Document Detail

Cariprazine (RGH-188), a D(3)-preferring dopamine D (3)/D (2) receptor partial agonist antipsychotic candidate demonstrates anti-abuse potential in rats.
MedLine Citation:
PMID:  23138433     Owner:  NLM     Status:  Publisher    
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.
V Román; I Gyertyán; K Sághy; B Kiss; Zs Szombathelyi
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-11-9
Journal Detail:
Title:  Psychopharmacology     Volume:  -     ISSN:  1432-2072     ISO Abbreviation:  Psychopharmacology (Berl.)     Publication Date:  2012 Nov 
Date Detail:
Created Date:  2012-11-9     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7608025     Medline TA:  Psychopharmacology (Berl)     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Pharmacology and Drug Safety Research, Gedeon Richter Plc, Budapest, Hungary,
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