Comparative anticonvulsant activity of N-acetyl-1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives in rodents
The anticonvulsant activity of competitive 2,3-dihydroxy-6-nitro-7-sulfamoyl-benzo (F)-quinoxaline (NBQX) and noncompetitive 2,3-benzodiazepines and tetrahydroisoquinolines (THIQs) AMPA/kainate receptor antagonists, was tested in different experimental seizure models and compared with diazepam, a co...
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| Veröffentlicht in: | Pharmacology, biochemistry and behavior biochemistry and behavior, 2004, Vol.77 (1), p.85-94 |
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| creator | Ferreri, Guido Chimirri, Alba Russo, Emilio Gitto, Rosaria Gareri, Pietro De Sarro, Angela De Sarro, Giovambattista |
| description | The anticonvulsant activity of competitive 2,3-dihydroxy-6-nitro-7-sulfamoyl-benzo (F)-quinoxaline (NBQX) and noncompetitive 2,3-benzodiazepines and tetrahydroisoquinolines (THIQs) AMPA/kainate receptor antagonists, was tested in different experimental seizure models and compared with diazepam, a conventional antiepileptic drug acting on GABAergic neurotransmission. In particular, the compounds were evaluated against audiogenic and maximal electroshock seizures (MES) test and pentetrazol (PTZ) seizures model, and all of them showed protective action.
In addition, NBQX, 2,3-benzodiazepines and THIQs, but not diazepam, were also protective against clonic and tonic seizures and lethality induced by kainate, AMPA and ATPA, but were ineffective against NMDA-induced seizures. Only 2,3-benzodiazepines and some THIQs were able to affect 4-aminopyridine- and mercaptopropionic-acid-induced seizures.
The duration of anticonvulsant action of 33 μmol/kg of some 2,3-benzodiazepines and THIQs was also investigated in DBA/2 mice, a strain genetically susceptible to audiogenic seizures, and it was observed that the derivative THIQ-10c, possessing an acetyl group at the N-2 and a chlorine atom on the C-1 phenyl ring, showed higher anticonvulsant activity and longer-lasting protective effects. |
| doi_str_mv | 10.1016/j.pbb.2003.09.019 |
| format | Article |
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In addition, NBQX, 2,3-benzodiazepines and THIQs, but not diazepam, were also protective against clonic and tonic seizures and lethality induced by kainate, AMPA and ATPA, but were ineffective against NMDA-induced seizures. Only 2,3-benzodiazepines and some THIQs were able to affect 4-aminopyridine- and mercaptopropionic-acid-induced seizures.
The duration of anticonvulsant action of 33 μmol/kg of some 2,3-benzodiazepines and THIQs was also investigated in DBA/2 mice, a strain genetically susceptible to audiogenic seizures, and it was observed that the derivative THIQ-10c, possessing an acetyl group at the N-2 and a chlorine atom on the C-1 phenyl ring, showed higher anticonvulsant activity and longer-lasting protective effects.</description><identifier>ISSN: 0091-3057</identifier><identifier>EISSN: 1873-5177</identifier><identifier>DOI: 10.1016/j.pbb.2003.09.019</identifier><identifier>PMID: 14724045</identifier><identifier>CODEN: PBBHAU</identifier><language>eng</language><publisher>New York, NY: Elsevier Inc</publisher><subject>2,3-Benzodiazepines ; AMPA/kainate receptor antagonists ; Animals ; Anticonvulsants - pharmacology ; Anticonvulsants - therapeutic use ; Audiogenic seizures ; Biological and medical sciences ; CFM-2 ; Chemoconvulsions ; DBA/2 mice ; Dose-Response Relationship, Drug ; Epilepsy ; Fundamental and applied biological sciences. Psychology ; GYKI 52466 ; GYKI 53655 ; GYKI 53773 ; Male ; Maximal electroshock ; Medical sciences ; Mice ; Mice, Inbred DBA ; Mice, Inbred ICR ; N-acetyl-1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolines ; NBQX ; Neuropharmacology ; Pharmacology. Drug treatments ; Psychology. Psychoanalysis. Psychiatry ; Psychology. Psychophysiology ; Quinoxalines - pharmacology ; Quinoxalines - therapeutic use ; Receptors, AMPA - antagonists & inhibitors ; Receptors, AMPA - physiology ; Seizures - prevention & control</subject><ispartof>Pharmacology, biochemistry and behavior, 2004, Vol.77 (1), p.85-94</ispartof><rights>2003 Elsevier Inc.</rights><rights>2004 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c445t-fa285f5f981acc954261d6b446ca008a9d80a607e8ca756d05c1385daff61aae3</citedby><cites>FETCH-LOGICAL-c445t-fa285f5f981acc954261d6b446ca008a9d80a607e8ca756d05c1385daff61aae3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.pbb.2003.09.019$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,4024,27923,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=15532680$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/14724045$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Ferreri, Guido</creatorcontrib><creatorcontrib>Chimirri, Alba</creatorcontrib><creatorcontrib>Russo, Emilio</creatorcontrib><creatorcontrib>Gitto, Rosaria</creatorcontrib><creatorcontrib>Gareri, Pietro</creatorcontrib><creatorcontrib>De Sarro, Angela</creatorcontrib><creatorcontrib>De Sarro, Giovambattista</creatorcontrib><title>Comparative anticonvulsant activity of N-acetyl-1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives in rodents</title><title>Pharmacology, biochemistry and behavior</title><addtitle>Pharmacol Biochem Behav</addtitle><description>The anticonvulsant activity of competitive 2,3-dihydroxy-6-nitro-7-sulfamoyl-benzo (F)-quinoxaline (NBQX) and noncompetitive 2,3-benzodiazepines and tetrahydroisoquinolines (THIQs) AMPA/kainate receptor antagonists, was tested in different experimental seizure models and compared with diazepam, a conventional antiepileptic drug acting on GABAergic neurotransmission. In particular, the compounds were evaluated against audiogenic and maximal electroshock seizures (MES) test and pentetrazol (PTZ) seizures model, and all of them showed protective action.
In addition, NBQX, 2,3-benzodiazepines and THIQs, but not diazepam, were also protective against clonic and tonic seizures and lethality induced by kainate, AMPA and ATPA, but were ineffective against NMDA-induced seizures. Only 2,3-benzodiazepines and some THIQs were able to affect 4-aminopyridine- and mercaptopropionic-acid-induced seizures.
The duration of anticonvulsant action of 33 μmol/kg of some 2,3-benzodiazepines and THIQs was also investigated in DBA/2 mice, a strain genetically susceptible to audiogenic seizures, and it was observed that the derivative THIQ-10c, possessing an acetyl group at the N-2 and a chlorine atom on the C-1 phenyl ring, showed higher anticonvulsant activity and longer-lasting protective effects.</description><subject>2,3-Benzodiazepines</subject><subject>AMPA/kainate receptor antagonists</subject><subject>Animals</subject><subject>Anticonvulsants - pharmacology</subject><subject>Anticonvulsants - therapeutic use</subject><subject>Audiogenic seizures</subject><subject>Biological and medical sciences</subject><subject>CFM-2</subject><subject>Chemoconvulsions</subject><subject>DBA/2 mice</subject><subject>Dose-Response Relationship, Drug</subject><subject>Epilepsy</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>GYKI 52466</subject><subject>GYKI 53655</subject><subject>GYKI 53773</subject><subject>Male</subject><subject>Maximal electroshock</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Mice, Inbred DBA</subject><subject>Mice, Inbred ICR</subject><subject>N-acetyl-1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolines</subject><subject>NBQX</subject><subject>Neuropharmacology</subject><subject>Pharmacology. Drug treatments</subject><subject>Psychology. Psychoanalysis. Psychiatry</subject><subject>Psychology. Psychophysiology</subject><subject>Quinoxalines - pharmacology</subject><subject>Quinoxalines - therapeutic use</subject><subject>Receptors, AMPA - antagonists & inhibitors</subject><subject>Receptors, AMPA - physiology</subject><subject>Seizures - prevention & control</subject><issn>0091-3057</issn><issn>1873-5177</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2004</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kE2P0zAQQC0EYrsLP4ALygVOdRgnceyI06piAWkFFzhbU3uidZXExXYryq_HSyvtjdOMRm--HmNvBNQCRP9hV--327oBaGsYahDDM7YSWrVcCqWesxXAIHgLUl2x65R2ANA1vXrJrkSnmg46uWJ_NmHeY8Tsj1Thkr0Ny_EwpZJWaEvV51MVxuobR0v5NHHBMZbQrxV3fqb8EH6fuFg363bd8Uw54sPJxeBT-HXwS5j8QpWj6I__VqTKL1UMjpacXrEXI06JXl_iDft59-nH5gu___756-b2ntuuk5mP2Gg5ynHQAq0dZHlBuH7bdb1FAI2D04A9KNIWlewdSCtaLR2OYy8Qqb1h789z97HcRCmb2SdL04QLhUMyGgSoRjcFFGfQxpBSpNHso5_Lu0aAeRRudqYIN4_CDQymCC89by_DD9uZ3FPHxXAB3l0ATBanMeJifXripGybXkPhPp45KiqOnqJJ1tNiyflINhsX_H_O-AvfxZ9K</recordid><startdate>2004</startdate><enddate>2004</enddate><creator>Ferreri, Guido</creator><creator>Chimirri, Alba</creator><creator>Russo, Emilio</creator><creator>Gitto, Rosaria</creator><creator>Gareri, Pietro</creator><creator>De Sarro, Angela</creator><creator>De Sarro, Giovambattista</creator><general>Elsevier Inc</general><general>Elsevier Science</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>2004</creationdate><title>Comparative anticonvulsant activity of N-acetyl-1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives in rodents</title><author>Ferreri, Guido ; Chimirri, Alba ; Russo, Emilio ; Gitto, Rosaria ; Gareri, Pietro ; De Sarro, Angela ; De Sarro, Giovambattista</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c445t-fa285f5f981acc954261d6b446ca008a9d80a607e8ca756d05c1385daff61aae3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2004</creationdate><topic>2,3-Benzodiazepines</topic><topic>AMPA/kainate receptor antagonists</topic><topic>Animals</topic><topic>Anticonvulsants - pharmacology</topic><topic>Anticonvulsants - therapeutic use</topic><topic>Audiogenic seizures</topic><topic>Biological and medical sciences</topic><topic>CFM-2</topic><topic>Chemoconvulsions</topic><topic>DBA/2 mice</topic><topic>Dose-Response Relationship, Drug</topic><topic>Epilepsy</topic><topic>Fundamental and applied biological sciences. Psychology</topic><topic>GYKI 52466</topic><topic>GYKI 53655</topic><topic>GYKI 53773</topic><topic>Male</topic><topic>Maximal electroshock</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Mice, Inbred DBA</topic><topic>Mice, Inbred ICR</topic><topic>N-acetyl-1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolines</topic><topic>NBQX</topic><topic>Neuropharmacology</topic><topic>Pharmacology. Drug treatments</topic><topic>Psychology. Psychoanalysis. Psychiatry</topic><topic>Psychology. Psychophysiology</topic><topic>Quinoxalines - pharmacology</topic><topic>Quinoxalines - therapeutic use</topic><topic>Receptors, AMPA - antagonists & inhibitors</topic><topic>Receptors, AMPA - physiology</topic><topic>Seizures - prevention & control</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Ferreri, Guido</creatorcontrib><creatorcontrib>Chimirri, Alba</creatorcontrib><creatorcontrib>Russo, Emilio</creatorcontrib><creatorcontrib>Gitto, Rosaria</creatorcontrib><creatorcontrib>Gareri, Pietro</creatorcontrib><creatorcontrib>De Sarro, Angela</creatorcontrib><creatorcontrib>De Sarro, Giovambattista</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>Pharmacology, biochemistry and behavior</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Ferreri, Guido</au><au>Chimirri, Alba</au><au>Russo, Emilio</au><au>Gitto, Rosaria</au><au>Gareri, Pietro</au><au>De Sarro, Angela</au><au>De Sarro, Giovambattista</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Comparative anticonvulsant activity of N-acetyl-1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives in rodents</atitle><jtitle>Pharmacology, biochemistry and behavior</jtitle><addtitle>Pharmacol Biochem Behav</addtitle><date>2004</date><risdate>2004</risdate><volume>77</volume><issue>1</issue><spage>85</spage><epage>94</epage><pages>85-94</pages><issn>0091-3057</issn><eissn>1873-5177</eissn><coden>PBBHAU</coden><abstract>The anticonvulsant activity of competitive 2,3-dihydroxy-6-nitro-7-sulfamoyl-benzo (F)-quinoxaline (NBQX) and noncompetitive 2,3-benzodiazepines and tetrahydroisoquinolines (THIQs) AMPA/kainate receptor antagonists, was tested in different experimental seizure models and compared with diazepam, a conventional antiepileptic drug acting on GABAergic neurotransmission. In particular, the compounds were evaluated against audiogenic and maximal electroshock seizures (MES) test and pentetrazol (PTZ) seizures model, and all of them showed protective action.
In addition, NBQX, 2,3-benzodiazepines and THIQs, but not diazepam, were also protective against clonic and tonic seizures and lethality induced by kainate, AMPA and ATPA, but were ineffective against NMDA-induced seizures. Only 2,3-benzodiazepines and some THIQs were able to affect 4-aminopyridine- and mercaptopropionic-acid-induced seizures.
The duration of anticonvulsant action of 33 μmol/kg of some 2,3-benzodiazepines and THIQs was also investigated in DBA/2 mice, a strain genetically susceptible to audiogenic seizures, and it was observed that the derivative THIQ-10c, possessing an acetyl group at the N-2 and a chlorine atom on the C-1 phenyl ring, showed higher anticonvulsant activity and longer-lasting protective effects.</abstract><cop>New York, NY</cop><pub>Elsevier Inc</pub><pmid>14724045</pmid><doi>10.1016/j.pbb.2003.09.019</doi><tpages>10</tpages></addata></record> |
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| subjects | 2,3-Benzodiazepines AMPA/kainate receptor antagonists Animals Anticonvulsants - pharmacology Anticonvulsants - therapeutic use Audiogenic seizures Biological and medical sciences CFM-2 Chemoconvulsions DBA/2 mice Dose-Response Relationship, Drug Epilepsy Fundamental and applied biological sciences. Psychology GYKI 52466 GYKI 53655 GYKI 53773 Male Maximal electroshock Medical sciences Mice Mice, Inbred DBA Mice, Inbred ICR N-acetyl-1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolines NBQX Neuropharmacology Pharmacology. Drug treatments Psychology. Psychoanalysis. Psychiatry Psychology. Psychophysiology Quinoxalines - pharmacology Quinoxalines - therapeutic use Receptors, AMPA - antagonists & inhibitors Receptors, AMPA - physiology Seizures - prevention & control |
| title | Comparative anticonvulsant activity of N-acetyl-1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives in rodents |
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