Vipadenant

Vipadenant is an adenosine receptor antagonist, with Kis of 1.3 nM and 68 nM for A2A and A1, respectively.

Signaling Pathways >> GPCR/G Protein >> Adenosine Receptor

Research Areas >> Neurological Disease

Ki: 1.3 nM (A2A), 68 nM (A1)[1], 1005 nM (A3)[2]

Vipadenant (0.3-30 mg/kg) produces a dose-dependent reduction in catalepsy. Vipadenant (10 mg/kg) does not produce any statistically significant dyskinetic episodes in 6-OHDA-lesioned rats during a 19-day dosing regimen[1]. In the mouse and rat haloperidol-induced hypolocomotion models, vipadenant has a minimum effective dose of 0.1 and 1 mg/kg, respectively. Vipadenant (3 and 10 mg/kg, p.o.) is able to increase contralateral rotations in 6-OHDA lesioned rats[2].

[1]. Jones N, et al. A2A receptor antagonists do not induce dyskinesias in drug-naive or L-dopa sensitized rats. Brain Res Bull. 2013 Sep;98:163-9.

[2]. Brian C. Shook, et al. Adenosine A2A Receptor Antagonists and Parkinson’s Disease. ACS Chem Neurosci. 2011 Oct 19; 2(10): 555-567.

CGS 21680 hydrochloride | Preladenant | ZM 241385 | CPI-444 | SCH 58261 | Istradefylline | Tozadenant | AZD-4635 | Capadenoson | 2-CL-IB-MECA | PSB-12379 | CD73-IN-1 | IB-MECA | Diprophylline | Doxofylline