Levosimendan CAS Registry Number: 141505-33-1 左西孟旦
CAS Name: [[4-[(4R)-1,4,5,6-Tetrahydro-4-methyl-6-oxo-3-pyridazinyl]phenyl]hydrazono]propanedinitrile
Additional Names: (-)-[p[(R)-1,4,5,6-tetrahydro-4-methyl-6-oxo-3-pyridazinyl]phenyl]hydrazone mesoxalonitrile; (R)-simendanTrademarks: Simdax (Orion)
Percent Composition: C 59.99%, H 4.32%, N 29.98%, O 5.71%
📌 参考资料/链接：
Literature References: Bioactive enantiomer of racemate, simendan. Positive inotropic agent with vasodilating activity. Binds to and sensitizes the myocardial contractile protein, troponin C, to calcium, thereby stabilizing the troponin conformation needed to trigger muscle contraction. Prepn: R. J. Backstrom et al., GB 2251615; P. Nore et al., US 5569657 (1992, 1996 both to Orion). Pharmacology: A. F. E. Rump et al., Pharmacol. Toxicol. 74, 244 (1994). Binding studies: P. Pollesello et al., J. Biol. Chem. 269, 28584 (1994). HPLC determn in plasma: M. Karlsson et al., Biomed. Chromatogr. 11, 54 (1997). Clinical pharmacokinetics: E.-P. Sandell et al., J. Cardiovasc. Pharmacol. 26, Suppl. 1, S57 (1995). Review of mechanism of action: H. Haikala, I.-B. Lindén, ibid., S10-S19 (1995); of pharmacology, toxicology and clinical evaluation: P. S. Pagel et al., Cardiovasc. Drug Rev. 14, 286-316 (1996). Comparison with dobutamine, q.v., in heart failure: F. Follath et al., Lancet 360, 196 (2002).
📄 详细内容
Properties: Yellow crystalline powder, mp 210-214°. [a]D25 -566° (tetrahydrofurane/methanol). Soluble in water. pKa 6.3. LD50 in male, female mice, male rats (mg/kg): 156, 152, 103 orally; 32, 50, 57 i.v. (Pagel).
Melting point: mp 210-214°
pKa: pKa 6.3
Optical Rotation: [a]D25 -566° (tetrahydrofurane/methanol)
Toxicity data: LD50 in male, female mice, male rats (mg/kg): 156, 152, 103 orally; 32, 50, 57 i.v. (Pagel)
Therap-Cat: Cardiotonic.
Keywords: Cardiotonic.
产品链接: 141505-33-1››