Technetium 99m-pyridoxylideneglutamate: a new hepatobiliary radiopharmaceutical. I. Experimental aspects.
The labeling of pyridoxal and the pyridoxylidene derivative of glutamic acid with 99mTc has been achieved by a simple autoclaving procedure. Technetium-99-m-pyridoxylideneglutamate (99mTc-PG) shows marked biliary excretion with accumulation of radioactivity in the gallbladder and intestines of experimental animals. This compound has been extensively investigated with a view to its application in the diagnosis of biliary disorders in man by scintigraphy. Both scintigraphic and quantitative distribution studies showed that 99mTc-PG passed rapidly through the mouse liver with progressive accumulation in the gallbladder, allowing visualization of this organ within 10 min of injection. In 30 min over 40% of the injected dose was excreted into the intestine with an equivalent amount appearing in the urine; however, renal activity remained low. Scintigraphic studies in dogs showed results similar to those obtained in mice. Studies of the toxicity in three animal species indicated a wide margin of safety for 99mTc-PG in the dose proposed for diagnostic purposes in humans.
D000818:Animals; D001646:Bile / Q000378:metabolism; D001659:Biliary Tract; D002415:Cats; D004285:Dogs; D005260:Female; D005704:Gallbladder / Q000378:metabolism; D005971:Glutamates / Q000378:metabolism / Q000633:toxicity; D006168:Guinea Pigs; D006863:Hydrogen-Ion Concentration; D007668:Kidney / Q000378:metabolism; D008099:Liver / Q000378:metabolism; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D011730:Pyridoxal / Q000031:analogs & derivatives* / Q000378:metabolism / Q000633:toxicity; D011877:Radionuclide Imaging; D051381:Rats; D013667:Technetium
D005971:Glutamates; C011096:pyridoxylideneglutamate; D011730:Pyridoxal; D013667:Technetium