Difenoxin Hydrochloride

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Cat Number

API35607364

CAS Number

35607-36-4

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Product Detail Description Customer Q&A

CAS Number

35607-36-4

Synonyms

Difenoxin HCl

Molecular Formula

C28H29ClN2O2

Molecular Weight

461

Smiles

C1CN(CCC1(C2=CC=CC=C2)C(=O)O)CCC(C#N)(C3=CC=CC=C3)C4=CC=CC=C4.Cl

General Description

Difenoxin Hydrochloride is the hydrochloride salt of difenoxin, a synthetic opioid antidiarrheal agent and the principal active metabolite of diphenoxylate. It is structurally related to meperidine but exhibits highly selective peripheral mu-opioid receptor activity in the gastrointestinal tract.

Mechanism of Action

Difenoxin Hydrochloride binds to mu-opioid receptors in the myenteric and submucosal plexuses of the gastrointestinal tract, reducing circular smooth muscle contraction and increasing segmental contractions. This decreases propulsive motility and intestinal fluid secretion while increasing water absorption.

Application

Indicated for the treatment of acute and chronic diarrhea. Difenoxin Hydrochloride is a synthetic opioid antidiarrheal and the active metabolite of diphenoxylate, providing selective peripheral mu-opioid receptor agonism in the gastrointestinal tract to reduce intestinal motility and fluid secretion.

How does Difenoxin compare to loperamide as an antidiarrheal?

Both act on peripheral gut mu-opioid receptors with limited CNS penetration, but Difenoxin is the active metabolite of diphenoxylate rather than a primary drug, offering a different pharmacokinetic profile.