High affinity histamine H3
receptor ligand (pKi
= 8.62) that acts as a protean agonist at recombinant and native receptors. In functional studies, activity ranges from full agonist to inverse agonist depending on system used. Displays partial agonist effects on cAMP inhibition and MAPK activity, neutral antagonist activity on histamine release and partial inverse agonism of [3
H]-arachidonic acid release.
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All Tocris products are intended for laboratory research use only.
The H3 receptor protean agonist proxyfan enhances the expression of fear memory in the rat.
Baldi et al.
G protein-dependent pharmacology of histamine H3 receptor ligands: evidence for heterogeneous active state receptor conformations.
Krueger et al.
Protean agonism at histamine H3 receptors in vitro and in vivo.
Gbahou et al.
The citations listed below are publications that use Tocris products. Selected citations for Proxyfan oxalate include:
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