5355. Landiolol

Nomenclature

CAS number: 133242-30-5
4-[(2S)-2-Hydroxy-3-[[2-[(4-morpholinylcarbonyl)amino]ethyl]amino]propoxy]benzenepropanoic acid [(4S)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl ester; ()-2,2-dimethyl-1,3-dioxolan-4S-ylmethyl 3-[4-[3-[2-(morpholinocarbonylamino)ethylamino]-2S-hydroxypropoxy]phenyl]propionate.
C25H39N3O8; mol wt 509.59.
C 58.92%, H 7.71%, N 8.25%, O 25.12%.

Description and references

Cardioselective β-adrenergic blocker. Prepn: S. Iguchi et al., EP 397031; US 5013734 (1990, 1991 both to Ono Pharm.); idem et al., Chem. Pharm. Bull. 40, 462 (1992). Electrophysiology: A. Sugiyama et al., J. Cardiovasc. Pharmacol. 34, 70 (1999). Clinical pharmacology: A. Kitamura et al., Eur. J. Clin. Pharmacol. 51, 467 (1997). Clinical pharmacokinetics in patients with cardiac tachyarrhythmias: H. Atarashi et al., Clin. Pharmacol. Ther. 68, 143 (2000).

Chemical structure

Derivative

Hydrochloride.

Nomenclature

CAS number: 144481-98-1
ONO-1101; Onoact (Ono).
C25H39N3O8.HCl; mol wt 546.05.
C 54.99%, H 7.38%, N 7.70%, O 23.44%, Cl 6.49%.

Properties

mp 125.4°. LD50 in mice (mg/kg): 290 i.v. (Iguchi).

Therapeutic Category

Antiarrhythmic.

Keywords

Antiarrhythmic; β-Adrenergic Blocker