Receptor reserve at striatal dopamine autoreceptors: Implications for selectivity of dopamine agonists

E. Meller, E. Helmer-Matyjek, K. Bohmaker, C. H. Adler, A. J. Friedhoff, M. Goldstein

Research output: Contribution to journalArticlepeer-review

63 Scopus citations

Abstract

The dose response curve for apomorphine reversal of γ-butyrolactone (GBL)-induced L-DOPA accumulation in rat striatum was shifted almost 6-fold to the right after partial irreversible blockade (83%) of dopamine (DA) autoreceptors with N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline (EEDQ); however, the maximal response was not reduced. In contrast, the major effect of a similar degree of irreversible blockade (86%) on the dose-response curve for the autoreceptor-selective agent EMD 23,448 was a reduction in maximal response (60% of control), indicating that EMD 23,448 is a partial agonist. A large receptor reserve therefore exists at the DA autoreceptor, which may explain in part why many DA agonists are more potent in models pre- than postsynaptic receptor activation.

Original languageEnglish (US)
Pages (from-to)311-314
Number of pages4
JournalEuropean Journal of Pharmacology
Volume123
Issue number2
DOIs
StatePublished - Apr 16 1986

Keywords

  • Apomorphine Receptor receptor reserve EMD 23,448
  • Dopamine autoreceptors Irreversible receptor inactivation
  • N-Ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline-butyrolactone

ASJC Scopus subject areas

  • Pharmacology

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