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.

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:

Recombinant

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

Fluorimetry

Measured Response:

Fluorescence

Testing Information

Incubation:

RT

Control Inhibitor:

[d(CH2)51,Tyr(Me)2]-AVP

Control Activator:

Vasopressin (10 nM)

Test Concentration / Dose:

Eurofins will provide IC/EC50 calculation if 5 or more concentrations are selected.

Test Sample Requirements:

Minimum for 1) Screen: 70 µL of 10 mM stock -OR- 1 mg (pre-weighed) for 10µM finµL 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:

16

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

60943

Name

Relcovaptan

Measurement

2.43nM - IC50

PubChem ID

Name

[d(CH2)51,Tyr(Me)2]-AVP

Measurement

6nM - IC50

PubChem ID

216237

Name

Tolvaptan

Measurement

123nM - IC50

PubChem ID

46200932

Name

Balovaptan

Measurement

2.82nM - IC50

Clinical Relevance

Therapeutic Area:

Cardiovascular

Adverse / Beneficial Action:

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 Raynauds disease.

Additional Information

Brand:

LeadHunter

Testing Location:

France - Celle L'Evescault

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