The 5-HT1A is a serotonin receptor subtype implicated in a number of neurological and psychiatric disorders, including major depressive disorder, schizophrenia and bulimia. Additionally, 5-HT1A is implicated in the action of antidepressants. Thus, a noninvasive imaging tracer for the 5-HT1A receptor would have significant utility in monitoring and understanding disease processes and evaluation of therapeutic effect. This technology is a {11C} labeled HT1A agonist PET tracer which permits the visualization and quantification of the 5-HT1A receptors in the high affinity state.
Current technologies for PET imaging of brain 5-HT1A receptors bind both high and low affinity sites with equal affinity. This technology would bind only high affinity sites, which are involved in signaling in the brain.
PET imaging measures the emission from radiopharmaceuticals such as those containing a 11C isotope. This technology provides a method for the incorporation of isotopic 11C into a 5-HT1A receptor agonist, allowing it to be monitored by PET. Current methods to study the 5-HT1A receptor rely on antagonists, which bind to both high affinity and low affinity sites with similar affinities. This technology, however, binds to only the high affinity sites of the 5-HT1A receptor. This is important as only the high affinity states are involved in the brain signaling, whereas the low affinity states provide an indirect measurement of 5-HT1A signal transduction. An appropriate radiolabeled 5-HT1A agonist would permit evaluation of functional 5-HT1A receptors involved in the signal transduction mechanism. As a potential 5-HT1A receptor agonist, this technology would provide the direct observation of functional 5-HT1A receptors, which would have significant utility in studying the pathophysiology of psychiatric and neurological disorders and the action of antidepressants on 5-HT1A receptors.
Patent Issued (US 20080138283)