Capadenoson

Research use only, not for human use.

A selective agonist of adenosine-A1 receptor.

A selective agonist of adenosine-A1 receptor.(In Vitro):To further elucidate the pharmacological properties of Capadenson, GTP shift assays are performed with the standard full A1-agonist CCPA and the A1-antagonist 8-cyclopentyl-1,3-dipropylxanthine (DPCPX). CCPA shows a Ki?value of 4.2 nM in the binding assay on rat cortical brain membranes. In the presence of 1 mM GTP this Ki?value shifts to a value of 64 nM. Therefore the GTP shift for CCPA is 15. DPCPX shows a GTP shift of 1 with virtually identical Ki?values in the absence and presence of GTP. Capadenson shows a Ki?value of 24 nM in the binding assay. In the presence of 1 mM GTP this Ki?value shifts to a value of 116 nM resulting in a GTP shift of 5 for Capadenoson.(In Vivo):In the in vivo experiments, Wistar rats and SHR are pre-treated with Capadenoson at a concentration of 0.15 mg/kg for 5 days. On day 5, a stress test (physical restraint) is performed for 2 hours. The plasma concentration of Capadenoson measured 3 hours after drug intake remains constant in the 5 days prior to the restraint stress test and averaged 7.63 μg/L on day 4 and 5, respectively.

To further elucidate the pharmacological properties of Capadenson, GTP shift assays are performed with the standard full A1-agonist CCPA and the A1-antagonist 8-cyclopentyl-1,3-dipropylxanthine (DPCPX). CCPA shows a Ki value of 4.2 nM in the binding assay on rat cortical brain membranes. In the presence of 1 mM GTP this Ki value shifts to a value of 64 nM. Therefore the GTP shift for CCPA is 15. DPCPX shows a GTP shift of 1 with virtually identical Ki values in the absence and presence of GTP. Capadenson shows a Ki value of 24 nM in the binding assay. In the presence of 1 mM GTP this Ki value shifts to a value of 116 nM resulting in a GTP shift of 5 for Capadenoson.

In the in vivo experiments, Wistar rats and SHR are pre-treated with Capadenoson at a concentration of 0.15 mg/kg for 5 days. On day 5, a stress test (physical restraint) is performed for 2 hours. The plasma concentration of Capadenoson measured 3 hours after drug intake remains constant in the 5 days prior to the restraint stress test and averaged 7.63 μg/L on day 4 and 5, respectively.

BAY 68-4986

Apoptosis

Adenosine Receptor

Adenosine Receptor

Cardiovascular Disease

——

544417-40-5

520.0257

C25H18ClN5O2S2

>98% (HPLC)

10 mM in DMSO

N#CC1=C(C2=CC=C(OCCO)C=C2)C(C#N)=C(SCC3=CSC(C4=CC=C(Cl)C=C4)=N3)N=C1N

3,5-Pyridinedicarbonitrile, 2-amino-6-[[[2-(4-chlorophenyl)-4-thiazolyl]methyl]thio]-4-[4-(2-hydroxyethoxy)phenyl]-

(-20℃)

With Ice Pack

≥ 2 years