Radioligands used previously for histamine H3 receptor (H3R) are accompanied by a
number of disadvantages. In this study, we report the synthesis of the new H3R radioligand …

Currently employed histamine H2 receptor (H2R) radioligands possess several drawbacks,
for example, high non-specificity, insurmountable binding, or short half-life. We report the …

Since the discovery of the histamine H2 receptor (H2R), radioligands were among the most
powerful tools to investigate its role and function. Initially, radiolabeling was used to …

Differences in sequence homology between human (h), mouse (m), and rat (r) histamine H4
receptors (H4R) cause discrepancies regarding affinities, potencies, and/or efficacies of …

Histamine mediates its various functions through four histamine receptor subtypes. The H3
subtype is mainly found in the central nervous system, where it modulates the release of …

The H₂R is one of four receptor subtypes which mediate the action of the biogenic amine
histamine. However, the (patho-) physical role of the H₂R, especially in the brain, is still far …

Selective radioligands for histamine H3 receptors have been used to characterize H3
receptor pharmacology by radioligand binding assays and to determine H3 receptor …

Publisher Summary This chapter discusses the synthesis of radioligands for the histamine H
3 receptor. Radiolabelled receptor ligands are of great importance for studying receptor …

A-349821 is a selective histamine H 3 receptor antagonist/inverse agonist. Herein, binding
of the novel non-imidazole H 3 receptor radioligand [3 H] A-349821 to membranes …

Radioligands are powerful tools for examining the pharmacological profiles of chemical
leads and thus facilitate drug discovery. In this study, we identified and characterized 3-([1 …