Methapyrilene Fumarate

CHEMBL3187246 Phase 4 已批准 Small molecule
Half-Life
Bioavailability
Protein Binding
Molecular Weight
871.0 g/mol
LogP
Phase
4

A fumarate form of methapyrilene with the same therapeutic properties. An antihistamine formerly used to treat allergy symptoms and as a sleep aid, this medication was withdrawn from the market after studies showed it caused liver cancer in animals.

分子量

871.0000 g/mol

TPSA

319.00 Ų

作用机制

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)

机制

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.

二维结构

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SMILES

CN(C)CCN(Cc1cccs1)c1ccccn1.CN(C)CCN(Cc1cccs1)c1ccccn1.O=C(O)/C=C/C(=O)O.O=C(O)/C=C/C(=O)O.O=C(O)/C=C/C(=O)O

InChI

InChI=1S/2C14H19N3S.3C4H4O4/c2*1-16(2)9-10-17(12-13-6-5-11-18-13)14-7-3-4-8-15-14;3*5-3(6)1-2-4(7)8/h2*3-8,11H,9-10,12H2,1-2H3;3*1-2H,(H,5,6)(H,7,8)/b;;3*2-1+

Molecular Formula

C40H50N6O12S2

HBD / HBA

6 / 20

可旋转键数

18

重原子数

60

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.

常见问题

A fumarate form of methapyrilene with the same therapeutic properties. An antihistamine formerly used to treat allergy symptoms and as a sleep aid, this medication was withdrawn from the market after studies showed it caused liver cancer in animals.

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, Methapyrilene Fumarate is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.

{# References & Data Sources section for drug detail pages. Renders standard pharmacological database links plus the drug's data_sources field. #}

References & Data Sources

  • ChEMBL — European Bioinformatics Institute (EBI). CHEMBL3187246. Open-access bioactivity database.
  • PubChem — National Center for Biotechnology Information (NCBI). CID 6436730. Chemical information database.

Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.

医疗免责声明

This content is for educational and informational purposes only. It is not a substitute for professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before making medication decisions.

Data sources: ChEMBL, PubChem, DailyMed.