包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
Animal experiment: | Rats: For intravenous PK, Basimglurant (RG7090) is formulated in N-methyl-pyrollidone (NMP)/saline (30%/70%) as vehicle and administered at a volume of 2 mL/kg. For oral gavage (p.o.) the compound is administered as suspension using gelatine/saline (7.5%/0.62% in water) at an administration volume of 4 mL/kg[1]. Monkey: For intravenous PK, Basimglurant (RG7090) is formulated in cyclodextrin solution as vehicle and administered at a volume of 2 mL/kg. For oral gavage (p.o.), the compound is administered in capsule (2 mg in size-2 capsules, i.e. ~0.3 mg/kg) to fasted or fed monkeys in a cross-over design[1]. |
产品描述 | Basimglurant (RG7090) is a potent, selective and orally available mGlu5 negative allosteric modulator with a Kd of 1.1 nM. [3H]-basimglurant saturation analysis on recombinant human mGlu5 reveals monophasic saturation isotherms with Kd of 1.1 nM. 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 with an IC50 of 5.9 nM. Basimglurant (RG7090) shows similar potencies in radioligand binding and functional assay on human and rodent mGlu5 receptor orthologues[1]. Basimglurant (RG7090) is a potent, selective, and safe mGlu5 inhibitor with good oral bioavailability and long half-life supportive of once-daily administration, good brain penetration, and high in vivo potency. It has antidepressant properties which are corroborated by its functional magnetic imaging (fMRI) profile, as well as anxiolytic-like and antinociceptive features[1]. It is currently in phase II clinical studies for the treatment of depression and fragile X syndrome. In the Vogel conflict drinking test, Basimglurant dose dependently increases the drinking time. The total plasma exposure of efficacious doses of Basimglurant (RG7090) ranges from 5 ng/mL (0.03 mg/kg) to 37 ng/mL (0.3 mg/kg)[2]. References: |