Tolcapone

Catalog No.S4021 Synonyms: Ro 40-7592

Tolcapone Chemical Structure

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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In DMSO USD 90 In stock
USD 60 In stock
USD 170 In stock
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Biological Activity

Description Tolcapone 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

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 273.24
Formula

 

C14H11NO5
CAS No. 134308-13-7
Storage powder
in solvent
Synonyms Ro 40-7592

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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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Transferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID