Phenylethanolamine N-methyltransferase inhibition: re-evaluation of kinetic data.

Article Details

Citation

Wu Q, Criscione KR, Grunewald GL, McLeish MJ

Phenylethanolamine N-methyltransferase inhibition: re-evaluation of kinetic data.

Bioorg Med Chem Lett. 2004 Aug 16;14(16):4217-20.

PubMed ID
15261273 [ View in PubMed
]
Abstract

Inhibitors of phenylethanolamine N-methyltransferase [PNMT, the enzyme that catalyzes the final step in the biosynthesis of epinephrine (Epi)] may be of use in determining the role of Epi in the central nervous system. Here we demonstrate that a routinely used assay for screening PNMT inhibitors is not appropriate for those inhibitors having K(i) values less than 1 microM. A revised assay has been developed that shows some inhibitors bind two orders of magnitude more tightly than previously reported.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
1,2,3,4-Tetrahydro-Isoquinoline-7-Sulfonic Acid AmidePhenylethanolamine N-methyltransferaseKi (nM)280N/AN/ADetails
7,8-Dichloro-1,2,3,4-tetrahydroisoquinolinePhenylethanolamine N-methyltransferaseKi (nM)3.1N/AN/ADetails
8,9-Dichloro-2,3,4,5-Tetrahydro-1h-Benzo[C]AzepinePhenylethanolamine N-methyltransferaseKi (nM)10N/AN/ADetails