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Loperamide hydrochloride

Cat. No. M2145
Loperamide hydrochloride Structure
Synonym:

R-18553 hydrochloride

Size Price Availability Quantity
50mg USD 45  USD45 In stock
100mg USD 55  USD55 In stock
500mg USD 90  USD90 In stock
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Quality Control & Documentation
Biological Activity

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. It can be used to construct animal models of functional constipation.

Chemical Information
Molecular Weight 513.51
Formula C29H33ClN2O2.HCl
CAS Number 34552-83-5
Solubility (25°C) DMSO 30 mg/mL
Storage 4°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] DeHaven-Hudkins DL, et al. J Pharmacol Exp Ther. Loperamide (ADL 2-1294), an opioid antihyperalgesic agent with peripheral selectivity.

[2] Church J, et al. Mol Pharmacol. Loperamide blocks high-voltage-activated calcium channels and N-methyl-D-aspartate-evoked responses in rat and mouse cultured hippocampal pyramidal neurons.

[3] Daly JW, et al. Biochem Pharmacol. Maitotoxin-elicited calcium influx in cultured cells. Effect of calcium-channel blockers.

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