talinolol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| beta-adrenoreceptor antagonists | 2557 | 57460-41-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Talinolol is a beta1-selective adrenoceptor antagonist well known for its cardioprotective and antihypertensive activity. By blocking beta1-adrenergic receptors, talinolol delays the conduction of stimuli in the AV node, reduces the sino-atrial conduction time, and impedes the sinus node automaticity.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.10 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 4 | Bocci G, Oprea TI, Benet LZ |
| S (Water solubility) | 0.02 mg/mL | Bocci G, Oprea TI, Benet LZ |
| EoM (Fraction excreted unchanged in urine) | 52.80 % | Benet LZ, Broccatelli F, Oprea TI |
| BA (Bioavailability) | 55 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 3.30 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 4.90 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.39 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 11 hours | Lombardo F, Berellini G, Obach RS |
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 | C07AB13 | CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS Beta blocking agents, selective |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D018674 | Adrenergic Antagonists |
| MeSH PA | D000319 | Adrenergic beta-Antagonists |
| MeSH PA | D000889 | Anti-Arrhythmia Agents |
| MeSH PA | D000959 | Antihypertensive Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Hypertensive disorder | indication | 38341003 | DOID:10763 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 12.9 | acidic |
| pKa2 | 13.52 | acidic |
| pKa3 | 9.31 | 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 | 6.62 | CHEMBL | |||||
| Beta-2 adrenergic receptor | GPCR | Ki | 6.05 | CHEMBL | |||||
| Multidrug resistance protein 1 | Transporter | WOMBAT-PK | |||||||
| Bifunctional epoxide hydrolase 2 | Enzyme | IC50 | 5.55 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D07184 | KEGG_DRUG |
| C0075783 | UMLSCUI |
| CHEBI:135533 | CHEBI |
| G3Q | PDB_CHEM_ID |
| CHEMBL152067 | ChEMBL_ID |
| DB11770 | DRUGBANK_ID |
| C011550 | MESH_SUPPLEMENTAL_RECORD_UI |
| 68770 | PUBCHEM_CID |
| 4664 | IUPHAR_LIGAND_ID |
| 3313 | INN_ID |
| 3S82268BKG | UNII |
| 37546 | RXNORM |
| 006590 | NDDF |
Pharmaceutical products:
None