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

PubChem ID

3442

Name

fusaric acid

Measurement

- IC50

PubChem ID

68309

Name

N-Methyl-L-tyrosine

Measurement

- IC50

PubChem ID

Name

3-iodo L-tyrosine

Measurement

574nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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