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Rolofylline
- KW3902
- Soluble in DMSO
- MF: C20H28N4O2
- MW: 356.46
Description
Rolofylline (KW3902) is a potent and selective adenosine A1 receptor antagonist with reported Ki values of 0.19 nM for A1 and 170 nM for A2 receptors.
Adenosine A1 receptor blockade can influence renal blood flow, tubular sodium handling and cardiorenal signaling. Rolofylline is relevant for studying adenosine receptor selectivity, diuretic mechanisms and renal dysfunction in heart failure-related models.
Key Features
- Potent adenosine A1 receptor antagonist
- Reported Ki: 0.19 nM for A1 versus 170 nM for A2 receptors
- High selectivity for A1 receptor signaling
- Pharmacology relevant to renal and cardiorenal research
Applications
- Adenosine A1 receptor pharmacology
- Renal hemodynamic and diuretic studies
- Heart failure and cardiorenal model research
- GPCR antagonist selectivity assays
More Information
| Parent CAS No. | 136199-02-5 |
|---|---|
| Chemical Name | 8-(Hexahydro-2,5-methanopentalen-3a(1H)-yl)-3,7-dihydro-1,3-dipropyl-1H-purine-2,6-dione |
| SMILES | C1(C23CC4CC(C2)CC3C4)=NC2N(CCC)C(=O)N(CCC)C(=O)C=2N1 |
| MFCD | N.A. |
| InChi | InChI=1S/C20H28N4O2/c1-3-5-23-16-15(17(25)24(6-4-2)19(23)26)21-18(22-16)20-10-12-7-13(11-20)9-14(20)8-12/h12-14H,3-11H2,1-2H3,(H,21,22) |
| InChiKey | PJBFVWGQFLYWCB-UHFFFAOYSA-N |
| CID | 64627 |
| Short Description | A1 antagonist |
References
- H Nonaka et al. KW-3902, a selective high affinity antagonist for adenosine A1 receptors. Br J Pharmacol. 1996, 117(8), 1645–1652.
- MM Givertz et al. The effects of KW-3902, an adenosine A1-receptor antagonist, on diuresis and renal function in patients with acute decompensated heart failure and renal impairment or diuretic resistance. J. Am. Coll. Cardiol. 2007, 50(16), 1551–60.
- BM Massie et al. Rolofylline, an Adenosine A1−Receptor Antagonist, in Acute Heart Failure. N. Engl. J. Med. 2010, 363(15), 1419-28.
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