Loperamide hydrochloride

Biological Activity

Loperamide hydrochloride is a high affinity μ-opioid receptor agonist with peripheral selectivity (K_i 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. Inhbits replication of MERS-CoV and SARS-CoV in vitro.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
   Fox JT, Sakamuru S, Huang R
   Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8.
2. Loperamide blocks high-voltage activated calcium channels and N-MthD.-aspartate -evoked responses in rat and mouse cultured hippocampal pyramidal neurons.
   Church et al.
   Mol.Pharmacol., 1994;45:747
3. Loperamide (ADL 2-1294), an opioid antihyperalgesic agent with peripheral selectivity.
   Dehaven-Hudkins et al.
   J.Pharmacol.Exp.Ther., 1999;289:494
4. Maitotoxin-elicited calcium influx in cultured cells - effect of calcium channel block.
   Daly et al.
   Biochem.Pharmacol., 1995;50:1187
5. Pharmacology of antidiarrheal drugs.
   Awouters et al.
   Annu.Rev.Pharmacol.Toxicol., 1983;23:279
6. Screening of an FDA-approved compound library identifies four small-molecule inhibitors of Middle East Respiratory Syndrome coronavirus replication in cell culture.
   de Wilde et al.
   Antimicrob.Agents.Chemother., 2014;58:4875

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