diperdipine
diperdipine Basic information
- Product Name:
- diperdipine
- Synonyms:
-
- diperdipine
- YS-201
- 3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-, 3-ethyl 5-[2-(1-piperidinyl)ethyl] ester
- YS201,YS 201
- 3-Ethyl 5-(2-(piperidin-1-yl)ethyl) 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
- 3-Ethyl 5-(2-(piperidin-1-yl)ethyl) 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate , YS-201
- CAS:
- 108852-42-2
- MF:
- C24H31N3O6
- MW:
- 457.52
- Mol File:
- 108852-42-2.mol
diperdipine Chemical Properties
- Boiling point:
- 593.9±50.0 °C(Predicted)
- Density
- 1?+-.0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- Solid
- pka
- 8.29±0.10(Predicted)
- color
- Light yellow to yellow
diperdipine Usage And Synthesis
Uses
YS-201 is a dihydropyridine-type calcium channel antagonist. YS-201 has the potential for angina pectoris and hypertension treatment.
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. DOI:10.1016/0002-8703(91)90188-n
[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. DOI:10.1007/BF03190202
[3] Herzog R, et al. Experimental studies on the toxicity of diperdipine following oral and parenteral application. Arzneimittelforschung. 1995 Mar;45(3):240-5. PMID:7741776
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