Catalog Number: 3753
Chemical Name: 4-((3R)-3-amino-pyrrolidin-1-yl)-6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-d]pyrimidin-2-ylamine
Biological Activity
Potent and selective histamine H4 receptor antagonist (pKi values are 7.15 and 8.12 at human and rat receptors respectively). Blocks inflammation in a peritonitis mouse model and displays efficacy in inflammatory pain and neuropathic pain models.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in water and to 100 mM in DMSO
  • Purity:
  • Storage:
    Store at +4°C
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Histamine H4-Receptors Inhibit Mast Cell Renin Release in Ischemia/Reperfusion via PKC{epsilon}-Dependent Aldehyde Dehydrogenase Type-2 Activation.
    Aldi et al.
    J.Pharmacol.Exp.Ther., 2014;349:508
  2. Molecular and biochemical pharmacology of the histamine H4 receptor.
    Leurs et al.
    Br.J.Pharmacol., 2009;157:14
  3. Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models.
    Cowart et al.
    J.Med.Chem., 2008;51:6547
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