D4.4 Human Dopamine GPCR GTPgammaS Agonist LeadHunter Assay - TW

Item: 310600-0

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OVERVIEW

DOCUMENTS/REFERENCES

Biological Information

Background Information:

Dopamine receptors belong to the superfamily of G protein-coupled seven transmembrane proteins. G-protein-coupled receptors constitute one of the major signal transduction systems in eukaryotic cells. Coding sequences for these receptors, in those regions believed to contribute to the agonist-antagonist binding site, are strongly conserved across mammalian species. Various members of the dopamine receptor family are generally classified as either ‘D1-like’ or ‘D2-like’. D2-like receptors comprise the D2, D3 and D4 receptors, which inhibit activation of adenylate cyclases via coupling to G1/G0 protein.

Family:

GPCR

Sub Family:

Dopamine

Class:

Class A

Protein Name:

Uniprot Number:

P21917

Gene Name:

DRD4

Gene ID:

1815

Gene Aliases:

DRD1B

Accession Number:

NM_000797

Organism:

Human

Construct Details:

Full Length, Recombinant

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

GTPgammaS

Functional Mode:

Agonist

Detection Method:

Radiometry

Measured Response:

Scintillation

Testing Information

Incubation:

30 min at 30°C

Control Activator:

Dopamine

Criteria For Significance:

≥ 50% Increase in bound [35S]GTPgammaS relative to dopamine response, ≥ 50% Inhibition of dopamine-induced bound [35S]GTPgammaS

Test Concentration / Dose:

Compounds are screened at 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.003 μM

Test Sample Requirements:

75 μl of 10 mM stock or 1 mg (pre-weighed) powder (assuming FW ≦500 and purity 100%)

Minimum Order Quantity:

Turnaround Time

Standard:

20 Business Days

Reference Compound Data

PubChem ID

901

Name

Acetylcholine

Measurement

0.22μM - EC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Adverse / Beneficial Action:

Dopamine D4 receptor antagonism may be useful in the treatment of psychosis, possibly without causing tardive dyskineasia and hyperprolactineamia; receptor antagonism has also been reported to reduce novelty seeking. No major pharmacological differences have been reported for the most common variants of this receptor (D4.2, D4.4 and D4.7).

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei