lysergide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| ergot alkaloid derivatives | 1621 | 50-37-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Semisynthetic derivative of ergot (Claviceps purpurea). It has complex effects on serotonergic systems including antagonism at some peripheral serotonin receptors, both agonist and antagonist actions at central nervous system serotonin receptors, and possibly effects on serotonin turnover. It is a potent hallucinogen, but the mechanisms of that effect are not well understood.
|
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.03 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1957 | YEAR INTRODUCED |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Drug abuse | 128.82 | 95.73 | 46 | 348 | 99050 | 34857487 |
| Substance abuse | 100.65 | 95.73 | 22 | 372 | 7619 | 34948918 |
| Alcohol abuse | 99.28 | 95.73 | 20 | 374 | 4670 | 34951867 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Drug abuse | 161.54 | 106.04 | 53 | 435 | 162638 | 79581262 |
| Drug dependence | 144.58 | 106.04 | 36 | 452 | 40733 | 79703167 |
| Alcohol abuse | 115.18 | 106.04 | 21 | 467 | 5342 | 79738558 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D006213 | Hallucinogens |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D011619 | Psychotropic Drugs |
| MeSH PA | D018490 | Serotonin Agents |
| MeSH PA | D012702 | Serotonin Antagonists |
| MeSH PA | D017366 | Serotonin Receptor Agonists |
| CHEBI has role | CHEBI:35499 | hallucinogens |
| CHEBI has role | CHEBI:35941 | serotonin agonists |
| CHEBI has role | CHEBI:51065 | Dopamine receptor agonist |
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 | 12.56 | acidic |
| pKa2 | 6.52 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Beta-1 adrenergic receptor | GPCR | Ki | 6.85 | CHEMBL | |||||
| Beta-2 adrenergic receptor | GPCR | Ki | 6.13 | CHEMBL | |||||
| D(2) dopamine receptor | GPCR | EC50 | 6.98 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 8.86 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | Ki | 9.12 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 2B | GPCR | Ki | 7.52 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 2C | GPCR | Ki | 8.30 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 6 | GPCR | Ki | 8.40 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 7 | GPCR | Kd | 8.52 | CHEMBL | |||||
| D(3) dopamine receptor | GPCR | Ki | 6.90 | WOMBAT-PK | |||||
| D(1B) dopamine receptor | GPCR | Ki | 6.47 | CHEMBL | |||||
| Histamine H1 receptor | GPCR | Ki | 5.81 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 1D | GPCR | Ki | 8.41 | CHEMBL | |||||
| D(4) dopamine receptor | GPCR | Ki | 7.25 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 5A | GPCR | Ki | 8.05 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 1E | GPCR | Ki | 7.03 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 8.30 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | Ki | 8.46 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 7 | GPCR | Ki | 8.70 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 2C | GPCR | Ki | 8.42 | CHEMBL | |||||
| D(1A) dopamine receptor | GPCR | Ki | 6.74 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 6 | GPCR | AGONIST | Ki | 8.70 | IUPHAR | ||||
| Serotonin 2 (5-HT2) receptor | GPCR | Ki | 8.60 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| C0024334 | UMLSCUI |
| CHEBI:6605 | CHEBI |
| 7LD | PDB_CHEM_ID |
| CHEMBL263881 | ChEMBL_ID |
| DB04829 | DRUGBANK_ID |
| 5761 | PUBCHEM_CID |
| 17 | IUPHAR_LIGAND_ID |
| 729 | INN_ID |
| 8NA5SWF92O | UNII |
| 001637 | NDDF |
| 15698006 | SNOMEDCT_US |
| D008238 | MESH_DESCRIPTOR_UI |
Pharmaceutical products:
None