Stereochemistry | ACHIRAL |
Molecular Formula | C18H20NO3PS |
Molecular Weight | 361.395 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCOP(=O)(CC1=CC=C(C=C1)C2=NC3=CC=CC=C3S2)OCC
InChI
InChIKey=FVYRUSCZCWSFLT-UHFFFAOYSA-N
InChI=1S/C18H20NO3PS/c1-3-21-23(20,22-4-2)13-14-9-11-15(12-10-14)18-19-16-7-5-6-8-17(16)24-18/h5-12H,3-4,13H2,1-2H3
Molecular Formula | C18H20NO3PS |
Molecular Weight | 361.395 |
Charge | 0 |
Count |
MOL RATIO
1 MOL RATIO (average) |
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Fostedil (KB-944) is a phosphonic acid derivative with potent vasodilator activity. KB-944 has been demonstrated to produce long lasting coronary vasodilator and hypotensive effects in conscious and anesthetized dogs; increase coronary blood flow in isolated, blood perfused heart preparations of dogs; and reduce systemic pressure in conscious normotensive and hypertensive rats. Slow channel calcium entry blockade is thought to contribute to the vasodilator activity of KB-944. Fostedil is longer acting in hypertensive animals than either nifedipine or diltiazem suggesting a potential clinical advantage for this compound. Unexpectedly, fostedil was shown to produce atrial fibrillation in 3 of 10 hypertensive patients in a placebo controlled study. Fostedil had been in phase II clinical trials for the treatment of angina pectoris. However, this research has been discontinued.
Originator
Approval Year
Doses
AEs
Sourcing
PubMed
Patents
Sample Use Guides
Fostedil (10(-5)-10(-4) M) decreased the action potential duration measured at 30% repolarization and hyperpolarized the resting membrane potential in ventricular trabeculae of the dog heart. In single ventricular cells of the guinea-pig heart, Fostedil (10(-4) M) abolished the slow inward current and produced an outward shift of the late current measured at the end of 200 msec clamp pulse.