CHEM 102 Lecture Notes - Lecture 5: Agonistic Behaviour, Methyl Group, Burimamide

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23 Aug 2016
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Pka in action the development of the drug cimetidine. The development of the anti-peptic ulcer drug cimetidine gives a fascinating insight into the important role of pka in chemistry. Peptic ulcers are a localized erosion of the mucous membrane, resulting from overproduction of gastric acid in the stomach. One of the compounds that controls the production of the acid is histamine. (histamine is also responsible for the symptoms of hay fever and allergies. ) Histamine works by binding into a receptor in the stomach lining and stimulating the production of acid. What the developers of cimetidine at smithkline beecham wanted was a drug that would bind to these receptors without activating them and thereby prevent histamine from binding but not stimulate acid secretion itself. Unfortunately, the antihistamine drugs successfully used in the treatment of hay fever did not work a different histamine receptor was involved. Notice that cimetidine and histamine both have an imidazole ring in their structure.