VUF-5681

VUF-5681

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ImageFile=VUF-5681.pngImageSize=220px
IUPACName=4- [3-(1H-Imidazol-4-yl)propyl] piperidine
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SMILES=C2CNCCC2CCCc1ncnc1
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Section2=Chembox Properties
Formula=C11H19N3
MolarMass=193.288
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VUF-5681 is a potent and selective histamine antagonist which binds selectively to the H3 subtype. [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] 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. [Baker JG. Antagonist affinity measurements at the Gi-coupled human histamine H3 receptor expressed in CHO cells. "BMC Pharmacology". 2008 Jun 6;8:9. PMID 18538007]

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  • Histamine H3 receptor — Histamine H3 receptors are expressed in the central nervous system and to a lesser extent the peripheral nervous system, where they act as autoreceptors in presynaptic histaminergic neurons, and also control histamine turnover by feedback… …   Wikipedia

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