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  • Title: Re-examination of [3H]mepyramine binding assay for histamine H1 receptor using quinine.
    Author: Liu YQ, Horio Y, Mizuguchi H, Fujimoto K, Imamura I, Abe Y, Fukui H.
    Journal: Biochem Biophys Res Commun; 1992 Nov 30; 189(1):378-84. PubMed ID: 1449491.
    Abstract:
    [3H]Mepyramine, a potent antagonist of the histamine H1 receptor, has been widely used as a radioligand binding assay for the H1 receptor. Previously, we purified a mepyramine binding protein (MBP) from rat liver, but found that its partial amino acid sequences were very similar to those of debrisoquine 4-hydroxylase isozymes (P450 db1 and db2), which are members of the superfamily of cytochrome P450. Using cloned histamine H1 receptor cDNA, we found that [3H]mepyramine could bind only the H1 receptor and did not bind MBP in the presence of 10(-5) M quinine, an inhibitor of debrisoquine 4-hydroxylase isozymes. We developed a method to determine the contents of the H1 receptor and MBP separately using [3H]mepyramine and quinine and found that MBP is abundant in certain areas of bovine brain.
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