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toliprolol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| beta-adrenoreceptor antagonists | 3616 | 2933-94-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
was MH 1975-92 (see under PROPANOLAMINES 1981-90, was DOBEROL see under PROPANOLAMINES 1975-80); KOE 592 was see TOLIPROLOL 1975-92; use PROPANOLAMINES to search TOLIPROLOL 1975-92; beta adrenergic blockader with some stimulant action; it has been proposed for angina pectoris
|
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 90 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 0.220 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.332 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 39.355 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 22.080 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 64.110 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 69.660 | % | High | 1 |
| herg | hERG pIC50 | 4.291 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 6.730 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 7.129 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 77.010 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,IKBKB,ITK,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK7,MET,NTRK2,PDK2,PDK4,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TGFBR1,ZAP70 | 38 | |||
| kinase-selectivity-class | AXL,CDK4,EIF2AK3,GRK2,PDK4 | 5 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.497 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 141.906 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 70.910 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.735 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 67.630 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 299.226 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 89.790 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 74.340 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 972.747 | 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:
None
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 | 9.19 | 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 | Kd | 9.42 | CHEMBL | |||||
| Beta-2 adrenergic receptor | GPCR | Kd | 8.92 | CHEMBL | |||||
| Beta-2 adrenergic receptor | GPCR | Kd | 7.36 | CHEMBL | |||||
| Beta-1 adrenergic receptor | GPCR | Kd | 8.75 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| C0033442 | UMLSCUI |
| CHEBI:134918 | CHEBI |
| CHEMBL67096 | ChEMBL_ID |
| 18047 | PUBCHEM_CID |
| C073327 | MESH_SUPPLEMENTAL_RECORD_UI |
| 3318 | INN_ID |
| DCP58J201D | UNII |
Pharmaceutical products:
None