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. The D2-like receptors include the two isoforms of the D2 receptor, differing in the length of their predicted third cytoplasmic loop, dubbed D2 short (D2S) and D2 long (D2L). The dopamine D2S receptor couples to PTX-sensitive G proteins (Gi/o) to initiate multiple signaling pathways. In cells of neuroendocrine origin, the D2S couples to "inhibitory" pathways, including inhibition of adenylyl cyclase, activation of potassium channels to hyperpolarize the cell membrane, and inhibition of L-type calcium channels, which in concert mediate inhibition of hormone secretion and gene transcription, and inhibition of cell proliferation. D2 dopamine receptors have been implicated in the pathophysiology of schizophrenia and Parkinson’s disease.

Family:

GPCR

Sub Family:

Dopamine

Class:

Class A

Protein Name:

D2

Uniprot Number:

P14416

Gene Name:

DRD2

Gene ID:

1813

Accession Number:

NM_000795

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H]methyl-spiperone

Ligand Kd (nM):

0.15

Ligand Concentration:

0.3 nM

Non Specific:

10 µM (+)butaclamol

Incubation:

60 min at RT

Control Inhibitor:

(+)-Butaclamol

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

681

Name

Dopamine

Measurement

16000nM -

PubChem ID

2818

Name

Clozapine

Measurement

610nM - IC50

PubChem ID

5018

Name

SCH 23390

Measurement

3100nM - IC50

PubChem ID

37459

Name

(+)-Butaclamol

Measurement

1.64nM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Adverse / Beneficial Action:

Dopamine D2L antagonist may be useful in the treatment of psychosis without development of tardive dyskinesia.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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