PET tracers for 5-HT(1A) receptors and uses thereof.
The serotonin 5-HT(1A) receptor is implicated in the pathophysiology of major neuropsychiatric disorders, including depression, suicidal behavior, panic disorder, epilepsy, bulimia, schizophrenia, Parkinson's disease, and Alzheimer's disease and is, therefore, an important target for drug therapy. 5-HT(1A) receptors are expressed as somatodendritic autoreceptors in serotonin neurons of the raphé nuclei (presynaptic) and as postsynaptic receptors in cortical and subcortical serotonin terminal fields in the brain. Due to the higher concentration and heterogeneous distribution of this receptor, it is an attractive target for quantification in vivo using positron emission tomography (PET) and single photon emission tomography (SPECT). Here, we review the PET radioligands employed for imaging 5-HT(1A) receptors in living brain.
Kumar
J S Dileep
JS
Department of Psychiatry, Columbia University College of Physicians and Surgeons & New York State Psychiatric Institute, New York, NY 10032, United States. dk2038@columbia.edu
Mann
J John
JJ
D017660:Autoreceptors / Q000037:antagonists & inhibitors / Q000378:metabolism; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism; D002250:Carbon Radioisotopes; D005462:Fluorine Radioisotopes; D006801:Humans; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics / Q000494:pharmacology; D044282:Receptor, Serotonin, 5-HT1A / Q000378:metabolism*; D058825:Serotonin 5-HT1 Receptor Agonists; D058829:Serotonin 5-HT1 Receptor Antagonists; D015899:Tomography, Emission-Computed, Single-Photon