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prenylamine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2261 | 390-64-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A drug formerly used in the treatment of angina pectoris but superseded by less hazardous drugs. Prenylamine depletes myocardial catecholamine stores and has some calcium channel blocking activity. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1406)
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.12 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 15 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 3.341 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 4.130 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 9.016 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 17.742 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 1.210 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 5.880 | % | High | 1 |
| herg | hERG pIC50 | 6.341 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 17.179 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 61.518 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 1.480 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT1,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK | 50 | |||
| kinase-selectivity-class | AKT3,AXL,EIF2AK3,GRK2,PDK4,SIK2,STK33 | 7 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 3.027 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 144.544 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 2.200 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 10.814 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 8.340 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 287.740 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 7.610 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 2.500 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 251.189 | uM | 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 | C01DX02 | CARDIOVASCULAR SYSTEM CARDIAC THERAPY VASODILATORS USED IN CARDIAC DISEASES Other vasodilators used in cardiac diseases |
| ATC | C01DX52 | CARDIOVASCULAR SYSTEM CARDIAC THERAPY VASODILATORS USED IN CARDIAC DISEASES Other vasodilators used in cardiac diseases |
| 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 | D018377 | Neurotransmitter Agents |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D049990 | Membrane Transport Modulators |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
Related Drugs by ATC class:
C01DX Other vasodilators used in cardiac diseases 18 drugs
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 | 9.32 | 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 channel alpha subunits; brain (Types I, II, III) | Ion channel | IC50 | 6.52 | CHEMBL | |||||
| Voltage-gated L-type calcium channel | Ion channel | Kd | 6.68 | CHEMBL | |||||
| Calmodulin | Cytosolic other | Kd | 6.30 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D02167 | KEGG_DRUG |
| 69-43-2 | SECONDARY_CAS_RN |
| C0033059 | UMLSCUI |
| CHEBI:8397 | CHEBI |
| CHEMBL24072 | ChEMBL_ID |
| DB04825 | DRUGBANK_ID |
| D011299 | MESH_DESCRIPTOR_UI |
| 9801 | PUBCHEM_CID |
| C053347 | MESH_SUPPLEMENTAL_RECORD_UI |
| 1196 | INN_ID |
| K2OH82Z000 | UNII |
| 34407 | RXNORM |
| 004026 | NDDF |
| 004027 | NDDF |
| 387288001 | SNOMEDCT_US |
| 51908007 | SNOMEDCT_US |
| K2OH82Z000 | INXIGHT DRUGS |
Pharmaceutical products:
None