Valiglurax (VU0652957) is a potent, orally active and selective mGlu4 positive allosteric modulator with EC50 values of 64.6 nM and 197 nM for hmGlu4/Gqi5 and rmGlu4 GIRK, respectively. Valiglurax is a central nervous system (CNS) penetrant. Valiglurax can be used in research of Parkinson's disease[1].
Valiglurax (VU0652957; 0.3-30 mg/kg; po) 以剂量依赖性方式逆转 haloperidol 诱导的大鼠僵直症 (HIC)[1]。
| Animal Model: | haloperidol-induced catalepsy (HIC) in rats[1] |
| Dosage: | 0.3-30 mg/kg |
| Administration: | Oral administration |
| Result: | Reversed haloperidol -induced catalepsy (HIC) in rats in a dose-dependent manner. |
[1]. Panarese JD, et, al. Discovery of VU2957 (Valiglurax): An mGlu4 Positive Allosteric Modulator Evaluated as a Preclinical Candidate for the Treatment of Parkinson's Disease. ACS Med Chem Lett. 2018 Oct 16;10(3):255-260.