生长抑素类似物及其标记核素

Recent development of radio-labeled somatostatin analogues as receptor image agent

  • 摘要: 利用标记小肽进行功能显像有望开创核素显像与肿瘤生物学研究的新纪元。为了提高肿瘤生长抑素受体显像的特异性和敏感性,从受体亚型水平开发受体显像剂,以及研究适合临床应用的简捷标记方法是今后的重要课题。综述了新的核素标记的生长抑素多肽受体配体的研究及其药代动力学性质并评价了其用于肿瘤受体显像的可行性。

     

    Abstract: The development of radiolabeled peptide-based radiopharmaceuticals for imaging a variety of tumors has seen a new era in nuclear medicine.Recently, a number of radio-labeled somatostatin analogues have proven to be useful diagnostic imaging agents.The challenge is to synthesize a wide range of biologically active somatostatin analogue peptides without affecting their receptor binding properties, and label bioactive peptides with radionuclides with high specific activity without impairing the biological properties of the peptides.This review presents recent developments in radio-labeled somatostatin analogues and their pharmacokinetic properties, their potential as diagnostic imaging agents are also addressed.

     

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