NK1 receptor ligand binding assay
The neurokinin (NK) 1 receptor is a member of the tachykinin family of G-protein-coupled receptors, which also includes NK2 and NK3 receptors. The NK1 receptor is localized in high concentrations in the CNS (particularly the striatum, amygdala and some hypothalamic and thalamic nuclei) and peripheral tissues.
An opioid-like receptor with a high degree of homology to µ, δ and κ-opioid receptors has been cloned and termed the orphan opioid receptor (NOP, ORL1). This receptor has a pharmacological profile distinct from the classical opioid receptors and an endogenous ligand, nociceptin (orphanin FQ) has been identified.
Tachykinin NK1 binding assay starter pack
| Products | Product reference | Product insert | MSDS |
| Tag-lite NK1 receptor red agonist - 5,000 tests | L0008RED | ||
| Tag-lite Tachykinin NK1 - 1 Million labeled cells | C1TT1NK1 | - | |
| 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 agonist is a substance P derivative labelled with a red emitting HTRF fluorescent probe.
- This ligand has been successfully used in a NK1 Tag-lite binding assay.
- Concentration: 10µM (H2O)
| Related products | Product reference | Product insert |
| Plasmid pSNAP-Alpha1A | PSNAPNK1 | |
| Tag-lite SNAP-Lumi4Tb - 2 nmoles | SSNPTBC | - |
Assay validation
NK1 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 L008RED (NK1 receptor red agonist) 5 nM.
Results obtained with radioligand assay and Tag-lite platform were very similar.
| Family | Receptor | Compounds | Radioactivity( Ki nM) | Tag-lite (Ki nM) |
| Tachykinin | NK1 | Substance P (agonist) | 0.29 (1) | 1.95 |
| L-712,138 (antagonist) | 1.25 - 134 (2) | 24.5 |
(1) Appell et al. J. Biomol Screening, 1998
(2) Cascieri et al. J. Biol Chem, 1994
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