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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:
  • Published online: 19 October 2009

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.

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:
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The International Journal of Neuropsychopharmacology
  • ISSN: 1461-1457
  • EISSN: 1469-5111
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