Title |
Antagonist affinity measurements at the Gi-coupled human histamine H3 receptor expressed in CHO cells
|
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Published in |
BMC Pharmacology, June 2008
|
DOI | 10.1186/1471-2210-8-9 |
Pubmed ID | |
Authors |
Jillian G Baker |
Abstract |
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 constant regardless of the state of the receptor, for others e.g. the beta-adrenoceptors, the antagonist affinity measurements vary considerably depending on which agonist-dependent state is being identified. The purpose of this study was to examine the antagonist affinity measurements at the Gi-coupling human H3 receptor, paying particular attention to measurements made in the presence of full agonists, partial agonists and the proxyfan protean agonist-induced state of the receptor. |
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