Chemistry:Proxyfan

From HandWiki

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

References

  1. ↑ Morisset, S.; Rouleau, A.; Ligneau, X.; Gbahou, F.; Tardivel-Lacombe, J.; Stark, H.; Schunack, W.; Ganellin, C. R. et al. (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. et al. (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. et al. (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. 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. 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. et al. (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. doi:10.1186/1471-2210-8-9. PMID 18538007. 




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