Might Adrenergic alpha2C-agonists/alpha2A-antagonists become novel therapeutic tools for pain treatment with morphine?

  • CARDINALETTI, CLAUDIA
  • MATTIOLI, LAURA
  • GHELFI, Francesca
  • DEL BELLO, FABIO
  • GIANNELLA, Mario
  • PERFUMI, Marina Cecilia
  • PIERGENTILI, Alessandro
  • QUAGLIA, Wilma
  • PIGINI, Maria
  • BRUZZONE A.
  • PARIS H.
Publication date
January 2009

Abstract

The imidazoline nucleus linked in position 2 via an oxyethylene bridge to a phenyl ring carrying an ortho substituent of moderate steric bulk provided α2-adrenergic (AR) ligands endowed with significant α2C-agonism/α2A-antagonism. Similar behavior was displayed by cirazoline (12). For their positive morphine analgesia modulation (due to α2C-AR stimulation) and sedation overcoming (due to α2A-AR antagonism), 8 and 11 might be useful as adjuvant agents in the management of pain with morphine

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