Abstract
The diaminodithiol (DADT) ligand has been conjugated to the neuromuscular blocking agent benzovesamicol (BVM) in the 5-position. DADT-BVM 1 was synthesized by coupling of 5-aminomethylbenzovesamicol with a BCA thiolactone reagent. 99mTc radiolabeling of 1 with [ 99mTc]glucoheptonate gave a 4.7:1 mixture of two 99mTc complexes as determined by HPLC. Biodistribution data of the major [ 99mTc]- 1 complex in CD-1 mice ( n = 4–5) showed very little uptake and no regional selectivity in the mouse brain. At all time points examined, the lung and liver showed the highest uptake. For whole brain, the % injected dose values were 0.27, 0.12, 0.04 and 0.01% at t = 1, 5, 30 and 240 min. The major [ 99mTc]- 1 product exhibited a log P = 3.13 ± 0.06 (SD) with an IC 50 = 140–280 nM for the corresponding [ 99Tc]- 1 vs ( − )- N-[ 3H]methyl-5-aminobenzovesamicol. The low brain uptake of [ 99mTc]- 1 vs 5-iodobenzovesamicol is attributed to its higher molecular weight (752) and lower binding affinity.
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