N-Desmethyl Loperamide

TargetMol
Product Code: TAR-T33615
Supplier: TargetMol
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TAR-T33615-100mg100mgEnquire
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TAR-T33615-500mg500mgEnquire
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Overview

Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20°C

Images

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Further Information

Bioactivity:
N-Desmethyl Loperamide is the major metabolite of loperamide. It is also used as the precusor for radiolabelled loperamide.
CAS:
66164-07-6
Molecular Weight:
463.01
Purity:
0.98
SMILES:
O=C(NC)C(C=1C=CC=CC1)(C=2C=CC=CC2)CCN3CCC(O)(C4=CC=C(Cl)C=C4)CC3

References

Vaz RJ, Kang J, Luo Y, Rampe D. Molecular determinants of loperamide and N-desmethyl loperamide binding in the hERG cardiac K(+) channel. Bioorg Med Chem Lett. 2017 Dec 15. pii: S0960-894X(17)31181-2. doi: 10.1016/j.bmcl.2017.12.020. [Epub ahead of print] PubMed PMID: 29274816. Bhatti Z, Norsworthy J, Szombathy T. Loperamide metabolite-induced cardiomyopathy and QTc prolongation. Clin Toxicol (Phila). 2017 Aug;55(7):659-661. doi: 10.1080/15563650.2017.1304555. Epub 2017 Mar 28. PubMed PMID: 28349724. Wanek T, R?mermann K, Mairinger S, Stanek J, Sauberer M, Filip T, Traxl A, Kuntner C, Pahnke J, Bauer F, Erker T, L?scher W, M?ller M, Langer O. Factors Governing P-Glycoprotein-Mediated Drug-Drug Interactions at the Blood-Brain Barrier Measured with Positron Emission Tomography. Mol Pharm. 2015 Sep 8;12(9):3214-25. doi: 10.1021/acs.molpharmaceut.5b00168. Epub 2015 Aug 3. PubMed PMID: 26202880; PubMed Central PMCID: PMC4566129. Damont A, Goutal S, Auvity S, Valette H, Kuhnast B, Saba W, Tournier N. Imaging the impact of cyclosporin A and dipyridamole on P-glycoprotein (ABCB1) function at the blood-brain barrier: A [(11)C]-N-desmethyl-loperamide PET study in nonhuman primates. Eur J Pharm Sci. 2016 Aug 25;91:98-104. doi: 10.1016/j.ejps.2016.06.005. Epub 2016 Jun 7. PubMed PMID: 27283486.