Date published: 2026-5-2

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N-Desmethyl Loperamide (CAS 66164-07-6)

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Application:
N-Desmethyl Loperamide is a metabolite of Loperamide
CAS Number:
66164-07-6
Purity:
98%
Molecular Weight:
463.01
Molecular Formula:
C28H31ClN2O2
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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N-Desmethyl Loperamide, also known as Desmethyl loperamide, the methylamide of 4-[4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl]-2,2-diphenylbutanoic acid, is a drug metabolite belonging to the piperidines and monochlorobenzenes. As a major metabolite of loperamide, it shares similar properties, including its activation of μ opioid receptors and its substrate status for the ATP-dependent efflux transporter, P-glycoprotein. Additionally, N-Desmethyl Loperamide is classified as a monocarboxylic acid amide and a tertiary alcohol.


N-Desmethyl Loperamide (CAS 66164-07-6) References

  1. Human brain imaging and radiation dosimetry of 11C-N-desmethyl-loperamide, a PET radiotracer to measure the function of P-glycoprotein.  |  Seneca, N., et al. 2009. J Nucl Med. 50: 807-13. PMID: 19372478
  2. Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.  |  Zamek-Gliszczynski, MJ., et al. 2012. Drug Metab Dispos. 40: 1825-33. PMID: 22711747
  3. A high-yield route to synthesize the P-glycoprotein radioligand [11C]N-desmethyl-loperamide and its parent radioligand [11C]loperamide.  |  Wang, M., et al. 2013. Bioorg Med Chem Lett. 23: 5259-63. PMID: 23981899
  4. Molecular determinants of loperamide and N-desmethyl loperamide binding in the hERG cardiac K+ channel.  |  Vaz, RJ., et al. 2018. Bioorg Med Chem Lett. 28: 446-451. PMID: 29274816
  5. A face-to-face comparison of claudin-5 transduced human brain endothelial (hCMEC/D3) cells with porcine brain endothelial cells as blood-brain barrier models for drug transport studies.  |  Gericke, B., et al. 2020. Fluids Barriers CNS. 17: 53. PMID: 32843059
  6. Successful Prediction of Human Steady-State Unbound Brain-to-Plasma Concentration Ratio of P-gp Substrates Using the Proteomics-Informed Relative Expression Factor Approach.  |  Storelli, F., et al. 2021. Clin Pharmacol Ther. 110: 432-442. PMID: 33675056
  7. An Opioid Hiding in Plain Sight: Loperamide-Induced False-Positive Fentanyl and Buprenorphine Immunoassay Results.  |  Geno, KA., et al. 2022. J Appl Lab Med. 7: 1318-1328. PMID: 36036092

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

N-Desmethyl Loperamide, 1 mg

sc-212189
1 mg
$400.00

N-Desmethyl Loperamide, 5 mg

sc-212189A
5 mg
$2000.00