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metergoline 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| ergot alkaloid derivatives | 1723 | 17692-51-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A dopamine agonist and serotonin antagonist. It has been used similarly to BROMOCRIPTINE as a dopamine agonist and also for MIGRAINE DISORDERS therapy.
|
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 23 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.57 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 9.60 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 0.93 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAP3K7,MAPK10,MAPK7,MAPKAPK2,MET,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKDC,TEK,TGFBR1 | 30 | |||
| kinase-selectivity-class | AXL,EIF2AK3 | 2 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
None
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 | G02CB05 | GENITO URINARY SYSTEM AND SEX HORMONES OTHER GYNECOLOGICALS OTHER GYNECOLOGICALS Prolactine inhibitors |
| MeSH PA | D012702 | Serotonin Antagonists |
| MeSH PA | D015259 | Dopamine Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018490 | Serotonin Agents |
| MeSH PA | D018491 | Dopamine Agonists |
| CHEBI has role | CHEBI:48279 | serotonergic antagonist |
| CHEBI has role | CHEBI:51065 | dopamine agonist |
| CHEBI has role | CHEBI:176497 | geroprotector |
Related Drugs by ATC class:
G02CB Prolactine inhibitors 5 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
None
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.11 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Substance-K receptor | GPCR | Ki | 5.87 | DRUG MATRIX | |||||
| D(1A) dopamine receptor | GPCR | Ki | 7.43 | DRUG MATRIX | |||||
| D(2) dopamine receptor | GPCR | Ki | 7.68 | DRUG MATRIX | |||||
| Alpha-2A adrenergic receptor | GPCR | Ki | 7.66 | DRUG MATRIX | |||||
| Sodium-dependent serotonin transporter | Transporter | Ki | 6.50 | DRUG MATRIX | |||||
| Sodium-dependent noradrenaline transporter | Transporter | Ki | 6.44 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 8.64 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | ANTAGONIST | Ki | 8.60 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 2B | GPCR | ANTAGONIST | Ki | 8.80 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 2C | GPCR | Ki | 9.30 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 6 | GPCR | ANTAGONIST | Ki | 7.40 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 7 | GPCR | Ki | 8.20 | CHEMBL | |||||
| Alpha-2B adrenergic receptor | GPCR | Ki | 8.12 | DRUG MATRIX | |||||
| D(3) dopamine receptor | GPCR | Ki | 8.58 | DRUG MATRIX | |||||
| Histamine H1 receptor | GPCR | Ki | 6.32 | DRUG MATRIX | |||||
| Histamine H2 receptor | GPCR | Ki | 6.02 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 1B | GPCR | ANTAGONIST | Ki | 7.20 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 1D | GPCR | ANTAGONIST | Ki | 9.20 | IUPHAR | ||||
| Alpha-2C adrenergic receptor | GPCR | Ki | 7.57 | DRUG MATRIX | |||||
| Sodium-dependent dopamine transporter | Transporter | Ki | 7.30 | DRUG MATRIX | |||||
| Cytochrome P450 2D6 | Enzyme | IC50 | 6.70 | DRUG MATRIX | |||||
| Alpha-1D adrenergic receptor | GPCR | Ki | 7.42 | DRUG MATRIX | |||||
| Acetylcholinesterase | Enzyme | IC50 | 5.87 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 5A | GPCR | ANTAGONIST | Ki | 6.20 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 1F | GPCR | ANTAGONIST | Ki | 6.50 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 1E | GPCR | ANTAGONIST | Ki | 6.10 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 4 | GPCR | Ki | 6.56 | DRUG MATRIX | |||||
| Alpha-1B adrenergic receptor | GPCR | Ki | 6.84 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 1B | GPCR | Ki | 7.60 | CHEMBL | |||||
| Alpha-1A adrenergic receptor | GPCR | IC50 | 7.02 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 8.22 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 7 | GPCR | Ki | 8.20 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 7 | GPCR | ANTAGONIST | Ki | 7.50 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 6 | GPCR | ANTAGONIST | Ki | 7.50 | IUPHAR | ||||
| Serotonin 1 (5-HT1) receptor | GPCR | Ki | 7.70 | CHEMBL | |||||
| Serotonin 2 (5-HT2) receptor | GPCR | Ki | 9.52 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| N0000167294 | NUI |
| D07218 | KEGG_DRUG |
| C0025641 | UMLSCUI |
| CHEBI:64216 | CHEBI |
| CHEMBL19215 | ChEMBL_ID |
| D008711 | MESH_DESCRIPTOR_UI |
| DB13520 | DRUGBANK_ID |
| 28693 | PUBCHEM_CID |
| 133 | IUPHAR_LIGAND_ID |
| 2378 | INN_ID |
| 1501393LY5 | UNII |
| 6834 | RXNORM |
| 006336 | NDDF |
| 1501393LY5 | INXIGHT DRUGS |
Pharmaceutical products:
None