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

  1. ^ 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. PMID 16769092. S2CID 25209099.
  2. ^ Baker JG (June 2008). "Antagonist affinity measurements at the Gi-coupled human histamine H3 receptor expressed in CHO cells". BMC Pharmacology. 8: 9. doi:10.1186/1471-2210-8-9. PMC 2430196. PMID 18538007.