Loperamide hydrochloride

Catalog # Availability Size / Price Qty
0840/1G
Loperamide hydrochloride | CAS No. 34552-83-5 | mu Opioid Receptor Agonists
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Description: Peripherally acting μ agonist; Ca2+ channel blocker

Chemical Name: 4-(4-Chlorophenyl)-4-hydroxy-N,N-dimethyl-α,α-diphenyl-1-piperidinebutanamide hydrochloride

Purity: ≥99%

Product Details
Citations (1)
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Biological Activity

Loperamide hydrochloride is a 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. Inhbits replication of MERS-CoV and SARS-CoV in vitro.

Technical Data

M.Wt:
513.51
Formula:
C29H33ClN2O2.HCl
Solubility:
Soluble to 20 mM in ethanol and to 20 mM in DMSO
Purity:
≥99%
Storage:
Store at RT
CAS No:
34552-83-5

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. 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
  2. Loperamide (ADL 2-1294), an opioid antihyperalgesic agent with peripheral selectivity.
    Dehaven-Hudkins et al.
    J.Pharmacol.Exp.Ther., 1999;289:494
  3. Maitotoxin-elicited calcium influx in cultured cells - effect of calcium channel block.
    Daly et al.
    Biochem.Pharmacol., 1995;50:1187
  4. Pharmacology of antidiarrheal drugs.
    Awouters et al.
    Annu.Rev.Pharmacol.Toxicol., 1983;23:279
  5. 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

Product Datasheets

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Citation for Loperamide hydrochloride

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

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