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Mu 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.

Mu opioid receptor binding kit

The ligand binding kit contains all the material to perform at least 120 tests (labeled cells, fluorescent ligands and Tag-lite buffer).
Ligand binding kit Product reference Product insert
Tag-lite Mu opioid binding kit - 120 tests 82MOPLBPEA pdf

Mu opioid ligand binding products

The following ligand binding products may 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 cells packaging, to achieve a minimum of 100 tests at a cell density of 10,000 cells/well.
Ligand binding products Product reference Product insert MSDS
Tag-lite Opioid receptors red antagonist - 5,000 tests L0005RED pdf pdf
Tag-lite Mu opioid - 1 Million labeled cells C1TT1MOP pdf -
Tag-lite buffer - 100 ml (5X) LABMED - -
Related products Product reference Product insert
Plasmid pSNAP-Mu opioid PSNAPMOP pdf
Tag-lite SNAP-Lumi4Tb - 2 nmoles SSNPTBC -
Features:
  • 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:

 

Mu 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 mu Naloxone 1.63(1) 5.08
Naltrindole 6.7 (2) 8.11

(1) Spetea et al. Eur. J. Neuroscience, 2003
(2) Korlipara et al. Eur J. Med Chem, 1997



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