Histamine H2-antagonists--past, present and future.
In this selective review of histamine H2-antagonists, we emphasize the significance of burimamide, the first specific H2-antagonist, in physiology and pharmacology and describe how its discovery led to the development of cimetidine as a new treatment of acid-aggravated disease of the alimentary tract. Developments since cimetidine, include ranitidine, which is a more potent, selectively acting H2-antagonist. A new series of H2-blockers with prolonged activity is discussed, and exemplified, particularly AH 23844. Its prolonged action and its unusual, apparently insurmountable, blocking action is explained in fundamental physicochemical terms.
D000818:Animals; D001241:Aspirin / Q000009:adverse effects; D002049:Burimamide / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D002927:Cimetidine / Q000494:pharmacology; D004285:Dogs; D005663:Furans / Q000494:pharmacology; D005744:Gastric Acid / Q000378:metabolism; D006146:Guanidines / Q000494:pharmacology; D006168:Guinea Pigs; D006207:Half-Life; D006635:Histamine H2 Antagonists / Q000378:metabolism / Q000494:pharmacology*; D006801:Humans; D007093:Imidazoles / Q000494:pharmacology; D008744:Methylamines / Q000494:pharmacology; D011899:Ranitidine / Q000494:pharmacology; D051381:Rats; D013270:Stomach / Q000187:drug effects; D013844:Thiazoles / Q000494:pharmacology; D014230:Triazoles / Q000494:pharmacology
D005663:Furans; D006146:Guanidines; D006635:Histamine H2 Antagonists; D007093:Imidazoles; D008744:Methylamines; D013844:Thiazoles; D014230:Triazoles; C039993:loxtidine; D002927:Cimetidine; D011899:Ranitidine; D001241:Aspirin; D002049:Burimamide