Biological Information

Background Information:

Adrenoreceptors 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. Adrenoreceptors are found in most peripheral tissue and within the central nervous system.

Family:

GPCR

Sub Family:

Adrenoceptor

Class:

Class A

Protein Name:

alpha1B

Uniprot Number:

P35368

Protein Aliases:

Alpha-1B adrenoceptor

Gene Name:

ADRA1B

Gene ID:

147

Accession Number:

XM_011534437

Organism:

Human

Construct Details:

Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometric

Measured Response:

Scintillation

Testing Information

Ligand:

[3H]prazosin

Ligand Kd (nM):

0.055

Ligand Concentration:

0.15 nM

Non Specific:

10 µM Phentolamine

Incubation:

60 min at RT

Control Inhibitor:

Prazosin

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:

15 Business Days

Reference Compound Data

PubChem ID

4636

Name

Oxymetazoline

Measurement

993nM - IC50

PubChem ID

4893

Name

Prazosin

Measurement

0.25nM - IC50

PubChem ID

6041

Name

Phenylephrine

Measurement

12300nM - IC50

PubChem ID

210172

Name

21102-95-4

Measurement

153nM - IC50

Clinical Relevance

Therapeutic Area:

Cardiovascular

Adverse / Beneficial Action:

Adrenergic a1B receptor antagonism may cause a reduction in blood pressureas well as orthostatic hypotension.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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