Article
Generation and characterization of highly constitutive active histamine H3 receptors.
The Journal of pharmacology and experimental therapeutics - 1 Oct 2003
Takahashi Kazuhiko, Tokita Shigeru, Kotani Hidehito
Abstract excerpt
Constitutive activation of G-protein-coupled receptors is a well recognized phenomenon, and G-protein-coupled receptor antagonists have been found to possess inverse agonist activity. Constitutive activation of histamine H3 receptor is recently documented in in vivo as well as in recombinant receptor systems in vitro. Several H3 antagonists have been shown to act as inverse agonists and such profiles of H3...
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