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:

D3

Uniprot Number:

P35462

Gene Name:

DRD3

Gene ID:

1814

Accession Number:

NM_000796.3

Organism:

Human

Construct Details:

Recombinant

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

HTRF

Testing Information

Incubation:

30 min at 37°C

Control Inhibitor:

(+)-Butaclamol

Control Activator:

dopamine (10 nM)

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

5018

Name

SCH 23390

Measurement

- IC50

PubChem ID

5265

Name

Spiperone

Measurement

3.3nM - IC50

PubChem ID

37459

Name

(+)-Butaclamol

Measurement

16nM - IC50

PubChem ID

133633

Name

L-741,626

Measurement

108nM - 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

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