Abstract
The effects of the catechol- O-methyltransferase (COMT) inhibitor 3′,4′-dihydroxy-2-methyl-propriophenone (U-0521) were studied in red blood cells (RBC) and corpus striatum in the rat. In vitro U-0521 inhibited RBC COMT activity in a dosedependent manner with an IC 50 of 6 × 10 −6M. In vivo maximum inhibition (90%) of enzyme activity in RBC was obtained with 250 mg/kg with a peak effect at 5 min and enzyme recovery within 90 min. In U-0521-pretreated rats l-3,4-dihydroxyphenylalanine ( l-DOPA) accumulation in RBC and corpus striatum, after injection of l-DOPA, was significantly higher than in nonpretreated rats. The use of COMT inhibitor along with l-DOPA may be of benefit in the treatment of Parkinson's disease.
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