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Proksifan

Proksifan je ligand histaminskog H3 receptora, koji je „proteanski agonist“. On proizvodi različite efekte u opsegu od punog agonista do antagonista, do inverznog agonista u različitim tkivima, u zavisnosti od nivoa konstitutivne aktivnosti histaminskog H3 receptora. To mu daje kompleksan profil aktivnosti in vivo.[5][6][7][8][9][10][11]

Proksifan
IUPAC ime
Drugi nazivi 5-[3-(benziloksi)propil]-1H-imidazol
Identifikacija
CAS registarski broj 177708-09-7
PubChem[1][2] 6421522
ChemSpider[3] 4927056
ChEMBL[4] CHEMBL19173
IUPHAR ligand 1255
Jmol-3D slike Slika 1
Svojstva
Molekulska formula C13H16N2O
Molarna masa 216.279 g/mol



Ukoliko nije drugačije napomenuto, podaci se odnose na standardno stanje (25 °C, 100 kPa) materijala

Infobox references

Reference uredi

  1. ↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519.  edit
  2. ↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1. 
  3. ↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846.  edit
  4. ↑ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594.  edit
  5. ↑ Morisset S, Rouleau A, Ligneau X, Gbahou F, Tardivel-Lacombe J, Stark H, Schunack W, Ganellin CR, Schwartz JC, Arrang JM. High constitutive activity of native H3 receptors regulates histamine neurons in brain. Nature. 2000 Dec 14;408(6814):860-4. PMID 11130725
  6. ↑ Fox GB, Pan JB, Esbenshade TA, Bitner RS, Nikkel AL, Miller T, Kang CH, Bennani YL, Black LA, Faghih R, Hancock AA, Decker MW. Differential in vivo effects of H3 receptor ligands in a new mouse dipsogenia model. Pharmacology, Biochemistry and Behaviour. 2002 Jun;72(3):741-50. PMID 12175472
  7. ↑ Gbahou F, Rouleau A, Morisset S, Parmentier R, Crochet S, Lin JS, Ligneau X, Tardivel-Lacombe J, Stark H, Schunack W, Ganellin CR, Schwartz JC, Arrang JM. Protean agonism at histamine H3 receptors in vitro and in vivo. Proceedings of the National Academy of Sciences USA. 2003 Sep 16;100(19):11086-91. PMID 12960366
  8. ↑ Baldi E, Bucherelli C, Schunack W, Cenni G, Blandina P, Passani MB. The H3 receptor protean agonist proxyfan enhances the expression of fear memory in the rat. Neuropharmacology. 2005 Feb;48(2):246-51. PMID 15695163
  9. ↑ Krueger KM, Witte DG, Ireland-Denny L, Miller TR, Baranowski JL, Buckner S, Milicic I, Esbenshade TA, Hancock AA. G protein-dependent pharmacology of histamine H3 receptor ligands: evidence for heterogeneous active state receptor conformations. Journal of Pharmacology and Experimental Therapeutics. 2005 Jul;314(1):271-81. DOI:10.1124/jpet.104.078865 PMID 15821027
  10. ↑ Arrang JM, Morisset S, Gbahou F. Constitutive activity of the histamine H3 receptor. Trends in Pharmacological Sciences. 2007 Jul;28(7):350-7. PMID 17573125
  11. ↑ Baker JG. Antagonist affinity measurements at the Gi-coupled human histamine H3 receptor expressed in CHO cells. BMC Pharmacology. 2008 Jun 6;8:9. DOI:10.1186/1471-2210-8-9 PMID 18538007

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