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CTEP
- RO 4956371
- Soluble in DMSO
- MF: C19H13ClF3N3O
- MW: 391.77
Description
CTEP (RO4956371) is a potent, long-acting and orally bioavailable negative allosteric modulator of mGluR5. It binds mGluR5 with low-nanomolar affinity and shows strong selectivity against other metabotropic glutamate receptor subtypes and diverse off-targets.
mGluR5 regulates excitatory glutamatergic signaling, synaptic plasticity and CNS circuit function. CTEP is a valuable tool for sustained mGluR5 blockade in neuropharmacology, behavioral models and disease-relevant studies such as Fragile X syndrome research.
Key Features
- Potent mGluR5 negative allosteric modulator (NAM)
- Long-acting and orally bioavailable pharmacological profile
- High selectivity across mGlu receptor subtypes
- Improved experimental utility compared with earlier mGluR5 NAMs
Applications
- mGluR5 receptor pharmacology
- Glutamatergic signaling studies
- CNS behavioral model research
- Fragile X and synaptic plasticity studies
Related information: Older mGluR5 antagonists such as MPEP (Axon 1222) and Fenobam (Axon 1345) are also available.
More Information
| Parent CAS No. | 871362-31-1 |
|---|---|
| Chemical Name | 2-chloro-4-((2,5-dimethyl-1-(4-(trifluoromethoxy)phenyl)-1H-imidazol-4-yl)ethynyl)pyridine |
| SMILES | C1(Cl)=NC=CC(C#CC2=C(C)N(C3=CC=C(OC(F)(F)F)C=C3)C(C)=N2)=C1 |
| MFCD | MFCD22665726 |
| InChi | InChI=1S/C19H13ClF3N3O/c1-12-17(8-3-14-9-10-24-18(20)11-14)25-13(2)26(12)15-4-6-16(7-5-15)27-19(21,22)23/h4-7,9-11H,1-2H3 |
| InChiKey | GOHCTCOGYKAJLZ-UHFFFAOYSA-N |
| CID | 11646823 |
| Short Description | mGluR5 NAM |
References
- L Lindemann et al. CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor. J. Pharmacol. Exp. Ther. 2011, 339(2), 474-486.
- A Michalon et al. Chronic Pharmacological mGlu5 Inhibition Corrects Fragile X in Adult Mice. Neuron 2012, 74(1), 49-56.
- C Harrison. Neurodevelopmental disorders: Glutamate blockers show benefit in models of autism spectrum disorders. Nature Rev. Drug Disc. 2012, 11, 440-441.
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