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Chemical Compound Review

CHEMBL122903     3-(5-methyl-1H-imidazol-4- yl)-1-(1...

Synonyms: SureCN4155303, CHEBI:301262, AC1NSK2E, CTK8G5937, GR65630, ...
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High impact information on GR65630

  • The specific binding of a single concentration of GR65630 (0.5 nM) defined by granisetron (10 microM) in these areas indicated that the density of 5-HT3 recognition sites varied from 2.4 +/- 1.0 to 10.1 +/- 1.0 fmol mg-1 protein [1].
  • In addition, we determined specific binding of [3H]DTG (1,3-di(2-tolyl)-guanidine), a selective sigma-site radioligand, and [3H] GR65630 (3-(5-methyl-1H-imidazol-4-yl)-1-(1-methyl-1H-indol-3-yl)-1- propanone), a selective 5-HT3 receptor antagonist, to membranes prepared from N1E-115 cells [2].
  • The radiolabelled derivative of the potent and selective 5-HT3 receptor antagonist, GR65630, has been shown to label 5-HT3 receptors in homogenates of rat entorhinal cortex [3].


  1. Identification and distribution of 5-HT3 recognition sites in the rat gastrointestinal tract. Champaneria, S., Costall, B., Naylor, R.J., Robertson, D.W. Br. J. Pharmacol. (1992) [Pubmed]
  2. Inhibition of 5-HT3 receptor function by imidazolines in mouse neuroblastoma cells: potential involvement of sigma 2 binding sites. Molderings, G.J., Schmidt, K., Bönisch, H., Göthert, M. Naunyn Schmiedebergs Arch. Pharmacol. (1996) [Pubmed]
  3. Binding of the 5-HT3 ligand, [3H]GR65630, to rat area postrema, vagus nerve and the brains of several species. Kilpatrick, G.J., Jones, B.J., Tyers, M.B. Eur. J. Pharmacol. (1989) [Pubmed]
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