Detail of "91094-14-3"

Reference

Comparisons of the inotropic effects of the b1-adrenoceptor partial agonists SL 75

Comparisons of the inotropic effects of the b1-adrenoceptor partial agonists SL 75.177.10 and ICI 118,587 with digoxin on the intact canine heart. Pouleur, H.; Van Mechelen, H.; Balasim, Habib; Rousseau, M. F.; Charlier, A. A. (Dep. Physiol., Univ. Louvain, Brussels, Belg.). J. Cardiovasc. Pharmacol., 6(4), 720-6 (English) 1984. CODEN: JCPCDT. ISSN: 0160-2446. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) The effects of the b1-adrenoceptor partial agonists ICI 118,587 (xamoterol)(I) [73210-73-8] and SL 75.177.10 (II) [91094-14-3] on the left ventricular inotropic state and relaxation rate were compared with those of digoxin in open-chest dogs. These agents were administered to 3 sep. groups of dogs (5, 6, and 7 dogs, resp.). In each animal, the inotropic effects were assessed at fixed heart rate (atrial pacing) and at similar end-diastolic left ventricular diam. Under these controlled conditions, ICI 118,587 (200 mg/kg) increased peak (+) dP/dt by 3176 mm Hg/s and the slope of the end-systolic pressure/end-systolic diam. relation rose by 190% above the control value. These changes were significantly greater than after digoxin (100 mg/kg) which increased these indexes, resp., by 2132 mm Hg/s and by 31%. SL 75.177.10 (200 mg/kg) also increased dP/dt, but significantly less than did digoxin or ICI 118,587 (+428 mm Hg/s); the increase in end-systolic pressure/diam. slope was not different from that obsd. after digoxin. In contrast to ICI 118,587 which accelerated isovolumic relaxation (-7.6 ms in time const. of isovolumic pressure fall), neither SL 75.177.10 nor digoxin modified this phase of the cardiac cycle. Finally, at the dose used in the study, digoxin induced ventricular arrhythmias in all animals, a side effect which was never obsd. after ICI 118,587 or SL 75.177.10. Thus, ICI 118,587 is a more powerful, pos. inotropic agent than digoxin; SL 75.177.10 appears weaker than the glycoside, although at clin. doses of digoxin, the difference might not be significant.