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| | Talinolol Basic information |
| Product Name: | Talinolol | | Synonyms: | 1-(3-(3-Cyclohexylureido)phenoxy)-3-(tert-butylamino)-2-propanol;1-(4-(Cyclohexylureido)phenoxy)-3-(tert-butylamino)-2-propanol;1-(4-Cyclohexylureidophenoxy)-2-hydroxy-3-tert-butylaminopropane;Cordanum;Racemic talinolol;rac-Talinolol
;1-(4-(3-(tert-butylamino)-2-hydroxypropoxy)phenyl)-3-cyclohexylurea;1-(4-(3-(tert-butylaMino)-2-hydroxypropoxy)phenyl)-3-cyclohexylu | | CAS: | 57460-41-0 | | MF: | C20H33N3O3 | | MW: | 363.49 | | EINECS: | | | Product Categories: | Amines;Aromatics;Intermediates & Fine Chemicals;Pharmaceuticals | | Mol File: | 57460-41-0.mol |  |
| | Talinolol Chemical Properties |
| Melting point | 160-162°C | | Boiling point | 520.0±50.0 °C(Predicted) | | density | 1.11±0.1 g/cm3(Predicted) | | storage temp. | -20°C Freezer | | solubility | DMSO (Slightly), Methanol (Slightly) | | form | Solid | | pka | 13.82±0.20(Predicted) | | color | White to Pale Pink | | InChI | 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) | | InChIKey | MXFWWQICDIZSOA-UHFFFAOYSA-N | | SMILES | N(C1CCCCC1)C(NC1=CC=C(OCC(O)CNC(C)(C)C)C=C1)=O |
| WGK Germany | WGK 3 | | HazardClass | IRRITANT | | Storage Class | 11 - Combustible Solids | | Toxicity | LD50 in rats, mice (mg/kg): 1180, 593 orally; 54.3, 74.7 i.p.; 29.7, 25.0 i.v. (Femmer) |
| | Talinolol Usage And Synthesis |
| Description | (±)-Talinolol is a β1-selective adrenoceptor antagonist well known for its cardioprotective and antihypertensive activity. By blocking β1-adrenergic receptors, talinolol delays the conduction of stimuli in the AV node, reduces the sino-atrial conduction time, and impedes the sinus node automaticity. Because its metabolism in human liver microsomes is well understood, (±)-talinolol is useful for examining the activity of the drug-transporting MDR1 gene product P-glycoprotein. | | Chemical Properties | Off-White to Pale Pink Solid | | Uses | Selective β1-adrenergic blocker structurally related to Practolol. Antihypertensive; antiarrhythmic. | | Definition | ChEBI: Talinolol is a member of ureas. | | in vivo | Talinolol (20 mg/kg; i.p.) plasma and liver AUC0-5 h are increased by Zosuquidar administration[2].
Bioavailability of Talinolol can be enhanced by coadministration with grapefruit juice (GFJ) in rats[3]. | | IC 50 | Beta-1 adrenergic receptor | | references | [1] abmann i. the actions of talinolol, a β1-selective beta blocker, in cardiac arrhythmia and acute myocardial infarction[j]. current medical research and opinion, 2008, 13(6): 325-342.
[2] trausch b, oertel r, richter k, et al. disposition and bioavailability of the β1‐adrenoceptor antagonist talinolol in man[j]. biopharmaceutics & drug disposition, 1995, 16(5): 403-414. |
| | Talinolol Preparation Products And Raw materials |
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