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| - Synthesis of Leukotriene B4 Antagonists Labeled with In-111 or Tc-99m toImage Infectious and Inflammatory Foci
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| - In previous studies we demonstrated that lipophilic 99mTc-labeled LTB4 antagonist 1 (RP517)accumulated in infectious foci in rabbits, but hepatobiliary clearance hampered imaging ofabdominal lesions. We now report the use of cysteic acid as a pharmacokinetic modifier toimprove the water solubility and renal clearance of three hydrophilic analogues of 1. DivalentLTB4 antagonist 17 (DPC11870-11) is a DTPA conjugate for radiolabeling with In-111.Monovalent LTB4 antagonists 15 (BMS57868-88) and divalent LTB4 antagonist 18 (BMS57868-81) are conjugated to bifunctional chelator HYNIC for radiolabeling with 99mTc. The threecompounds labeled efficiently with 111In or 99mTc with high radiochemical purity and specificactivities. Scintigraphic images obtained in New Zealand White rabbits having acuteintramuscular E. coli infection demonstrated that all agents were able to clearly visualize theabscess, and clearance was exclusively renal. The biodistribution of the 99mTc-labeled LTB4antagonists was affected by the coligands used with the HYNIC chelator and by the monovalentor divalent nature of the receptor binding moiety. The best scintigraphic images were obtainedwith monovalent HYNIC conjugate 15 using tricine and isonicotinic acid as coligands withHYNIC for coordination with 99mTc.
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