Loperamide hydrochloride

Cat. No. 0840

Loperamide hydrochloride C29H33ClN2O2.HCl [34552-83-5]

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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

Soluble to 20 mM in ethanol and to 20 mM in DMSO
>99 %
Store at RT

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

Certificate of Analysis / Product Datasheet
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References are publications that support the products' biological activity.

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

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

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

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

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

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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Keywords: Loperamide hydrochloride, supplier, Ca2+, channel, blockers, HVA, L/N-type, NMDA, antagonists, reduces, flux, Peripherally, peripheral, μ-opioid, mu-opioid, agonists, Calcium, CaV, Channels, L-Type, N-Type, voltage-gated, voltage-dependent, Glutamate, Receptors, N-Methyl-D-Aspartate, iGluR, Ionotropic, MOP, OP3, Tocris Bioscience, μ Opioid Receptor Agonist products

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