Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: 2E-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-di-(ethyl-d5)-2-propenamide
Purity: ≥99% deuterated forms (d1-d10)
Formula Markup: C14H5D10N3O5
Formula Weight: 315.4
CAS Number: 1185241-19-3
Notes: Entacapone-d10 is intended for use as an internal standard for the quantification of entacapone (Item No. 14153) by GC- or LC-MS. Entacapone is a reversible catechol O-methyltransferase (COMT) inhibitor (IC50s = 10, 10, 20, and 160 nM for rat duodenum, brain, erythrocyte, and liver COMT, respectively).{42398} It is selective for COMT over monoamine oxidase A (MAO-A) and MAO-B and phenolsulphotransferase M (PST-M) and PST-P (IC50s = >50 µM). Entacapone (10 mg/kg), in combination with L-DOPA (Item No. 13248) and carbidopa (Item No. 23783), reduces 3-O-methyldopa (3-OMD) levels in the rat striatum and hypothalamus to 52 and 27%, respectively, of the levels in control animals receiving only L-DOPA and carbidopa.{22703} In a 6-OHDA rat model of Parkinson's disease, entacapone (10 mg/kg), in combination with L-DOPA and benserazide (Item No. 20298), increases contralateral turning behavior and striatal extracellular dopamine levels.{42399} Entacapone also inhibits contraction of colon longitudinal muscle explants from a 6-OHDA rat model of Parkinson's disease (EC50 = 200 µM).{42400} Formulations containing entacapone have been used in the treatment of Parkinson's disease.
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