V1A Human Vasopressin / Oxytocin GPCR Binding Antagonist Radioligand LeadHunter Assay - TW

Item: 287530

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OVERVIEW

DOCUMENTS/REFERENCES

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:

Full Length, Recombinant

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Binding

Detection Method:

Radiometry

Measured Response:

Scintillation

Testing Information

Procedure Summary:

Human recombinant vasopressin V1A receptors expressed in HEK-293 cells are used in modified Tris-HCl buffer pH 7.4. A 0.26 μg‡ aliquot is incubated with 0.03 nM [¹²⁵I]Phenylacetyl-D-Tyr(Me)-Phe-Gln-Asn-Arg-Pro-Arg-Tyr-NH2 for 120 minutes at 25°C. Non-specific binding is estimated in the presence of 1 μM [Arg8]Vasopressin. Receptors are filtered and washed, the filters are then counted to determine [¹²⁵I]Phenylacetyl-D-Tyr(Me)-Phe-Gln-Asn-Arg-Pro-Arg-Tyr-NH2 specifically bound. Compounds are screened at 10 μM.
Note: ‡Membrane protein may change from lot to lot, the concentration used will be adjusted if necessary

Ligand:

[¹²⁵I] PhenylacetylTyr(Me)PheGlnAsnArgProArgTyr

Ligand Kd (nM):

0.0074

Ligand Concentration:

0.03 nM

Non Specific:

1 µM (Arg⁸)-Vasopressin

Incubation:

120 min at 25°C

Control Inhibitor:

(Arg⁸)-Vasopressin

Criteria For Significance:

≥ 50% of max stimulation or inhibition

Test Concentration / Dose:

Suggested concentration for initial testing is 10 uM

Test Sample Requirements:

Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).

Minimum Order Quantity:

Turnaround Time

Standard:

15 Business Days

Reference Compound Data

PubChem ID

44419026

Name

Dvdavp

Measurement

0.022μM - IC50

PubChem ID

Name

(Arg8)-Vasopressin

Measurement

0.00033μM - IC50

PubChem ID

Name

(Phenylac1Tyr(Me)2,Arg68Tyr-NH29)-Vasopressin

Measurement

0.000019μM - IC50

PubChem ID

Name

(d(CH2)51,D-Ile2,Ile4,Arg8,Ala-NH29)-Vasopressin

Measurement

0.0073μM - 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:

Taiwan - Taipei