OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
The glycine transporter belongs to a family of Na+/Cl- dependent neurotransmitter transporters, predicted to contain as many as 12 transmembrane domains. In neurons and glial cells, the transporter actively takes up glycine, thus contributing to the recycling of messengers and the termination of the synaptic transmission. Two distinct types of these transporters, referred to as GlyT-1 and GlyT-2, have been characterized. Both transporters are members of the sodium/chloride dependent family, which also includes transporters for GABA and for biogenic amines. Inhibitors of glycine transporter are of potential therapeutic interest for the treatment of schizophrenia.
Family:
Transporter
Sub Family:
SLC6 / Glycine
Class:
SLC
Protein Name:
GLYT1
Uniprot Number:
P48067
Gene Name:
SLC6A9
Gene ID:
6536
Gene Aliases:
GLYT1
Organism:
Rat
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Antagonist
Detection Method:
Radiometry
Measured Response:
Scintillation
Testing Information
Procedure Summary:
This assay measures the uptake of [³H] Glycine by a rat glycine transporter. Brain aggregates of male Wistar-derived rats weighing 175 ± 25 g are prepared in modified HEPES pH 7.4 buffer using standard techniques. A 1 mg‡ aliquot of cell aggregates is incubated with 50 nM [³H] Glycine for 15 minutes at 37℃. Non-specific binding is estimated in the presence of 10 mM Glycine. Cell aggregates are filtered and washed 3 times, and the filters are counted to determine [³H] Glycine specifically bound. Compounds are screened at 10 µM.
Note: ‡Membrane protein may change from lot to lot; the concentration used will be adjusted if necessary.
Ligand:
[³H] Glycine
Ligand Concentration:
0.05 µM
Non Specific:
10000 µM Glycine
Incubation:
15 min at 37°C
Control Inhibitor:
Sarcosine
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:
16
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
CNS/Addiction/Pain
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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