CTEP (Ro4956371) is a research drug developed by
Hoffmann-La Roche that acts as a selective
allostericantagonist of the
metabotropic glutamate receptor 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 mGluR5 antagonists such as
MPEP and
fenobam.[1]
References
^Lindemann L, Jaeschke G, Michalon A, Vieira E, Honer M, Spooren W, Porter R, Hartung T, Kolczewski S, Büttelmann B, Flament C, Diener C, Fischer C, Gatti S, Prinssen EP, Parrott N, Hoffmann G, Wettstein JG (November 2011). "CTEP: a novel, potent, long-acting, and orally bioavailable metabotropic glutamate receptor 5 inhibitor". The Journal of Pharmacology and Experimental Therapeutics. 339 (2): 474–86.
doi:
10.1124/jpet.111.185660.
PMID21849627.
S2CID2554923.