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108852-42-2

108852-42-2 structure
108852-42-2 structure
  • Name: YS-201
  • Chemical Name: 3-O-ethyl 5-O-(2-piperidin-1-ylethyl) 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
  • CAS Number: 108852-42-2
  • Molecular Formula: C24H31N3O6
  • Molecular Weight: 457.51900
  • Catalog: Signaling Pathways Membrane Transporter/Ion Channel Calcium Channel
  • Create Date: 2017-11-21 03:08:11
  • Modify Date: 2025-08-25 21:46:21
  • YS-201 is a dihydropyridine-type calcium channel antagonist previously in clinical trials for the treatment of angina pectoris and hypertension.
Name 3-O-ethyl 5-O-(2-piperidin-1-ylethyl) 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
Synonyms Epddnp
YS 201
YS-201
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

[1]. Di Donato M, et al. Acute hemodynamic effects of intravenous diperdipine, a new dihydropyridine derivative, in coronary heart disease. Am Heart J. 1991 Mar;121(3 Pt 1):776-81.

[2]. Greiner PO, et al. Evaluation of first pass effect and biliary excretion of diperdipine in the dog. Eur J Drug Metab Pharmacokinet. 1990 Jul-Sep;15(3):185-90.

[3]. Herzog R, et al. Experimental studies on the toxicity of diperdipine following oral and parenteral application. Arzneimittelforschung. 1995 Mar;45(3):240-5.
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℃
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