YS-201
Names
Biological Activity
[Description]:
YS-201 is a dihydropyridine-type calcium channel antagonist previously in clinical trials for the treatment of angina pectoris and hypertension.
[Related Catalog]:
[In Vivo]
YS-201 (Diperdipine) markedly reduces systemic vascular resistance and improves stroke index and left ventricular ejection fraction. Mean pulmonary artery and wedge pressures are slightly increased as a possible consequence of enhanced venous return, whereas right atrial and left ventricular end-diastolic pressures are not significantly changed. Nevertheless, an increase in preload is clearly indicated by an augmented left ventricular end-diastolic volume index after administration of diperdipine[1]. After intravenous and oral doses, absolute bioavailability is calculated to be 18.7%. Biliaryexcretion accounts for about 0.1% of the total clearance of diperdipine and does not contribute to the overall elimination of the drug. After intraportal administration, the bioavailable fraction of diperdipine is increasing up to 44.3% suggesting a prehepatic site of loss of the drug[2]. The single application of diperdipine to mice and rats by gavage causes intolerance reactions starting at the lowest tested dose level of 200 mg/kg b.w. p.o. (mice) and at 250 mg/kg b.w. p.o. (rats). In the rat, toxic effects occur from 15 mg diperdipine/kg b.w./day p.o. onwards[3].
[References]
[Related Small Molecules]
Chemical & Physical Properties
[ Density]:
1.207g/cm3
[ Boiling Point ]:
593.9ºC at 760 mmHg
[ Molecular Formula ]:
C24H31N3O6
[ Molecular Weight ]:
457.51900
[ Flash Point ]:
313ºC
[ Exact Mass ]:
457.22100
[ PSA ]:
113.69000
[ LogP ]:
4.21170
[ Vapour Pressure ]:
4.47E-14mmHg at 25°C
[ Index of Refraction ]:
1.556
[ Storage condition ]:
2-8℃