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

Elliott Richelson, Albert Nelson

Research output: Contribution to journalArticle

194 Citations (Scopus)

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

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Molindone
Neurotransmitter Receptor
Clozapine
Spiperone
Caudate Nucleus
Mesoridazine
Brain
Histamine H1 Receptors
Nucleus Accumbens
Muscarinic Receptors
Haloperidol
Adrenergic Receptors
Cholinergic Agents
Histamine
Antipsychotic Agents
Autopsy
Dopamine
In Vitro Techniques
neuroleptic receptor

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

Antagonism by neuroleptics of neurotransmitter receptors of normal human brain in vitro. / Richelson, Elliott; Nelson, Albert.

In: European Journal of Pharmacology, Vol. 103, No. 3-4, 17.08.1984, p. 197-204.

Research output: Contribution to journalArticle

Richelson, Elliott ; Nelson, Albert. / Antagonism by neuroleptics of neurotransmitter receptors of normal human brain in vitro. In: European Journal of Pharmacology. 1984 ; Vol. 103, No. 3-4. pp. 197-204.
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