V1A receptor ligand binding assay
Vasopressin receptors are a group of G-protein-coupled receptors that mediate vasoconstriction, antidiuresis and ACTH release. They are currently divided into three subtypes, V1A, V1B and V2, and are closely related to oxytocin receptors (OT).
Vasopressin/Oxytocin V1A binding assay starter pack
| Products | Product reference | Product insert | MSDS |
| Vasopressin receptors red antagonist - 5,000 tests | L0003RED | ||
| Tag-lite Vassopressin V1A - 1 Million labeled cells | C1TT1V1A | - | |
| Tag-lite buffer - 100 ml (5X) | LABMED | - | - |
The binding assay starter pack consists of three references, the labeled cells, the fluorescent ligand and the Tag-lite buffer. Each component must be ordered separately. The cells express the SNAP-receptor labeled with terbium cryptate (labeling performed with Tag-lite SNAP-Lumi4 Tb). The labeled cells are proposed in a 1 million cell pack, to achieve a minimum of 100 tests at a cell density of 10,000 cells/well.
- This antagonist is an Arginine-Vasopressin (AVP) derivative labelled with a Red Emitting HTRF fluorescent probe.
- This ligand has been successfully used in a V1AR Tag-lite binding assay. But does not bind the V2 receptor.
- Concentration: 10µM, H2O
- Molecular Weight: 1925
| Related products | Product reference | Product insert |
| Plasmid pSNAP-V1A | PSNAPV1A | |
| Tag-lite SNAP-Lumi4Tb - 2 nmoles | SSNPTBC | - |
Assay validation
Vasopressin V1A receptor ligand binding assay was performed using the starter pack reagents.
Kd was determined and signal inhibition (IC50) by agonist and antagonist was performed with L0003RED (Tag-lite Vasopressin receptors red antagonist) 1 nM.
Results obtained with radioligand assay and Tag-lite platform were very similar.
| Family | Receptor | Compounds | Radioactivity( Ki nM) | Tag-lite (Ki nM) |
| Vasopressin | V1a | AVP (agonist) | 0.7 - 1.7 (1-2) | 1.06 |
| HO-LVA (antagonist) | 0.08 - 0.27 (1-2) | 0.14 | ||
| SR49059 (antagonist) | 0.62 - 1 (3-4) | 0.60 |
(1) Durroux et al J Med Chem 1999
(2) Albizu et al. J. Med. Chem. 2007
(3) Albizu et al. J. Med. Chem. 2007
(4) Durroux et al J Med Chem 1999
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