Binding interactions of lysergic acid diethylamide and related agents with dopamine receptors in the brain

D. R. Burt, I. Creese, S. H. Snyder

Research output: Contribution to journalArticlepeer-review

Abstract

In most brain regions saturable binding of d [3H]lysergic acid diethylamide ([3H]LSD) appears to involve postsynaptic serotonin receptors. In calf caudate, however, a portion of [3H]LSD binding involves postsynaptic dopamine receptors. Thus, in the hippocampus of calf brain, dopamine competes for [3H]LSD binding sites with a single low-affinity component, while in the caudate dopamine competition for [3H]LSD binding displays both high and low affinity components. The high affinity component, accounting for 15 to 20% of [3H]LSD binding, displays a K(i) value for dopamine of about 30nM, similar to the K(D) for the binding of [3H]dopamine itself to postsynaptic dopamine receptors in the calf caudate. Addition of serotonin to the incubations increases the proportion of [3H]LSD binding in the caudate competed for by dopamine with high affinity, presumably by occupying serotonin receptors. d LSD competes stereospecifically for [3H]dopamine binding in the caudate, consistent with the conclusion that LSD binds to dopamine receptors. Of numerous serotonin agonists and antagonists examined, several ergot alkaloids have high affinity for [3H]dopamine receptor binding in calf caudate, with K(i) values similar to that of d LSD.

Original languageEnglish (US)
Pages (from-to)631-638
Number of pages8
JournalMolecular Pharmacology
Volume12
Issue number4
StatePublished - Dec 1 1976

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology

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