[99mTc] Teboroxime and [99mTc]Cl(DMG)3B2MP: binding characteristics andmetabolism of two [99mTc]BATOs in blood and tissues.
Studies were performed in vitro and in vivo to evaluate the binding properties and metabolism of [99mTc]Cl(CDO)3BMe (Teboroxime) and [99mTc]Cl(DMG)3B2MP in blood and target tissues of rats. Both radiopharmaceuticals displayed rapid binding (within 1-3 min) with high affinity to plasma proteins and blood cells. The amounts of radioactivity associated with blood components became progressively greater with time of exposure to either compound. There was a higher proportion of the radiopharmaceuticals associated with blood components during in vivo conditions, likely due, at least in part, to clearance of the free fraction from the plasma pool. Exposure of both compounds to blood results in axial ligand exchange of the chloro atom to a hydroxyl. The results suggest that it is the free species that is extracted primarily by tissues.
Bristol-Myers Squibb Pharmaceutical Research Institute, New Brunswick, NJ 08903.
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Rosenspire
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Rumsey
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Jurisson
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Hirth
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Narra
D000818:Animals; D001798:Blood Proteins / Q000378:metabolism; D001897:Boronic Acids / Q000097:blood / Q000378:metabolism* / Q000493:pharmacokinetics; D002851:Chromatography, High Pressure Liquid; D004912:Erythrocytes / Q000378:metabolism; D008297:Male; D015609:Organotechnetium Compounds / Q000097:blood / Q000378:metabolism* / Q000493:pharmacokinetics; D010091:Oximes / Q000097:blood / Q000378:metabolism* / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D014018:Tissue Distribution
D001798:Blood Proteins; D001897:Boronic Acids; D015609:Organotechnetium Compounds; D010091:Oximes; C060156:technetium Tc 99m teboroxime