CTEP
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CAS No. | 871362-31-1 | Cat. No. | BCP06140 |
Name | CTEP | ||
Synonyms | mGluR5 inhibitor; | ||
SMILES | |||
Chemical Name | |||
Formula | C19H13ClF3N3O | M. Wt | 391.77 |
Purity | 98% | Storage | Store at 4-8°C |
Description | IC50 Value: 2.2 nM Target: mGluR5 in vivo: CTEP is a novel, potent, selective and orally bioavailable allosteric antagonist of the metabotropic glutamate receptor subtype mGluR5. CTEP binds mGlu5 with low nanomolar affinity and shows >1000-fold selectivity when tested against 103 targets, including all known mGlu receptors. In animal studies CTEP was found to have a high oral bioavailability and a long duration of action, lasting 18 hours after a single dose, giving it considerably improved properties over older mGluR5 antagonists such as MPEP and fenobam. in vivo: CTEP (2 mg/kg p.o. bid) achieves uninterrupted mGlu5 occupancy per 48 hours in mice. CTEP (2 mg/kg p.o.) treatment corrects elevated hippocampal long-term depression, excessive protein synthesis, and audiogenic seizures in the Fmr1 knockout mouse. CTEP is significantly active at doses of 0.1 mg/kg and 0.3 mg/kg in treatment of anxiety in mouse. CTEP significantly increases drinking time at doses of 0.3 mg/kg and 1.0 mg/kg in |
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