Biological Activity
Isoproterenol-d7 is intended for use as an internal standard for the quantification of isoproterenol by GC- or LC-MS. Isoproterenol is an agonist of β1- and β2-adrenergic receptors (β1- and β2-ARs; Kis = 224 and 458 nM, respectively).1 It is selective for β1- and β2-ARs over β3-ARs (Ki = 1,570 nM). Isoproterenol inhibits contractions in isolated field-stimulated rat vas deferens (EC50 = 45.6 nM).2 In vivo, isoproterenol (0.33 mg/kg) decreases blood pressure and increases water intake in nephrectomized rats.3 It reduces blood pressure and increases heart rate in renal hypertensive rabbits.4 Isoproterenol inhibits histamine-induced bronchospasms in anesthetized dogs.5 Formulations containing isoproterenol have been used in the treatment of bradydysrhythmias and to improve breathing during anesthesia.
References
1.Hoffmann, C., Leitz, M.R., Oberdorf-Maass, S., et al.Comparative pharmacology of human β-adrenergic receptor subtypes—characterization of stably transfected receptors in CHO cellsNaunyn Schmiedebergs Arch. Pharmacol.369(2)151-159(2004)
2.Lotti, V.J., Cerino, D., and Kling, P.Characterization of the adrenoreceptor activities of isoprenaline in the field stimulated rat vas deferens: Selective supersensitivity to β2-mediated responses following reserpine treatmentJ. Auton. Pharmacol.2(3)169-174(1982)
3.Hosutt, J.A., Rowland, N., and Stricker, E.M.Hypotension and thirst in rats after isoproterenol treatmentPhysiol. Behav.21(4)593-598(1978)
4.van Boom, M., and Saxena, P.R.Systemic and regional haemodynamic responses to isoprenaline in conscious renal hypertensive rabbitsClin. Exp. Pharmacol. Physiol.8(3)227-239(1981)
5.Wasserman, M.A., and Levy, B.Cardiovascular and bronchomotor responses to selective beta adrenergic receptor agonists in the anesthetized dogJ. Pharmacol. Exp. Ther.189(2)445-455(1974)
