SLV 320 - CAS 251945-92-3
Category: Inhibitor
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Adenosine Receptor
SLV 320 is a potent and selective adenosine A1 receptor antagonist (Ki = 1, 200, 398 and 3981 nM at human A1, A3, A2A and A2B receptors, respectively). SLV320 prevents nephrectomy-dependent rise in plasma levels of creatinine kinase (CK), ALT and AST. SLV 320 inhibits cardiac fibrosis and attenuates albuminuria, without affecting blood pressure in animal models of chronic renal failure.
Brife Description:
adenosine A1 receptor antagonist
≥99% by HPLC
SLV320; SLV-320; SLV 320; Derenofylline; trans-4-[(2-Phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclohexanol
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1.Cardio-renal effects of the A1 adenosine receptor antagonist SLV320 in patients with heart failure.
Mitrovic V;Seferovic P;Dodic S;Krotin M;Neskovic A;Dickstein K;de Voogd H;Böcker C;Ziegler D;Godes M;Nakov R;Essers H;Verboom C;Hocher B Circ Heart Fail. 2009 Nov;2(6):523-31. doi: 10.1161/CIRCHEARTFAILURE.108.798389. Epub 2009 Sep 24.
BACKGROUND: ;Blocking the tubuloglomerular feedback mechanism with adenosine A1 receptor antagonists seems to improve diuresis and sodium excretion without compromising the glomerular filtration rate in patients with heart failure. However, the direct cardiac effects of this compound class have not been investigated to date.;METHODS AND RESULTS: ;In total, 111 patients (109 men and 2 women) received a 1-hour infusion of 5, 10, and 15 mg SLV320, an adenosine A1 receptor antagonist, placebo, or 40 mg furosemide. Mean age was 57.9 years, mean ejection fraction was 28.1%, 82 patients were of New York Heart Association class II, and 29 patients were of New York Heart Association class III. Hemodynamic parameters (heart rate, blood pressure, pulmonary capillary wedge pressure, mean pulmonary arterial pressure, systemic vascular resistance, right atrial pressure, and cardiac output) were determined. Kidney function was assessed by cystatin C measurements and by analysis of urine output and urine electrolytes. In addition, pharmacokinetics of SLV320 and ex vivo inhibition of adenosine A1 receptor activity were performed. SLV320 was well tolerated, and no serious adverse events were observed.
2.A1 adenosine receptor antagonists, agonists, and allosteric enhancers.
Kiesman WF;Elzein E;Zablocki J Handb Exp Pharmacol. 2009;(193):25-58. doi: 10.1007/978-3-540-89615-9_2.
Intense efforts of many pharmaceutical companies and academicians in the A(1) adenosine receptor (AR) field have led to the discovery of clinical candidates that are antagonists, agonists, and allosteric enhancers. The A(1)AR antagonists currently in clinical development are KW3902, BG9928, and SLV320. All three have high affinity for the human (h) A(1)AR subtype (hA(1) K (i) < 10 nM), > 200-fold selectivity over the hA(2A) subtype, and demonstrate renal protective effects in multiple animal models of disease and pharmacologic effects in human subjects. In the A(1)AR agonist area, clinical candidates have been discovered for the following conditions: atrial arrhythmias (tecadenoson, selodenoson and PJ-875); Type II diabetes and insulin sensitizing agents (GR79236, ARA, RPR-749, and CVT-3619); and angina (BAY 68-4986). The challenges associated with the development of any A(1)AR agonist are to obtain tissue-specific effects but avoid off-target tissue side effects and A(1)AR desensitization leading to tachyphylaxis. For the IV antiarrhythmic agents that act as ventricular rate control agents, a selective response can be accomplished by careful IV dosing paradigms. The treatment of type II diabetes using A(1)AR agonists in the clinic has met with limited success due to cardiovascular side effects and a well-defined desensitization of full agonists in human trials (GR79236, ARA, and RPR 749).
3.Rationale, design, and results from RENO-DEFEND 1: a randomized, dose-finding study of the selective A1 adenosine antagonist SLV320 in patients hospitalized with acute heart failure.
Pang PS;Mehra M;Maggioni AP;Filippatos G;Middlebrooks J;Turlapaty P;Kazei D;Gheorghiade M;RENO-DEFEND Investigators Am Heart J. 2011 Jun;161(6):1012-23.e3. doi: 10.1016/j.ahj.2011.03.004.
BACKGROUND: ;Baseline renal impairment as well as worsening renal function during hospitalization is associated with worse short- and long-term outcomes in patients hospitalized for acute heart failure (AHF). We hypothesized that selective A1 adenosine receptor blockade would induce natriuresis while preserving renal function in AHF patients with renal dysfunction.;METHODS: ;A phase II, randomized, double-blind, placebo-controlled, parallel group, multicenter study to evaluate the efficacy and safety of 2.5, 7.5, 15, and 30 mg/d SLV320 (1 hour intravenous infusions of 1.25, 3.75, 7.5, and 15 mg SLV320, every 12 hours for 3 days [a total of 6 doses] in addition to standard therapy) in subjects hospitalized with AHF and renal impairment who meet all inclusion/exclusion criteria. The study planned to enroll 450 subjects, with 90 subjects allocated equally to each treatment arm.;RESULTS: ;The study was terminated early. The decision, which was unrelated to the study conduct or results, with a total of 46 subjects randomized. Of those randomized, 6:8:8:8 and 6 patients, respectively, completed the study in each of the dosing subgroups, with placebo as the fifth group. For the 1.25-mg study group, the mean age was 73 years; mean (SD) systolic blood pressure (SBP), 128.
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CAS 251945-92-3 SLV 320

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