Diphenoxylate
An opioid-related antidiarrheal agent used to reduce intestinal motility and treat acute and chronic diarrhea. It is combined with a small amount of atropine in commercial preparations (e.g., Lomotil) to discourage abuse, as the atropine causes unpleasant effects if large doses are taken. At recommended doses, very little is absorbed systemically.
Molecular Weight
452.6000 g/mol
LogP
5.70
TPSA
53.30 Ų
Lipinski RO5
Pass
Therapeutic Areas
Mechanism of Action
Binds to mu (μ), kappa (κ), and/or delta (δ) opioid receptors in the central and peripheral nervous system, mimicking endogenous endorphins. Activation of these G-protein-coupled receptors inhibits pain signal transmission and modulates the emotional response to pain.
Pharmacokinetics (PK)
Pharmacodynamics (PD)
Binds to mu (μ), kappa (κ), and/or delta (δ) opioid receptors in the central and peripheral nervous system, mimicking endogenous endorphins. Activation of these G-protein-coupled receptors inhibits pain signal transmission …
2D Structure
Cite this structure
Embed this structure
SMILES
CCOC(=O)C1(c2ccccc2)CCN(CCC(C#N)(c2ccccc2)c2ccccc2)CC1
InChI
InChI=1S/C30H32N2O2/c1-2-34-28(33)29(25-12-6-3-7-13-25)18-21-32(22-19-29)23-20-30(24-31,26-14-8-4-9-15-26)27-16-10-5-11-17-27/h3-17H,2,18-23H2,1H3
Molecular Formula
C30H32N2O2
HBD / HBA
- / 4
Rotatable Bonds
9
Heavy Atoms
34
No targets recorded
Target interaction data is not yet available for this drug.
No interactions recorded
Drug interaction data is not yet available for this compound.
No side effects recorded
Side effect data is not yet available for this drug.
Frequently Asked Questions
An opioid-related antidiarrheal agent used to reduce intestinal motility and treat acute and chronic diarrhea. It is combined with a small amount of atropine in commercial preparations (e.g., Lomotil) to discourage abuse, as the atropine causes unpleasant effects if large doses are taken. At recommended doses, very little is absorbed systemically.
Binds to mu (μ), kappa (κ), and/or delta (δ) opioid receptors in the central and peripheral nervous system, mimicking endogenous endorphins. Activation of these G-protein-coupled receptors inhibits pain signal transmission and modulates the emotional response to pain.
Yes, Diphenoxylate is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.
References & Data Sources
- ChEMBL — European Bioinformatics Institute (EBI). CHEMBL1201294. Open-access bioactivity database.
- PubChem — National Center for Biotechnology Information (NCBI). CID 13505. Chemical information database.
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-04.
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