Synthesis and characterization of 99Tcm-p-halophenethyl diaminodithiol analogs.

Abstract:

:In an effort to develop new, clinically useful 99Tcm-diaminodithiol (99Tcm-DADT) complexes for the evaluation of regional cerebral perfusion, basic diaminodithiols (DADT-TM, DADT-HM and DADT-MHM) and three diaminodithiol ligands functionalized with p-iodophenethyl (DADT-IPE), N-ethyl-p-fluorophenethyl amine (DADT-EFPE) or N-ethyl-p-iodophenethyl amine (DADT-EIPE), whose chemical structures are analogous to N-isopropyl-p-iodoamphetamine (IMP), were synthesized, labelled with 99Tcm and evaluated comparatively in experimental animals. In addition, the relationships between the chemical properties of the derivatives and their brain uptake and retention were investigated. The results were: (1) Isomeric configuration of 99Tcm-DADT complexes has an influence on uptake and retention in the rat brain. (2) In basic 99Tcm-DADT complexes, a correlation exists between initial brain uptake and lipophilicity, but in 99Tcm-DADT complexes containing a chemical structure similar to that of IMP, no correlation exists. (3) 99Tcm-DADT-IPE has relatively high uptake and long retention in the rat brain.

journal_name

Nucl Med Commun

authors

Shiba K,Mori H,Matsuda H,Hisada K

doi

10.1097/00006231-199112000-00007

subject

Has Abstract

pub_date

1991-12-01 00:00:00

pages

1057-65

issue

12

eissn

0143-3636

issn

1473-5628

journal_volume

12

pub_type

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