Biological Information

Background Information:

Phenylethanolamine N-methyltransferase (PNMT) is the enzyme that catalyzes the S-adenosyl-methionine (AdoMet)-dependent methylation of norepinephrine to epinephrine in the adrenal medulla but occurs in other tissues throughout the body i.e. brain, eye, spinal cord, lung, kidney, heart, liver, spleen and pancreas. PNMT plays role in trace amine and catecholamine biosynthesis concerned with the regulation of automatic function, heart rate, blood pressure, blood glucose. PNMT may be regulated neutrally via the stimulation of the splanchnic nerve and hormonally via the hypothalamic-pituitary-adrenal axis and positively influenced by glucocorticoids. PNMT inhibitor might be useful in the treatment of hypertension, metabolic and hormonal responses.

Family:

Neurotransmitter Metabolism

Sub Family:

Catecholamine Turnover

Protein Name:

Phenylethanolamine N-Methyltransferase

Uniprot Number:

P11086

Gene Name:

PNMT

Gene ID:

5409

Accession Number:

NM_002686

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

MS

Measured Response:

Peak Area Response

Testing Information

Substrate:

DL-Normetanephrine (35 µM)

Tracer:

SAM (6 µM)

Incubation:

45 min at 22°C

Control Inhibitor:

SAH-d4

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.

Test Sample Requirements:

Minimum for 1) Screen: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM final testing. 2) Dose Response: 90 μl of 10 mM stock -OR- 1 mg (pre-weighed) for a top concentration at 10 µM.

Minimum Order Quantity:

2

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

5816

Name

Epinephrine

Measurement

53µM - IC50

PubChem ID

123920

Name

7,8-dichloro-1,2,3,4-tetrahydroisoquinoline

Measurement

122nM - IC50

PubChem ID

101252761

Name

DCMB

Measurement

215nM - IC50

PubChem ID

Name

SAH-d4

Measurement

11µM - IC50

Clinical Relevance

Therapeutic Area:

Cardiovascular

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault