methysergide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| ergot alkaloid derivatives | 1775 | 361-37-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An ergot derivative that is a congener of LYSERGIC ACID DIETHYLAMIDE. It antagonizes the effects of serotonin in blood vessels and gastrointestinal smooth muscle, but has few of the properties of other ergot alkaloids. Methysergide is used prophylactically in migraine and other vascular headaches and to antagonize serotonin in the carcinoid syndrome.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 4 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Hosey CM, Chan R, Benet LZ |
| BA (Bioavailability) | 13 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| S (Water solubility) | 4.70 mg/mL | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Feb. 12, 1962 | FDA |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N02CA04 | NERVOUS SYSTEM ANALGESICS ANTIMIGRAINE PREPARATIONS Ergot alkaloids |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018490 | Serotonin Agents |
| MeSH PA | D012702 | Serotonin Antagonists |
| MeSH PA | D014662 | Vasoconstrictor Agents |
| CHEBI has role | CHEBI:48279 | serotonin antagonists |
| CHEBI has role | CHEBI:66991 | sympatholytic drug |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Migraine Prevention | indication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 13.6 | acidic |
| pKa2 | 6.73 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 2B | GPCR | AGONIST | Ki | 9.34 | SCIENTIFIC LITERATURE | IUPHAR | |||
| 5-hydroxytryptamine receptor 2C | GPCR | AGONIST | Ki | 8.34 | SCIENTIFIC LITERATURE | IUPHAR | |||
| Alpha-2A adrenergic receptor | GPCR | Ki | 6.21 | DRUG MATRIX | |||||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | IC50 | 6.04 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | PARTIAL AGONIST | Ki | 7.51 | DRUG MATRIX | ||||
| 5-hydroxytryptamine receptor 6 | GPCR | ANTAGONIST | Ki | 6.80 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 7 | GPCR | ANTAGONIST | Ki | 7.80 | IUPHAR | ||||
| Alpha-2B adrenergic receptor | GPCR | Ki | 5.66 | DRUG MATRIX | |||||
| D(3) dopamine receptor | GPCR | Ki | 7.23 | DRUG MATRIX | |||||
| Histamine H1 receptor | GPCR | Ki | 5.52 | PDSP | |||||
| Muscarinic acetylcholine receptor M1 | GPCR | Ki | 5.26 | PDSP | |||||
| Muscarinic acetylcholine receptor M2 | GPCR | Ki | 5.21 | PDSP | |||||
| Muscarinic acetylcholine receptor M3 | GPCR | Ki | 5.33 | PDSP | |||||
| 5-hydroxytryptamine receptor 1B | GPCR | ANTAGONIST | Ki | 7.60 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 1D | GPCR | ANTAGONIST | Ki | 8.90 | IUPHAR | ||||
| Alpha-2C adrenergic receptor | GPCR | Ki | 7.05 | PDSP | |||||
| 5-hydroxytryptamine receptor 5A | GPCR | ANTAGONIST | Ki | 7 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 1F | GPCR | ANTAGONIST | Ki | 8.20 | IUPHAR | ||||
| D(1A) dopamine receptor | GPCR | Ki | 6.33 | DRUG MATRIX | |||||
| Induced myeloid leukemia cell differentiation protein Mcl-1 | Cytosolic other | IC50 | 4.69 | CHEMBL | |||||
| Bcl-2-like protein 1 | Cytosolic other | IC50 | 4.65 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | AGONIST | Ki | 9.45 | SCIENTIFIC LITERATURE | ||||
| 5-hydroxytryptamine receptor 1E | GPCR | ANTAGONIST | Ki | 6.80 | IUPHAR | ||||
| D(2) dopamine receptor | GPCR | Ki | 6.57 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 1B | GPCR | Ki | 6.97 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | IC50 | 7.27 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | Ki | 8.80 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 7 | GPCR | Ki | 7.90 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 7 | GPCR | ANTAGONIST | Ki | 7.90 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 6 | GPCR | ANTAGONIST | Ki | 6.60 | IUPHAR | ||||
| Zinc finger protein mex-5 | Cytosolic other | EC50 | 4.91 | CHEMBL | |||||
| Serotonin 2 (5-HT2) receptor | GPCR | Ki | 8.28 | CHEMBL | |||||
| Cytoplasmic zinc-finger protein | Unclassified | EC50 | 4.99 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 5A | GPCR | ANTAGONIST | Ki | 6.70 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 5A | GPCR | ANTAGONIST | Ki | 7.20 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 1F | GPCR | ANTAGONIST | IC50 | 7.80 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| D00681 | KEGG_DRUG |
| 129-49-7 | SECONDARY_CAS_RN |
| 4018758 | VANDF |
| 4019833 | VANDF |
| C0025842 | UMLSCUI |
| CHEBI:584020 | CHEBI |
| H8J | PDB_CHEM_ID |
| CHEMBL1065 | ChEMBL_ID |
| CHEMBL485253 | ChEMBL_ID |
| DB00247 | DRUGBANK_ID |
| D008784 | MESH_DESCRIPTOR_UI |
| 9681 | PUBCHEM_CID |
| 134 | IUPHAR_LIGAND_ID |
| 1000 | INN_ID |
| XZA9HY6Z98 | UNII |
| 203190 | RXNORM |
| 1450 | MMSL |
| 5097 | MMSL |
| d00821 | MMSL |
| 003414 | NDDF |
| 004806 | NDDF |
| 11796006 | SNOMEDCT_US |
| 20340009 | SNOMEDCT_US |
| 387044000 | SNOMEDCT_US |
| CHEMBL3989558 | ChEMBL_ID |
| CHEMBL1200938 | ChEMBL_ID |
Pharmaceutical products:
None