Kappa opioid receptor ligand binding assay
Opioid receptors are currently classified into three groups, the κ, δ and µ receptors. Subtypes within each group have been suggested, including µ1, µ2, δ1, δ2, κ1, κ2, and κ3.
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.
Kappa opioid receptor ligand binding assay starter pack
| Products | Product reference | Product insert | MSDS |
| Tag-lite Opioid receptors red antagonist - 5,000 tests | L0005RED | ||
| Tag-lite Kappa opioid - 1 Million labeled cells | C1TT1KOP | ||
| 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 200 tests at a cell density of 5,000 cells/well.
- This antagonist is naltrexone derivative labeled with a Red Emitting HTRF fluorescent probe.
- This ligand has been successfully used both in a µ, δ and κ-opiod Tag-lite binding assays.
- Buffer: HEPES pH7.4 + 10% DMSO
- Molecular Weight: 1144.4
Assay Validation:
Kappa opioid receptor ligand binding assay was performed using the starter pack reagents.
Kd was determined and signal inhibition (IC50) by antagonists was performed with L0005RED (Tag-lite opioid receptors red antagonist) 8 nM.
Results obtained with radioligand assay and Tag-lite platform were very similar.
| Family | Receptor | Compounds (antagonist) | Radioactivity( Ki nM) | Tag-lite (Ki nM) |
| Opioid | kappa | Naloxone | 2.4 (1) | 9.6 |
| Naltrindole | 10.1 (1) | 2.69 |
(1) Toll et al. NIDA Red Monogr., 1998
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