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Loperamide hydrochloride

Cat. No. M2145
Loperamide hydrochloride Structure
Size Price Availability Quantity
50mg USD 80 In stock
200mg USD 160 In stock
1g USD 380 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • 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 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.

Chemical Information
Molecular Weight 513.51
Formula C29H33ClN2O2.HCl
CAS Number 34552-83-5
Purity >99%
Solubility DMSO
Ethanol
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Loperamide hydrochloride supplier, Opioid Receptor, inhibitors

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