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D2 receptor ligand binding assay

Dopamine D2 receptor inhibits adenylyl cyclase activity. A missense mutation in this gene causes myoclonus dystonia; other mutations have been associated with schizophrenia. Alternative splicing of the gene results in two transcript variants encoding different isoforms. A third variant has been described, but it has not yet been determined whether this form is normal or due to aberrant splicing.

Dopamine D2 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 D2 binding kit - 120 tests 82D2LBPEA pdf

Dopamine D2 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 cell pack, 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 Dopamine D2 receptor red antagonist - 5,000 tests L0002RED pdf pdf
Tag-lite Dopamine D2 - 1 Million labeled cells C1TT1D2 pdf -
Tag-lite buffer - 100 ml (5X) LABMED - -
Related products Product reference Product insert
Plasmid pSNAP-D2 PSNAPD2 pdf
Tag-lite SNAP-Lumi4Tb - 2 nmoles SSNPTBC -
Features:
  • This D2R antagonist is a spiperone derivative labelled with a Red Emitting HTRF fluorescent probe.
  • This ligand has been successfully used in a D2R Tag-lite binding assay.
  • Concentration: 10µM
  • Buffer: HEPES pH7.4 + 10% DMSO
  • Molecular Weight: 1294.6

Assay Validation:

 

Dopamine D2 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 L002RED (dopamine D2 Red Antagonist) 3 nM.

Results obtained with radioligand assay and Tag-lite platform were very similar.

Family Receptor Compounds Radioactivity ( Ki nM) Tag-lite (Ki nM)
Dopamine D2 NAPS (antagonist) 0.14 (1) 7.65
Bromocriptine (agonist) 8 (2) 11.9
PPHT (agonist) 0.64 (2) 13.3

(1) Monsma et al. J Neurochemistry, 1989
(2) Backthavachalam et al J Med Chem, 1991



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