Ligand id: 7164

Name: diphenoxylate

IUPHAR Pharmacology Education Project (PEP) logo

View more information in the IUPHAR Pharmacology Education Project: diphenoxylate

Structure and Physico-chemical Properties

2D Structure
Click here for structure editor
Calculated Physico-chemical Properties
Hydrogen bond acceptors 4
Hydrogen bond donors 0
Rotatable bonds 9
Topological polar surface area 53.33
Molecular weight 452.25
XLogP 6.29
No. Lipinski's rules broken 1

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Used to treat diarrhea. The US FDA website only has records for this compound as an active component in formulations also containing atropine. Such formulations appear to have been approved since at least 1960. Neither the EMA or eMC list any drugs containing diphenoxylate.
Mechanism Of Action and Pharmacodynamic Effects
Diphenoxylate is a chemical relative of pethidine, an opioid analgesic. CHEMBL list the drug target as the μ opioid receptor (OPRM1). This drug is believed to increase intestinal transit time by slowing peristalsis. This allows the gut to re-absorb more water, producing firmer stools. See the DrugBank link for further details.