6 Ranitidine and Other H2-Receptor Antagonists: Recent Developments

Abstract

Publisher Summary The first H2-receptor antagonists developed were based on a chemical similarity to histamine. The development of an antagonist, burimamide, allowed the definition of a second class of receptor, the H2-receptors. The main clinical indication for Hz-antagonists has been in the control of gastric acid secretion and the treatment of acid aggravated diseases of the upper gastrointestinal tract, such as duodenal ulcer, gastric ulcer and reflux oesophagitis. The need for an improved H2-receptor antagonist led to take a fresh look at the structural requirements for an action at H2-receptor sites. The chapter discusses the biological test systems suitable for assessing activity at H2-receptor sites. It has been primarily concerned with antagonists, but appropriate test systems for assessing new structures need to be able to respond to both agonists and antagonists. There are three main reasons for measuring activity at H2-receptor sites has been mentioned. The chapter has been primarily concerned with assessing new chemical structures both qualitatively and quantitatively in testing and developing the novel compounds described in this chapter.