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. Adrenergic a2C receptor may cause peripheral vasoconstriction; antagonism may act peripherally to increase the skeletal muscle blood flow.

Family:

GPCR

Sub Family:

Adrenoceptor

Class:

Class A

Protein Name:

alpha2C

Uniprot Number:

P18825

Protein Aliases:

Alpha-2C adrenoreceptor|Alpha-2C adrenoceptor|Alpha-2CAR

Gene Name:

ADRA2C

Gene ID:

152

Gene Aliases:

ADRA2L2|ADRA2RL2

Accession Number:

NM_000683

Organism:

Human

Construct Details:

Full Length, Recombinant

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

GTPgammaS

Functional Mode:

Antagonist

Detection Method:

Radiometry

Measured Response:

Scintillation

Testing Information

Incubation:

30 min at 30°C

Control Inhibitor:

Yohimbine

Criteria For Significance:

≥ 50% Inhibition of UK-14304-induced bound [35S]GTPgammaS, ≥50% Increase in bound [35S]GTPgammaS relative to UK-14304 response

Test Concentration / Dose:

Compounds are screened at 10, 3, 1, 0.3, 0.1, 0.03, 0.01 and 0.003 μM

Test Sample Requirements:

75 μl of 10 mM stock or 1 mg (pre-weighed) powder (assuming FW ≦500 and purity 100%)

Minimum Order Quantity:

16

Turnaround Time

Standard:

20 Business Days

Reference Compound Data

PubChem ID

8969

Name

Yohimbine

Measurement

0.016μM - IC50

Clinical Relevance

Therapeutic Area:

CNS/Addiction/Pain

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

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