Characterization of the adrenergic activity of carbuterol (SK&F 40383-A).

摘要: Carbuterol is a β-adrenergic bronchodilator with selectivity for bronchial smooth muscle relative to cardiac and vascular tissues of several species including man. The present studies were undertaken further characterize its adrenergic profile. In vitro demonstrated that carbuterol was direct acting agonist, not dependent on endogenous catecholamine release, devoid α-adrenergic agonist activity. activity the racemate shown reside primarily in l-enantiomer. inhibited immunologically induced release histamine slow reacting substance anaphylaxis from passively sensitized fragmented Rhesus monkey lung also passive cutaneous rats. relatively weak stimulant β1 receptors mediating both rate force contraction confirmed anesthetized open-chest dogs. cat, significantly less potent than isoproterenol decreasing diastolic blood pressure, increasing heart rate, tension degree fusionof incomplete tetanic soleus muscle.