Loperamide hydrochloride

SKU: orb1310834

Description

Loperamide hydrochloride is a synthetic piperidine-based opioid receptor agonist used as an antidiarrheal agent. It is widely utilized in pharmacological research to study μ-opioid receptor function and gastrointestinal motility in both in vitro binding assays and in vivo animal models of diarrhea.

Research Area

Cell Biology, Metabolism Research, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 34552-83-5
• MW: 513.50
• Purity: 99.94%
• Formula: C₂₉H₃₄Cl₂N₂O₂
• SMILES: Cl.CN(C)C(=O)C(CCN1CCC(O)(CC1)c1ccc(Cl)cc1)(c1ccccc1)c1ccccc1
• Target: Opioid Receptor,Autophagy
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.43 mM);DMSO:99 mg/mL (192.79 mM);Ethanol:10.3 mg/mL (20.06 mM)

Bioactivity

• Target IC50:
  δ opioid receptor:48 nM(Ki)|μ opioid receptor:3.3 nM(Ki)
• In Vivo:
  In human Chinese hamster ovary cells transfected with opioid receptors, Loperamide potently stimulates the binding of [35S]guanosine 5'-O-(3-thio)triphosphate (EC50=56 nM) and inhibits the accumulation of cAMP induced by forskolin (IC50=25 nM). Loperamide reversibly blocks the increase in intracellular calcium ([Ca2+]i) triggered by extracellular potassium ([K+]o) in a concentration-dependent manner (IC50=0.9 mM).
• In Vitro:
  In mice, ropivacaine cannot cross the blood-brain barrier. Subcutaneous injection of ropivacaine at the neck region (4 mg/kg) or at the site of tibial tumor mass (7.5-75 mg) can inhibit thermal hyperalgesia and mechanical allodynia.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Autophagy, ADL 2-1294, Inhibitor, inhibit, Loperamide Hydrochloride, Loperamide, Loperamide HCl, Loperamide hydrochloride, OpioidReceptor, Opioid Receptor, R 18553, R18553, R-18553, R-18553 (hydrochloride), δ-opioid receptor, μ-opioid receptor, κ-opioid receptor

Compound Identifiers

PubChem CID

71420