Imaging of sigma1 receptors in the human brain using PET and [11C]SA4503.

Abstract

Sigma(1) receptors were imaged in living human brain by positron emission tomography (PET) using [(11)C] SA4503. A dynamic 90-min scan and kinetic analysis enabled quantification of receptor density in the brain. The sigma(1) receptors were distributed throughout the brain in normal subjects, but decreased in the frontal, temporal, and occipital lobes, cerebellum and thalamus in patients with early Alzheimer's disease and in the putamen in patients with Parkinson's disease. In addition, rates of receptor occupancy by the neuroleptic haloperidol and the selective serotonin reuptake inhibitor fluvoxamine were evaluated by [(11)C]SA4503-PET and found to be high. [(11)C]SA4503-PET is useful for studying the pathophysiology of neurological and psychiatric disorders such as schizophrenia and for evaluation of the pharmacodynamics of psychiatric drugs.

• Authors: Jun Toyohara, Muneyuki Sakata, Kiichi Ishiwata
• Journal: Central nervous system agents in medicinal chemistry (Cent Nerv Syst Agents Med Chem) Vol. 9 Issue 3 Pg. 190-6 (Sep 2009) ISSN: 1875-6166 [Electronic] United Arab Emirates
• PMID: 20021353 (Publication Type: Journal Article, Review)

Chemical References

• Piperazines
• Psychotropic Drugs
• Radiopharmaceuticals
• Receptors, sigma
• sigma-1 receptor
• SA 4503

Topics

• Animals
• Brain (diagnostic imaging)
• Brain Chemistry (physiology)
• Central Nervous System Diseases (diagnostic imaging)
• Humans
• Piperazines (metabolism, pharmacokinetics)
• Positron-Emission Tomography (methods)
• Psychopharmacology (methods)
• Psychotropic Drugs (pharmacokinetics)
• Radiopharmaceuticals (metabolism, pharmacokinetics)
• Receptors, sigma (metabolism)
• Whole-Body Counting