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

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H]SCH 23390

Ligand Kd (nM):

0.25

Ligand Concentration:

0.3 nM

Non Specific:

10 µM SCH 23390

Incubation:

60 min at RT

Control Inhibitor:

SCH 23390

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:

2

Turnaround Time

Standard:

10 Business Days

Reference Compound Data

PubChem ID

2818

Name

Clozapine

Measurement

300nM - IC50

PubChem ID

5018

Name

SCH 23390

Measurement

0.39nM - IC50

PubChem ID

5355

Name

Sulpiride

Measurement

- IC50

PubChem ID

37459

Name

(+)-Butaclamol

Measurement

3nM - 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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