An in vivo alpha-2 assay reversal of opioid-induced muscular rigidity and neuroleptic-induced ptosis

Mark J. Benvenga, Robert A. Del Vecchio, John F. Capacchione, Thomas P. Jerussi

Research output: Contribution to journalArticlepeer-review

5 Scopus citations

Abstract

A method is described to detect selective α-2 adrenergic agonists in vivo. Palpebral ptosis is induced in rats by the neuroleptic agent haloperidol (Hal), or by tetrabenazine (TBZ) methanesulfonate. Twenty minutes later, test compounds are injected, and ptosis is scored. In a separate test, muscular rigidity is induced by the opioid, fentanyl, and subsequently, test compounds are assessed for their ability to reverse muscular rigidity. Results indicate that only α-2 agonists reliably reverse neuroleptic-induced and TBZ-induced ptosis, as well as opioid-induced rigidity. An α-1 antagonist reversed only rigidity, whereas, α-2 antagonists and β-agonists were generally ineffective in all tests. Therefore, the ability to reverse neuroleptic and TBZ-induced ptosis along with the ability to reverse opioid-induced muscular rigidity is a characteristic unique to α-2 agonists.

Original languageEnglish (US)
Pages (from-to)45-50
Number of pages6
JournalJournal of Pharmacological and Toxicological Methods
Volume27
Issue number1
DOIs
StatePublished - Mar 1992

Keywords

  • Alpha-2 agonists
  • Opioid rigidity
  • Palpebral ptosis

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