Biological Information

Background Information:

The actions of several neurotransmitters, including serotonin, are regulated through their rapid uptake and clearance from synaptic junctions by plasma membrane transport proteins. The serotonin transporter in central serotoninergic neurons 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 concentration 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:

SERT

Uniprot Number:

P31645

Protein Aliases:

serotonin transporter 1

Gene Name:

SLC6A4

Gene ID:

6532

Gene Aliases:

5-HTT|SERT1|HTT

Accession Number:

NM_001045

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H]imipramine

Ligand Kd (nM):

1.7

Ligand Concentration:

2 nM

Non Specific:

10 µM Imipramine

Incubation:

60 min at RT

Control Inhibitor:

imipramine

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

2771

Name

citalopram

Measurement

3.8nM - IC50

PubChem ID

3696

Name

Imipramine

Measurement

2.1nM - IC50

PubChem ID

5202

Name

serotonin

Measurement

4300nM - IC50

PubChem ID

5365247

Name

zimelidine

Measurement

3600nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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