CTEP (Ro4956371) is a research drug developed by
Hoffmann-La Roche that acts as a selective
allosteric antagonist of the
metabotropic glutamate receptor
The metabotropic glutamate receptors, or mGluRs, are a type of glutamate receptor that are active through an indirect metabotropic process. They are members of the group C family of G-protein-coupled receptors, or GPCRs. Like all glutamate re ...
subtype
mGluR5, binding with nanomolar affinity and over 1000 times selectivity over all other receptor targets tested. In animal studies it 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 mGluR
5 antagonists such as
MPEP and
fenobam
Fenobam is an imidazole derivative developed by McNeil Laboratories in the late 1970s as a novel anxiolytic drug with an at-the-time-unidentified molecular target in the brain. Subsequently, it was determined that fenobam acts as a potent and s ...
.
References
Alkyne derivatives
Imidazoles
MGlu5 receptor antagonists
Pyridines
Trifluoromethyl ethers
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