| Stereochemistry | RACEMIC |
| Molecular Formula | C20H33N3O3 |
| Molecular Weight | 363.4943 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)(C)NCC(O)COC1=CC=C(NC(=O)NC2CCCCC2)C=C1
InChI
InChIKey=MXFWWQICDIZSOA-UHFFFAOYSA-N
InChI=1S/C20H33N3O3/c1-20(2,3)21-13-17(24)14-26-18-11-9-16(10-12-18)23-19(25)22-15-7-5-4-6-8-15/h9-12,15,17,21,24H,4-8,13-14H2,1-3H3,(H2,22,23,25)
Talinolol (brand name Cordanurn) is the cardioselective beta-receptor antagonist which has been used for a long time in the treatment of various cardiovascular diseases and in tachyarrhythmia. The mean dosage is 10-20 mg intravenously administered over a period of 3-5 minutes, while the chronic oral dosage for this patient group amounts to 300mg/day. Cordanum eliminates the stimulating effect of catecholamines on the heart for physical and psychoemotional stress. The hypotensive effect is stabilized by the end of 2 weeks of course treatment. Reduces the frequency and severity of angina attacks; Contributes to the limitation of the heart attack zone and reduces the risk of arrhythmia in the presence of myocardial infarction, resulting in a decrease in mortality and the frequency of relapses. In average therapeutic doses, it has a less pronounced effect on the smooth muscles of the bronchi, myometrium, and peripheral arteries compared to non-selective beta-blockers. Talinolol is used in supraventricular (atrial fibrillation and flutter with high ventricular rate, paroxysmal supraventricular 1 tachycardia, sinus tachycardia) as well as ventricular extrasystoles and ventricular tachyarrhythmias. Patients with an increased tonus of the sympathetic nervous system related to sinus tachycardia, exercise-induced arrhythmias, hypertension, hyperthyroidism and coronary heart disease show a particularly positive reaction.
CNS Activity
Originator
Approval Year
Doses
AEs
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as perpetrator
Drug as victim
Tox targets
PubMed
Patents
Sample Use Guides
50 mg (1 table) 1-2 times a day or 100 mg (2 tablets) once a day.
Route of Administration:
Other
Caco-2 cells were used for activity evaluation. Transport experiments were performed at 37°C in Hanks’ Balanced Salt Solution (HBSS) containing 10 mM MES buffered to pH 6.5. Five milliliters of the prewarmed 0.25-5.0 mM rac-talinolol solution in buffered HBSS were added to either the apical (a) or the basolateral (b) side of the cell monolayer and drug-free buffered HBSS was added to the opposite side. Each chamber was bubbled with carbogen (95% O2, 5% CO2) for homogeneous mixing of each cell’s contents. The permeation experiment lasted for 2 hours. Samples (600 mkl) were taken every 20 minutes (for apical-to-basal transports from the basal side and vice versa) and were replaced with equal volumes of fresh buffered HBSS immediately. The samples were stored at — 20°C until analysis. Experiments with the P-gp inhibitor verapamil were performed at 500 jjlM verapamil concentrations on the apical and basolateral side; verapamil concentrations of 100 mkM have already been reported to reduce the efflux of drugs
ACTIVE MOIETY
