Chapter: Basic & Clinical Pharmacology : Histamine, Serotonin, & the Ergot Alkaloids

H2-Receptor Antagonists

The development of H2-receptor antagonists was based on the observation that H1 antagonists had no effect on histamine-induced acid secretion in the stomach.

H₂-RECEPTOR ANTAGONISTS

The development of H₂-receptor antagonists was based on the observation that H₁ antagonists had no effect on histamine-induced acid secretion in the stomach. Molecular manipulation of the histamine molecule resulted in drugs that blocked acid secretion and had no H₁ agonist or antagonist effects. Like the other hista-mine receptors, the H₂ receptor displays constitutive activity, and some H₂ blockers are inverse agonists.

The high prevalence of peptic ulcer disease created great interest in the therapeutic potential of the H₂-receptor antagonists when first discovered. Although these agents are not the most efficacious avail-able, their ability to reduce gastric acid secretion with very low toxicity has made them extremely popular as over-the-counter preparations.

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Basic & Clinical Pharmacology : Histamine, Serotonin, & the Ergot Alkaloids : H2-Receptor Antagonists |