THE SYNTHESIS, RADIOIODINATION AND PRELIMINARY BIOLOGICAL STUDY OF THE NEW CARBOXYLIC DERIVATIVES OF DITHIZONE

Synthesis, characteristics and radioiodination of the new carboxylic d erivatives of dithizone are described in this paper. We have applied t he carboxy dithizones for preparation of radioactive compounds by coup ling with [I-131]-histamine. Preliminary biological studies of the new radiodithizone were done in rats after two different application rout s: peripheral i.v. injection and direct injection to splenic artery. B iodistribution of the carboxy dithizone-[I-131]-histamine conjugate (i .v. injection) was quite different than that for free [I-131]-histamin e. However, uptake of activity in pancreas was low (0.81% g(-1) of tis sue). Direct application of the conjugate to splenic artery resulted i n high activity retention in pancreas after 30 and 45 min post injecti on (respectively 8.8 and 12.4% g(-1) of tissue) indicating potential u sefulness of the new radiodithizone for in vivo monitoring of pancreas . (C) 1998 Elsevier Science Ltd. All rights reserved.