Tolcapone

Catalog No.S4021 Synonyms: Ro 40-7592

For research use only.

Tolcapone (Ro 40-7592) is a selective, potent and reversible of catechol-O-methyl transferase (COMT) inhibitor with Ki of 30 nM.

Tolcapone Chemical Structure

CAS No. 134308-13-7

Selleck's Tolcapone has been cited by 1 Publication

Purity & Quality Control

Choose Selective COMT Inhibitors

Biological Activity

Description Tolcapone (Ro 40-7592) is a selective, potent and reversible of catechol-O-methyl transferase (COMT) inhibitor with Ki of 30 nM.
Targets
COMT [4]
()
30 nM(Ki)
In vitro

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. [1] 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. [2]

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. [3] 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. [4] 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). [5]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 55 mg/mL
(201.28 mM)
Water Insoluble
Ethanol '55 mg/mL

Chemical Information

Molecular Weight 273.24
Formula

 

C14H11NO5
CAS No. 134308-13-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC=C(C=C1)C(=O)C2=CC(=C(C(=C2)O)O)[N+](=O)[O-]

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Molarity Calculator

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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 SaulnierSholler|Atrium Health December 2015 Phase 1
NCT02929485 Withdrawn 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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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