340021-17-2

340021-17-2 structure

Name: Tonapofylline
Chemical Name: Tonapofylline
CAS Number: 340021-17-2
Molecular Formula: C₂₂H₃₂N₄O₄
Molecular Weight: 416.51400
Catalog: Signaling Pathways GPCR/G Protein Adenosine Receptor
Create Date: 2016-02-14 00:45:17
Modify Date: 2024-01-10 09:02:31
Tonapofylline (BG 9928) is an orally active and selective adenosine A1 receptor antagonist with a Ki of 7.4 nM for human adenosine A1 receptor (hA1), which displays 915-fold selectivity versus human adenosine A2A receptor and 12-fold selectivity versus human adenosine A2B receptor and is used in development for the treatment of heart failure[1][2].

Name	Tonapofylline
Synonyms	3-[4-(2,6-dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1H-purin-8-yl)-bicyclo[2.2.2]oct-1-yl]-proprionic acid 4-(2,3,6,7-TETRAHYDRO-2,6-DIOXO-1,3-DIPROPYL-1H-PURIN-8-YL)-BICYCLO[2.2.2]OCTANE-1-PROPANOIC ACID 3-[4-(2,6-dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1H-purin-8-yl)-bicyclo[2.2.2]oct-1-yl]-propionic acid

Description	Tonapofylline (BG 9928) is an orally active and selective adenosine A1 receptor antagonist with a Ki of 7.4 nM for human adenosine A1 receptor (hA1), which displays 915-fold selectivity versus human adenosine A2A receptor and 12-fold selectivity versus human adenosine A2B receptor and is used in development for the treatment of heart failure[1][2].
Related Catalog	Research Areas >> Cardiovascular Disease Research Areas >> Metabolic Disease Signaling Pathways >> GPCR/G Protein >> Adenosine Receptor
Target	Ki: 7.4 nM (Human adenosine A1 receptor)[1]
References	[1]. Kiesman WF, et al. Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists. J Med Chem. 2006 Nov 30;49(24):7119-31. [2]. Ensor CR, et al. Tonapofylline: a selective adenosine-1 receptor antagonist for the treatment of heart failure. Expert Opin Pharmacother. 2010 Oct;11(14):2405-15.