Loperamide hydrochloride

Pricing Availability Delivery Time Qty
Cat.No. 0840 - Loperamide hydrochloride | C29H33ClN2O2.HCl | CAS No. 34552-83-5
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)
Datasheet
Citations (1)
Literature

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

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

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


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View Related Products by Product Action

View all μ Opioid Receptor Agonists

Keywords: 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

1 Citation for Loperamide hydrochloride

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

SaƂaga 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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