Nitecapone Reference: 18656-10 An S-COMT inhibitor (IC50 = 300 nM in rat liver); is selective for S-COMT over tyrosine hydroxylase, dopamine-β-hydroxylase, DOPA decarboxylase, MAO-A, and MAO-B (IC50s = >1 µM for all); inhibits liver, duodenal, and brain S-COMT (ID50s = 5, 5, and 25 mg/kg, respectively); reduces 3-OMD formation and increases serum and brain L-DOPA, dopamine, and DOPAC levels when administered in combination with L-DOPA and carbidopa from 3-30 mg/kg; reduces mechanical and cold allodynia in a rat model of spinal nerve ligation-induced neuropathy at 30 mg/kg
Nitecapone Reference: 18656-25 An S-COMT inhibitor (IC50 = 300 nM in rat liver); is selective for S-COMT over tyrosine hydroxylase, dopamine-β-hydroxylase, DOPA decarboxylase, MAO-A, and MAO-B (IC50s = >1 µM for all); inhibits liver, duodenal, and brain S-COMT (ID50s = 5, 5, and 25 mg/kg, respectively); reduces 3-OMD formation and increases serum and brain L-DOPA, dopamine, and DOPAC levels when administered in combination with L-DOPA and carbidopa from 3-30 mg/kg; reduces mechanical and cold allodynia in a rat model of spinal nerve ligation-induced neuropathy at 30 mg/kg
Nitecapone Reference: 18656-5 An S-COMT inhibitor (IC50 = 300 nM in rat liver); is selective for S-COMT over tyrosine hydroxylase, dopamine-β-hydroxylase, DOPA decarboxylase, MAO-A, and MAO-B (IC50s = >1 µM for all); inhibits liver, duodenal, and brain S-COMT (ID50s = 5, 5, and 25 mg/kg, respectively); reduces 3-OMD formation and increases serum and brain L-DOPA, dopamine, and DOPAC levels when administered in combination with L-DOPA and carbidopa from 3-30 mg/kg; reduces mechanical and cold allodynia in a rat model of spinal nerve ligation-induced neuropathy at 30 mg/kg