The use of quaternary narcotic antagonists in opiate research

D. R. Brown, L. I. Goldberg

Research output: Contribution to journalReview articlepeer-review

219 Scopus citations

Abstract

Quaternary ammonium derivatives of narcotic antagonists are commonly used in determining sites of action of opiates in the central nervous system and the periphery because it is widely assumed that they do not readily cross the blood-brain barrier, in contrast to their relatively non-polar tertiary counterparts. However, these compounds possess several unique pharmacological properties which have not been taken into consideration in the design of numerous investigations. This article reviews the current state of knowledge concerning the pharmacology of the quaternary narcotic antagonists, examines their use in physiological and behavioral studies of action of opiates, and proposes guidelines for the design of experiments involving these compounds.

Original languageEnglish (US)
Pages (from-to)181-191
Number of pages11
JournalNeuropharmacology
Volume24
Issue number3
DOIs
StatePublished - Mar 1985

Bibliographical note

Funding Information:
Acknowlednements-The authorsw ouldl ike to thankD r H. N. Sapru (New Jersey Medical School),D r ThomasG iles and Dr Gary Sander (Tulane University), Dr James H. Woods (Universityo f Michigan) and Dr Luciano Manara (Sanofi-Midy, S.p.A., Milan, Italy) for graciouslys upplying manuscriptosf their researchw ork prior to publicationa, nd Dr Charis R. Schuster( Universit; of Chicago)f or helpful discussionso n this manuscriptT. his work was supportedin part by NIMH Postdoctoral Training Fellowship MH 14274to D.R.B. and NIH grant GM-22220.

Keywords

  • N
  • N-diallyl nalorphine
  • N-methyllevallorphan
  • N-methylnalorphine
  • N-methylnaloxone
  • N-methylnaltrexone
  • central nervous system
  • quaternary opiate antagonists
  • quaternary opiates
  • sites of opiate action

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