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Submit ReviewLoperamide hydrochloride
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)
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 |
| InChI Key | PGYPOBZJRVSMDS-UHFFFAOYSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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
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
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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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