N-Desmethyl-loperamide

N-Desmethyl-loperamide

Loperamide is a synthetic opiate that efficiently and selectively activates the μ opioid receptors Ki = 0.16 nM, exclusively at the periphery. N-Desmethyl-loperamide (dLop) is the main metabolite of loperamide. dLop is a substrate of an ATP-dependent outflow conveyor, P-glycoprotein. As a result, both the initial compound and the mapping of metabolites, limited by passage through the blood, can be analyzed by various methods.

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Loperamide is an anti-diarrheal agent that is available as various over-the-counter products for treating diarrhea.7 The drug was first synthesized in 1969 and used medically in 1976.1 It is a highly lipophilic synthetic phenylpiperidine opioid 1 that is structurally similar to opiate receptor agonists such as diphenoxylate and haloperidol.2 Due to pharmacological properties, loperamide has been misused and abused to self-manage opioid withdrawal symptoms and to induce euphoria.1,4 However, loperamide is associated with a risk for experiencing a range of adverse effects, often life-threatening, if taking for non-therapeutic reasons or at doses higher than the recommended dose.8

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N-Desmethyl-loperamide is intended for Pharmaceuticals applications. All information about N-Desmethyl-loperamide is provided in the MSDS. We deliver compounds with high purity levels and a comprehensive Certificate of Analysis. Connect to your member account to consult the documents.