Abstract
This study sought to determine whether cannabinoid-1 (CB(1)) receptor binding was altered in the postmortem dorsolateral prefrontal cortex (DLPFC) of individuals with schizophrenia (schizophrenia; n=47) compared to controls (n=43). The CB(1) receptor inverse agonist radioligand [(3)H]MePPEP was used to measure specific binding to CB(1) receptors. The specific binding of [(3)H]MePPEP to CB(1) receptors was 20% higher in patients with schizophrenia than in controls. Power analyses suggested that 53 subjects per group would be needed to detect a similar difference in vivo with positron emission tomography (PET) and the structurally related inverse agonist radioligand [(18)F]FMPEP-d(2) (80% statistical power, p<0.05).
Published by Elsevier B.V.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, N.I.H., Intramural
MeSH terms
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Adult
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Aged
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Cohort Studies
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Female
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Fluorine Radioisotopes / pharmacokinetics
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Humans
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Male
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Middle Aged
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Polymorphism, Single Nucleotide / genetics
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Positron-Emission Tomography
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Prefrontal Cortex / diagnostic imaging*
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Prefrontal Cortex / drug effects
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Protein Binding / drug effects
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Pyrrolidinones / pharmacokinetics
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Receptor, Cannabinoid, CB1 / genetics
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Receptor, Cannabinoid, CB1 / metabolism*
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Regression Analysis
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Schizophrenia / diagnostic imaging*
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Schizophrenia / genetics
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Schizophrenia / pathology*
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Tissue Distribution / drug effects
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Tritium / pharmacokinetics
Substances
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5-((3-fluoromethoxy)phenyl)-3-(1-phenylethylamino)-1-(4-trifluoromethylphenyl)pyrrolidin-2-one
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5-(3-methoxyphenyl)-3-(1-phenylethylamino)-1-(4-trifluoromethylphenyl)pyrrolidin-2-one
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CNR1 protein, human
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Fluorine Radioisotopes
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Pyrrolidinones
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Receptor, Cannabinoid, CB1
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Tritium