| Bioactivity | N-Desmethyl-loperamide is a major metabolite of loperamide, a drug that selectively activates peripheral μopioid receptors with a Ki value of 0.16 nM. N-Desmethyl-loperamide is a substrate of the ATP-dependent efflux transporter P-glycoprotein[1][2][3]. |
| CAS | 66164-07-6 |
| Formula | C28H31ClN2O2 |
| Molar Mass | 463.01 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Sklerov J, et al. Tissue distribution of loperamide and N-desmethylloperamide following a fatal overdose. J Anal Toxicol. 2005 Oct;29(7):750-4. [2]. Kalgutkar AS, et al. Identification of an N-methyl-4-phenylpyridinium-like metabolite of the antidiarrheal agent loperamide in human liver microsomes: underlying reason(s) for the lack of neurotoxicity despite the bioactivation event. Drug Metab Dispos. 2004 Sep;32(9):943-52. [3]. Kannan P, et al. N-desmethyl-loperamide is selective for P-glycoprotein among three ATP-binding cassette transporters at the blood-brain barrier. Drug Metab Dispos. 2010 Jun;38(6):917-22. |
N-Desmethyl-loperamide
CAS: 66164-07-6 F: C28H31ClN2O2 W: 463.01
N-Desmethyl-loperamide is a major metabolite of loperamide, a drug that selectively activates peripheral μopioid recept
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