| 99mTc-Labeling of a hydrazinonicotinamide-conjugated LTB(4) receptor antagonist useful for imaging infection and inflammation. | |
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MedLine Citation:
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PMID: 12121145 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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Shuang Liu; Anthony R Harris; Neal E Williams; D Scott Edwards |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Bioconjugate chemistry Volume: 13 ISSN: 1043-1802 ISO Abbreviation: Bioconjug. Chem. Publication Date: 2002 Jul-Aug |
Date Detail:
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Created Date: 2002-07-17 Completed Date: 2003-08-05 Revised Date: 2004-11-17 |
Medline Journal Info:
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Nlm Unique ID: 9010319 Medline TA: Bioconjug Chem Country: United States |
Other Details:
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Languages: eng Pagination: 881-6 Citation Subset: IM |
Affiliation:
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Bristol-Myers Squibb Medical Imaging, 331 Treble Cove Road, North Billerica, Massachusetts 01862, USA. shuang.liu@bms.com |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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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:
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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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