Chemical Name: 4-(4-Chlorophenyl)-4-hydroxy-N,N-dimethyl-α,α-diphenyl-1-piperidinebutanamide hydrochloride
Biological ActivityLoperamide 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Loperamide blocks high-voltage activated calcium channels and N-MthD.-aspartate -evoked responses in rat and mouse cultured hippocampal pyramidal neurons.
Church et al.
Loperamide (ADL 2-1294), an opioid antihyperalgesic agent with peripheral selectivity.
Dehaven-Hudkins et al.
Maitotoxin-elicited calcium influx in cultured cells - effect of calcium channel block.
Daly et al.
Pharmacology of antidiarrheal drugs.
Awouters et al.
Screening of an FDA-approved compound library identifies four small-molecule inhibitors of Middle East Respiratory Syndrome coronavirus replication in cell culture.
de Wilde et al.
Citation for Loperamide hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for Loperamide hydrochloride include:
1 Citation: Showing 1 - 1
Calea zacatechichi dichloromethane extract exhibits antidiarrheal and antinociceptive effects in mouse models mimicking irritable bowel syndrome.
Authors: Sałaga Et al.
J Pharmacol Exp Ther 2015;388:1069
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