Antagonism by neuroleptics of neurotransmitter receptors of normal human brain in vitro

Elliott Richelson, Albert Nelson

Research output: Contribution to journalArticle

194 Scopus citations

Abstract

Using radioligand binding techniques, we determined the equilibrium dissociation constants (KD's) for a series of neuroleptics at the dopamine (D-2), muscarinic, histamine H1, α1- and α2-adrenergic receptors of normal human brain tissue obtained at autopsy. Seventeen different compounds were studied at the D-2 receptor and 15 compounds at the remaining receptors. At the D-2 receptor of caudate nucleus, spiperone was the most potent compound (KD = 0.16 nM); clozapine the least potent (KD = 180 nM). The KD's for six compounds at the D-2 receptor of nucleus accumbens were not significantly different from their respective KD's in the caudate nucleus. The most potent and least potent compounds at the other receptors were clozapine and molindone at the muscarinic receptor, mesoridazine and molindone at the H1 receptor, spiperone and molindone at the α1-receptor, and clozapine and haloperidol at the α2-receptor, respectively.

Original languageEnglish (US)
Pages (from-to)197-204
Number of pages8
JournalEuropean Journal of Pharmacology
Volume103
Issue number3-4
DOIs
StatePublished - Aug 17 1984

    Fingerprint

Keywords

  • Antipsychotics
  • Dopamine (D-2) receptor
  • Histamine H receptor
  • Muscarinic receptor
  • α-Adrenergic receptors

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

Cite this