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Loperamide Hydrochloride (CAS 34552-83-5)

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Alternate Names:
4-(4-Chlorophenyl)-4-hydroxy-N,N-dimethyl-α,α-diphenyl-1-piperidinebutanamide Hydrochloride
Application:
Loperamide Hydrochloride is a Ca2+ channel protein inhibitor and MOR activator
CAS Number:
34552-83-5
Purity:
≥98%
Molecular Weight:
513.51
Molecular Formula:
C29H33ClN2O2•HCl
Supplemental Information:
This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Loperamide Hydrochloride is an opiate agonist with selectivity for the MOR (mu-opiod receptor). This specificity for mu-opioid receptors and limited penetrability into the brain prevent Loperamide from demonstrating central systemic effects generally associated with opiates, instead demonstrating localized action on the nociceptor and resultant antihyperalgesic action. Loperamide is shown to have an effect on the Ca2+ flux through high-voltage-activated calcium channels in response to high levels of extracellular K+, and at higher concentrations Loperamide is also a calcium channel protein inhibitor via the N-methyl-D-aspartate (NMDA) receptor-operated ion channel.


Loperamide Hydrochloride (CAS 34552-83-5) References

  1. Loperamide (ADL 2-1294), an opioid antihyperalgesic agent with peripheral selectivity.  |  DeHaven-Hudkins, DL., et al. 1999. J Pharmacol Exp Ther. 289: 494-502. PMID: 10087042
  2. Loperamide-simethicone vs loperamide alone, simethicone alone, and placebo in the treatment of acute diarrhea with gas-related abdominal discomfort. A randomized controlled trial.  |  Kaplan, MA., et al. 1999. Arch Fam Med. 8: 243-8. PMID: 10333820
  3. Spectrophotometric determination of loperamide hydrochloride by acid-dye and charge-transfer complexation methods in the presence of its degradation products.  |  El Sherif, ZA., et al. 2000. J Pharm Biomed Anal. 22: 13-23. PMID: 10727119
  4. Effect of finite doses of propylene glycol on enhancement of in vitro percutaneous permeation of loperamide hydrochloride.  |  Trottet, L., et al. 2004. Int J Pharm. 274: 213-9. PMID: 15072797
  5. LC-MS determination and bioavailability study of loperamide hydrochloride after oral administration of loperamide capsule in human volunteers.  |  Yu, JH., et al. 2004. J Pharm Biomed Anal. 36: 421-7. PMID: 15496339
  6. Tolerance develops to the antiallodynic effects of the peripherally acting opioid loperamide hydrochloride in nerve-injured rats.  |  He, SQ., et al. 2013. Pain. 154: 2477-2486. PMID: 23880055
  7. Analytical studies on the charge transfer complexes of loperamide hydrochloride and trimebutine drugs. Spectroscopic and thermal characterization of CT complexes.  |  Elqudaby, HM., et al. 2014. Spectrochim Acta A Mol Biomol Spectrosc. 129: 84-95. PMID: 24727166
  8. Acute diarrhoeal disease in rabbit: bacteriological diagnosis and efficacy of oral rehydration in combination with loperamide hydrochloride.  |  Banerjee, AK., et al. 1987. Lab Anim. 21: 314-7. PMID: 3695388
  9. Comparison of loperamide with bismuth subsalicylate for the treatment of acute travelers' diarrhea.  |  Johnson, PC., et al. 1986. JAMA. 255: 757-60. PMID: 3944976
  10. Pharmacology of antidiarrheal drugs.  |  Awouters, F., et al. 1983. Annu Rev Pharmacol Toxicol. 23: 279-301. PMID: 6307123
  11. A double-blind crossover study of the effect of loperamide hydrochloride and codeine phosphate on ileostomy output.  |  King, RF., et al. 1982. Aust N Z J Surg. 52: 121-4. PMID: 7044361
  12. Maitotoxin-elicited calcium influx in cultured cells. Effect of calcium-channel blockers.  |  Daly, JW., et al. 1995. Biochem Pharmacol. 50: 1187-97. PMID: 7488233
  13. 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. 1994. Mol Pharmacol. 45: 747-57. PMID: 8183255

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Loperamide Hydrochloride, 5 g

sc-203116
5 g
$77.00