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Proxyfan

From Wikipedia, the free encyclopedia
Proxyfan
Names
Preferred IUPAC name
4-[3-(Benzyloxy)propyl]-1H-imidazole
Identifiers
3D model (JSmol)
ChEBI
ChEMBL
ChemSpider
UNII
  • InChI=1S/C13H16N2O/c1-2-5-12(6-3-1)10-16-8-4-7-13-9-14-11-15-13/h1-3,5-6,9,11H,4,7-8,10H2,(H,14,15)
    Key: WNWALBVQAAIULR-UHFFFAOYSA-N
  • C1=CC=C(C=C1)COCCCC2=CN=CN2
Properties
C13H16N2O
Molar mass216.284 g·mol−1
Except where otherwise noted, data are given for materials in theirstandard state (at 25 °C [77 °F], 100 kPa).
Chemical compound

Proxyfan is ahistamine H3 receptor ligand which is a "protean agonist", producing different effects ranging from fullagonist, toantagonist, toinverse agonist in different tissues, depending on the level of constitutive activity of the histamine H3 receptor. This gives it a complex activity profilein vivo which has proven useful for scientific research.[1][2][3][4][5][6][7]

References

[edit]
  1. ^Morisset, S.; Rouleau, A.; Ligneau, X.; Gbahou, F.; Tardivel-Lacombe, J.; Stark, H.; Schunack, W.; Ganellin, C. R.; Schwartz, J. C.; Arrang, J. M. (2000). "High constitutive activity of native H3 receptors regulates histamine neurons in brain".Nature.408 (6814):860–864.doi:10.1038/35048583.PMID 11130725.
  2. ^Fox, G. B.; Pan, J. B.; Esbenshade, T. A.; Bitner, R. S.; Nikkel, A. L.; Miller, T.; Kang, C. H.; Bennani, Y. L.; Black, L. A.; Faghih, R.; Hancock, A. A.; Decker, M. W. (2002). "Differential in vivo effects of H3 receptor ligands in a new mouse dipsogenia model".Pharmacology, Biochemistry, and Behavior.72 (3):741–750.doi:10.1016/s0091-3057(02)00745-1.PMID 12175472.
  3. ^Gbahou, F.; Rouleau, A.; Morisset, S.; Parmentier, R.; Crochet, S.; Lin, J. S.; Ligneau, X.; Tardivel-Lacombe, J.; Stark, H.; Schunack, W.; Ganellin, C. R.; Schwartz, J. C.; Arrang, J. M. (2003)."Protean agonism at histamine H3 receptors in vitro and in vivo".Proceedings of the National Academy of Sciences of the United States of America.100 (19):11086–11091.doi:10.1073/pnas.1932276100.PMC 196931.PMID 12960366.
  4. ^Baldi, E.; Bucherelli, C.; Schunack, W.; Cenni, G.; Blandina, P.; Passani, M. B. (2005). "The H3 receptor protean agonist proxyfan enhances the expression of fear memory in the rat".Neuropharmacology.48 (2):246–251.doi:10.1016/j.neuropharm.2004.09.009.hdl:2158/220558.PMID 15695163.
  5. ^Krueger, Kathleen M.; Witte, David G.; Ireland-Denny, Lynne; Miller, Thomas R.; Baranowski, John L.; Buckner, Steve; Milicic, Ivan; Esbenshade, Timothy A.; Hancock, Arthur A. (2005). "G Protein-Dependent Pharmacology of Histamine H3 Receptor Ligands: Evidence for Heterogeneous Active State Receptor Conformations".Journal of Pharmacology and Experimental Therapeutics.314 (1):271–281.doi:10.1124/jpet.104.078865.PMID 15821027.
  6. ^Arrang, J. M.; Morisset, S.; Gbahou, F. (2007). "Constitutive activity of the histamine H3 receptor".Trends in Pharmacological Sciences.28 (7):350–357.doi:10.1016/j.tips.2007.05.002.PMID 17573125.
  7. ^Baker, Jillian G. (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.
H1
Agonists
Antagonists
H2
Agonists
Antagonists
H3
Agonists
Antagonists
H4
Agonists
Antagonists


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