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perhexiline 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2106 | 6621-47-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
2-(2,2-Dicyclohexylethyl)piperidine. Coronary vasodilator used especially for angina of effort. It may cause neuropathy and hepatitis.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.20 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.00 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 18.02 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 73.50 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 1 | High | 1 |
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 | C08EX02 | CARDIOVASCULAR SYSTEM CALCIUM CHANNEL BLOCKERS NON-SELECTIVE CALCIUM CHANNEL BLOCKERS Other non-selective calcium channel blockers |
| MeSH PA | D000077264 | Calcium-Regulating Hormones and Agents |
| MeSH PA | D002121 | Calcium Channel Blockers |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D014665 | Vasodilator Agents |
| MeSH PA | D049990 | Membrane Transport Modulators |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
Related Drugs by ATC class:
C08EX Other non-selective calcium channel blockers 1 drug
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 | 10.2 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 5.96 | DRUG MATRIX | |||||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 5.11 | CHEMBL | |||||
| Sodium-dependent noradrenaline transporter | Transporter | Ki | 5.49 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M1 | GPCR | Ki | 6.19 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M3 | GPCR | Ki | 6.18 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M4 | GPCR | Ki | 6.30 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M5 | GPCR | Ki | 6.11 | DRUG MATRIX | |||||
| Cytochrome P450 2D6 | Enzyme | IC50 | 6.03 | DRUG MATRIX | |||||
| Voltage-dependent T-type calcium channel subunit alpha-1G | Ion channel | WOMBAT-PK | |||||||
| Voltage-dependent T-type calcium channel subunit alpha-1H | Ion channel | Ki | 5.36 | WOMBAT-PK | |||||
| Voltage-dependent T-type calcium channel subunit alpha-1I | Ion channel | WOMBAT-PK | |||||||
| Carnitine O-palmitoyltransferase 1, liver isoform | Enzyme | WOMBAT-PK | |||||||
| Carnitine O-palmitoyltransferase 2, mitochondrial | Enzyme | IC50 | 4.14 | CHEMBL | |||||
| Epidermal growth factor receptor | Kinase | IC50 | 5.83 | DRUG MATRIX | |||||
| Tyrosine-protein kinase Fyn | Kinase | IC50 | 5.39 | DRUG MATRIX | |||||
| Carnitine O-palmitoyltransferase 1, muscle isoform | Enzyme | IC50 | 4.96 | CHEMBL | |||||
| Adrenergic receptor alpha-1 | GPCR | Kd | 6.70 | CHEMBL | |||||
| Carnitine palmitoyltransferase 2 | Enzyme | IC50 | 4.10 | CHEMBL | |||||
| Carnitine palmitoyltransferase 1A | Enzyme | IC50 | 4.11 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D05442 | KEGG_DRUG |
| 6724-53-4 | SECONDARY_CAS_RN |
| C0031013 | UMLSCUI |
| CHEBI:35553 | CHEBI |
| CHEMBL75880 | ChEMBL_ID |
| CHEMBL1334033 | ChEMBL_ID |
| DB01074 | DRUGBANK_ID |
| D010480 | MESH_DESCRIPTOR_UI |
| 4746 | PUBCHEM_CID |
| C023470 | MESH_SUPPLEMENTAL_RECORD_UI |
| 1850 | INN_ID |
| KU65374X44 | UNII |
| 33169 | RXNORM |
| 005713 | NDDF |
| 005714 | NDDF |
| 1332137007 | SNOMEDCT_US |
| 421776000 | SNOMEDCT_US |
| 421817009 | SNOMEDCT_US |
| KU65374X44 | INXIGHT DRUGS |
Pharmaceutical products:
None