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.
|Related Opioid Receptor Products|
Met-Enkephalin (H-Tyr-Gly-Gly-Phe-Met-OH) inhibits tumor growth via binding to the opioid receptor.
Trimebutine maleate is a drug with antimuscarinic and weak mu opioid agonist effects.
Trimebutine is an agonist of peripheral mu, kappa and delta opiate receptors, used as spasmolytic agent for treatment of both acute and chronic abdominal pain.
Docusate Sodium is a laxative used to treat constipation, for constipation due to the use of opiates it maybe used with a stimulant laxative, can be taken by mouth or rectally.
Alvimopan dihydrate(LY 246736; ADL 8-2698) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.
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