Catalog Number: 4020
Chemical Name: 1-[3-[4-(1-Piperidinylmethyl)phenoxy]propyl]piperidine hydrochloride
Biological Activity
High affinity histamine H3 receptor neutral antagonist (pKi values are 8.9 and 9.2 in rat and human respectively). Brain penetrant and orally active. Has 3- and 100-fold higher affinity than thioperamide (Cat. No. 0644) for rat and human H3 receptors respectively. Suppresses slow-wave sleep; exhibits wake-promoting effects in rodent arousal models.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 50 mM in water and to 20 mM in DMSO with gentle warming
  • Purity:
  • Storage:
    Desiccate at RT
  • 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.
Additional Information
Licensing Caveats:
Sold with the permission of Ortho-McNeil-Janssen Pharmaceuticals, Inc.
Background References
  1. Acute wake-promoting actions of JNJ-5207852, a novel, diamine-based H3 antagonist.
    Barbier et al.
    Br.J.Pharmacol., 2004;143:649
  2. Effects of histamine H3 antagonists and donepezil on learning and mnemonic deficits induced by pentylenetetrazol kindling in weanling mice.
    Jia et al.
    Neuropharmacology, 2005;50:404
  3. Correlation between ex vivo receptor occupancy and wake-promoting activity of selective H3 receptor antagonists.
    Le et al.
    J.Pharmacol.Exp.Ther., 2008;325:902
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