VUF-5681
VUF-5681.svg
Names
Preferred IUPAC name
4-[3-(1H-Imidazol-5-yl)propyl]piperidine
Identifiers
3D model (JSmol)
ChemSpider
  • InChI=1S/C11H19N3/c1(3-11-8-13-9-14-11)2-10-4-6-12-7-5-10/h8-10,12H,1-7H2,(H,13,14) ☒N
    Key: YPGRNKJNOSUCLY-UHFFFAOYSA-N ☒N
  • InChI=1/C11H19N3/c1(3-11-8-13-9-14-11)2-10-4-6-12-7-5-10/h8-10,12H,1-7H2,(H,13,14)
    Key: YPGRNKJNOSUCLY-UHFFFAOYAZ
  • C1CNCCC1CCCC2=CN=CN2
Properties
C11H19N3
Molar mass 193.288 g/mol
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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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.