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New Trends and Current Status of Positron-Emission Tomography and Single-Photon-Emission Computerized Tomography Radioligands for Neuronal Serotonin Receptors and Serotonin Transporter
Bioconjugate Chemistry ( IF 4.7 ) Pub Date : 2017-10-13 00:00:00 , DOI: 10.1021/acs.bioconjchem.7b00243
Puja Panwar Hazari 1 , Ankita Pandey 1 , Shubhra Chaturvedi 1 , Anil Kumar Mishra 1
Affiliation  

The critical role of serotonin (5-hydroxytryptamine; 5-HT) and its receptors (5-HTRs) in the pathophysiology of diverse neuropsychiatric and neurodegenerative disorders render them attractive diagnostic and therapeutic targets for brain disorders. Therefore, the in vivo assessment of binding of 5-HT receptor ligands under a multitude of physiologic and pathologic scenarios may support more-accurate identification of disease and its progression and the patient’s response to therapy as well as the screening of novel therapeutic strategies. The present Review aims to focus on the current status of radioligands used for positron-emission tomography (PET) and single-photon-emission computerized tomography (SPECT) imaging of human brain serotonin receptors. We further elaborate upon and emphasize the attributes that qualify a radioligand for theranostics on the basis of its frequency of use in clinics, its benefit to risk assessment in humans, and its continuous evolution, along with the major limitations.

中文翻译:

神经元5-羟色胺受体和5-羟色胺转运体的正电子发射断层扫描和单光子发射计算机断层摄影放射配体的新趋势和现状

血清素(5-羟色胺; 5-HT)及其受体(5-HTRs)在多种神经精神疾病和神经退行性疾病的病理生理中的关键作用使它们成为脑部疾病的有吸引力的诊断和治疗靶标。因此,在多种生理和病理情况下的体内5-HT受体配体结合的体内评估可支持更准确地识别疾病及其进展,患者对治疗的反应以及筛选新的治疗策略。本综述的重点是用于人类脑5-羟色胺受体的正电子发射断层扫描(PET)和单光子发射计算机断层扫描(SPECT)成像的放射性配体的当前状态。
更新日期:2017-10-13
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