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Development of a Conformational Histamine H3 Receptor Biosensor for the Synchronous Screening of Agonists and Inverse Agonists

Schihada, Hannes ; Ma, Xiaoyuan ; Zabel, Ulrike ; Vischer, Henry F. ; Schulte, Gunnar ; Leurs, Rob ; Pockes, Steffen ; Lohse, Martin J.


The histamine H-3 receptor (H3R) represents a highly attractive drug target for the treatment of various central nervous system disorders, but the discovery of novel H3R targeting compounds relies on the assessment of highly amplified intracellular signaling events that do not only reflect H3R modulation and carry the risk of high false-positive and -negative screening rates. To address these ...


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