Catalog No.S4021 Synonyms: Ro 40-7592
Molecular Weight(MW): 273.24
Tolcapone is a selective, potent and reversible of catechol-O-methyl transferase (COMT) inhibitor with Ki of 30 nM.
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|Description||Tolcapone is a selective, potent and reversible of catechol-O-methyl transferase (COMT) inhibitor with Ki of 30 nM.|
Tolcapone functions as a selective peripheral and central COMT inhibitor, exerting no effect on adrenergic, serotonergic, or cholinergic receptors or other enzymes involved in synthesis or catabolism of catecholamines.  Tolcapone produces a concentration-dependent decrease in COMT activity in liver homogenates of developing (3 days-old) and adult (60 days-old) rats with Vmax, Km and IC50 of 5.3 nM/mg/h, 3.3 μM, 41 nM, and 2.9 nM/mg/h, 13.1 μM, 720 nM, respectively. Tolcapone produces a concentration-dependent decrease in COMT activity in kidney of developing (3 days-old) and adult (60 days-old) rats with Vmax, Km and IC50 of 2.6 nM/mg/h, 2.7 μM, 8 nM, and 3.5 nM/mg/h, 24 μM, 177 nM, respectively. 
|In vivo||Tolcapone orally administrated is able to crosses the blood-brain barrier. Acute administration of Tolcapone increases basal levels of L-DOPA and dihydroxyphenylacetic acid (DOPAC) and decreases basal homovanillic acid (HVA) levels, but does not affect basal dopamine levels.  Tolcapone (30 mg/kg p.o.) combined with benserazide (15 mg/kg p.o.) and a low dose of L-dopa (10 mg/kg p.o.) almost completely blockes (for about 6 h) the formation of 3-O-methyldopa (3-OMD) in brain and plasma, producing a long-lasting increase of L-DOPA in plasma and a parallel marked increase of L-DOPA and dopamine in the brain.  Tolcapone displays behavioural and neurochemical benefits on animals. Tolcapone (30 mg/kg p.o.) increases the effect of L-DOPA (plus benserazide) on locomotor activity, reserpine-induced hypothermia, and catalepsy induced by pimozide, haloperidol and fluphenazine. Tolcapone also increases locomotor hyperactivity induced by amphetamine or nomifensine, as well as stereotypy induced by amphetamine (but not apomorphine). |
-  Zürcher G, et al. Adv Neurol, 1990, 53:497-50
-  Vieira-Coelho MA, et al. Br J Pharmacol, 1996, 117(3), 516-520.
-  Brannan T, et al. Neurology, 1992, 42(3 Pt 1), 683-685.
|In vitro||DMSO||55 mg/mL (201.28 mM)|
|Ethanol||55 mg/mL (201.28 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03591757||Completed||Drug: Tolcapone||Transthyretin Amyloidosis|Amyloidosis Leptomeningeal Transthyretin-Related||Boston University|Corino Therapeutics Inc.||October 30 2018||Early Phase 1|
|NCT02630043||Terminated||Drug: Tolcapone|Drug: Oxaliplatin||Neuroblastoma||Giselle Sholler|Spectrum Health Hospitals||December 2015||Phase 1|
|NCT02929485||Completed||Drug: Tolcapone|Drug: Placebo|Drug: Bromocriptine||Addiction||University of California Berkeley|University of California San Francisco||July 2013||Phase 4|
|NCT02080715||Completed||Drug: Tolcapone|Drug: Placebo||Healthy||University of Zurich||June 2013||Phase 1|
|NCT00604591||Completed||Drug: Tolcapone|Drug: Placebo||Frontotemporal Lobar Degeneration||Columbia University|National Institute of Neurological Disorders and Stroke (NINDS)||July 2011||Phase 2|
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