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

Elliott Richelson, Albert Nelson

Research output: Contribution to journalArticlepeer-review

195 Scopus citations


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
Issue number3-4
StatePublished - Aug 17 1984


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

ASJC Scopus subject areas

  • Pharmacology


Dive into the research topics of 'Antagonism by neuroleptics of neurotransmitter receptors of normal human brain in vitro'. Together they form a unique fingerprint.

Cite this