Cat. No. 0840
Chemical Name: 4-(4-Chlorophenyl)-4-hydroxy-N,N-dimethyl-α,α-diphenyl-1-piperidinebutanamide hydrochloride
Biological ActivityHigh 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.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Certificate of Analysis / Safety Data Sheet
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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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
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