Loperamide hydrochloride

An Antagonist of L-type and T-type CaV Channels, HCN Channels, NMDA Receptors and an Agonist of μ-Opioid Receptors
    Cat #: L-100
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 513.5
    Purity: >99%
    Effective concentration 1-100 µM.
    • Loperamide hydrochloride
    Chemical name 4-(4-Chlorophenyl)-4-hydroxy-N,N-dimethyl-α,α-diphenyl-1-piperidinebutanamide hydrochloride.
    Molecular formula C29H34Cl2N2O2.
    CAS No.: 34552-83-5.
    Activity Loperamide hydrochloride inhibits (IC50 = 2.5 μM) HVA CaV in hippocampal cells. It acts as a μ-opioid receptor positive modulator and also affects NMDA receptors1.
    1. Church J. et al. (1994) Mol. Pharmacol. 45, 747.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility Ethanol. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Loperamide hydrochloride
      Alomone Labs Loperamide hydrochloride inhibits L-type voltage-gated Ca2+ currents heterologously expressed in Xenopus oocytes.
      A. Time course of CaV1.2/α2-δ1/β2a (L-type) current inhibition by 20 µM of Loperamide hydrochloride (#L-100). Currents were elicited by application of voltage steps from a holding potential of -100 mV to 0 mV (100 msec). B. Superimposed example traces of current responses before and during perfusion of 20 µM Loperamide hydrochloride as indicated.
    References - Scientific background
    1. Church J. et al. (1994) Mol. Pharmacol. 45, 747.
    2. Hanauer, S.B. (2008) Rev. Gastroenterol. Disord. 8, 15.
    3. Baker, D.E.  (2007) Rev. Gastroenterol. Disord. 7, S11.
    4. Guan, Y. et al. (2008) Pain 138, 318.
    5. DeHaven-Hudkins, D.L. et al. (1999) J. Pharmacol. Exp. Ther. 289, 494.
    6. Church J. et al. (1994) Mol. Pharmacol. 45, 747.
    7. Vasilyev, D.V. et al. (2007) J. Neurophysiol. 97, 3713.
    Scientific background

    Loperamide hydrochloride is an off the counter medication for treatment of various diarrhea syndromes. By decreasing peristalsis of the intestine, it prolongs the gastrointestinal transit time and increases absorption of fluids and electrolytes from the stool to the gastrointestinal tract1.

    Loperamide is a synthetic derivative of phenylpiperidine, and is very similar to diphenoxylate, another derivative used to treat diarrhea. It is a strong agonist of μ-opiate receptors found in both the central nervous system and the gastrointestinal tract. Nevertheless, loperamide is considered to be a specific and safe treatment, when administered systemically or orally due to its inability to cross the blood-brain barrier and affect opiatic receptors in the brain2-4.

    Besides its effect as an opiate-receptor agonist, loperamide also behaves as a calcium-calmodulin antagonist and was shown to inhibit NMDA receptors5, HCN channels, and voltage-gated Ca2+ channels6.

    Target L-type, T-type Ca2+, HCN channels, NMDA, μ-opioid receptors
    Last update: 24/01/2020

    Loperamide hydrochloride (#L-100) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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