Phenoxybenzamine

alpha-Adrenergic Blocker — CARDIOVASCULAR SYSTEM

Key facts

Phenoxybenzamine is an ofp drug in the alpha-Adrenergic Blocker class catalogued in DrugCentral. It was first approved by the FDA in 1953. Its mechanism of action is classified as Adrenergic alpha-Antagonists. DrugCentral lists 8 molecular targets, including Adra1b|Adra1d|Adra1a, ADRA2B and ADRA1D. Recorded indications include Pheochromocytoma.

• Approval status: ofp (first approved 1953 by the FDA).
• Drug class: alpha-Adrenergic Blocker.
• Mechanism of action: Adrenergic alpha-Antagonists.
• Molecular targets: Adra1b|Adra1d|Adra1a, ADRA2B, ADRA1D and ADRA1A (8 listed in DrugCentral).
• Indications: Pheochromocytoma.
• ATC code: C04AX02 (Other peripheral vasodilators).
• Molecular formula: C18H22ClNO; molecular weight 303.83 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Pheochromocytoma

Contraindications (5)

• Acute cerebrovascular insufficiency
• Disorder of coronary artery
• Kidney disease
• Low blood pressure
• Lower respiratory tract infection

Mechanism & targets

• Mechanism of action (MoA): Adrenergic alpha-Antagonists
• Established pharmacologic class: alpha-Adrenergic Blocker

Molecular targets (8)

Target	Gene	Action	Activity
Adrenergic receptor alpha-1	Adra1b|Adra1d|Adra1a	unknown	Ki 8.74
Alpha-2B adrenergic receptor	ADRA2B	antagonist	Ki 8.46
Alpha-1D adrenergic receptor	ADRA1D	antagonist	Ki 8.40
Alpha-1A adrenergic receptor	ADRA1A	antagonist	IC50 7.27
Dopamine receptor	Drd1|Drd3|Drd5|Drd4|Drd2	unknown	Ki 6.92
Alpha-2A adrenergic receptor	ADRA2A	antagonist	IC50 6.28
Solute carrier family 22 member 1	SLC22A1	unknown	IC50 4.82
Sodium channel alpha subunits; brain (Types I, II, III)	SCN1A|SCN2A|SCN3A	unknown	IC50 4.35

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1953-01-26	FDA	—	COVIS PHARMA SARL

ATC classification

ATC code	Therapeutic hierarchy
C04AX02	CARDIOVASCULAR SYSTEM › PERIPHERAL VASODILATORS › PERIPHERAL VASODILATORS › Other peripheral vasodilators

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Phenoxybenzamine is on its molecule page.

• Molecular formula: C₁₈H₂₂ClNO
• Molecular weight: 303.83 g/mol
• CAS number: 59-96-1
• InChIKey: QZVCTJOXCFMACW-UHFFFAOYSA-N
• PubChem CID: 4768

CC(COC1=CC=CC=C1)N(CCCl)CC1=CC=CC=C1

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Phenoxybenzamine used for?

DrugCentral lists the following indications for Phenoxybenzamine: Pheochromocytoma.

How does Phenoxybenzamine work?

Phenoxybenzamine is classified as Adrenergic alpha-Antagonists; its molecular targets in DrugCentral include Adra1b|Adra1d|Adra1a, ADRA2B (antagonist), ADRA1D (antagonist) and ADRA1A (antagonist).

When was Phenoxybenzamine first approved?

Phenoxybenzamine was first approved by the FDA in 1953.

What drug class does Phenoxybenzamine belong to?

Phenoxybenzamine is in the alpha-Adrenergic Blocker class.

What is the chemical formula of Phenoxybenzamine?

Phenoxybenzamine has the molecular formula C18H22ClNO and a molecular weight of 303.83 g/mol.

Sources

• DrugCentral drug card 2136 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1200787 — compound record and bioactivity
• PubChem CID 4768 — chemical identifiers
• DrugBank DB00925 — drug record
• FDA UNII 0TTZ664R7Z — substance identity
• DailyMed: FDA labels for Phenoxybenzamine — current prescribing information (label search)
• UniProt P18089 (ADRA2B) — target protein
• UniProt P25100 (ADRA1D) — target protein
• UniProt P35348 (ADRA1A) — target protein
• UniProt P08913 (ADRA2A) — target protein
• UniProt O15245 (SLC22A1) — target protein

How this page is built: methodology · editorial policy & corrections.