Document Detail


Novel 99mTc-labeled neurotensin analogues with optimized biodistribution properties.
MedLine Citation:
PMID:  16509599     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Veronique Maes; Elisa Garcia-Garayoa; Peter Bläuenstein; Dirk Tourwé
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Publication Detail:
Type:  In Vitro; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  49     ISSN:  0022-2623     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2006 Mar 
Date Detail:
Created Date:  2006-03-02     Completed Date:  2006-04-25     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  1833-6     Citation Subset:  IM    
Affiliation:
Department of Organic Chemistry, Vrije Universiteit Brussel, Pleinlaan 2, B-1050 Brussels, Belgium.
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MeSH Terms
Descriptor/Qualifier:
Animals
Chelating Agents / chemical synthesis*,  chemistry,  pharmacokinetics
Drug Stability
Humans
Mice
Mice, Nude
Neoplasm Transplantation
Neurotensin / chemical synthesis*,  chemistry,  pharmacokinetics
Oligopeptides / chemical synthesis*,  chemistry,  pharmacokinetics
Organotechnetium Compounds / chemical synthesis*,  chemistry,  pharmacokinetics
Peptide Fragments / chemical synthesis*,  chemistry,  pharmacokinetics
Plasma
Radiopharmaceuticals / chemical synthesis*,  chemistry,  pharmacokinetics
Shikimic Acid / chemistry
Structure-Activity Relationship
Tissue Distribution
Transplantation, Heterologous
Chemical
Reg. No./Substance:
0/(99mTc(CO)(3))-(NalphaHis)acetyl-arginyl-N-methylarginyl-prolyl-2',6'-dimethyltyrosyl-alpha-tert-butylglycyl-leucine; 0/Chelating Agents; 0/Oligopeptides; 0/Organotechnetium Compounds; 0/Peptide Fragments; 0/Radiopharmaceuticals; 138-59-0/Shikimic Acid; 39379-15-2/Neurotensin; 60482-95-3/neurotensin (8-13)

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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