N-甲基-D-天冬氨酸受体显像剂研究进展

Advance in studies of the tracer of N-methyl-D-aspartate receptor

  • 摘要: N-甲基-D-天冬氨酸(NMDA)受体已成为发展帕金森病、阿尔茨海默病、精神分裂症、癫痫、亨廷顿舞蹈症等神经变性疾病药物的新靶点。NMDA受体显像剂的研制将为神经变性疾病的早期诊断和治疗提供灵敏的分子探针和特异的诊断方法。多数NMDA受体显像剂因脂溶性和亲和力欠佳而不宜用于临床,有希望成为NMDA受体显像剂的是123I-CNS1261。该文综述了近年来关于NMDA受体显像剂的研究进展。

     

    Abstract: N-methyl-D-aspartate receptors have recently been a novel target of drug development related to neurodegenerative diseases such as Parkinson diseases, Alzheimer disease, schizophrenia, epilepsy and Huntingtons disease. NMDA receptor imaging agents can provide a sensitive molecular prob and a powerful diagnostic tool for the early diagnosis and therapy of neurodegenerative diseases. Because of inadequate lipophilicity and affinity, many NMDA receptor imaging agents couldn't be used in clinical. 123I-N-(1-napthyl)-N'-(3-iodophenyl)-N-methylguanidine (123I-CNS1261)has the potential to be a NMDA receptor imaging agent. Basing on the researches which has accomplished in the abroad at present, this review concluded the progresses of the tracer of NMDA receptor.

     

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