10055. Xamoterol

Nomenclature

CAS number: 81801-12-9
N-[2-[[2-Hydroxy-3-(4-hydroxyphenoxy)propyl]amino]ethyl]-4-morpholinecarboxamide; 1-(4-hydroxyphenoxy)-3-[2-(4-morpholinocarboxamido)ethylamino]-2-propanol.
C16H25N3O5; mol wt 339.39.
C 56.62%, H 7.42%, N 12.38%, O 23.57%.

Description and references

β1-Adrenoceptor partial agonist. Prepn: BE 867376; B. G. Main, J. J. Barlow, US 4143140 (1978, 1979 both to ICI); prepn and adrenoceptor stimulant activity: J. J. Barlow et al., J. Med. Chem. 24, 315 (1981). Cardiovascular activity: A. Nuttall, H. M. Snow, Br. J. Pharmacol. 77, 381 (1982). Hemodynamics, cardioselectivity and kinetics: G. Jennings et al., Clin. Pharmacol. Ther. 35, 594 (1984). Hemodynamic effects: J.-M. R. Detry et al., Eur. Heart J. 4, 584 (1983); H. Sato et al., Circulation 75, 213 (1987). Metabolism: T. R. Marten et al., Drug Metab. Dispos. 12, 652 (1984). HPLC determn in biological fluids: C. J. Oddie et al., J. Chromatogr. 308, 370 (1984). Clinical evaluations: F. L. Tseu et al., Br. Heart J. 56, 469 (1986); L. Barrios et al., Eur. J. Clin. Pharmacol. 29, 667 (1986). Clinical comparison with atenolol, q.v., in asthmatic patients: J. W. J. Lammers et al., Br. J. Clin. Pharmacol. 22, 595 (1986).

Chemical structure

Derivative

Hemifumarate.

Nomenclature

CAS number: 73210-73-8
ICI-118587; Corwin (Zeneca).
(C16H25N3O5)2.C4H4O4; mol wt 794.85.
C 54.40%, H 6.85%, N 10.57%, O 28.18%.

Properties

Crystals from ethanol, mp 168-169° (dec).

Therapeutic Category

Cardiotonic.

Keywords

β-Adrenergic Agonist; Cardiotonic