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levallorphan 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| opioid receptor antagonists/agonists, morphinan derivates | 1560 | 152-02-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An opioid antagonist with properties similar to those of NALOXONE; in addition it also possesses some agonist properties. It should be used cautiously; levallorphan reverses severe opioid-induced respiratory depression but may exacerbate respiratory depression such as that induced by alcohol or other non-opioid central depressants. (From Martindale, The Extra Pharmacopoeia, 30th ed, p683)
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP2K6,MAP3K7,MAPK10,MAPK7,MAPKAPK2,MET,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ZAP70 | 45 | |||
| kinase-selectivity-class | EIF2AK3,GRK2 | 2 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| None | FDA | ROCHE |
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 |
|---|---|---|
| MeSH PA | D009292 | Narcotic Antagonists |
| MeSH PA | D018689 | Sensory System Agents |
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 | 10.05 | acidic |
| pKa2 | 9.05 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Mu-type opioid receptor | GPCR | ANTAGONIST | Ki | 9.32 | CHEMBL | CHEMBL | |||
| Mu-type opioid receptor | GPCR | IC50 | 9.20 | CHEMBL | |||||
| Acetylcholinesterase | Enzyme | Ki | 4.92 | CHEMBL | |||||
| Opioid receptor | GPCR | IC50 | 9.27 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| N0000167305 | NUI |
| D02238 | KEGG_DRUG |
| C0023554 | UMLSCUI |
| CHEBI:6431 | CHEBI |
| CHEMBL1254682 | ChEMBL_ID |
| DB00504 | DRUGBANK_ID |
| CHEMBL2062276 | ChEMBL_ID |
| D007977 | MESH_DESCRIPTOR_UI |
| 5359371 | PUBCHEM_CID |
| 7209 | IUPHAR_LIGAND_ID |
| 264 | INN_ID |
| 71-82-9 | SECONDARY_CAS_RN |
| 353613BU4U | UNII |
| 235419 | RXNORM |
| 001613 | NDDF |
| 004660 | NDDF |
| 17008002 | SNOMEDCT_US |
Pharmaceutical products:
None