| Description | Basimglurant (CTEP Derivative) is a potent, selective and orally available modulator of mGlu5 negative allosteric(Kd of 1.1 nM). |
| In vitro | In competition binding experiments on human recombinant mGlu5, Basimglurant (RG7090) fully displaces [3H]-MPEP with a Ki of 35.6 nM and [3H]-ABP688 with a Ki of 1.4 nM. In HEK293 cells stably expressing human mGlu5, Basimglurant (RG7090) inhibits quisqualate induced Ca2+ mobilization with an IC50 of 7.0 nM and [3H]-inositolphosphate accumulation (IC50 of 5.9 nM). Basimglurant shows similar potencies in radioligand binding and functional assay on human and rodent mGlu5 receptor orthologues[1]. |
| In vivo | Basimglurant is selective and safe inhibitor of mGlu5 with good oral bioavailability and long half-life supportive of once-daily administration, good brain penetration, and high in vivo potency. Basimglurant has antidepressant properties which are corroborated by its functional magnetic imaging (fMRI) profile, as well as anxiolytic-like and antinociceptive features[1]. |
| Target activity | mGlu5 receptor:1.1 nM (Kd) |
| Synonyms | CTEP Derivative, RG7090 |
| molecular weight | 325.77 |
| Molecular formula | C18H13ClFN3 |
| CAS | 802906-73-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 60 mg/mL (184.18 mM), Sonication is recommended. |
| References | 1. Lindemann L, et al. Pharmacology of basimglurant (RO4917523, RG7090), a unique metabotropic glutamate receptor 5 negative allosteric modulator in clinical development for depression. J Pharmacol Exp Ther. 2015 Apr;353(1):213-33. 2. Jaeschke G, et al. Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. |