Phenylethanolamine N-Methyltransferase Human Enzymatic LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
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:
Fragment (1-282), Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometry
Measured Response:
Scintillation
Testing Information
Procedure Summary:
Human recombinant PNMT expressed in E. coli is used. Test compound and/or vehicle is preincubated with 0.5 μg/ml enzyme‡ in Tris-HCl buffer pH 8.5 for 30 minutes at 37⁰C. The reaction is initiated by addition of 100 μM normetarephrine for another 30 minutes incubation. Determination of the amount of complex formed is read on a liquid scintillation counter. Compounds are screened at 10 µM.
Substrate:
100 µM Normetarephrine
Incubation:
30 min at 37°C
Control Inhibitor:
LY 78335
Criteria For Significance:
≥ 50% of max stimulation or inhibition
Test Concentration / Dose:
Suggested concentration for initial testing is 10 uM
Test Sample Requirements:
Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).
Minimum Order Quantity:
2
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Cardiovascular
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
RELATED SOLUTIONS
HNMT Histamine N-Methyltransferase Human SMMT Enzymatic LeadHunter Assay - TW
Item: 125010
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