Relationship of agonist efficacy to changes in GABA sensitivity and anticonvulsant tolerance following chronic benzodiazepine ligand exposure
Benzodiazepine ligands of differing efficacy including the agonist, diazepam, the partial agonist, Ro 16–6028 and the antagonist, Ro 15–1788, were administered in vivo to rats continuously for 3 weeks. The magnitude of change in various measures of GABA sensitivity could be correlated directly with...
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| Veröffentlicht in: | European journal of pharmacology 1989-11, Vol.170 (3), p.145-155 |
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| container_title | European journal of pharmacology |
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| creator | Hernandez, Theresa D. Heninger, Catherine Wilson, Marlene A. Gallager, Dorothy W. |
| description | Benzodiazepine ligands of differing efficacy including the agonist, diazepam, the partial agonist, Ro 16–6028 and the antagonist, Ro 15–1788, were administered in vivo to rats continuously for 3 weeks. The magnitude of change in various measures of GABA sensitivity could be correlated directly with increasing agonist efficacy: maximal changes were seen following chronic treatment with diazepam, intermediate changes were seen following the partial agonist Ro 16–6028 and no changes were observed following chronic Ro 15–1788 administration. The magnitude of change could also be correlated with increasing potential for tolerance development to anticonvulsant efficacy following chronic exposure to these benzodiazepine ligands. |
| doi_str_mv | 10.1016/0014-2999(89)90535-9 |
| format | Article |
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The magnitude of change in various measures of GABA sensitivity could be correlated directly with increasing agonist efficacy: maximal changes were seen following chronic treatment with diazepam, intermediate changes were seen following the partial agonist Ro 16–6028 and no changes were observed following chronic Ro 15–1788 administration. The magnitude of change could also be correlated with increasing potential for tolerance development to anticonvulsant efficacy following chronic exposure to these benzodiazepine ligands.</description><identifier>ISSN: 0014-2999</identifier><identifier>EISSN: 1879-0712</identifier><identifier>DOI: 10.1016/0014-2999(89)90535-9</identifier><identifier>PMID: 2515976</identifier><identifier>CODEN: EJPHAZ</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>Agonist efficacy ; Animals ; Anticonvulsants ; Anticonvulsants. Antiepileptics. Antiparkinson agents ; Behavior, Animal - drug effects ; Benzodiazepines (chronic) ; Benzodiazepines - pharmacology ; Benzodiazepinones - pharmacology ; Bicuculline - metabolism ; Bicuculline - pharmacology ; Biological and medical sciences ; Brain Chemistry - drug effects ; Diazepam - pharmacology ; Drug Tolerance ; Electrophysiology ; Flumazenil - pharmacology ; GABA ; gamma-Aminobutyric Acid - physiology ; Male ; Medical sciences ; Neuropharmacology ; Pharmacology. Drug treatments ; Raphe Nuclei - drug effects ; Raphe Nuclei - physiology ; Rats ; Rats, Inbred Strains ; Seizures - physiopathology ; Tolerance</subject><ispartof>European journal of pharmacology, 1989-11, Vol.170 (3), p.145-155</ispartof><rights>1989</rights><rights>1990 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c483t-39f258fcb589f77f2041691299d1030dd067023f1272336b39ad74c5287e8a5e3</citedby><cites>FETCH-LOGICAL-c483t-39f258fcb589f77f2041691299d1030dd067023f1272336b39ad74c5287e8a5e3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/0014299989905359$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=6627974$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/2515976$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Hernandez, Theresa D.</creatorcontrib><creatorcontrib>Heninger, Catherine</creatorcontrib><creatorcontrib>Wilson, Marlene A.</creatorcontrib><creatorcontrib>Gallager, Dorothy W.</creatorcontrib><title>Relationship of agonist efficacy to changes in GABA sensitivity and anticonvulsant tolerance following chronic benzodiazepine ligand exposure</title><title>European journal of pharmacology</title><addtitle>Eur J Pharmacol</addtitle><description>Benzodiazepine ligands of differing efficacy including the agonist, diazepam, the partial agonist, Ro 16–6028 and the antagonist, Ro 15–1788, were administered in vivo to rats continuously for 3 weeks. The magnitude of change in various measures of GABA sensitivity could be correlated directly with increasing agonist efficacy: maximal changes were seen following chronic treatment with diazepam, intermediate changes were seen following the partial agonist Ro 16–6028 and no changes were observed following chronic Ro 15–1788 administration. The magnitude of change could also be correlated with increasing potential for tolerance development to anticonvulsant efficacy following chronic exposure to these benzodiazepine ligands.</description><subject>Agonist efficacy</subject><subject>Animals</subject><subject>Anticonvulsants</subject><subject>Anticonvulsants. Antiepileptics. Antiparkinson agents</subject><subject>Behavior, Animal - drug effects</subject><subject>Benzodiazepines (chronic)</subject><subject>Benzodiazepines - pharmacology</subject><subject>Benzodiazepinones - pharmacology</subject><subject>Bicuculline - metabolism</subject><subject>Bicuculline - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Brain Chemistry - drug effects</subject><subject>Diazepam - pharmacology</subject><subject>Drug Tolerance</subject><subject>Electrophysiology</subject><subject>Flumazenil - pharmacology</subject><subject>GABA</subject><subject>gamma-Aminobutyric Acid - physiology</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Neuropharmacology</subject><subject>Pharmacology. Drug treatments</subject><subject>Raphe Nuclei - drug effects</subject><subject>Raphe Nuclei - physiology</subject><subject>Rats</subject><subject>Rats, Inbred Strains</subject><subject>Seizures - physiopathology</subject><subject>Tolerance</subject><issn>0014-2999</issn><issn>1879-0712</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1989</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkcGKFDEQhhtR1nH1DRRyENFDa5LudDoXYVx0FRYE0XPIpCuzJZmkTbpHZ9_BdzbtDHPUQ0igvvqp1FdVTxl9zSjr3lDK2porpV726pWiohG1uletWC9VTSXj96vVGXlYPcr5O6VUKC4uqgsumFCyW1W_v4A3E8aQb3Ek0RGzjQHzRMA5tMYeyBSJvTVhC5lgINfrd2uSIWSccI_TgZgwlDOhjWE_-1yepcNDMsECcdH7-BPDtkSkkmvJBsJdHNDcwYgBiMftEgC_xpjnBI-rB874DE9O92X17cP7r1cf65vP15-u1je1bftmqhvluOid3YheOSkdpy3rFCsfHRht6DDQTlLeOMYlb5pu0ygzyNYK3kvojYDmsnpxzB1T_DFDnvQOswXvTYA4Zy1V27Wyp_8FmWhFJ6QqYHsEbYo5J3B6TLgz6aAZ1YsuvbjQiwvdK_1Xl17anp3y580OhnPTyU-pPz_VTbbGu2WtmM9Y13GpZFuwt0cMytL2CElni1AMDJjATnqI-O85_gBb_LMO</recordid><startdate>19891107</startdate><enddate>19891107</enddate><creator>Hernandez, Theresa D.</creator><creator>Heninger, Catherine</creator><creator>Wilson, Marlene A.</creator><creator>Gallager, Dorothy W.</creator><general>Elsevier B.V</general><general>Elsevier</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>7TK</scope><scope>7X8</scope></search><sort><creationdate>19891107</creationdate><title>Relationship of agonist efficacy to changes in GABA sensitivity and anticonvulsant tolerance following chronic benzodiazepine ligand exposure</title><author>Hernandez, Theresa D. ; Heninger, Catherine ; Wilson, Marlene A. ; Gallager, Dorothy W.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c483t-39f258fcb589f77f2041691299d1030dd067023f1272336b39ad74c5287e8a5e3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1989</creationdate><topic>Agonist efficacy</topic><topic>Animals</topic><topic>Anticonvulsants</topic><topic>Anticonvulsants. Antiepileptics. Antiparkinson agents</topic><topic>Behavior, Animal - drug effects</topic><topic>Benzodiazepines (chronic)</topic><topic>Benzodiazepines - pharmacology</topic><topic>Benzodiazepinones - pharmacology</topic><topic>Bicuculline - metabolism</topic><topic>Bicuculline - pharmacology</topic><topic>Biological and medical sciences</topic><topic>Brain Chemistry - drug effects</topic><topic>Diazepam - pharmacology</topic><topic>Drug Tolerance</topic><topic>Electrophysiology</topic><topic>Flumazenil - pharmacology</topic><topic>GABA</topic><topic>gamma-Aminobutyric Acid - physiology</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Neuropharmacology</topic><topic>Pharmacology. Drug treatments</topic><topic>Raphe Nuclei - drug effects</topic><topic>Raphe Nuclei - physiology</topic><topic>Rats</topic><topic>Rats, Inbred Strains</topic><topic>Seizures - physiopathology</topic><topic>Tolerance</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Hernandez, Theresa D.</creatorcontrib><creatorcontrib>Heninger, Catherine</creatorcontrib><creatorcontrib>Wilson, Marlene A.</creatorcontrib><creatorcontrib>Gallager, Dorothy W.</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>Neurosciences Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>European journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Hernandez, Theresa D.</au><au>Heninger, Catherine</au><au>Wilson, Marlene A.</au><au>Gallager, Dorothy W.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Relationship of agonist efficacy to changes in GABA sensitivity and anticonvulsant tolerance following chronic benzodiazepine ligand exposure</atitle><jtitle>European journal of pharmacology</jtitle><addtitle>Eur J Pharmacol</addtitle><date>1989-11-07</date><risdate>1989</risdate><volume>170</volume><issue>3</issue><spage>145</spage><epage>155</epage><pages>145-155</pages><issn>0014-2999</issn><eissn>1879-0712</eissn><coden>EJPHAZ</coden><abstract>Benzodiazepine ligands of differing efficacy including the agonist, diazepam, the partial agonist, Ro 16–6028 and the antagonist, Ro 15–1788, were administered in vivo to rats continuously for 3 weeks. The magnitude of change in various measures of GABA sensitivity could be correlated directly with increasing agonist efficacy: maximal changes were seen following chronic treatment with diazepam, intermediate changes were seen following the partial agonist Ro 16–6028 and no changes were observed following chronic Ro 15–1788 administration. The magnitude of change could also be correlated with increasing potential for tolerance development to anticonvulsant efficacy following chronic exposure to these benzodiazepine ligands.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>2515976</pmid><doi>10.1016/0014-2999(89)90535-9</doi><tpages>11</tpages></addata></record> |
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| ispartof | European journal of pharmacology, 1989-11, Vol.170 (3), p.145-155 |
| issn | 0014-2999 1879-0712 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Agonist efficacy Animals Anticonvulsants Anticonvulsants. Antiepileptics. Antiparkinson agents Behavior, Animal - drug effects Benzodiazepines (chronic) Benzodiazepines - pharmacology Benzodiazepinones - pharmacology Bicuculline - metabolism Bicuculline - pharmacology Biological and medical sciences Brain Chemistry - drug effects Diazepam - pharmacology Drug Tolerance Electrophysiology Flumazenil - pharmacology GABA gamma-Aminobutyric Acid - physiology Male Medical sciences Neuropharmacology Pharmacology. Drug treatments Raphe Nuclei - drug effects Raphe Nuclei - physiology Rats Rats, Inbred Strains Seizures - physiopathology Tolerance |
| title | Relationship of agonist efficacy to changes in GABA sensitivity and anticonvulsant tolerance following chronic benzodiazepine ligand exposure |
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