66164-07-6
66164-07-6
Chemical Structure
N-Desmethyl-loperamide
- CAS No.: 66164-07-6
- Formula:C28H31ClN2O2
- Molecular Weight:463.01
IUPAC Name: 4-(4-(4-chlorophenyl)-4-hydroxypiperidin-1-yl)-N-methyl-2,2-diphenylbutanamide
InChIKey: ZMOPTLXEYOVARP-UHFFFAOYSA-N
SMILES: O=C(C(C1=CC=CC=C1)(CCN2CCC(C3=CC=C(C=C3)Cl)(CC2)O)C4=CC=CC=C4)NC
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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N-Desmethyl-loperamide | 98.36% | 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. | ||||||||||||||||||||
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N-Desmethyl-loperamide-d3 | N-Desmethyl-loperamide-d3 is the deuterium labeled N-Desmethyl-loperamide. | |||||||||||||||||||||
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References
- [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. [Content Brief]
- [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. [Content Brief]
- [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. [Content Brief]
