Chlorpheniramine
A first-generation antihistamine of the alkylamine class that blocks H1 receptors to relieve allergic rhinitis, hay fever, urticaria, and cold symptoms. It crosses the blood-brain barrier and commonly causes sedation. It is widely available in over-the-counter preparations, often in combination with decongestants and analgesics.
Molecular Weight
274.7900 g/mol
LogP
3.40
TPSA
16.10 Ų
Lipinski RO5
Pass
Therapeutic Areas
Mechanism of Action
Competitively blocks histamine H1 receptors on effector cells, preventing histamine-mediated vasodilation, increased vascular permeability, bronchoconstriction, and pruritus. First-generation agents also cross the blood-brain barrier, causing sedation.
Pharmacokinetics (PK)
Pharmacodynamics (PD)
Competitively blocks histamine H1 receptors on effector cells, preventing histamine-mediated vasodilation, increased vascular permeability, bronchoconstriction, and pruritus. First-generation agents also cross the blood-brain barrier, causing sedation.
2D Structure
Cite this structure
Embed this structure
SMILES
CN(C)CCC(c1ccc(Cl)cc1)c1ccccn1
InChI
InChI=1S/C16H19ClN2/c1-19(2)12-10-15(16-5-3-4-11-18-16)13-6-8-14(17)9-7-13/h3-9,11,15H,10,12H2,1-2H3
Molecular Formula
C16H19ClN2
HBD / HBA
- / 2
Rotatable Bonds
5
Heavy Atoms
19
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 first-generation antihistamine of the alkylamine class that blocks H1 receptors to relieve allergic rhinitis, hay fever, urticaria, and cold symptoms. It crosses the blood-brain barrier and commonly causes sedation. It is widely available in over-the-counter preparations, often in combination with decongestants and analgesics.
Competitively blocks histamine H1 receptors on effector cells, preventing histamine-mediated vasodilation, increased vascular permeability, bronchoconstriction, and pruritus. First-generation agents also cross the blood-brain barrier, causing sedation.
Yes, Chlorpheniramine 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). CHEMBL505. Open-access bioactivity database.
- PubChem — National Center for Biotechnology Information (NCBI). CID 2725. Chemical information database.
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-04.
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