同义名 :	BAY 68-4986
	CAS号 :	544417-40-5
	货号 :	A146488
	分子式 :	C25H18ClN5O2S2
	纯度 :	99%+
	分子量 :	520.03
	MDL号 :	MFCD09954113
	存储条件：	Pure form Keep in dark place, inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性
描述	Adenosine receptor plays important roles in the fertilization process, kidney function and ethanol intoxication as well as angina and heart failure, thus becoming a promising target in clinic. Capadenoson is a selective agonist of adenosine receptor showing Ki of 4.2 nM when binding on rat cortical brain membranes. Capadenoson could also decrease neurotransmitter norepinephrine (NE) releasing at very low concentration. At a concentration of 0.15 mg/kg, capadenoson treatment led to 15% increasing in heart rate during stress[1]. In another investigation, sixty-two male patients with stable angina were studied and treated with capadenoson at oral doses of 1, 2.5, 5, 10 and 20 mg respectively and placebo group was settled as the control. In 10 mg group heart rate was reduced by 12.2 bpm which was 6.8 bpm in 20 mg group in the primary efficacy analysis. Mean HR reduction after dosing for 24 h were 9.9 and 10.3 bpm for 10 mg and 20 mg respectively. In terms of safety, 32% of these patients had suffered at least one adverse events (AE), which was 36%, 30%, 20% and 30% in the control, the 5 mg, 10 mg and 20 mg respevtively, suggesting the 10 mg dose could be the best concentration to reduce heart rate in clinic[2][3].
作用机制	Capadenoson binding to the adenosine-A1 receptor that can inhibit adenylcyclase and decrease cAMP production by activating A1-coupled Gi protein[3] .

临床研究
NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00568945	Atrial Fibrillation	Phase 2	Completed	-	Germany ... 展开 >> Erfurt, Thüringen, Germany, 99084 收起 <<
NCT00518921	Chronic Stable Angina	Phase 2	Withdrawn	November 2008	Czech Republic ... 展开 >> Brno, Czech Republic, 656 91 Hodonin, Czech Republic, 695 26 Kromeriz, Czech Republic, 767 55 Olomouc, Czech Republic, 775 20 Ostrava, Czech Republic, 708 52 Plzen, Czech Republic, 30599 Praha 13, Czech Republic, 158 00 Praha 6, Czech Republic, 169 02 Hungary Balatonfured, Hungary, 8230 Kecskemet, Hungary, 6000 Miskolc, Hungary, 3526 Pecs, Hungary, 7624 Zalaegerszeg, Hungary, 8900 Israel Hadera, Israel, 38100 Rehovot, Israel, 76100 Safed, Israel, 13100 Italy Mestre, Venezia, Italy, 30174 Genova, Italy, 16132 Pavia, Italy, 27100 Trieste, Italy, 34100 Poland Bialystok, Poland, 15-276 Gdansk, Poland, 80-952 Gdynia, Poland, 81-519 Katowice, Poland, 40-635 Krakow, Poland, 30-501 Legnica, Poland, 59-220 Lodz, Poland, 91-347 Starogard Gdanski, Poland, 83-200 Szczecin, Poland, 70-111 Warszawa, Poland, 03-401 Wroclaw, Poland, 50-420 Wroclaw, Poland, 50-981 Slovakia Bratislava, Slovakia, 811 04 Bratislava, Slovakia, 813 69 Nitra, Slovakia, 949 01 Nove Zamky, Slovakia, 940 34 收起 <<

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	1.92mL 0.38mL 0.19mL	9.61mL 1.92mL 0.96mL	19.23mL 3.85mL 1.92mL

参考文献

[1]Bott-Flügel L, Bernshausen A, et al. Selective attenuation of norepinephrine release and stress-induced heart rate increase by partial adenosine A1 agonism. PLoS One. 2011;6(3):e18048. [2]Elzein E, Zablocki J. A1 adenosine receptor agonists and their potential therapeutic applications. Expert Opin Investig Drugs. 2008;17(12):1901-10. [3]Tendera M, Bernshausen A, et al. The new oral adenosine A1 receptor agonist capadenoson in male patients with stable angina. Clin Res Cardiol. 2012 Jul;101(7):585-91. [4]Albrecht-Küpper BE, Leineweber K, et al. Partial adenosine A1 receptor agonists for cardiovascular therapies. Purinergic Signal. 2012 Feb;8(Suppl 1):91-9. [5]Bailey IR, Laughlin B, et al. Optimization of Thermolytic Response to A1 Adenosine Receptor Agonists in Rats. J Pharmacol Exp Ther. 2017 Sep;362(3):424-430. [6]Meibom D, Albrecht-Küpper B, et al. Neladenoson Bialanate Hydrochloride: A Prodrug of a Partial Adenosine A1 Receptor Agonist for the Chronic Treatment of Heart Diseases. ChemMedChem. 2017 May 22;12(10):728-737.