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Histamine H2-antagonists--past, present and future.

R T Brittain, D Jack

Journal of Clinical Gastroenterology

|January 1, 1983

Summary

The discovery of burimamide, the first histamine H2-antagonist, paved the way for cimetidine and other advanced H2-blockers like ranitidine. Further research introduced long-acting H2-blockers, such as AH 23844, with unique blocking properties.

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Area of Science:

Pharmacology
Gastroenterology
Medicinal Chemistry

Background:

Histamine H2-receptors play a crucial role in regulating gastric acid secretion.
Acid-aggravated diseases of the alimentary tract represent a significant medical challenge.

Purpose of the Study:

To review the development and significance of histamine H2-antagonists.
To highlight the pharmacological advancements from early H2-antagonists to newer agents.

Main Methods:

Selective review of scientific literature on histamine H2-antagonists.
Discussion of key compounds including burimamide, cimetidine, ranitidine, and AH 23844.
Explanation of physicochemical properties underlying drug action.

Main Results:

Burimamide was the first specific H2-antagonist, leading to the development of cimetidine for acid-related disorders.
Cimetidine's success spurred the creation of more potent and selective agents like ranitidine.
Newer H2-blockers, exemplified by AH 23844, demonstrate prolonged activity and unique blocking mechanisms.

Conclusions:

The evolution of histamine H2-antagonists has significantly improved the treatment of acid-aggravated gastrointestinal diseases.
Understanding the physicochemical basis of H2-blocker action is key to developing more effective therapies.

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