Biological Information

Background Information:

The actions of several neurotransmitters, including dopamine, are regulated through their rapid uptake and clearance from synaptic junctions by plasma membrane transport proteins. The dopamine transporter in central dopaminergic neurones is responsible for the recovery of up to 90% of released transmitter. The monoamine transporters are high affinity targets for a number of psychoactive agents such as cocaine, amphetamine, and antidepressants. These agents, by blocking transporters and consequently preventing neuronal uptake, elevate levels of extracellular neurotransmitter concentrations in both the central and peripheral nervous system, contributing to their behavioral and autonomic effects.

Family:

Transporter

Sub Family:

SLC6 / Monoamine

Class:

SLC

Protein Name:

DAT

Uniprot Number:

Q01959

Protein Aliases:

dopamine transporter

Gene Name:

SLC6A3

Gene ID:

6531

Gene Aliases:

DAT|DAT1

Accession Number:

NM_001044

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H]BTCP

Ligand Kd (nM):

4.5

Ligand Concentration:

4 nM

Non Specific:

10 µM BTCP

Incubation:

120 min at 4°C

Control Inhibitor:

BTCP

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:

10 Business Days

Reference Compound Data

PubChem ID

681

Name

Dopamine

Measurement

10000nM - IC50

PubChem ID

4528

Name

Nomifensine

Measurement

15nM - IC50

PubChem ID

104920

Name

GBR 12909 dihydrochloride

Measurement

5nM - IC50

PubChem ID

123692

Name

BTCP

Measurement

7.1nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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