Catalog Number: 0840
Chemical Name: 4-(4-Chlorophenyl)-4-hydroxy-N,N-dimethyl-α,α-diphenyl-1-piperidinebutanamide hydrochloride
Biological Activity
High affinity μ-opioid receptor agonist with peripheral selectivity (Ki values are 2, 48 and 1156 nM for μ-, δ- and κ-opioid receptors respectively). Antidiarrhoeal and antihyperalgesic agent. Also a Ca2+ channel blocker; at low micromolar concentrations it blocks broad spectrum neuronal HVA Ca2+ channels and at higher concentrations it reduces Ca2+ flux through NMDA receptor operated channels.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 20 mM in ethanol and to 20 mM in DMSO
  • Purity:
  • Storage:
    Store 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.
Background References
  1. Pharmacology of antidiarrheal drugs.
    Awouters et al.
    Annu.Rev.Pharmacol.Toxicol., 1983;23:279
  2. Loperamide (ADL 2-1294), an opioid antihyperalgesic agent with peripheral selectivity.
    Dehaven-Hudkins et al.
    J.Pharmacol.Exp.Ther., 1999;289:494
  3. Loperamide blocks high-voltage activated calcium channels and N-Methyl-D-aspartate -evoked responses in rat and mouse cultured hippocampal pyramidal neurons.
    Church et al.
    Mol.Pharmacol., 1994;45:747
  4. Maitotoxin-elicited calcium influx in cultured cells - effect of calcium channel block.
    Daly et al.
    Biochem.Pharmacol., 1995;50:1187

The citations listed below are publications that use Tocris products. Selected citations for Loperamide hydrochloride include:

1 Citations: Showing 1 - 1

  1. Calea zacatechichi dichloromethane extract exhibits antidiarrheal and antinociceptive effects in mouse models mimicking irritable bowel syndrome.
    Authors: Sałaga Et al.
    J Pharmacol Exp Ther 2015;388:1069

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