9H-Xanthene-9-carboxamide, N-[4-(trifluoromethyl)-2-oxazolyl]-

Biological Activity

RO0711401 is a selective and orally active positive allosteric modulator of mGlu1 receptor with an EC50 of 56 nM[1][2]. RO0711401 (10 mg/kg; s.c.; once) causes a long-lasting improvement in motor performance, which is maintained to the same extent at least for 6 days[1].Systemic injection of RO0711401 is shown to reduce the frequency of spike-and-wave discharges in a rat model of absence epilepsy, and to improve motor signs in autoimmune encephalomyelitis (EAE) mice[1].

References

[1]. Serena Notartomaso, et al. Pharmacological enhancement of mGlu1 metabotropic glutamate receptors causes a prolonged symptomatic benefit in a mouse model of spinocerebellar ataxia type 1. Mol Brain. 2013 Nov 19;6:48. [2]. Eric Vieira, et al. Fluorinated 9H-xanthene-9-carboxylic acid oxazol-2-yl-amides as potent, orally available mGlu1 receptor enhancers. Bioorg Med Chem Lett. 2009 Mar 15;19(6):1666-9.