[3H]WAY–100635 for 5–HT1A receptor autoradiography in human brain: a comparison with [3H]8–OH–DPAT and demonstration of increased binding in the frontal cortex in schizophrenia

  title={[3H]WAY–100635 for 5–HT1A receptor autoradiography in human brain: a comparison with [3H]8–OH–DPAT and demonstration of increased binding in the frontal cortex in schizophrenia},
  author={Philip W J Burnet and Sharon L. Eastwood and Paul J. Harrison},
  journal={Neurochemistry International},

Brain serotonin 5-HT(1A) receptor binding in schizophrenia measured by positron emission tomography and [11C]WAY-100635.

The biological significance of elevated 5-HT(1A) receptor density in schizophrenia remains unclear and needs to be viewed in light of preclinical evidence supporting a role for 5-hydroxytryptamine-1A receptors in mediating antipsychotic action and extrapyramidal adverse effects of drugs.

A Database of [11C]WAY-100635 Binding to 5-HT1A Receptors in Normal Male Volunteers: Normative Data and Relationship to Methodological, Demographic, Physiological, and Behavioral Variables

The binding of [(11)C]WAY-100635 was insensitive to changes in brain 5-HT induced by tryptophan infusion and depletion and there were no significant correlations of regional and global BP with common radiochemical, demographic, physiological, and personality variables.

Parametric and Regional Maps of Free Serotonin 5HT1A Receptor Sites in Human Brain as Function of Age in Healthy Humans

The results demonstrate that the number of available 5HT1A-binding sites declines with age, and the correlation between pB and age applied to regions-of-interest revealed significant decline of pB at the rate of 3 or 4% per decade.

Measurement of serotonin 5-HT1A receptor binding using positron emission tomography and [carbonyl-11C]WAY-100635—considerations on the validity of cerebellum as a reference region

Exceptionally high uptake of [carbonyl-11C]WAY-100635 in the gray matter of cerebellum in one healthy male subject, which was reproducible in repeated PET scanning and most likely represents specific binding to 5-HT1A receptors in cerebellar gray matter.

Measurement of 5-HT1A Receptor Density and in-vivo Binding Parameters of [18F]mefway in the Nonhuman Primate

  • D. WootenA. Hillmer B. Christian
  • Biology, Medicine
    Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism
  • 2012
Results show that M-I [18F]mefway PET experiments can be used for the in-vivo measurement of 5-HT1A receptor density, and specific binding parameters koff and kon for estimation of apparent KD.

Serotonin 5-HT1A Receptor Binding Potential Declines with Age as Measured by [11C]WAY-100635 and PET

Synthesis and initial evaluation of [11C](R)-RWAY in monkey—a new, simply labeled antagonist radioligand for imaging brain 5-HT1A receptors with PET

R-[11C]RWAY is simply prepared and an effective antagonist for imaging brain 5-HT1A receptors and resists hydrolysis in vivo, gives less lipophilic radiometabolites, and warrants further PET studies in human subjects.