An analysis of the ß-adrenergic action of Oxyfedrine (cas 15687-41-9)

Add time:09/02/2019    Source:sciencedirect.com

1-3-methoxy-ω-(1-hydroxy-1-phenylisopropylamino)-propiophenone hydrochloride (oxyfedrine) (10−8–10−6 g/ml) produces a positive inotropic effect on electrically driven guinea-pig left atria which is prevented by propranolol; higher concentrations depress contractile force. Oxyfedrine (10−8–10−6 g/ml) effectively antagonizes the action of isoprenaline but not that of theophylline ethylenediamine. Oxyfedrine (10−5 g/ml)-induced relaxation of the guinea-pig tracheal chain is not reversed by repeated washing but is antagonized by propranolol (10−7 g/ml). The relaxed tracheal chain contracts when an additional dose of oxyfedrine (10−5 g/ml) or quinidine (10−5 g/ml) was administered. The oxyfedrine-induced contraction is relaxed by papaverine (5 × 10−6 g/ml), theophylline ethylene-diamine (10−5 g/ml) or adenosine (5 × 10−5 g/ml) but not by isoprenaline (2 × 10−8 g/ml) or adrenaline (10−7 g/ml) nor is it prevented by dibenamine (10−5 g/ml), methysergide (10−6 g/ml), atropine (10−5 g/ml) or tripelennamine (10−7 g/ml). These observations suggest that oxyfedrine interacts with the ß-adrenergic receptor, inducing at adequate concentrations, stimulation and blockade to catecholamines simultaneously; in this interaction, higher concentrations of oxyfedrine produces a direct depression (quinidine-like) of cardiac muscle and a contraction of tracheal muscle.

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