Comparative in vivo lead mobilization of meso- and rac-2,3-dimercaptosuccinic acids in albino Wistar rats.
Comparison of the racemic and meso forms of 2,3-dimercaptosuccinic acid (DMSA) in lead mobilization from lead-loaded albino Wistar rats demonstrates that the racemic form is significantly more effective in reducing femur lead levels. After four oral doses at 0.5 mmol/kg, femur lead levels were reduced to 87% of control values by meso-DMSA and to 50% of control levels by rac-DMSA. Similarly, when the dose was increased to 1.0 mmol/kg, femur lead levels were reduced to 69% of control levels by meso-DMSA and to 45% of control levels by rac-DMSA. A similar pattern was found for renal lead levels. Brain lead concentrations were significantly lower in treated groups than in control groups, but no differences were found between rac- and meso-DMSA. Rac-DMSA is more soluble than meso-DMSA in acetonitrile, ethyl acetate, and ethyl ether. The partition coefficient of rac-DMSA in the n-octanol/water system was found to be about 2.8. These results indicate that rac-DMSA deserves further attention as a possible substitute for meso-DMSA.
Jones
M M
MM
Department of Chemistry, Vanderbilt University, Nashville, TN 37235, USA.
Singh
P K
PK
Kostial
K
K
Blanusa
M
M
Piasek
M
M
Restek-Samarozija
N
N
D000818:Animals; D001835:Body Weight / Q000187:drug effects; D001923:Brain Chemistry / Q000187:drug effects; D005260:Female; D005269:Femur / Q000737:chemistry; D007668:Kidney / Q000737:chemistry; D007854:Lead / Q000032:analysis / Q000378:metabolism*; D008099:Liver / Q000737:chemistry; D051381:Rats; D017208:Rats, Wistar; D013237:Stereoisomerism; D004113:Succimer / Q000494:pharmacology*
D007854:Lead; D004113:Succimer