Catalog Number: 4019
Chemical Name: 4-[3-[4-[Piperidinyl]but-1-ynyl]benzyl]morpholine dihydrochloride
Biological Activity
Histamine H3 receptor antagonist (pKi values are 8.15 and 8.93 for rat and human H3 receptors respectively). Increases extracellular norepinephrine and acetylcholine levels in rat frontal cortex but does not stimulate dopamine release. Brain penetrant.
Technical Data
  • M.Wt:
    385.37
  • Formula:
    C20H28N2O.2HCl
  • Solubility:
    Soluble to 100 mM in water and to 25 mM in ethanol
  • Purity:
    >98%
  • Storage:
    Desiccate at RT
  • CAS No:
    544707-20-2
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.
Additional Information
Licensing Caveats:
Sold with the permission of Ortho-McNeil-Janssen Pharmaceuticals, Inc.
Background References
  1. Histamine H3 receptor antagonists: from target identification to drug leads.
    Bonaventure et al.
    Biochem.Pharmacol., 2007;73:1084
  2. The histamine H3 receptor: an attractive target for the treatment of cognitive disorders.
    Esbenshade et al.
    Br.J.Pharmacol., 2008;154:1166
  3. JNJ-10181457, a selective non-imidazole histamine H3 receptor antagonist, normalizes acetylcholine neurotransmission and has efficacy in translational rat models of cognition.
    Boggs et al.
    Neuropharmacology, 2009;56:1131
Citations:

The citations listed below are publications that use Tocris products. Selected citations for JNJ 10181457 dihydrochloride include:

1 Citations: Showing 1 - 1

  1. JNJ10181457, a histamine H3 receptor inverse agonist, regulates in vivo microglial functions and improves depression-like behaviours in mice.
    Authors: Iida
    Biochem Biophys Res Commun 2017;488(3):534

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