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Article

Asp73-dependent and -independent regulation of the affinity of ligands for human histamine H1 receptors by Na.

Biochemical pharmacology - 15 Mar 2017

Hishinuma Shigeru, Kosaka Kiyoe, Akatsu Chizuru, Uesawa Yoshihiro, Fukui Hiroyuki, Shoji Masaru

Abstract excerpt

The affinity of ligands for G-protein-coupled receptors (GPCRs) is allosterically regulated by Na+ via a highly conserved aspartate residue (Asp2.50) in the second transmembrane domain of GPCRs. In the present study, we examined the Na+-mediated regulation of the affinity of ligands for Gq/11-protein-coupled human histamine H1 receptors in Chinese hamster ovary cells. The affinities of 3 agonists and 20...

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Identifiers

PMID: 28040476
DOI: 10.1016/j.bcp.2016.12.021

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