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
V1A Human Vasopressin / Oxytocin GPCR Cell Based Agonist IP1 LeadHunter Assay - TW
Item
364510-0
Protein
V1A
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
V1A Human Vasopressin / Oxytocin GPCR Cell Based Antagonist IP1 LeadHunter Assay - TW
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
Clinical Relevance
Therapeutic Area:
Cardiovascular
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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