Biological Information

Background Information:

Vasopressin 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. Vasopressin receptors are currently classified into V1A, V1B (V3) and V2 subtypes. The V1A receptor, the most widespread vasopressin receptor subtype, is found in many central nervous system structures and peripheral tissues. Vasopressin V1A receptor agonism may cause hypertension and coronary vasospasm as well as increase platelet aggregation and vascular smooth muscle cell proliferation. Receptor antagonism may be useful in the treatment of dysmenorrhea and Raynaud’s disease.

No. of Assays on Panel:

2

Assays on Panel:

Family

GPCR

Name

Item

364510-0

Protein

V1A

Organism

Human

Assay Sub Type

Cell Based

Family

GPCR

Name

Item

364510-1

Protein

V1A

Organism

Human

Assay Sub Type

Cell Based

Family:

GPCR

Sub Family:

Vasopressin and Oxytocin

Class:

Class A

Protein Name:

V1A

Uniprot Number:

P37288

Protein Aliases:

AVPR V1a|Antidiuretic hormone receptor 1a|Vascular/hepatic-type arginine vasopressin receptor

Gene Name:

AVPR1A

Gene ID:

552

Gene Aliases:

AVPR1

Accession Number:

NM_000706

Organism:

Human

Construct Details:

Full Length, Recombinant

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Agonist & Antagonist

Detection Method:

TR-FRET

Measured Response:

Fluorescence

Testing Information

Procedure Summary:

Human recombinant vasopressin V1A receptors expressed in CHO-K1 cells are used. Test compound and/or vehicle is incubated with the cells (1.5 x 10^6 /ml) in stimulation buffer of IP1 Tb kit for 30 minutes at 37°C. Test compound-induced increase of fluorescence by 50 percent or more (≥50%) relative to the 1 μM AVP response indicates possible V1A receptor agonist activity. Test compound-induced inhibition of 10 nM AVP-induced increase of fluorescence response by 50 percent or more (≥50%) indicates receptor antagonist activity.

Incubation:

30 min at 37°C

Control Inhibitor:

SR 49059

Control Activator:

AVP

Criteria For Significance:

≥ 50% increase in IP-one relative to AVP response, ≥ 50% inhibition of AVP-induced 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

60943

Name

Relcovaptan

Measurement

0.0018μM - IC50

PubChem ID

439302

Name

OXYTOCIN

Measurement

0.22μM - EC50

PubChem ID

6918320

Name

L-371257

Measurement

1.9μM - IC50

PubChem ID

9549168

Name

Argipressin acetate

Measurement

0.00074μM - EC50

PubChem ID

9895468

Name

Nelivaptan

Measurement

0.25μM - IC50

PubChem ID

11957585

Name

L-368,899

Measurement

0.34μM - IC50

Clinical Relevance

Therapeutic Area:

Cardiovascular

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

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