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Loperamide hydrochloride

Cat. No. 0840

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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 (K_i 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

Solubility:

Soluble to 50 mM in ethanol and to 50 mM in DMSO

Purity:

>99 %

Storage:

Store at RT

CAS No:

34552-83-5

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

References

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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