Peripheral selective μ opioid receptor agonist. Ki values are 3, 48 and 1156 nM for opioid receptor subtypes μ, δ and κ, respectively. High doses allow central μ receptor activation. Antidiarrheal, antipruritic and antihyperalgesic agent.
Store at Room Temperature. The product can be stored for up to 12 months.
Soluble in DMSO to 50 mM and in ethanol to 50 mM (with warming)
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
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DeHaven-Hudkins DL et al. Loperamide (ADL 2-1294), an opioid antihyperalgesic agent with peripheral selectivity. J Pharmacol Exp Ther289:494-502 (1999).
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Banerjee AK et al. Acute diarrhoeal disease in rabbit: bacteriological diagnosis and efficacy of oral rehydration in combination with loperamide hydrochloride. Lab Anim21:314-7 (1987).
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Mackerer CR et al. Loperamide binding to opiate receptor sites of brain and myenteric plexus. J Pharmacol Exp Ther199:131-40 (1976).
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