The dopamine receptor: Differential binding of d-LSD and related agents to agonist and antagonist states

Ian Creese, David R. Burt, Solomon H. Snyder

Research output: Contribution to journalArticle

Abstract

Dopamine receptor binding is calf striatal membranes of 3H-dopamine and 3H-haloperidol appears to differentiate agonist and antagonist states of the receptor. Agonists and antagonists have selective affinities for dopamine and haloperidol sites respectively. In evaluating relative affinities for dopamine and haloperidol binding sites, we have observed that d-LSD interacts with considerable affinity at the dopamine receptor. Its similar competition petition for binding of the two tritiated ligands suggests that it is a mixed agonist-antagonist, which is consistent with its interactions with the dopamine-sensitive adenylate cyclase. The effects of LSD on dopamine receptor binding are stereospecific, with d-LSD being 1,000 times more potent than d-LSD. 2-Bromo-LSD has more of an antagonist profile than d-LSD for the dopamine receptor. In binding experiments methiothepin behaves like a potent and relatively pure antagonist at dopamine receptors.

Original languageEnglish (US)
Pages (from-to)1715-1719
Number of pages5
JournalLife Sciences
Volume17
Issue number11
DOIs
StatePublished - Dec 1 1975

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)

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