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.
|Storage||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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 513.51. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.95 mL||9.74 mL||19.47 mL|
|5 mM||0.39 mL||1.95 mL||3.89 mL|
|10 mM||0.19 mL||0.97 mL||1.95 mL|
|50 mM||0.04 mL||0.19 mL||0.39 mL|
References are publications that support the products' biological activity.
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-Methyl-D-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
If you know of a relevant reference for Loperamide hydrochloride, please let us know.
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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, Mu, Opioid, Receptors, NMDA, Receptors, Voltage-gated, Calcium, Channels, Mu, Opioid, Receptors, Tocris Bioscience
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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