Antagonism by neuroleptics of serotonin 5-HT1A and 5-HT2 receptors of normal human brain in vitro

Theodore J. Wander, Albert Nelson, Haruo Okazaki, Elliott Richelson

Research output: Contribution to journalArticle

60 Scopus citations

Abstract

Using radioligand binding techniques and human frontal cortex, we determined the equilibrium dissociation constants (KDS ) of 17 neuroleptics at the serotonin 5-HT1A and serotonin 5-HT2 receptors with [3H]WB4101 and [3H]ketanserin, respectively. At the serotonin 5-HT1A receptor, the most and least potent neuroleptics were chlorprothixene (KD = 230 nM) and fluphenazine (KD = 40 μM), respectively. At the serotonin 5-HT2 receptor, the most and least potent neuroleptics were spiperone (KD = 0.38 nM)and molindone, (KD = 5 μM), respectively.

Original languageEnglish (US)
Pages (from-to)279-282
Number of pages4
JournalEuropean Journal of Pharmacology
Volume143
Issue number2
DOIs
StatePublished - Nov 10 1987
Externally publishedYes

Keywords

  • (Human)
  • Brain
  • Neuroleptics
  • Serotonin receptors

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

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