Involvement of 5-HT2A receptor and α2-adrenoceptor blockade in the asenapine-induced elevation of prefrontal cortical monoamine outflow.

Synapse
Olivia FrånbergT H Svensson

Abstract

The psychotropic drug asenapine is approved for the treatment of schizophrenia and manic or mixed episodes associated with bipolar I disorder. Asenapine exhibits higher affinity for several 5-HT receptors and α(2)-adrenoceptors than for D(2) receptors. Noteworthy, blockage of both the 5-HT(2A) and α(2)-adrenergic receptors has been shown to enhance prefrontal dopamine release induced by D(2) receptor antagonists. Previous results show that asenapine, both systemically and locally, increases dopamine, noradrenaline, and serotonin release in the medial prefrontal cortex (mPFC), and that the increased dopamine release largely depends on an intracortical action. Using reverse microdialysis in freely moving rats, we here assessed the potency of low concentrations of asenapine to cause a pharmacologically significant blockage in vivo of 5-HT(2A) receptors and α(2)-adrenoceptors within the mPFC, and thus its ability to affect cortical monoamine release by these receptors. Intracortical administration of 1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane hydrochloride (DOI), a 5-HT(2A/2C) receptor agonist, increased cortical monoamine release, effects that were antagonized both by asenapine and the selective 5-HT(2A) antagonist M100907. App...Continue Reading

References

Jul 1, 1992·Progress in Neuro-psychopharmacology & Biological Psychiatry·Y MizukiM Yamada
Nov 1, 1991·The American Journal of Psychiatry·K L DavisM Davidson
Apr 1, 1990·International Clinical Psychopharmacology·Y MizukiM Yamada
Feb 1, 1995·Schizophrenia Research·A Breier
Aug 1, 1993·Journal of Clinical Psychopharmacology·R E LitmanD Pickar
Jan 1, 1996·Neuropharmacology·A Newman-TancrediM J Millan
May 1, 1996·The British Journal of Psychiatry : the Journal of Mental Science·R E LitmanD Pickar
Jan 1, 1997·The Journal of Neuropsychiatry and Clinical Neurosciences·A Abi-DarghamJ Krystal
Jul 1, 1997·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·P HertelT H Svensson
Jan 22, 1998·Proceedings of the National Academy of Sciences of the United States of America·R L Jakab, P S Goldman-Rakic
Aug 17, 1999·The British Journal of Psychiatry : the Journal of Mental Science·M PoyurovskyA Weizman
Feb 7, 2001·The Journal of Comparative Neurology·S SchroeterR D Blakely
Mar 14, 2002·International Clinical Psychopharmacology·R ShilohA Weizman
Mar 26, 2003·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·Michael PoyurovskyRonit Weizman
Jun 11, 2003·Archives of General Psychiatry·John M DavisIra D Glick
Dec 4, 2003·Progress in Neuro-psychopharmacology & Biological Psychiatry·Torgny H Svensson
Feb 26, 2004·Proceedings of the National Academy of Sciences of the United States of America·Guojun ChenZhen Yan
May 1, 2004·Psychopharmacology·Patricia S Goldman-RakicGraham V Williams
Sep 15, 2004·Progress in Neuro-psychopharmacology & Biological Psychiatry·Kenichi Yamamoto, Oleh Hornykiewicz

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Citations

Feb 7, 2015·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·Chris A OosterhofPierre Blier
Mar 17, 2015·Trends in Pharmacological Sciences·Salomon Z Langer
May 14, 2014·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·Mark J MillanWilliam P Horan
Jul 1, 2016·CNS Drugs·Greg L Plosker, Emma D Deeks
Jul 25, 2013·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Renata S CouraSylvie Granon
Apr 19, 2017·CNS Neuroscience & Therapeutics·Sarah DelcourteNasser Haddjeri

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