Loperamide hydrochloride

Pricing Availability   Qty
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% (HPLC)
Citations (1)
Literature (2)

Biological Activity for Loperamide hydrochloride

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 for Loperamide hydrochloride

M. Wt 513.51
Formula C29H33ClN2O2.HCl
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 34552-83-5
PubChem ID 71420
Smiles Cl.CN(C)C(=O)C(CCN1CCC(O)(CC1)C1=CC=C(Cl)C=C1)(C1=CC=CC=C1)C1=CC=CC=C1

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.

Solubility Data for Loperamide hydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
ethanol 10.27 20
DMSO 10.27 20

Preparing Stock Solutions for Loperamide hydrochloride

The following data is based on the product molecular weight 513.51. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.2 mM 9.74 mL 48.68 mL 97.37 mL
1 mM 1.95 mL 9.74 mL 19.47 mL
2 mM 0.97 mL 4.87 mL 9.74 mL
10 mM 0.19 mL 0.97 mL 1.95 mL

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Product Datasheets for Loperamide hydrochloride

Certificate of Analysis / Product Datasheet
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References for Loperamide hydrochloride

References are publications that support the biological activity of the product.

Awouters et al (1983) Pharmacology of antidiarrheal drugs. Annu.Rev.Pharmacol.Toxicol. 23 279 PMID: 6307123

Church et al (1994) Loperamide blocks high-voltage activated calcium channels and N-MthD.-aspartate -evoked responses in rat and mouse cultured hippocampal pyramidal neurons. Mol.Pharmacol. 45 747 PMID: 8183255

Daly et al (1995) Maitotoxin-elicited calcium influx in cultured cells - effect of calcium channel block. Biochem.Pharmacol. 50 1187 PMID: 7488233

Dehaven-Hudkins et al (1999) Loperamide (ADL 2-1294), an opioid antihyperalgesic agent with peripheral selectivity. J.Pharmacol.Exp.Ther. 289 494 PMID: 10087042

de Wilde et al (2014) Screening of an FDA-approved compound library identifies four small-molecule inhibitors of Middle East Respiratory Syndrome coronavirus replication in cell culture. Antimicrob.Agents.Chemother. 58 4875

If you know of a relevant reference for Loperamide hydrochloride, please let us know.

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1 Citation for Loperamide hydrochloride

Citations are publications that use Tocris products. Selected citations for Loperamide hydrochloride include:

Sałaga et al (2015) Calea zacatechichi dichloromethane extract exhibits antidiarrheal and antinociceptive effects in mouse models mimicking irritable bowel syndrome. J Pharmacol Exp Ther 388 1069 PMID: 26068703

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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