Receptor mediated uptake of a radiolabeled contrast agent sensitive to beta-galactosidase activity.
Radiolabeling of the MRI contrast agent 1-[2-(beta-galactopyranosyloxy)propyl]-4,7,10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecane with (111)In, and its evaluation is reported. Radiolabeling was performed in acetate buffer with 50-78% radiochemical yield. In vitro studies revealed that the asialoglycoprotein receptor-poor cell line MH1C1 has low uptake, while the receptor-rich cell lines BNL-CL2 and Hep G2 have higher uptake. In vivo, the uptake of the compound in receptor-rich organ liver was very high. Blocking the receptor in vivo, reduced liver uptake by 90% suggesting that the compound localizes in receptor-enriched tissues by binding to the asialoglycoprotein receptor.
Department of Radiology, PET Imaging Science Center, University of Southern California, Los Angeles, CA, USA.
Mian M
MM
Alauddin
Angelique Y
AY
Louie
Antranik
A
Shahinian
Thomas J
TJ
Meade
Peter S
PS
Conti
D000818:Animals; D037263:Asialoglycoprotein Receptor / Q000378:metabolism*; D006801:Humans; D008113:Liver Neoplasms / Q000378:metabolism*; D008114:Liver Neoplasms, Experimental / Q000378:metabolism*; D051379:Mice; D008807:Mice, Inbred BALB C; D009942:Organometallic Compounds / Q000378:metabolism / Q000493:pharmacokinetics*; D051381:Rats; D014018:Tissue Distribution
D037263:Asialoglycoprotein Receptor; C407367:EgadMe; D009942:Organometallic Compounds