Document Detail


99mTc-Labeling of a hydrazinonicotinamide-conjugated LTB(4) receptor antagonist useful for imaging infection and inflammation.
MedLine Citation:
PMID:  12121145     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
This report describes the (99m)Tc labeling of a hydrazinonicotinamide (HYNIC)-conjugated LTB(4) receptor antagonist (SG380). The ternary ligand technetium complex [(99m)Tc(SG38)(tricine)(TPPTS)] (RP517) was prepared using a non-SnCl(2)-containing formulation ((2001) J. Pharm. Sci. 90, 114-123). Unlike other HYNIC-conjugated small biomolecules, SG380 is lipophilic and has low solubility in the kit matrix. Using a combination of a solubilizing agent (Lysolecithin) and a cosolvent (ethanol), we have developed a new formulation for routine preparation of RP517. Using this formulation, RP517 can be prepared in high radiochemical purity (RCP > 90%) and remains stable in the kit matrix for at least 6 h. We also prepared the corresponding (99)Tc analogue, [(99)Tc]RP517. An HPLC concordance experiment using RP517 and [(99)Tc]RP517 showed that the same technetium complex was prepared at both the tracer and macroscopic levels. The LC-MS data are completely consistent with the 1:1:1:1 composition for Tc:SG380:tricine:TPPTS.
Authors:
Shuang Liu; Anthony R Harris; Neal E Williams; D Scott Edwards
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Bioconjugate chemistry     Volume:  13     ISSN:  1043-1802     ISO Abbreviation:  Bioconjug. Chem.     Publication Date:    2002 Jul-Aug
Date Detail:
Created Date:  2002-07-17     Completed Date:  2003-08-05     Revised Date:  2004-11-17    
Medline Journal Info:
Nlm Unique ID:  9010319     Medline TA:  Bioconjug Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  881-6     Citation Subset:  IM    
Affiliation:
Bristol-Myers Squibb Medical Imaging, 331 Treble Cove Road, North Billerica, Massachusetts 01862, USA. shuang.liu@bms.com
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MeSH Terms
Descriptor/Qualifier:
Chromatography, High Pressure Liquid
Cross-Linking Reagents / chemistry
Drug Stability
Humans
Hydrazines / chemistry*
Infection / radionuclide imaging
Inflammation / radionuclide imaging
Ligands
Niacinamide / analogs & derivatives*,  chemistry*
Organotechnetium Compounds / chemical synthesis*,  standards
Radiopharmaceuticals / chemical synthesis*,  diagnostic use
Receptors, Leukotriene B4 / antagonists & inhibitors*
Technetium / diagnostic use
Chemical
Reg. No./Substance:
0/Cross-Linking Reagents; 0/Hydrazines; 0/Ligands; 0/Organotechnetium Compounds; 0/RP517; 0/Radiopharmaceuticals; 0/Receptors, Leukotriene B4; 0/hydrazino nicotinamide; 7440-26-8/Technetium; 98-92-0/Niacinamide

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


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