Description
A reversible COMT inhibitor (IC50s = 10, 10, 20, and 160 nM for rat duodenum, brain, erythrocyte, and liver COMT, respectively); selective for COMT over MAO-A, MAO-B, PST-M, and PST-P (IC50s = >50 µM); in combination with L-DOPA and carbidopa, reduces 3-OMD levels in the rat striatum and hypothalamus to 52 and 27%, respectively, of the levels in control animals receiving only L-DOPA and carbidopa; in combination with L-DOPA and benserazide, increases contralateral turning behavior and striatal extracellular dopamine levels in a 6-OHDA rat model of Parkinson's disease; inhibits contraction of colon longitudinal muscle explants from a 6-OHDA rat model of Parkinson's disease (EC50 = 200 µM)