Asenapine induces differential regional effects on serotonin receptor subtypes.

Journal of Psychopharmacology
Frank I TaraziMohammed Shahid

Abstract

Asenapine, a novel psychopharmacologic agent being developed for the treatment of schizophrenia and bipolar disorder, has high affinity for a wide range of receptors, including the serotonergic receptors 5-HT(1A), 5-HT(1B), 5-HT(2A), 5-HT( 2B), 5-HT(2C), 5-HT(5A), 5-HT(6) and 5-HT( 7). We examined the long-term effects in rat brain of multiple doses of asenapine on representative serotonin receptor subtypes: 5-HT(1A), 5-HT(2A) and 5-HT(2C). Rats were given asenapine (0.03, 0.1 or 0.3 mg/kg) subcutaneously twice daily or vehicle for 4 weeks. Brain sections were collected from the medial prefrontal cortex (mPFC), dorsolateral frontal cortex (DFC), caudate putamen, nucleus accumbens, hippocampal CA( 1) and CA(3) regions, and entorhinal cortex and processed for in-vitro receptor autoradiography. Asenapine 0.1 and 0.3 mg/kg significantly increased 5-HT(1A) binding in mPFC (by 24% and 33%, respectively), DFC (27%, 31%) and hippocampal CA(1) region (23%, 25%) (all P < 0.05). All three asenapine doses (0.03, 0.1 and 0.3 mg/kg) significantly decreased 5-HT(2A) binding by a similar degree in mPFC (40%, 44%, 47%, respectively) and DFC (45%, 51%, 52%) (all P < 0.05), but did not alter 5-HT(2A) binding in the other brain regions studied. In...Continue Reading

References

Jan 1, 1988·Schizophrenia Bulletin·A BleichH M van Praag
Jan 1, 1987·Annual Review of Biochemistry·A G Gilman
Jan 16, 1995·The Journal of Comparative Neurology·D E WrightL Jennes
Oct 1, 1993·Archives of General Psychiatry·M LaruelleJ E Kleinman
Jun 1, 1993·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·J N JoyceJ E Kleinman
Oct 6, 1997·Biological Psychiatry·E V Gurevich, J N Joyce
Aug 5, 1999·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·H Y Meltzer
May 30, 2001·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·F M Benes, S Berretta
Jul 10, 2001·Molecular Psychiatry·M S SodhiP J Harrison
Jan 5, 2002·CNS Drugs·Daniel TarsyFrank I Tarazi
Dec 4, 2003·Progress in Neuro-psychopharmacology & Biological Psychiatry·Herbert Y MeltzerJunji Ichikawa
Apr 13, 2005·Clinical Therapeutics·John W Newcomer
Nov 25, 2005·The Journal of Neuroscience : the Official Journal of the Society for Neuroscience·Llorenç Díaz-MataixFrancesc Artigas
Feb 24, 2006·NeuroRx : the Journal of the American Society for Experimental NeuroTherapeutics·Shitij KapurMing Li
Aug 15, 2006·Annual Review of Medicine·L Fredrik JarskogJeffrey A Lieberman
Mar 30, 2007·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Miroslav M SavićJames M Cook
Oct 27, 2007·The Journal of Clinical Psychiatry·Steven G PotkinJohn Panagides

❮ Previous
Next ❯

Citations

May 21, 2009·Journal of Molecular Neuroscience : MN·Yong Kee ChoiFrank I Tarazi
Nov 16, 2013·CNS Spectrums·Yong Kee ChoiFrank I Tarazi
Aug 2, 2012·Expert Opinion on Pharmacotherapy·Frank I Tarazi, Stephen M Stahl
Jul 5, 2011·Expert Review of Neurotherapeutics·Maurizio PompiliPaolo Girardi
Feb 5, 2015·European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology·Andrea de BartolomeisCarmine Tomasetti
Oct 20, 2009·The International Journal of Neuropsychopharmacology·Yong Kee ChoiFrank I Tarazi
Jul 1, 2016·CNS Drugs·Greg L Plosker, Emma D Deeks
Jun 28, 2016·Expert Opinion on Drug Safety·L OrsoliniD De Berardis
Jun 10, 2017·Synapse·Yong Kee ChoiFrank I Tarazi
May 4, 2018·Expert Opinion on Drug Discovery·Anna WesołowskaMarcin Kołaczkowski
Dec 1, 2011·Therapeutic Advances in Psychopharmacology·Gavin P Reynolds
Jul 2, 2011·Journal of Clinical Psychopharmacology·Mohammad Jafferany, Melissa A Silverman
Aug 10, 2018·Journal of Molecular Neuroscience : MN·Yong Kee Choi, Frank I Tarazi
Mar 23, 2011·Current Opinion in Pharmacology·H Y Meltzer, B W Massey

❮ Previous
Next ❯

Related Concepts

Related Feeds

Bipolar Disorder

Bipolar disorder is characterized by manic and/or depressive episodes and associated with uncommon shifts in mood, activity levels, and energy. Discover the latest research this illness here.

Basal Ganglia

Basal Ganglia are a group of subcortical nuclei in the brain associated with control of voluntary motor movements, procedural and habit learning, emotion, and cognition. Here is the latest research.