Kumar J S Dileep, Mann J John
Department of Psychiatry, Columbia University College of Physicians and Surgeons & New York State Psychiatric Institute, New York, NY 10032, United States.
Drug Discov Today. 2007 Sep;12(17-18):748-56. doi: 10.1016/j.drudis.2007.07.008. Epub 2007 Aug 27.
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.
血清素5-HT(1A)受体与包括抑郁症、自杀行为、恐慌症、癫痫、贪食症、精神分裂症、帕金森病和阿尔茨海默病在内的主要神经精神疾病的病理生理学有关，因此是药物治疗的重要靶点。5-HT(1A)受体在中缝核的血清素神经元中作为躯体树突自身受体（突触前）表达，并在大脑皮质和皮质下血清素终末场作为突触后受体表达。由于该受体浓度较高且分布不均一，它是使用正电子发射断层扫描（PET）和单光子发射断层扫描（SPECT）在体内进行定量的一个有吸引力的靶点。在此，我们综述了用于活体脑成像5-HT(1A)受体的PET放射性配体。
