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Influence of neuroleptics on the binding of met-enkephalin, morphine and dihydromorphine to synaptosome-enriched fractions of rat brain

Authors
Journal
Neuropharmacology
0028-3908
Publisher
Elsevier
Publication Date
Volume
17
Issue
8
Identifiers
DOI: 10.1016/0028-3908(78)90151-x
Keywords
  • Opiates
  • Neuroleptics
  • Enkephalin
  • Binding Studies
  • Chlorpromazine
  • Haloperidol
  • Met-Enkephalin
  • Opiate Receptor

Abstract

Abstract The influence of three neuroleptics on the binding of tritiated met-enkephalin to synaptosomeenriched fractions of rat brain was studied in the high-affinity binding region. All three drugs tested blocked the binding of met-enkephalin in a dose-dependent fashion with inhibition constants ( k i) of 11.6, 39.5 and 29.5 μM for haloperidol, chlorpromazine and prochlorperazine, respectively. Hill plots suggest that the inhibitory mechanism involves negative allosteric effects between neuroleptic molecules. The effects of these neuroleptics on the binding of tritiated morphine and dihydromorphine were also studied.

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