Some effects of CB1 antagonists with inverse agonist and neutral biochemical properties
Abstract The CB1 inverse agonist/antagonist SR141716A recently has been introduced for the management of obesity (rimonabant; Acomplia) and appears to have beneficial effects. However, its utility may be hampered in some individuals by adverse effects including nausea or emesis or by mood depression...
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| Veröffentlicht in: | Physiology & behavior 2008-03, Vol.93 (4), p.666-670 |
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| creator | Bergman, Jack Delatte, Marcus S Paronis, Carol A Vemuri, Kiran Thakur, Ganesh A Makriyannis, Alex |
| description | Abstract The CB1 inverse agonist/antagonist SR141716A recently has been introduced for the management of obesity (rimonabant; Acomplia) and appears to have beneficial effects. However, its utility may be hampered in some individuals by adverse effects including nausea or emesis or by mood depression. The recent development of biochemically ‘neutral’ antagonists such as AM4113 (Sink et al., 2007) has allowed an initial evaluation of the proposition that adverse effects of SR141716A are associated with its inverse agonist activity. Thus far, data comparing SR141716A and AM4113 across several species indicate that both drugs produce dose-related direct effects on operant behavior within the same range of doses that serve to antagonize the behavioral and hypothermic effects of a CB1 agonist. However, initial observations suggest that AM4113 may not produce preclinical indications of nausea or emesis. Further studies with AM4113 and other novel CB1 antagonists differing in efficacy should amplify our understanding of the relationship between the pharmacological activity of CB1 antagonists and their behavioral effects. |
| doi_str_mv | 10.1016/j.physbeh.2007.11.007 |
| format | Article |
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However, its utility may be hampered in some individuals by adverse effects including nausea or emesis or by mood depression. The recent development of biochemically ‘neutral’ antagonists such as AM4113 (Sink et al., 2007) has allowed an initial evaluation of the proposition that adverse effects of SR141716A are associated with its inverse agonist activity. Thus far, data comparing SR141716A and AM4113 across several species indicate that both drugs produce dose-related direct effects on operant behavior within the same range of doses that serve to antagonize the behavioral and hypothermic effects of a CB1 agonist. However, initial observations suggest that AM4113 may not produce preclinical indications of nausea or emesis. Further studies with AM4113 and other novel CB1 antagonists differing in efficacy should amplify our understanding of the relationship between the pharmacological activity of CB1 antagonists and their behavioral effects.</description><identifier>ISSN: 0031-9384</identifier><identifier>EISSN: 1873-507X</identifier><identifier>DOI: 10.1016/j.physbeh.2007.11.007</identifier><identifier>PMID: 18076956</identifier><language>eng</language><publisher>Cambridge: Elsevier Inc</publisher><subject>AM4054 ; AM4113 ; Animals ; Behavior ; Behavior, Animal - drug effects ; Behavioral psychophysiology ; Biological and medical sciences ; Conditioning, Operant - drug effects ; Drug Interactions ; Fundamental and applied biological sciences. Psychology ; Hypothermia ; Inverse agonism ; Neutral antagonism ; Piperidines - pharmacology ; Psychiatry ; Psychology. Psychoanalysis. Psychiatry ; Psychology. Psychophysiology ; Pyrazoles - pharmacology ; Receptor, Cannabinoid, CB1 - agonists ; Receptor, Cannabinoid, CB1 - antagonists & inhibitors ; Receptor, Cannabinoid, CB1 - physiology ; Rimonabant ; SR141716A</subject><ispartof>Physiology & behavior, 2008-03, Vol.93 (4), p.666-670</ispartof><rights>Elsevier Inc.</rights><rights>2007 Elsevier Inc.</rights><rights>2008 INIST-CNRS</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c526t-485ce58a741a2aefa79d66f6f28088d832889d898f2aa57e03a9a2b93db0bb473</citedby><cites>FETCH-LOGICAL-c526t-485ce58a741a2aefa79d66f6f28088d832889d898f2aa57e03a9a2b93db0bb473</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.physbeh.2007.11.007$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=20242535$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/18076956$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Bergman, Jack</creatorcontrib><creatorcontrib>Delatte, Marcus S</creatorcontrib><creatorcontrib>Paronis, Carol A</creatorcontrib><creatorcontrib>Vemuri, Kiran</creatorcontrib><creatorcontrib>Thakur, Ganesh A</creatorcontrib><creatorcontrib>Makriyannis, Alex</creatorcontrib><title>Some effects of CB1 antagonists with inverse agonist and neutral biochemical properties</title><title>Physiology & behavior</title><addtitle>Physiol Behav</addtitle><description>Abstract The CB1 inverse agonist/antagonist SR141716A recently has been introduced for the management of obesity (rimonabant; Acomplia) and appears to have beneficial effects. However, its utility may be hampered in some individuals by adverse effects including nausea or emesis or by mood depression. The recent development of biochemically ‘neutral’ antagonists such as AM4113 (Sink et al., 2007) has allowed an initial evaluation of the proposition that adverse effects of SR141716A are associated with its inverse agonist activity. Thus far, data comparing SR141716A and AM4113 across several species indicate that both drugs produce dose-related direct effects on operant behavior within the same range of doses that serve to antagonize the behavioral and hypothermic effects of a CB1 agonist. However, initial observations suggest that AM4113 may not produce preclinical indications of nausea or emesis. Further studies with AM4113 and other novel CB1 antagonists differing in efficacy should amplify our understanding of the relationship between the pharmacological activity of CB1 antagonists and their behavioral effects.</description><subject>AM4054</subject><subject>AM4113</subject><subject>Animals</subject><subject>Behavior</subject><subject>Behavior, Animal - drug effects</subject><subject>Behavioral psychophysiology</subject><subject>Biological and medical sciences</subject><subject>Conditioning, Operant - drug effects</subject><subject>Drug Interactions</subject><subject>Fundamental and applied biological sciences. Psychology</subject><subject>Hypothermia</subject><subject>Inverse agonism</subject><subject>Neutral antagonism</subject><subject>Piperidines - pharmacology</subject><subject>Psychiatry</subject><subject>Psychology. Psychoanalysis. Psychiatry</subject><subject>Psychology. Psychophysiology</subject><subject>Pyrazoles - pharmacology</subject><subject>Receptor, Cannabinoid, CB1 - agonists</subject><subject>Receptor, Cannabinoid, CB1 - antagonists & inhibitors</subject><subject>Receptor, Cannabinoid, CB1 - physiology</subject><subject>Rimonabant</subject><subject>SR141716A</subject><issn>0031-9384</issn><issn>1873-507X</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2008</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkUtv1DAQgC1ERbeFnwDKBW4JYzuOnQsIVuUhVeqhRXCzHGfMesljaydF--9xtBFIXOrLWKNvZuxvCHlJoaBAq7f74rA7xgZ3BQOQBaVFCk_IhirJcwHyx1OyAeA0r7kqz8lFjHtIh5f8GTmnCmRVi2pDvt-OPWboHNopZqPLth9pZobJ_BwHH1Pqt592mR8eMETM1mwC2mzAeQqmyxo_2h323qb7IYwHDJPH-JycOdNFfLHGS_Lt09Xd9kt-ffP56_bDdW4Fq6a8VMKiUEaW1DCDzsi6rSpXOaZAqVZxplTdqlo5ZoyQCNzUhjU1bxtomlLyS_Lm1DeNvp8xTrr30WLXmQHHOWqavl8LYAkUJ9CGMcaATh-C7004agp6Mar3ejWqF6OaUp1Cqnu1DpibHtt_VavCBLxeAROTAxfMYH38yzFgJRNcJO79icOk48Fj0NF6HCy2PiT5uh39o095918H2_lhEf8Ljxj34xyG5FpTHZkGfbusf9k-SICyLCn_A-qLrHE</recordid><startdate>20080318</startdate><enddate>20080318</enddate><creator>Bergman, Jack</creator><creator>Delatte, Marcus S</creator><creator>Paronis, Carol A</creator><creator>Vemuri, Kiran</creator><creator>Thakur, Ganesh A</creator><creator>Makriyannis, Alex</creator><general>Elsevier Inc</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>7QG</scope><scope>7TK</scope></search><sort><creationdate>20080318</creationdate><title>Some effects of CB1 antagonists with inverse agonist and neutral biochemical properties</title><author>Bergman, Jack ; Delatte, Marcus S ; Paronis, Carol A ; Vemuri, Kiran ; Thakur, Ganesh A ; Makriyannis, Alex</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c526t-485ce58a741a2aefa79d66f6f28088d832889d898f2aa57e03a9a2b93db0bb473</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2008</creationdate><topic>AM4054</topic><topic>AM4113</topic><topic>Animals</topic><topic>Behavior</topic><topic>Behavior, Animal - drug effects</topic><topic>Behavioral psychophysiology</topic><topic>Biological and medical sciences</topic><topic>Conditioning, Operant - drug effects</topic><topic>Drug Interactions</topic><topic>Fundamental and applied biological sciences. 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However, its utility may be hampered in some individuals by adverse effects including nausea or emesis or by mood depression. The recent development of biochemically ‘neutral’ antagonists such as AM4113 (Sink et al., 2007) has allowed an initial evaluation of the proposition that adverse effects of SR141716A are associated with its inverse agonist activity. Thus far, data comparing SR141716A and AM4113 across several species indicate that both drugs produce dose-related direct effects on operant behavior within the same range of doses that serve to antagonize the behavioral and hypothermic effects of a CB1 agonist. However, initial observations suggest that AM4113 may not produce preclinical indications of nausea or emesis. 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| ispartof | Physiology & behavior, 2008-03, Vol.93 (4), p.666-670 |
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| subjects | AM4054 AM4113 Animals Behavior Behavior, Animal - drug effects Behavioral psychophysiology Biological and medical sciences Conditioning, Operant - drug effects Drug Interactions Fundamental and applied biological sciences. Psychology Hypothermia Inverse agonism Neutral antagonism Piperidines - pharmacology Psychiatry Psychology. Psychoanalysis. Psychiatry Psychology. Psychophysiology Pyrazoles - pharmacology Receptor, Cannabinoid, CB1 - agonists Receptor, Cannabinoid, CB1 - antagonists & inhibitors Receptor, Cannabinoid, CB1 - physiology Rimonabant SR141716A |
| title | Some effects of CB1 antagonists with inverse agonist and neutral biochemical properties |
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