lofepramine Indications/Contra | FAERs | Orange Book | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| substances of the imipramine group | 1592 | 23047-25-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A psychotropic IMIPRAMINE derivative that acts as a tricyclic antidepressant and possesses few anticholinergic properties. It is metabolized to DESIPRAMINE.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.11 | g | O |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1977 | YEAR INTRODUCED |
FDA Adverse Event Reporting System
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N06AA07 | NERVOUS SYSTEM PSYCHOANALEPTICS ANTIDEPRESSANTS Non-selective monoamine reuptake inhibitors |
| MeSH PA | D000928 | Antidepressive Agents |
| MeSH PA | D000929 | Antidepressive Agents, Tricyclic |
| MeSH PA | D002491 | Central Nervous System Agents |
| MeSH PA | D011619 | Psychotropic Drugs |
| CHEBI has role | CHEBI:35469 | antidepressant |
Drug Use (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Depressive disorder | indication | 35489007 | DOID:2848 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 7.05 | Basic |
| pKa2 | 5.01 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Sodium-dependent noradrenaline transporter | Transporter | INHIBITOR | Ki | 8.27 | WOMBAT-PK | IUPHAR | |||
| Sodium-dependent serotonin transporter | Transporter | INHIBITOR | Ki | 7.15 | WOMBAT-PK | IUPHAR | |||
| Muscarinic acetylcholine receptor M5 | GPCR | Ki | 6.34 | WOMBAT-PK | |||||
| Muscarinic acetylcholine receptor M4 | GPCR | Ki | 6.47 | WOMBAT-PK | |||||
| Muscarinic acetylcholine receptor M3 | GPCR | Ki | 6.89 | WOMBAT-PK | |||||
| Muscarinic acetylcholine receptor M2 | GPCR | Ki | 6.48 | WOMBAT-PK | |||||
| D(2) dopamine receptor | GPCR | Ki | 5.70 | PDSP | |||||
| Histamine H1 receptor | GPCR | Ki | 6.44 | WOMBAT-PK | |||||
| Alpha-1A adrenergic receptor | GPCR | Ki | 7 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 2C | GPCR | Ki | 6.70 | WOMBAT-PK | |||||
| Muscarinic acetylcholine receptor M1 | GPCR | Ki | 7.17 | WOMBAT-PK | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 5.34 | PDSP |
External reference:
| ID | Source |
|---|---|
| N0000167255 | NUI |
| C0023961 | UMLSCUI |
| 7551 | IUPHAR_LIGAND_ID |
| D01285 | KEGG_DRUG |
| 6465 | RXNORM |
| 321831005 | SNOMEDCT_US |
| 395772004 | SNOMEDCT_US |
| N0000167255 | NDFRT |
| 004095 | NDDF |
| CHEMBL87708 | ChEMBL_ID |
| 3947 | PUBCHEM_CID |
| CHEMBL2106638 | ChEMBL_ID |
| D008127 | MESH_DESCRIPTOR_UI |
| OCA4JT7PAW | UNII |
| 2909 | INN_ID |
| 26786-32-3 | SECONDARY_CAS_RN |
| CHEBI:47782 | CHEBI |
Pharmaceutical products:
None