Biological Information

Background Information:

Translocator protein (TSPO), previously called peripheral benzodiazepine receptor (PBR), was originally discovered as an alternative binding site for diazepam, a benzodiazepine. PBR/TSPO is a multimeric receptor composed of the Mr 18,000 receptor protein and the Mr 34,000 voltage-dependent anion channel protein. Expression of PBR has been found in every tissue examined; however, it is most abundant in steroid-producing tissues such as the adrenals, testes, ovaries, placenta, and brain, where it is primarily localized in the outer mitochondrial membrane. The primary function of PBR is the regulation of steroidogenesis, its existence in nonsteroidogenic tissues suggests that there may be other roles for PBR.

Family:

Mitochondrial Function

Sub Family:

Mitochondrial-Associated Protein

Protein Name:

PBR

Uniprot Number:

B1AH88|P30536

Protein Aliases:

peripheral-type benzodiazepine receptor/recognition site

Gene Name:

TSPO

Gene ID:

706

Gene Aliases:

PBR|MBR|PKBS|mDRC|DBI|IBP|pk18

Accession Number:

NM_007311

Organism:

Human

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H] PK 11195

Ligand Kd (nM):

5.3

Ligand Concentration:

0.5 nM

Non Specific:

10µM PK 11195

Incubation:

15 min at RT

Control Inhibitor:

PK 11195

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

1345

Name

PK 11195

Measurement

4.4nM - IC50

PubChem ID

24893306

Name

Diazepam

Measurement

1100nM - IC50

PubChem ID

24278437

Name

Ro 151788

Measurement

- IC50

Clinical Relevance

Therapeutic Area:

Cardiovascular

Adverse / Beneficial Action:

Agonist and/or antagonist may disturb steroidogenesis.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

RELATED SOLUTIONS

Item: 29
Item: P3
Item: P411