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’. D1-like receptors comprise the D1 and D5 receptors, which activate adenylate cyclases via coupling to GS protein.

Family:

GPCR

Sub Family:

Dopamine

Class:

Class A

Protein Name:

D5

Uniprot Number:

P21918

Gene Name:

DRD5

Gene ID:

1816

Gene Aliases:

DRD1B

Accession Number:

NM_000798

Organism:

Human

Construct Details:

Recombinant

Cell Type:

GH4

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

HTRF

Testing Information

Incubation:

30 min at RT

Control Inhibitor:

SCH 23390

Control Activator:

dopamine (50 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

PubChem ID

5018

Name

SCH 23390

Measurement

0.35nM - IC50

PubChem ID

133633

Name

L-741,626

Measurement

1300nM - IC50

PubChem ID

4302960

Name

GR 103691

Measurement

20000nM - IC50

PubChem ID

5311200

Name

L-745870

Measurement

30000nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Adverse / Beneficial Action:

D5 receptor agonism may be of therapeutic benefit in the treatment of Parkinsons disease as well as induce dyskinesia, extreme arousal, locomotor activation, vasodilatation and hypotension.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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