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99mTc-(NαHis)Ac-(Arg-N-CH3)-Arg-Pro-(dimethyl-Tyr)-(tertary-Leu)-Leu.

Authors

Leung K.

Source

Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2013.
2009 Aug 05 [updated 2009 Sep 18].

Excerpt

Neurotensin (NT) is a tridecapeptide produced in the hypothalamus (1). It binds to NT receptors (NTRs) with high affinity and is implicated in the regulation of luteinizing hormone and prolactin release, and it has significant interaction with the dopaminergic system. There are three NTR subtypes, namely NTR1, NTR2, and NTR3. Most of the NT actions are mediated by NTR1, which is a G-protein–coupled receptor. The functions of NTR2 and NTR3 are not well known. The findings of NTR1 overexpression in various human tumors (2, 3), such as breast, lung, colon, pituitary, and pancreatic cancers, provide opportunities for tumor imaging by designing specific molecular imaging agents to target the NTR1. NT is rapidly metabolized in plasma by proteinases (4). Several NT analogs have been developed by modifications of the amino acid cleavage sites of NT(8-13) to increase plasma stability (5, 6). Maes et al. (6) has identified a modified peptide, (NαHis)Ac-(Arg-N-CH3)-Arg-Pro-(dimethyl-Tyr)-(tertary-Leu)-Leu (NT-XIX), to be metabolically stable in plasma with good affinity for NTR1. 99mTc-Labeled NT-XIX (99mTc-NT-XIX) has been evaluated as a single-photon emission computed tomography (SPECT) imaging agent of NTR1 in nude mice bearing human colon adenocarcinoma HT-29 cells (5).

PMID:
20641832
[PubMed]
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