Chemistry:Tonapofylline
From HandWiki
Tonapofylline (BG-9928) is a drug which acts as a potent and selective antagonist for the adenosine A1 receptor. It was developed as a potential agent for the treatment of heart failure by increasing sodium excretion by the kidneys, and reached Phase III human clinical trials, showing reasonable efficacy with a good safety profile. However, it was ultimately not adopted for medical use, though it continues to be used in research.[1][2][3][4][5][6][7] Its activity as a phosphodiesterase inhibitor does not appear to have been tested, though most related xanthine derivatives are phosphodiesterase inhibitors as well as adenosine receptor antagonists.
See also
- DPCPX
References
- ↑ "Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists". Journal of Medicinal Chemistry 49 (24): 7119–7131. November 2006. doi:10.1021/jm0605381. PMID 17125264.
- ↑ "Effects of multiple oral doses of an A1 adenosine antagonist, BG9928, in patients with heart failure: results of a placebo-controlled, dose-escalation study". Journal of the American College of Cardiology 50 (7): 600–606. August 2007. doi:10.1016/j.jacc.2007.03.059. PMID 17692744.
- ↑ "Role of adenosine antagonism in the cardiorenal syndrome". Cardiovascular Therapeutics 26 (4): 276–286. 2008. doi:10.1111/j.1755-5922.2008.00059.x. PMID 19035879.
- ↑ "A1 Adenosine Receptor Antagonists, Agonists, and Allosteric Enhancers". Adenosine Receptors in Health and Disease. Handbook of Experimental Pharmacology. 193. 2009. pp. 25–58. doi:10.1007/978-3-540-89615-9_2. ISBN 978-3-540-89614-2.
- ↑ "Tonapofylline: a selective adenosine-1 receptor antagonist for the treatment of heart failure". Expert Opinion on Pharmacotherapy 11 (14): 2405–2415. October 2010. doi:10.1517/14656566.2010.514605. PMID 20807184.
- ↑ "Dual A1/A2B Receptor Blockade Improves Cardiac and Renal Outcomes in a Rat Model of Heart Failure with Preserved Ejection Fraction". The Journal of Pharmacology and Experimental Therapeutics 356 (2): 333–340. February 2016. doi:10.1124/jpet.115.228841. PMID 26585572.
- ↑ "Design and synthesis of novel, potent and selective hypoxanthine analogs as adenosine A1 receptor antagonists and their biological evaluation". Bioorganic & Medicinal Chemistry 25 (6): 1963–1975. March 2017. doi:10.1016/j.bmc.2017.02.029. PMID 28238512.
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