Name | 3-[(4-amino-3-methylphenyl)methyl]-7-(furan-2-yl)triazolo[4,5-d]pyrimidin-5-amine |
---|---|
Synonyms |
VER-ADO-49
VER-A00-11 Vipadenant V-2006 CEB-4520 UNII-LDR3USH1NJ |
Description | Vipadenant is an adenosine receptor antagonist, with Kis of 1.3 nM and 68 nM for A2A and A1, respectively. |
---|---|
Related Catalog | |
Target |
Ki: 1.3 nM (A2A), 68 nM (A1)[1], 1005 nM (A3)[2] |
In Vivo | 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]. |
References |
Molecular Formula | C16H15N7O |
---|---|
Molecular Weight | 321.33700 |
Exact Mass | 321.13400 |
PSA | 122.40000 |
LogP | 2.51370 |
Storage condition | 2-8℃ |
~91% 442908-10-3 |
Literature: BIOGEN IDEC MA INC.; VERNALIS RESEARCH LIMITED Patent: WO2008/86201 A1, 2008 ; Location in patent: Page/Page column 21 ; WO 2008/086201 A1 |
~% 442908-10-3 |
Literature: Gillespie, Roger J.; Bamford, Samantha J.; Botting, Ruth; Comer, Mike; Denny, Sarah; Gaur, Suneel; Griffin, Michael; Jordan, Allan M.; Knight, Anthony R.; Lerpiniere, Joanne; Leonardi, Stefania; Lightowler, Sean; McAteer, Steven; Merrett, Angela; Misra, Anil; Padfield, Antony; Reece, Mark; Saadi, Mona; Selwood, Daniel L.; Stratton, Gemma C.; Surry, Dominic; Todd, Richard; Tong, Xin; Ruston, Vicki; Upton, Rebecca; Weiss, Scott M. Journal of Medicinal Chemistry, 2009 , vol. 52, # 1 p. 33 - 47 |
Precursor 2 | |
---|---|
DownStream 0 |