Abstract
TOLAZOLINE (2-benzyl-2-imidazoline), a peripheral vasodilator and adrenergic blocking agent used to treat peripheral vascular disease and (formerly) hypertension, has actions similar to those of histamine, including vasodilation, pressor responses in the rabbit and stimulation of intestinal smooth muscle, gastric secretion and the heart. The cardiac stimulation has usually been referred to as sympathomimetic. Tachycardia and gastrointestinal distress are prominent clinical side effects of tolazoline. It has been used in place of histamine as a diagnostic agent for gastric function1,2. The effects of tolazoline on gastric acid secretion and heart rate have, however, not been explained adequately in terms of mechanism or receptor theory. We have now been able to investigate this aspect using two specific H2-receptor antagonists3, burimamide and metiamide. Our results indicate that the actions of tolazoline on sinus rate and gastric acid secretion can be classified as H2-histaminergic. Recognition that tolazoline interacts with specific histamine receptors helps to explain why the drug has so many diverse actions affecting almost every organ in the body.
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YELLIN, T., SPEROW, J. & BUCK, S. Antagonism of tolazoline by histamine H2-receptor blockers. Nature 253, 561–563 (1975). https://doi.org/10.1038/253561a0
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DOI: https://doi.org/10.1038/253561a0
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