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Synthesis, DTPA coupling and radio labeling of cationic aminodextran

Conference · · J. Nucl. Med.; (United States)
OSTI ID:6932764

In glomerular diseases, the normal anionic charge of the basement membrane is lost at an early stage. Glomerular damage in rats has been detected more readily with cationic dextrans than with inulin. Hence, the authors attempted to demonstrate this phenomenon in vivo in rats with labeled cationic dextran. Aminated Dextran (AMDEX) was prepared by treating Dextran(mol. wt approx. = 15k) with sodium methoxide followed by a bromethylamine HBr in DMSO resulting in 10-25 aminogroups per mole. DTPA cyclic dianhydride was coupled to AMDEX using a weight ratio of 1:10 in 0.2 - 1.0 ml 0.42 M Hepes buffer at pH 7.4. Free DTPA was removed by gel filtration (Sephadex P6DG) or by using Centricon-10 (AMICON) centrifugal microconcentrators. AMDEX coupled with DTPA was labeled with Indium-111 in 0.25 M acetate buffer. Labeling yields were >90% by gel chromatography and electrophoresis (pH8.2 Barbitol buffer). AMEXDTPA was labeled also by ligand exchange with Tc-99m-Sn-citrate at neutral pH with a labeling yield of 30%. On electrophoresis, all the labeled samples retained their cationic character. The distribution of purified In-111 AMDEX, was compared with simultaneously IV injected Tc-99m DTPA in rats. The 2 hour urinary excretion, and renal clearance (calculated from the biexponential plasma clearance) were slower (70 to 80%) than those of DTPA, due to the larger molecular size of AMDEX. By 1 hr., 5% of the administered activity was retained in each kidney, probably due to adherence to anionic binding sites.

Research Organization:
Upstate Medical Center, Syracuse, NY
OSTI ID:
6932764
Report Number(s):
CONF-840619-
Journal Information:
J. Nucl. Med.; (United States), Journal Name: J. Nucl. Med.; (United States) Vol. 25:5; ISSN JNMEA
Country of Publication:
United States
Language:
English

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