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A new receptor
The histamine molecule has a ringlike structure with a short side chain attached. Black's first
idea was to alter the ring by tacking on chemical groups. Although no antagonists were found, it
did produce an agonist called 4-methylhistamine, which stimulated acid secretion without any of the
other histamine responses. This proved the existence of a second receptor, thus establishing a clear
target for drug research. The project was then renamed the H2-receptor program. However, finding and synthesizing potential histamine antagonists turned out to be more difficult than
expected. By 1968, of the 200-odd compounds made, none had shown any activity in the assays. Fortunately,
Parsons recognized that modifying the assays would increase their sensitivity. The team then retested a
compound Durant had made earlier and found that it showed partial antagonism.
A new era of logical drug design |
Discovery of H2-receptor antagonists |
A new receptor
Success at last |
A better manufacturing process |
The people |
Landmark designation and acknowledgments
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