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Labetalol-d5 is intended for use as an internal standard for the quantification of labetalol (Item No. 20249) by GC- or LC-MS. Labetalol is an adrenergic receptor (AR) antagonist.1 It inhibits agonist-induced contraction of rabbit aortic strips, decreases in contractile force in isolated guinea pig atria, and vasorelaxation in isolated guinea pig tracheal strips (pA2s = 6.99, 7.68, and 7.54, respectively), tissues that endogenously express high levels of α-, β1-, and β2-ARs, respectively. Labetalol (2.5-25 mg/kg) reduces blood pressure in spontaneously hypertensive rats. It reduces blood pressure in DOC-salt rats, two-kidney Goldblatt rats, and one-kidney dogs. Labetalol (5 mg/kg) reduces infarct size in a dog model of myocardial infarction induced by occlusion of the left anterior descending artery. Topical administration of labetalol (0.25-1% v/v) reduces intraocular pressure in rabbits. Formulations containing labetalol have been used in the treatment of hypertension.
WARNING This product is not for human or veterinary use.
1. Pharmacology of labetalol in experimental animals. Am. J. Med. 75(4A), 15-23 (1983).