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No evidence for functional selectivity of proxyfan at the human histamine H3 receptor coupled to defined Gi/Go protein heterotrimers.

Schnell, David ; Burleigh, Katrina ; Seifert, Roland ; Trick, Jonathan



Abstract

Numerous structurally diverse ligands were developed to target the human histamine H-3 receptor (hH(3)R), a presynaptic G(i)/G(o)-coupled auto- and heteroreceptor. Proxyfan was identified to be functionally selective, with different efficacies toward G(i)/G(o) dependent hH(3)R signaling pathways. However, the underlying molecular mechanism of functional selectivity of proxyfan is still unclear. ...

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