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Loperamide HCl

Synonyms: ADL 2-1294,R-18553 hydrochloride

Loperamide HCl (ADL 2-1294,R-18553 hydrochloride) is a selective μ-opioid receptor agonist opioid with Ki of 3.3 nM, 15-fold and 350-fold selective over the δ subtype and the κ subtype of the opioid receptor, used against diarrhea resulting from gastroenteritis or inflammatory bowel disease.

Loperamide HCl Chemical Structure

Loperamide HCl Chemical Structure

CAS: 34552-83-5

Selleck's Loperamide HCl has been cited by 7 Publications

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Purity & Quality Control

Batch: Purity: 99.89%
99.89

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Biological Activity

Description Loperamide HCl (ADL 2-1294,R-18553 hydrochloride) is a selective μ-opioid receptor agonist opioid with Ki of 3.3 nM, 15-fold and 350-fold selective over the δ subtype and the κ subtype of the opioid receptor, used against diarrhea resulting from gastroenteritis or inflammatory bowel disease.
Targets
μ-opioid receptor [1] δ-opioid receptor [1]
3.3 nM(Ki) 48 nM(Ki)
In vitro
In vitro

Loperamide exhibits 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 stimulates [35S]guanosine-5'-O-(3-thio)triphosphate binding with EC50 of 56 nM, and inhibits forskolin-stimulated cAMP accumulation (IC50 = 25 nM) in Chinese hamster ovary cells transfected with the human mu opioid receptor. Loperamide potently inhibits late-phase formalin-induced flinching after intrapaw injection (A50 = 6 mg). [1] Loperamide is a strong inhibitor of CES2, with a K(i) of 1.5 muM, but it only weakly inhibits CES1A1 (IC50 = 0.44 mM). [2] Loperamide reversibly blocks rises in [Ca2+]i evoked by high [K+] in a concentration-dependent manner, with an IC50 of 0.9 mM. Loperamide (0.1-50 mM) produces a concentration-dependent reduction of the peak IBa with an IC50 value of 2.5 mM and, at the highest concentration tested, could fully block IBa in the absence of any other pharmacological agent. Loperamide also attenuates NMDA-evoked currents recorded at a membrane potential of -60 mV, with an IC50 of 73 mM. [3]
In Vivo
In vivo

Loperamide, an opioid agonist unable to cross the blood-brain barrier, inhibits both thermal and mechanical hyperalgesia when s.c. injected, locally over the tibial tumoral mass (7.5-75 mg) or distantly, under the fur of the neck (4 mg/kg) in mice. [4]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04225078 Completed Healthy Participants Janssen Research & Development LLC January 17 2020 Phase 1

Chemical lnformation & Solubility

Molecular Weight 513.5 Formula

C29H33ClN2O2.HCl
CAS No. 34552-83-5 SDF Download Loperamide HCl SDF
Smiles CN(C)C(=O)C(CCN1CCC(CC1)(C2=CC=C(C=C2)Cl)O)(C3=CC=CC=C3)C4=CC=CC=C4.Cl
Storage (From the date of receipt)

In vitro
Batch:

Ethanol : 27 mg/mL

DMSO : 22 mg/mL ( (42.84 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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