Loperamide hydrochloride is an opioid-receptor agonist and acts on the μ-opioid receptors. Loperamide exhibited potent affinity and selectivity for the cloned micro (Ki = 3 nM) compared with the delta (Ki = 48 nM) and kappa (Ki = 1156 nM) human opioid receptors. Loperamide potently inhibited forskolin-stimulated cAMP accumulation (IC50 = 25 nM) in Chinese hamster ovary cells transfected with the human mu opioid receptor. Loperamide hydrochloride is also a Ca2+ channel blocker. Loperamide hydrochloride blocks broad spectrum neuronal HVA Ca2+ channels at low micromolar concentrations and at higher concentrations it reduces Ca2+ flux through NMDA receptor operated channels. Loperamide is effective for the treatment of a number of types of diarrhea.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Loperamide (ADL 2-1294), an opioid antihyperalgesic agent with peripheral selectivity.
DeHaven-Hudkins DL, et al. J Pharmacol Exp Ther. 1999 Apr;289(1):494-502. PMID: 10087042.
Loperamide blocks high-voltage-activated calcium channels and N-methyl-D-aspartate-evoked responses in rat and mouse cultured hippocampal pyramidal neurons.
Church J, et al. Mol Pharmacol. 1994 Apr;45(4):747-57. PMID: 8183255.
Maitotoxin-elicited calcium influx in cultured cells. Effect of calcium-channel blockers.
Daly JW, et al. Biochem Pharmacol. 1995 Oct 12;50(8):1187-97. PMID: 7488233.
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