Mathematical analysis of the sodium sensitivity of the human histamine H3 receptor.

ABSTRACT:

Purpose

It was shown by several experimental studies that some G protein coupled receptors (GPCR) are sensitive to sodium ions. Furthermore, mutagenesis studies or the determination of crystal structures of the adenosine A2A or δ-opioid receptor revealed an allosteric Na(+) binding pocket near to the highly conserved Asp(2.50). Within a previous study, the influence of NaCl concentration onto the steady-state GTPase activity at the human histamine H3 receptor (hH3R) in presence of the endogenous histamine or the inverse agonist thioperamide was analyzed. The purpose of the present study was to examine and quantify the Na(+)-sensitivity of hH3R on a molecular level.

Methods

To achieve this, we developed a set of equations, describing constitutive activity and the different li

SUBMITTER: Wittmann HJ 

PROVIDER: S-EPMC4644138 | biostudies-literature | 2014 Dec

REPOSITORIES: biostudies-literature