| Literature DB >> 16509599 |
Veronique Maes1, Elisa Garcia-Garayoa, Peter Bläuenstein, Dirk Tourwé.
Abstract
Two new 99mTc-labeled neurotensin(8-13) analogues containing the retro-N(alpha)-carboxymethyl-histidine ((N(alpha)His)Ac) chelator were synthesized as potential radiopharmaceuticals for visualization of pancreatic carcinoma. To improve the pharmacokinetic properties, (N(alpha)His)Ac-Arg-NMeArg-Pro-Tyr-Tle-Leu (NT-XII), which is metabolically stabilized at two positions, was further modified. Shikimic acid (3,4,5-trihydroxy-1-cyclohexene-1-carboxylic acid) was introduced to obtain a more hydrophilic peptide (NT-XVIII), or Tyr11 was replaced by 2,6-dimethyltyrosine (Dmt) resulting in a triple-stabilized NT(8-13) analogue (NT-XIX). The latter has the best biodistribution profile.Entities:
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Year: 2006 PMID: 16509599 DOI: 10.1021/jm051172f
Source DB: PubMed Journal: J Med Chem ISSN: 0022-2623 Impact factor: 7.446