - drug effects</topic><topic>Receptors, GABA-A</topic><topic>Reflex - drug effects</topic><topic>Respiration - drug effects</topic><topic>Saimiri</topic><topic>Seizures - chemically induced</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Bonetti, E P</creatorcontrib><creatorcontrib>Pieri, L</creatorcontrib><creatorcontrib>Cumin, R</creatorcontrib><creatorcontrib>Schaffner, R</creatorcontrib><creatorcontrib>Pieri, M</creatorcontrib><creatorcontrib>Gamzu, E R</creatorcontrib><creatorcontrib>Müller, R K</creatorcontrib><creatorcontrib>Haefely, W</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>Neurosciences Abstracts</collection><jtitle>Psychopharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Bonetti, E P</au><au>Pieri, L</au><au>Cumin, R</au><au>Schaffner, R</au><au>Pieri, M</au><au>Gamzu, E R</au><au>Müller, R K</au><au>Haefely, W</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Benzodiazepine antagonist Ro 15-1788: neurological and behavioral effects</atitle><jtitle>Psychopharmacology</jtitle><addtitle>Psychopharmacology (Berl)</addtitle><date>1982</date><risdate>1982</risdate><volume>78</volume><issue>1</issue><spage>8</spage><epage>18</epage><pages>8-18</pages><issn>0033-3158</issn><abstract>In neurological and behavioral studies in mice, rats, dogs and squirrel monkeys, the imidazobenzodiazepinone Ro 15-1788 acted as a potent benzodiazepine antagonist. 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| identifier | ISSN: 0033-3158 |
| ispartof | Psychopharmacology, 1982, Vol.78 (1), p.8-18 |
| issn | 0033-3158 |
| language | eng |
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| source | MEDLINE; SpringerLink Journals - AutoHoldings |
| subjects | Animals Avoidance Learning - drug effects Behavior, Animal - drug effects Benzodiazepinones - pharmacology Conditioning, Operant - drug effects Dogs Dose-Response Relationship, Drug Exploratory Behavior - drug effects Female Flumazenil Male Motor Activity - drug effects Motor Skills - drug effects Muridae Nervous System - drug effects Pentylenetetrazole - pharmacology Rabbits Rats Receptors, Drug - drug effects Receptors, GABA-A Reflex - drug effects Respiration - drug effects Saimiri Seizures - chemically induced |
| title | Benzodiazepine antagonist Ro 15-1788: neurological and behavioral effects |
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