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A study of antagonist affinities for the human histamine H2 receptor

✍ Scribed by J G Baker

Book ID
110009898
Publisher
Nature Publishing Group
Year
2009
Tongue
English
Weight
271 KB
Volume
153
Category
Article
ISSN
0007-1188

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The requirements for H -antagonist activity so far identified for most of 2 the known antagonists of histamine are the presence of a heterocyclic ring containing a basic center linked via a methylene chain to a substituted guanidine or thiourea polar Ε½ . side chain. Metiamide is a potent H antagonis

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## Background The H3 histamine receptor is a Gi-coupled GPCR that has been proven to exist in different agonist-induced states, including that defined by the protean agonist proxyfan. Several GPCRs are now known to exist in different states. For some of these, antagonist affinity measurement remain