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Loperamide hydrochloride

Cat. No. M2145
Loperamide hydrochloride Structure
Size Price Availability Quantity
50mg USD 80  USD80 In stock
200mg USD 160  USD160 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 513.51
Formula C29H33ClN2O2.HCl
CAS Number 34552-83-5
Purity >98%
Solubility DMSO
Ethanol
Storage at -20°C
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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