Portal de Periódicos da CAPES

Preparation of [123I]- and [125I]epidepride: A dopamine D-2 receptor antagonist radioligand

1991; Wiley; Volume: 29; Issue: 7 Linguagem: Inglês

10.1002/jlcr.2580290703

1099-1344

J A Clanton, Tomas de Paulis, D. E. Schmidt, Mohammed Saleh Al Ansari, Ronald G. Manning, Ronald M. Baldwin, Robert Kessler,

Cardiac electrophysiology and arrhythmias

Abstract ( S )‐(−)‐ N ‐[(1‐ethyl‐2‐pyrrolidinyl)methyl]‐5‐[ 123 I]iodo‐2,3‐dimethoxybenzamide (TDP 517) (proposed generic name, [ 123 I]epidepride) is the iodine‐123 substituted analogue of isoremoxipride (FLB 457), both of which are very potent dopamine D‐2 antagonists (epidepride K D 0.024 nM). [ 123 I]Epidepride was radioiodinated in 60–70% radiochemical yields in 35 min from the corresponding 5‐(tributyltin) derivative using Na 123 I with a specific radioactivity of 3000 Ci/mmol, and oxidized in situ with chloramine‐T. The aryltin precursor was prepared from non‐labelled epidepride by palladium‐catalyzed stannylation using bis(tri‐ n ‐butyltin) in triethylamine. Alternatively, using no carrier‐added Na 125 I as the radioisotope, [ 125 I]epidepride at 2000 Ci/mmol specific radioactivity was prepared in 86% radiochemical yield and 99% radiochemical purity after purification by reverse phase HPLC in ethanolic phosphate buffer.