| Cariprazine (RGH-188), a D(3)-preferring dopamine D (3)/D (2) receptor partial agonist antipsychotic candidate demonstrates anti-abuse potential in rats. | |
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MedLine Citation:
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PMID: 23138433 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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RATIONALE: Cariprazine (RGH-188) is a D(3)-preferring dopamine D(3)/D(2) receptor partial agonist antipsychotic candidate for the treatment of schizophrenia and bipolar mania. Substance abuse is a frequent comorbidity of both disorders and is associated with serious health issues. Based on preclinical efficacy, dopamine D(2) and D(3) receptor partial agonists and antagonists are assumed to have relapse-preventing potential in human cocaine addiction. OBJECTIVES: We investigated the anti-abuse potential of cariprazine in cocaine self-administration paradigms. Aripiprazole and bifeprunox were used as comparators because of their pharmacological similarity to cariprazine. METHODS: The effects of compounds on cocaine's rewarding effect were investigated in a continuous self-administration regimen. The relapse-preventing potential of drugs was studied in rats with a history of cocaine self-administration after a period of complete abstinence in a relapse to cocaine-seeking paradigm. RESULTS: Cariprazine, as well as aripiprazole and bifeprunox, were able to reduce the rewarding effect of cocaine (minimum effective doses were 0.17, 1, and 0.1 mg/kg, respectively) and attenuated relapse to cocaine seeking with half maximal effective dose [ED(50)] values of 0.2, 4.2, and 0.17 mg/kg, respectively. CONCLUSIONS: These results may predict a relapse-preventing action for cariprazine in humans in addition to its already established antipsychotic and antimanic efficacy. |
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Authors:
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V Román; I Gyertyán; K Sághy; B Kiss; Zs Szombathelyi |
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Publication Detail:
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Type: JOURNAL ARTICLE Date: 2012-11-9 |
Journal Detail:
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Title: Psychopharmacology Volume: - ISSN: 1432-2072 ISO Abbreviation: Psychopharmacology (Berl.) Publication Date: 2012 Nov |
Date Detail:
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Created Date: 2012-11-9 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 7608025 Medline TA: Psychopharmacology (Berl) Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Affiliation:
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Pharmacology and Drug Safety Research, Gedeon Richter Plc, Budapest, Hungary, v.roman@richter.hu. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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