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VUF-5681 is a potent and selective histamine antagonist which binds selectively to the H3 subtype. 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.
- Moreno-Delgado D, Torrent A, Gómez-Ramírez J, de Esch I, Blanco I, Ortiz J. Constitutive activity of H3 autoreceptors modulates histamine synthesis in rat brain through the cAMP/PKA pathway. Neuropharmacology. 2006 Sep;51(3):517-23. PMID 16769092
- Baker, JG (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.
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