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Biomedical subjects

S Fénard

Publications and source records attributed to S Fénard.

13 recordsLinked to original sources
PubMed1992

Efficacy and safety of the novel Na+,K(+)-ATPase inhibitor 20R 14 beta-amino 3 beta-rhamnosyl 5 beta-pregnan 20 beta-ol in a dog model of heart failure.

20R 14 beta-amino 3 beta-rhamnosyl 5 beta-pregnan 20 beta-ol (LND 623, CAS 90520-42-6) was investigated and compared to digoxin in anesthetized dogs. The hemodynamic profiles showed: a) a pure positive inotropic action of LND-623; b) its potency was four-fold higher than that of digoxin and more marked in heart failure; c) its duration of action was maintained for at least 6 h. The onset and reversal of the inotropic effects of a single dose (3.3 nmol.kg-1.min-1) were faster with LND-623 than those of digoxin. This reversal is consistent with the faster dissociation profile observed at the level of the high affinity cardiac Na+,K(+)-ATPase receptor form. The advantage of LND-623 over digoxin resides in its larger therapeutic index (ratio of arrhythmogenic to inotropic responses) in anesthetized dogs with propranolol-induced heart failure. This index was 6 for LND-623 and 2 for digoxin.

Anesthesia↗
PubMed1991

Tissue localization of active Na,K-ATPase isoenzymes by determination of their profile of inhibition with ouabain, digoxin, digitoxigenin and LND 796, a new aminosteroid cardiotonic.

Recently, Na,K-ATPase isoforms with differential affinities for digitalis have been identified that may contribute to different toxicity profiles. Our objectives were to localize them and to define tissue receptor patterns by examining the effect of different glycosides on the Na,K-ATPase activity. The digitalis derivatives used exhibit variation in lipophilicity and rate of enzyme inhibition. Membrane fractions enriched in Na,K-ATPase were prepared from canine heart, brain, aorta and peripheral nerves. The inhibition of enzyme activities indicates a pattern of differential sensitivities with IC50 values starting from 3 nM in heart and 30 nM in brain. Therefore, high and low affinity active forms of the Na,K-ATPase enzyme coexist in these tissues. The data also suggest the existence of two Na,K-ATPase isoforms in aorta and peripheral nerves as identified by the action of digitoxigenin and LND 796 where the predominant expression is that of a high affinity form. The comparison of the patterns of digitalis sensitivities in these different tissues, suggests a more complex molecular interaction than that which can be explained by the presence of only two forms.

Animals↗
PubMed1977

Vascular beta-adrenoceptor stimulating properties of phenylephrine.

In pithed rats pretreated with propranolol changes occurred in the slopes of dose--pressor response curves to i.v. phenylephrine and noradrenaline but not to LD 3098, a pure alpha-adrenoceptor stimulant. In dogs, cats, and spontaneously hypertensive rats pretreated with an alpha-adrenoceptor blocker, i.v. phenylephrine induced vasodilatory responses which were antagonised by propranolol. These results indicate that phenylephrine, in addition to its known beta1-agonistic properties, stimulates the vascular beta2-adrenoceptors.

Adrenergic beta-Agonists↗