VUF-5681 is a potent and selective
histamine antagonist which binds selectively to the
H3 subtype.[1] However while VUF-5681 blocks the activity of more potent H3 agonists, recent studies suggest that it may have some weak
partial agonist activity when administered by itself.[2]
References
^Moreno-Delgado D, Torrent A, Gómez-Ramírez J, de Esch I, Blanco I, Ortiz J (September 2006). "Constitutive activity of H3 autoreceptors modulates histamine synthesis in rat brain through the cAMP/PKA pathway". Neuropharmacology. 51 (3): 517–23.
doi:
10.1016/j.neuropharm.2006.04.010.
PMID16769092.
S2CID25209099.