Biological Information
Background Information:
Tyrosine hydroxylase (tyrosine-3-monooxygenase, tyrosine oxidase, E.E.1.14.13.41) which catalyzes the hydroxylation of tyrosine is generally regarded as a rate-limiting step in the biosynthesis of catecholamines. The enzyme is activated following stimulation of adrenergic nerves or the adrenal medulla. Tyrosine hydroxylase is a substrate for cyclic AMP-dependent kinase, and kinase-catalyzed phosphorylation is associated with increased hydroxylase activity. The enzyme is also a substrate for Ca2+-activated protein kinases. In addition, tyrosine hydroxylase is inhibited by catechol compounds in a manner that is competitive with its pterin cofactor, tetrahydrobiopterin. It is thus subject to end-producr feedback inhibition. A potent and selective inhibitor of this enzyme may prove useful as a therapeutic agent in the treatment of hypertension as well as schizophrenia and tardive dyskinesia.
Family:
Neurotransmitter Metabolism
Sub Family:
Amino Acid Hydroxylase
Protein Name:
Tyrosine Hydroxylase
Uniprot Number:
P07101
Protein Aliases:
tyrosine 3-monooxygenase
Gene Name:
TH
Gene ID:
7054
Gene Aliases:
DYT5b
Accession Number:
NM_000360
Organism:
Rat
Tissue:
Brain
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Radiometric
Measured Response:
Scintillation
Testing Information
Substrate:
[3H]tyrosine (10 µM)
Incubation:
10 min at 37°C
Control Inhibitor:
3-iodo L-tyrosine
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
Clinical Relevance
Therapeutic Area:
CNS/Addiction/Pain
Additional Information
Brand:
LeadHunter
Testing Location:
France - Celle L'Evescault
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