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mazindol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 1640 | 22232-71-9 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Tricyclic anorexigenic agent unrelated to and less toxic than AMPHETAMINE, but with some similar side effects. It inhibits uptake of catecholamines and blocks the binding of cocaine to the dopamine uptake transporter.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.12 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 93 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| S (Water solubility) | 0.14 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,BRAF,EIF2AK3,GRK2,ITK,PDK1,PDK2,PDK4 | 8 | |||
| kinase-selectivity-class | AXL,GRK2 | 2 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 14, 1973 | 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 | A08AA05 | ALIMENTARY TRACT AND METABOLISM ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS ANTIOBESITY PREPARATIONS, EXCL. DIET PRODUCTS Centrally acting antiobesity products |
| MeSH PA | D000697 | Central Nervous System Stimulants |
| MeSH PA | D014179 | Neurotransmitter Uptake Inhibitors |
| MeSH PA | D015259 | Dopamine Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D018759 | Adrenergic Uptake Inhibitors |
| MeSH PA | D018765 | Dopamine Uptake Inhibitors |
| MeSH PA | D049990 | Membrane Transport Modulators |
| CHEBI has role | CHEBI:74518 | anti-obesity agent |
Related Drugs by ATC class:
A08AA Centrally acting antiobesity products 15 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Obesity | indication | 414916001 | DOID:9970 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 12.93 | acidic |
| pKa2 | 10.1 | 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 serotonin transporter | Transporter | INHIBITOR | Ki | 7.30 | CHEMBL | CHEMBL | |||
| Sodium-dependent dopamine transporter | Transporter | INHIBITOR | Ki | 8 | CHEMBL | CHEMBL | |||
| Sodium-dependent noradrenaline transporter | Transporter | INHIBITOR | Kd | 9.30 | CHEMBL | CHEMBL | |||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | IC50 | 6.63 | CHEMBL | |||||
| Histamine H1 receptor | GPCR | Ki | 6.22 | PDSP | |||||
| Sodium-dependent dopamine transporter | Transporter | Kd | 8.06 | CHEMBL | |||||
| Transporter | Transporter | Ki | 9.10 | CHEMBL | |||||
| Sodium-dependent dopamine transporter | Transporter | IC50 | 7.89 | CHEMBL | |||||
| Sodium-dependent serotonin transporter | Transporter | Ki | 6.61 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4018025 | VUID |
| N0000146368 | NUI |
| D00367 | KEGG_DRUG |
| 4018025 | VANDF |
| C0024977 | UMLSCUI |
| CHEBI:6702 | CHEBI |
| CHEMBL781 | ChEMBL_ID |
| DB00579 | DRUGBANK_ID |
| D008454 | MESH_DESCRIPTOR_UI |
| 4020 | PUBCHEM_CID |
| 4797 | IUPHAR_LIGAND_ID |
| 2895 | INN_ID |
| C56709M5NH | UNII |
| 227434 | RXNORM |
| 1629 | MMSL |
| 5025 | MMSL |
| d00811 | MMSL |
| 001874 | NDDF |
| 387232005 | SNOMEDCT_US |
| 4194004 | SNOMEDCT_US |
Pharmaceutical products:
None