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
Cell Type:
CHO-K1
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Agonist
Detection Method:
TR-FRET
Measured Response:
Fluorescence
Testing Information
Incubation:
30 min at 37°C
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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