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  • The International Journal of Neuropsychopharmacology, Volume 13, Issue 3
  • April 2010, pp. 405-410

Repeated effects of asenapine on adrenergic and cholinergic muscarinic receptors

  • Yong Kee Choi (a1) (a2), Erik H. F. Wong (a3), Brian Henry (a4), Mohammed Shahid (a5) and Frank I. Tarazi (a1) (a2)
  • DOI: http://dx.doi.org/10.1017/S1461145709990824
  • Published online: 19 October 2009
Abstract
Abstract

Adrenergic (α1 and α2) and cholinergic muscarinic (M1–M5) receptor binding in rat forebrain was quantified after 4 wk of twice-daily subcutaneous administration of asenapine or vehicle. Asenapine (0.03, 0.1, and 0.3 mg/kg) produced increases in [3H]prazosin binding to α1-adrenergic receptors in the medial prefrontal cortex (mPFC: 30%, 39%, 57%) and dorsolateral frontal cortex (DFC: 27%, 37%, 53%) and increased [3H]RX821002 binding to α2-adrenergic receptors in mPFC (36%, 43%, 50%) and DFC (41%, 44%, 52%). Despite showing no appreciable affinity for muscarinic receptors, asenapine produced regionally selective increases in binding of [3H]QNB to M1–M5 receptors in mPFC (26%, 31%, 43%), DFC (27%, 34%, 41%), and hippocampal CA1 (40%, 44%, 42%) and CA3 (25%, 52%, 48%) regions. These regionally selective effects of asenapine on adrenergic and cholinergic muscarinic receptor subtypes may contribute to its beneficial clinical effects in the treatment of schizophrenia and bipolar disorder.

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Corresponding author
Address for correspondence: Dr F. I. Tarazi, Laboratory of Psychiatric Neuroscience, McLean Hospital, Harvard Medical School, 115 Mill Street, Belmont, MA 02478, USA. Tel.: 617-855-3176Fax: 617-855-3479Email: ftarazi@hms.harvard.edu
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The International Journal of Neuropsychopharmacology
  • ISSN: 1461-1457
  • EISSN: 1469-5111
  • URL: /core/journals/the-international-journal-of-neuropsychopharmacology
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