Biological Information

Background Information:

The actions of several neurotransmitters, including norepinephrine, are regulated through their rapid uptake and clearance from synaptic junctions by plasma membrane transport proteins. The norepinephrine transporter in central adrenergic neurones is responsible for the recovery of up to 90 percent 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 systems, contributing to their behavioral and autonomic effects.

Family:

Transporter

Sub Family:

SLC6 / Monoamine

Class:

SLC

Protein Name:

NET

Uniprot Number:

P23975

Protein Aliases:

norepinephrine transporter

Gene Name:

SLC6A2

Gene ID:

6530

Gene Aliases:

NET

Organism:

Human

Cell Type:

CHO

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Tracer:

[3H] Norepinephrine (250 nM)

Incubation:

180 min at 22°C

Control Inhibitor:

protriptyline

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:

16

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

4976

Name

protriptyline

Measurement

0.5nM - IC50

PubChem ID

24277909

Name

GBR 12909

Measurement

224nM - IC50

PubChem ID

24278097

Name

imipramine

Measurement

19nM - IC50

PubChem ID

24278094

Name

desipramine

Measurement

0.14nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

RELATED SOLUTIONS

Item: P347
Item: P460-EU
Item: P452-EU