D3 Human Dopamine GPCR Binding Antagonist Radioligand LeadHunter Assay - FR

Item: 48

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OVERVIEW

DOCUMENTS/REFERENCES

Biological Information

Background Information:

Five subtypes of dopamine receptors, D1, D2, D3, D4 and D5, were identified on the basis of pharmacological or biochemical criteria. Dopamine receptors have been classified into either the D1-like (D1, D1B, and D5) or D2-like (D2, D3, and D4). The selective D3 receptor involvement in regulating cognition and awareness states, and not generalized motor coordination, have potential therapeutic utility in treating attention deficit disorders.

Family:

GPCR

Sub Family:

Dopamine

Class:

Class A

Protein Name:

Uniprot Number:

P35462

Gene Name:

DRD3

Gene ID:

1814

Accession Number:

NM_000796.3

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H]methyl-spiperone

Ligand Kd (nM):

0.25

Ligand Concentration:

0.25 nM

Non Specific:

10 µM (+)butaclamol

Incubation:

60 min at RT

Control Inhibitor:

Butaclamol

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:

Turnaround Time

Standard:

10 Business Days

Reference Compound Data

PubChem ID

24278400

Name

butaclamol

Measurement

3nM - IC50

PubChem ID

24277892

Name

clozapine

Measurement

1136nM - IC50

PubChem ID

24277910

Name

SCH23390

Measurement

2223nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Adverse / Beneficial Action:

Dopamine D3 receptor antagonist may be useful in treatment of psychosis, possibly without causing tardive dyskinesia, attention deficit disorder and hyperprolactemia; receptor antagonism has also been reported to attenuate cocaine addiction

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault