propranolol β‐adrenergic receptors affect a person's heart rate and vasoconstriction. Epinephrine (16) is an endogenous ligand for the β‐adrenergic receptors. When pharmaceuticals started researching β‐ adrenergic receptor antagonists as potential blood pressure therapies, epinephrine was a natural starting point.
The first β‐adrenergic receptor antagonist, called a β‐blocker, was dichloroisoprenaline (17). Dichloroisoprenaline was not sufficiently active in humans, but continued research in the field afforded propranolol (18), the first successful β‐blocker. Both dichloroisoprenaline and propranolol have obvious structural similarities to epinephrine.
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Published on May 6, 2014