Biological Information

Background Information:

GABA is the major inhibitory transmitter in the mammalian central nervous system, contributes to motor control and many other cortical functions. It also regulates anxiety, often used for the sedative/hypnotic and anxiolytic effects. GABA-transaminase (GABA-T) (4-aminobutyrate :2-oxoglutarate amino transferase) is the primary catabolic enzyme for GABA and its inhibition significantly elevates GABA concentrations in the brain, but also found in peripheral tissues. GABA-T inhibitors and the pharmacological consequences of inhibition of this enzyme suggest some therapeutic uses.

Family:

Neurotransmitter Metabolism

Sub Family:

GABA Turnover

Protein Name:

GABA Transaminase

Uniprot Number:

P80404

Protein Aliases:

4-aminobutyrate transaminase

Gene Name:

ABAT

Gene ID:

18

Gene Aliases:

GABAT

Accession Number:

NM_031003

Organism:

Rat

Construct Details:

Endogenous

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

Spectrofluorimetry

Measured Response:

Fluorescence

Testing Information

Procedure Summary:

Crude GABA transaminase prepared from rat brain is used. Test compound or vehicle and 9 mM GABA are combined with 0.8 mg/ml‡ of enzyme for 60 minutes at 37⁰C in Boric acid buffer pH 8.2. Coupling reagent is added for another 30 minute incubation period at 60⁰C. Place the plate at room temperature and stay for 10 minutes for precipitation. Transfer end-mixture supernatant to another plate. Read plate on a spectrophotometer (Excitation: 405 nm, Emission: 510 nm). Compounds are screened at 10 μM.

Substrate:

9000 µM GABA

Incubation:

60 min at 37°C

Control Inhibitor:

2921-14-4

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

PubChem ID

2723609

Name

2921-14-4

Measurement

0.068μM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

Questions? Contact Us

You can easily get in touch with a Eurofins Discovery Expert or get help from our Customer Service team. Reach out with questions, or to discuss your specific discovery challenges.

Questions? Contact Us