Lofexidine
A central alpha-2 adrenergic agonist used to manage the physical symptoms of opioid withdrawal and as an adjunct in treating ADHD. It reduces the release of norepinephrine to ease symptoms like anxiety, agitation, sweating, and muscle aches.
Molecular Weight
259.1300 g/mol
LogP
2.60
TPSA
33.60 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
CC(Oc1c(Cl)cccc1Cl)C1=NCCN1
InChI
InChI=1S/C11H12Cl2N2O/c1-7(11-14-5-6-15-11)16-10-8(12)3-2-4-9(10)13/h2-4,7H,5-6H2,1H3,(H,14,15)
Molecular Formula
C11H12Cl2N2O
HBD / HBA
1 / 2
Rotatable Bonds
3
Heavy Atoms
16
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
A central alpha-2 adrenergic agonist used to manage the physical symptoms of opioid withdrawal and as an adjunct in treating ADHD. It reduces the release of norepinephrine to ease symptoms like anxiety, agitation, sweating, and muscle aches.
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, Lofexidine 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). CHEMBL17860. Open-access bioactivity database.
- PubChem — National Center for Biotechnology Information (NCBI). CID 30668. Chemical information database.
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-04.
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