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prenalterol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| bronchodilators, phenethylamine derivatives | 2258 | 57526-81-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A partial adrenergic agonist with functional beta 1-receptor specificity and inotropic effect. It is effective in the treatment of acute CARDIAC FAILURE, postmyocardial infarction low-output syndrome, SHOCK, and reducing ORTHOSTATIC HYPOTENSION in the SHY-RAGER SYNDROME.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 10 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 1.48 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 33 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 4.28 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 22.10 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 2.85 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -1.253 | Moderate | 0.74 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.488 | Moderate | 0.74 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 0.929 | 10^-6 cm/s | Moderate | 0.74 |
| dh-clint | Dog hepatocyte intrinsic clearance | 7.079 | uL/min/10^6 cells | Moderate | 0.74 |
| dppb | Dog plasma protein binding (% unbound) | 90.420 | % | Moderate | 0.74 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 81.980 | % | Moderate | 0.74 |
| herg | hERG pIC50 | 4.111 | pIC50 | Moderate | 0.74 |
| hh-clint | Human hepatocyte intrinsic clearance | 2.716 | uL/min/10^6 cells | Moderate | 0.74 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.673 | uL/min/mg protein | Moderate | 0.74 |
| hppb | Human plasma protein binding (% unbound) | 91.830 | % | Moderate | 0.74 |
| kinase-safety-class | ACVR2A,ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,IKBKB,ITK,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK7,MAPKAPK2,NTRK2,PDK2,PDK4,PIK3CB,PIM2,PLK1,PRKDC,SIK2,STK33,SYK,TEK,TGFBR1,ZAP70 | 38 | |||
| kinase-selectivity-class | AXL,CAMK2D,CDK4,EIF2AK3,GRK2,SIK2,TEK | 7 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 1.050 | Moderate | 0.67 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.735 | Moderate | 0.74 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 44.055 | Moderate | 0.74 | |
| mppb | Mouse plasma protein binding (% unbound) | 91.690 | Moderate | 0.74 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.678 | Moderate | 0.74 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 0 | Moderate | 0.65 | |
| pppb | Pig plasma protein binding (% unbound) | 90.200 | % | Moderate | 0.74 |
| rat-kpuu-brain | Rat brain Kpuu | 0.110 | % | Moderate | 0.67 |
| rh-clint | Rat hepatocyte intrinsic clearance | 18.239 | uL/min/10^6 cells | Moderate | 0.74 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 94.250 | % | Moderate | 0.74 |
| rppb | Rat plasma protein binding (% unbound) | 86.180 | % | Moderate | 0.74 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 879.023 | uM | Moderate | 0.74 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1980 | YEAR INTRODUCED |
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 | C01CA13 | CARDIOVASCULAR SYSTEM CARDIAC THERAPY CARDIAC STIMULANTS EXCL. CARDIAC GLYCOSIDES Adrenergic and dopaminergic agents |
| MeSH PA | D000318 | Adrenergic beta-Agonists |
| MeSH PA | D002316 | Cardiotonic Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D013566 | Sympathomimetics |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D020011 | Protective Agents |
| MeSH PA | D058665 | Adrenergic beta-1 Receptor Agonists |
Related Drugs by ATC class:
C01CA Adrenergic and dopaminergic agents 25 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 | 10.48 | acidic |
| pKa2 | 9.19 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Beta-1 adrenergic receptor | GPCR | Ki | 6.60 | WOMBAT-PK | |||||
| Beta-2 adrenergic receptor | GPCR | Kd | 5.97 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| C0033051 | UMLSCUI |
| CHEBI:8391 | CHEBI |
| CHEMBL1160714 | ChEMBL_ID |
| DB13777 | DRUGBANK_ID |
| D011294 | MESH_DESCRIPTOR_UI |
| 42396 | PUBCHEM_CID |
| 537 | IUPHAR_LIGAND_ID |
| 4121 | INN_ID |
| M4G34404CX | UNII |
| M4G34404CX | INXIGHT DRUGS |
Pharmaceutical products:
None