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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
Chemical Compound Review

Iodoproxyfan     4-[3-[(4- iodophenyl)methoxy]propyl]- 3H...

Synonyms: CHEMBL19010, SureCN3089477, CHEBI:121917, DNC003690, PDSP1_000544, ...
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High impact information on Iodoproxyfan

  • The potency of iodoproxyfan is more than 300 times lower at H1, H2, alpha1, alpha2, beta1, 5-HT2A, 5-HT3, and M3 receptors than at histamine H3 receptors [1].
  • The most active compound in the functional test (-log Ki = 8.3) and in binding studies with [3H]-(R)-alpha-methylhistamine on rat cerebral cortex (-log Ki = 9.0) in vitro was 3-(1H-imidazol-4-yl)propyl (4-iodophenyl)methyl ether (iodoproxyfan, 19) exhibiting no central H3 receptor antagonist activity in vivo [1].
  • Iodoproxyfan, i.e., 3-(1H-imidazol-4-yl)propyl-(4-iodophenyl)-methyl ether, is a novel potent and selective histamine H3 receptor antagonist [2].
  • When expressed in CHO-K1 or Cos-1 cells, the H3(445), H3(413), and H3(397) were found to generate specific 125I iodoproxyfan binding of similar pharmacological profile [3].
  • Potencies of antagonists chemically related to iodoproxyfan at histamine H3 receptors in mouse brain cortex and guinea-pig ileum: evidence for H3 receptor heterogeneity [4]?

Gene context of Iodoproxyfan

  • We determined the affinity and/or potency of the novel H3 receptor antagonist iodoproxyfan at alpha 2 and 5-HT3 receptors [5].


  1. [125I]iodoproxyfan and related compounds: a reversible radioligand and novel classes of antagonists with high affinity and selectivity for the histamine H3 receptor. Stark, H., Purand, K., Hüls, A., Ligneau, X., Garbarg, M., Schwartz, J.C., Schunack, W. J. Med. Chem. (1996) [Pubmed]
  2. [125I]iodoproxyfan, a new antagonist to label and visualize cerebral histamine H3 receptors. Ligneau, X., Garbarg, M., Vizuete, M.L., Diaz, J., Purand, K., Stark, H., Schunack, W., Schwartz, J.C. J. Pharmacol. Exp. Ther. (1994) [Pubmed]
  3. The rat H3 receptor: gene organization and multiple isoforms. Morisset, S., Sasse, A., Gbahou, F., Héron, A., Ligneau, X., Tardivel-Lacombe, J., Schwartz, J.C., Arrang, J.M. Biochem. Biophys. Res. Commun. (2001) [Pubmed]
  4. Potencies of antagonists chemically related to iodoproxyfan at histamine H3 receptors in mouse brain cortex and guinea-pig ileum: evidence for H3 receptor heterogeneity? Schlicker, E., Kathmann, M., Bitschnau, H., Marr, I., Reidemeister, S., Stark, H., Schunack, W. Naunyn Schmiedebergs Arch. Pharmacol. (1996) [Pubmed]
  5. Effects of iodoproxyfan, a potent and selective histamine H3 receptor antagonist, on alpha 2 and 5-HT3 receptors. Schlicker, E., Pertz, H., Bitschnau, H., Purand, K., Kathmann, M., Elz, S., Schunack, W. Inflamm. Res. (1995) [Pubmed]
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