Methysergide

NERVOUS SYSTEM

Key facts

Methysergide is an ofm drug catalogued in DrugCentral. It was first approved by the FDA in 1962. DrugCentral lists 36 molecular targets, including HTR2A, HTR2B and HTR1D. Recorded indications include Migraine Prevention.

• Approval status: ofm (first approved 1962 by the FDA).
• Molecular targets: HTR2A, HTR2B, HTR1D and Htr2a (36 listed in DrugCentral).
• Indications: Migraine Prevention.
• ATC code: N02CA04 (Ergot alkaloids).
• Molecular formula: C21H27N3O2; molecular weight 353.47 g/mol.

Indications & contraindications

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

Indications (1)

• Migraine Prevention

Mechanism & targets

Molecular targets (36)

Target	Gene	Action	Activity
5-hydroxytryptamine receptor 2A	HTR2A	agonist	Ki 9.45
5-hydroxytryptamine receptor 2B	HTR2B	agonist	Ki 9.34
5-hydroxytryptamine receptor 1D	HTR1D	antagonist	Ki 8.90
5-hydroxytryptamine receptor 2A	Htr2a	unknown	Ki 8.80
5-hydroxytryptamine receptor 2C	HTR2C	agonist	Ki 8.34
Serotonin 2 (5-HT2) receptor	Htr2c|Htr2a|Htr2b	unknown	Ki 8.28
5-hydroxytryptamine receptor 1F	HTR1F	antagonist	Ki 8.20
5-hydroxytryptamine receptor 7	Htr7	antagonist	Ki 7.90
5-hydroxytryptamine receptor 7	Htr7	unknown	Ki 7.90
5-hydroxytryptamine receptor 1F	Htr1f	antagonist	IC50 7.80
5-hydroxytryptamine receptor 7	HTR7	antagonist	Ki 7.80
5-hydroxytryptamine receptor 1B	HTR1B	antagonist	Ki 7.60
5-hydroxytryptamine receptor 1A	HTR1A	partial agonist	Ki 7.51
5-hydroxytryptamine receptor 1A	Htr1a	unknown	IC50 7.27
D(3) dopamine receptor	DRD3	unknown	Ki 7.23
5-hydroxytryptamine receptor 5A	Htr5a	antagonist	Ki 7.20
Alpha-2C adrenergic receptor	ADRA2C	unknown	Ki 7.05
5-hydroxytryptamine receptor 5A	HTR5A	antagonist	Ki 7.00
5-hydroxytryptamine receptor 1B	Htr1b	unknown	Ki 6.97
5-hydroxytryptamine receptor 1E	HTR1E	antagonist	Ki 6.80

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1962-02-12	FDA	—	—

ATC classification

ATC code	Therapeutic hierarchy
N02CA04	NERVOUS SYSTEM › ANALGESICS › ANTIMIGRAINE PREPARATIONS › Ergot alkaloids

Chemical structure

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

• Molecular formula: C₂₁H₂₇N₃O₂
• Molecular weight: 353.47 g/mol
• CAS number: 361-37-5
• InChIKey: KPJZHOPZRAFDTN-ZRGWGRIASA-N
• PubChem CID: 9681

CC[C@@H](CO)NC(=O)[C@H]1CN(C)[C@@H]2CC3=CN(C)C4=CC=CC(=C34)C2=C1

Frequently asked questions

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

What is Methysergide used for?

DrugCentral lists the following indications for Methysergide: Migraine Prevention.

How does Methysergide work?

Its molecular targets in DrugCentral include HTR2A (agonist), HTR2B (agonist), HTR1D (antagonist) and Htr2a.

When was Methysergide first approved?

Methysergide was first approved by the FDA in 1962.

What is the chemical formula of Methysergide?

Methysergide has the molecular formula C21H27N3O2 and a molecular weight of 353.47 g/mol.

Sources

• DrugCentral drug card 1775 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1065 — compound record and bioactivity
• PubChem CID 9681 — chemical identifiers
• DrugBank DB00247 — drug record
• FDA UNII XZA9HY6Z98 — substance identity
• DailyMed: FDA labels for Methysergide — current prescribing information (label search)
• UniProt P28223 (HTR2A) — target protein
• UniProt P41595 (HTR2B) — target protein
• UniProt P28221 (HTR1D) — target protein
• UniProt P28335 (HTR2C) — target protein
• UniProt P30939 (HTR1F) — target protein
• UniProt P34969 (HTR7) — target protein

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