D4.4 Human Dopamine GPCR Cell Based Antagonist cAMP LeadHunter Assay - FR
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:
D4
Uniprot Number:
P21917
Gene Name:
DRD4
Gene ID:
1815
Gene Aliases:
DRD1B
Accession Number:
NM_000797
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:
10 min at 37°C
Control Inhibitor:
Clozapine
Control Activator:
dopamine (100 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 finµL 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
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:
France - Celle L'Evescault
RELATED SOLUTIONS
D4.4 Human Dopamine GPCR Cell Based Agonist & Antagonist cAMP LeadHunter Assay - FR
Item: G017
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