一个有效的、选择性的、具有口服活性的腺苷A1 受体的拮抗剂,其对腺苷A1、A3 和A2A 受体的 Ki 值分别为 1 nM、200 nM 和 398 nM。Derenofylline可抑制心肌纤维化,降低蛋白尿,且不影响大鼠血压。
Derenofylline, also known as SLV320, is a selective and potent adenosine A(1) antagonist in vitro (Ki=1 nM) with a selectivity factor of at least 200 versus other adenosine receptor subtypes. SLV320 significantly decreased albuminuria by about 50%, but did not alter glomerular filtration rate (GFR). SLV320 prevented nephrectomy-dependent rise in plasma levels of creatinine kinase (CK), ALT and AST. SLV320 suppresses cardiac fibrosis and attenuates albuminuria without affecting blood pressure in rats with 5/6 nephrectomy.