Abstract: Overexpression of somatostatin receptors (SSTR), especially SSTR2 is a common feature of neuroendocrine neoplasms (NEN) and an ideal target for NEN molecular imaging and radionuclide-targeted therapy. In the past, researchers have been working on radionuclide-labeled SSTR agonists, and have successfully used them for clinical imaging and treatment of NEN. Recent studies have shown that radionuclide-labeled SSTR antagonists have better pharmacokinetic characteristics, higher tumor uptake rates, longer retention time, and higher image contrast obtained than agonists. They are more superior in molecular imaging and radionuclide-targeted therapy of NEN. In this paper, the research progress of radionuclide-labeled SSTR antagonists in the imaging and treatment of NEN is reviewed, in order to provide reference for the clinical diagnosis and treatment of NEN.