Time course of 5-HT(2A) receptor occupancy in the human brain after a single oral dose of the putative antipsychotic drug MDL 100,907 measured by positron emission tomography

Gerhard Gründer, Fuji Yokoi, Steve J. Offord, Hayden T. Ravert, Robert F. Dannals, Joanne K. Salzmann, Sally Szymanski, P. David Wilson, Daniel R. Howard, Dean F. Wong

Research output: Contribution to journalArticlepeer-review

Abstract

MDL 100,907 is a potent and selective antagonist of 5-HT(2A) serotonin receptors. Animal studies suggest that MDL 100,907 may behave as an atypical antipsychotic drug. Positron emission tomography (PET) using [11C]NMSP as the radiotracer was used to define the time course of 5-HT2 receptor occupancy in the human frontal cerebral cortex after a single oral dose of MDL 100,907 (10 or 20 mg) in nine healthy subjects. After the baseline scan each subject was studied three times post dosing at various time points. 5-HT2 occupancies were in the range of 70 and 90% after each dose. While the occupancy remains in this range over 24 hours after 20 mg MDL 100,907, it decreases by about 20% at 24 hours compared to the timepoint at 8 hours, when only 10 mg are administered (p < 0.05). Our results should allow determination of the appropriate dosing regimen for future trials in schizophrenic patients.

Original languageEnglish (US)
Pages (from-to)175-185
Number of pages11
JournalNeuropsychopharmacology
Volume17
Issue number3
DOIs
StatePublished - Sep 1997

Keywords

  • 5-HT receptors
  • Antipsychotic drugs
  • Human
  • MDL 100,907
  • Positron emission tomography

ASJC Scopus subject areas

  • Pharmacology
  • Psychiatry and Mental health

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