| Stereochemistry | ABSOLUTE |
| Molecular Formula | C18H24N4O3 |
| Molecular Weight | 344.4082 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 5 / 5 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CCCN1C2=C(NC(=N2)[C@H]3C[C@H]4C[C@@H]3[C@@H]5O[C@H]45)C(=O)N(CCC)C1=O
InChI
InChIKey=OQCJPFYWFGUHIN-GJKBLCTNSA-N
InChI=1S/C18H24N4O3/c1-3-5-21-16-12(17(23)22(6-4-2)18(21)24)19-15(20-16)11-8-9-7-10(11)14-13(9)25-14/h9-11,13-14H,3-8H2,1-2H3,(H,19,20)/t9-,10+,11+,13-,14+/m1/s1
| Molecular Formula | C18H24N4O3 |
| Molecular Weight | 344.4082 |
| Charge | 0 |
| Count |
MOL RATIO
1 MOL RATIO (average) |
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 5 / 5 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Naxifylline [CVT 124, BG 9719], a small molecule diuretic, is one of a new class of potent and highly selective adenosine A1 receptor antagonists discovered at University of Florida. Naxifylline is an A1 adenosine receptor antagonist used for the treatment of edema associated with congestive heart failure. Naxifylline appears to be one of the more potent and clearly the most A1-selective antagonist reported to date, with K1 values of 0.67 and 0.45 nM, respectively, at the rat and cloned human A1-receptors and with 1800-fold (rat) and 2400-fold (human) subtype selectivity. Naxifylline protects against the decline in renal function observed with diuretic therapy by promoting urine output.
Approval Year
PubMed
Patents
Sample Use Guides
Rats: Thereafter, rats of group 1 received a bolus injection of vehicle (Veh; 0.3 ml of a 3% solution of polyethylene glycol-400 plus 2% ethanol in 0.154 M NaCl solution), followed, at 30-min intervals, by CVT-124 at 0.1, 0.3, 0.5, and 1 mg/kg. Rats of group 2 received intravenous bolus injections of 0.3 ml of the CVT-124 vehicle, following the same course as for group 1. CVT-124 (0.1 to 1 mg/kg) caused dose-dependent increases in urine flow and fractional and absolute sodium excretion of by six- to 10-fold and, at 0.1 mg/kg, increased the GFR.
Route of Administration:
Intravenous
