ABP-688 C-11 (8 (3-(6-methyl-pyridin-2-ylethynyl)-cyclohex-2-enoneO-11C-methyl-oxime), a noncompetitive and highly selective antagonist for the metabotropic glutamate receptor subtype 5 (mGluR5). It is a promising PET ligand for the quantification of mGlu5 receptors in humans and animals. It readily crosses the blood-brain barrier. The temporal and spatial changes in mGluR5 availability suggest ABP-688 C-11 PET imaging in epilepsy provide abnormal glutamatergic network during epileptogenesis. ABP-688 C-11 was used in receptors imaging in Major Depressive disorder, chronic neuropathic pain, anxiety and other brain disease investigations.
CNS Activity
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16595505 | https://www.ncbi.nlm.nih.gov/pubmed/17110115
Curator's Comment: # Novartis
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Radiosynthesis and preclinical evaluation of 11C-ABP688 as a probe for imaging the metabotropic glutamate receptor subtype 5. | 2006 Apr |
|
| In vivo variation in same-day estimates of metabotropic glutamate receptor subtype 5 binding using [(11)C]ABP688 and [(18)F]FPEB. | 2017 Aug |
Patents
Sample Use Guides
ABP688 was originally shown to be a potent antagonist of quisqualate-induced phosphoinositol (PI) accumulation in L(tk-) cells expressing recombinant human mGluR5 (hmGluR5), with an IC50 value of 2.4 nM (95% CI: 0.5–12 nM) . In the same preparation, ABP688 completely inhibited glutamate-induced calcium release with an IC50 value of 2.3 nM (95% CI: 2.1–2.5) nM and had no effect, up to 10 uM, on ATP-induced PI accumulation via stimulation
of endogenously expressed purinergic receptors in hmGluR5-expressing cells, or on quisqualate-induced PI accumulation in hmGluR1-expressing cells.
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