Molfile
Inchi
Smiles
Synonyms:
-
entacapone
-
entacom
-
comtess
|
Entacapone is a selective and reversible inhibitor of COMT. COMT catalyzes the transfer of the methyl group of S-adenosyl-L-methionine to the phenolic group of substrates that contain a catechol structure. Physiological substrates of COMT include dopa, catecholamines (dopamine, norepinephrine, and epinephrine) and their hydroxylated metabolites. The function of COMT is the elimination of biologically active catechols and some other hydroxylated metabolites. When entacapone is given in conjunction with levodopa and an aromatic amino acid decarboxylase inhibitor, such as carbidopa, plasma levels of levodopa are greater and more sustained than after administration of levodopa and an aromatic amino acid decarboxylase inhibitor alone. It is believed that at a given frequency of levodopa administration, these more sustained plasma levels of levodopa result in more constant dopaminergic stimulation in the brain, leading to greater effects on the signs and symptoms of Parkinson's disease.
- Molecular weight: 305.29
- Formula: C14H15N3O5
- CLOGP: 2.66
- LIPINSKI: 0
- HAC: 8
- HDO: 2
- TPSA: 130.38
- ALOGS: -3.58
- ROTB: 5
- Status: OFP
Legend: OFP - off patent OFM - off market ONP - on patent
|