99mTc-Labeling of a hydrazinonicotinamide-conjugated LTB(4) receptor antagonist useful for imaging infection and inflammation.
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.
Bristol-Myers Squibb Medical Imaging, 331 Treble Cove Road, North Billerica, Massachusetts 01862, USA. shuang.liu@bms.com
Shuang
S
Liu
Anthony R
AR
Harris
Neal E
NE
Williams
D Scott
DS
Edwards
D002851:Chromatography, High Pressure Liquid; D003432:Cross-Linking Reagents / Q000737:chemistry; D004355:Drug Stability; D006801:Humans; D006834:Hydrazines / Q000737:chemistry*; D007239:Infections / Q000000981:diagnostic imaging; D007249:Inflammation / Q000000981:diagnostic imaging; D008024:Ligands; D009536:Niacinamide / Q000031:analogs & derivatives* / Q000737:chemistry*; D015609:Organotechnetium Compounds / Q000138:chemical synthesis* / Q000592:standards; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*; D018102:Receptors, Leukotriene B4 / Q000037:antagonists & inhibitors*; D013667:Technetium
D003432:Cross-Linking Reagents; D006834:Hydrazines; D008024:Ligands; D015609:Organotechnetium Compounds; C425527:RP517; D019275:Radiopharmaceuticals; D018102:Receptors, Leukotriene B4; C117288:hydrazino nicotinamide; D009536:Niacinamide; D013667:Technetium