Asenapine, a novel psychopharmacologic agent: preclinical evidence for clinical effects in schizophrenia.

Asenapine, a novel psychopharmacologic agent: preclinical evidence for clinical effects in schizophrenia. Research Abstract Details 

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Asenapine, a novel psychopharmacologic agent: preclinical evidence for clinical effects in schizophrenia. Abstract Text:

Olivia Frånberg,Charlotte Wiker,Monica M Marcus,Asa Konradsson,Kent Jardemark,Björn Schilström,Mohammed Shahid,Erik H F Wong,Torgny H Svensson,Olivia ,Charlotte Wiker,Monica M Marcus,Asa Konradsson,Kent Jardemark, ,Mohammed Shahid,Erik H F Wong,Torgny H Svensson,

RATIONALE: Asenapine is a novel psychopharmacologic agent being developed for the treatment of schizophrenia and bipolar disorder. MATERIALS AND METHODS: The present study was undertaken to investigate the effects of asenapine using animal models predictive of antipsychotic efficacy (conditioned avoidance response [CAR]) and extrapyramidal side effects (EPS; catalepsy). In parallel, the effects of asenapine on regional dopamine output using in vivo microdialysis in freely moving rats, dopamine output in the core and shell subregions of nucleus accumbens (NAc) using in vivo voltammetry in anesthetized rats, and N-methyl-D: -aspartate (NMDA)-induced currents in pyramidal neurons of the medial prefrontal cortex (mPFC) using the electrophysiological technique intracellular recording in vitro were assessed. RESULTS: Asenapine (0.05-0.2 mg/kg, subcutaneous [s.c.]) induced a dose-dependent suppression of CAR (no escape failures recorded) and did not induce catalepsy. Asenapine (0.05-0.2 mg/kg, s.c.) increased dopamine efflux in both the mPFC and the NAc. Low-dose asenapine (0.01 mg/kg, intravenous [i.v.]) increased dopamine efflux preferentially in the shell compared to the core of NAc, whereas at a higher dose (0.05 mg/kg, i.v.), the difference disappeared. Finally, like clozapine (100 nM), but at a considerably lower concentration (5 nM), asenapine significantly potentiated the NMDA-induced responses in pyramidal cells of the mPFC. CONCLUSIONS: These preclinical data suggest that asenapine may exhibit highly potent antipsychotic activity with very low EPS liability. Its ability to increase both dopaminergic and glutamatergic activity in rat mPFC suggests that asenapine may possess an advantageous effect not only on positive symptoms in patients with schizophrenia, but also on negative and cognitive symptoms.

Asenapine, a novel psychopharmacologic agent: preclinical evidence for clinical effects in schizophrenia. Publishing Authors By Initials

O Frånberg,C Wiker,MM Marcus,A Konradsson,K Jardemark,B Schilström,M Shahid,EH Wong,TH Svensson,O ,C Wiker,MM Marcus,A Konradsson,K Jardemark,B ,M Shahid,EH Wong,TH Svensson,

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Asenapine, a novel psychopharmacologic agent: preclinical evidence for clinical effects in schizophrenia. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Psychopharmacology

VOLUME: 196

Page Numbers: 417-29

Journal Abbreviation: Psychopharmacology (Berl.)

ISSN: 0033-3158

DAY: 17

MONTH: 10

YEAR: 2007

Asenapine, a novel psychopharmacologic agent: preclinical evidence for clinical effects in schizophrenia. Information

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LANGUAGE: eng

NlmUniqueID: 7608025

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AFFILIATION: Department of Physiology and Pharmacology, Section of Neuropsychopharmacology, Karolinska Institutet, Nanna Svartz väg 2, 171 77, Stockholm, Sweden.

Country: Germany

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MEDLINETA: Psychopharmacology (Berl)

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