Entacapone - CAS 130929-57-6
Catalog number:
130929-57-6
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C14H15N3O5
Molecular Weight:
305.29
COA:
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Targets:
COMT
Description:
Entacapone inhibits catechol-O-methyltransferase(COMT) with IC50 of 151 nM.
Publictions citing BOC Sciences Products
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Purity:
>98%
Synonyms:
OR-611
MSDS:
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1. Four-level levodopa adsorption on C60 fullerene for transdermal and oral administration: a computational study
Nilton F. Frazao, Eudenilson L. Albuquerque. Ewerton W. S. Caetano*. RSC Adv., 2012, 2, 8306–8322
In the current PD standard treatment, levodopa is administered combined with DOPA decarboxylase (such as cardidopa or benserazide) and catechol-O-methyltransferase (COMT) (such as entacapone and tolcapone) inhibitors. DOPA decarboxylase inhibitors prevent the breakdown of levodopa in the blood-stream, and also delay the conversion of levodopa into dopamine until it reaches the brain, reducing adverse side effects. The peripheral levodopa conversion to dopamine by the enzyme DOPA decarboxylase is responsible for the typical gastrointestinal (nausea, emesis) and cardiovascular (arrhythmia, hypotension) side effects. On the other hand, the inhibition of COMT leads to both an increase in the amount of levodopa in the central nervous system (CNS) and reduced formation of the peripheral metabolite 3-O-methyldopa, which is a competitive inhibitor of the active transport of levodopa through the intestinal mucosa and across the BBB. In multiple clinical trials, the addition of the COMT inhibitors entacapone and tolcapone to levodopa in fluctuating patients has been shown to improve clinical outcomes. As a matter of fact, a recent double-blind clinical trial in early PD patients found that carbidopa-25–levodopa-100–entacapone-200 improved PD signs and symptoms significantly more than carbidopa-25–levodopa-100 without an increase in the development of motor complications.
2. Derection of the polymorphic form of entacapone using an electrochemical tuneable surface template
Ana Kwokal and Kevin J. Roberts*. CrystEngComm,2014, 16, 3487–3493
The electrochemical behaviour of gold in mixed aqueous/acetone solutions, as studied using cyclic voltammetry, both with and without the presence of entacapone in the solution, has been previously described. In this study two different potentials were chosen to test the influence of template polarisation on crystallisation behaviour; the open circuit potential (at about 200 mV) in which entacapone spontaneously adsorbs and the negative potential of −150 mV where the surface is free from gold oxide and hydrogen evolution is not evident. The latter conditions are consistent with an electric field strength of ca. 8Vm-1.
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