| Autor: |
del Rosario RB; Division of Nuclear Medicine, University of Michigan Medical Center, Ann Arbor 48109-0552, USA., Jung YW, Baidoo KE, Lever SZ, Wieland DM |
| Jazyk: |
angličtina |
| Zdroj: |
Nuclear medicine and biology [Nucl Med Biol] 1994 Feb; Vol. 21 (2), pp. 197-203. |
| DOI: |
10.1016/0969-8051(94)90009-4 |
| Abstrakt: |
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 IC50 = 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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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