Falintolol, (Z)-
目录号 : GC32418Falintolol,(Z)是一种新的β-肾上腺素能拮抗剂,其特征在于存在肟功能。
Cas No.:106401-52-9
Sample solution is provided at 25 µL, 10mM.
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Falintolol, (Z)-, a new β-adrenergic antagonist, is characterized by the presence of an oxime function.
[1]. Himber J, et al. Determination of falintolol, a new aliphatic beta-adrenergic antagonist, in whole blood by gaschromatography with electron-capture detection: geometric isomers resolution. J Chromatogr Sci. 1987 Jan;25(1):33-7.
Cas No. | 106401-52-9 | SDF | |
Canonical SMILES | C/C(C1CC1)=N/OCC(O)CNC(C)(C)C | ||
分子式 | C12H24N2O2 | 分子量 | 228.33 |
溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 4.3796 mL | 21.8981 mL | 43.7963 mL |
5 mM | 0.8759 mL | 4.3796 mL | 8.7593 mL |
10 mM | 0.438 mL | 2.1898 mL | 4.3796 mL |
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Determination of Falintolol, a new aliphatic beta-adrenergic antagonist, in whole blood by gas chromatography with electron-capture detection: geometric isomers resolution
J Chromatogr Sci 1987 Jan;25(1):33-7.PMID:2880859DOI:10.1093/chromsci/25.1.33.
Falintolol oxalate, a new beta-adrenergic antagonist, is characterized by the presence of an oxime function and exists in a racemic form as a mixture of syn- and anti- isomers in a ratio of about 8:2. This article describes a selective gas chromatographic method for the resolution of the geometric isomers and the quantitation of the drug. The unchanged falintolol and internal standard, a related compound, are separated from blood by a solvent extraction under alkaline conditions, and then the drug is derivatized. The heptafluorobutyric derivatives are chromatographed on an SE-30 capillary quartz column and detected with a nickel-63 electron-capture detector. Because the syn- and anti- isomers of falintolol display comparable chromatographic responses, the sum of the two geometrical isomers is used for the quantitation of falintolol in blood. This method allows small serial blood samples in conscious rats, and 0.05 microgram of falintolol/0.1 mL of blood can be routinely determined. A calibration curve is prepared for the blood extracts. Linearity is observed in the study range (0.05 to 1 microgram/0.1 mL of blood). No interference by endogenous substances is observed. The procedure is applied successfully to drug absorption in rats when repeated oral doses are administered.
In vitro potential measurement, anaesthetic and antimicrobial effects as indicators of beta-blocker toxicity of the cornea
Methods Find Exp Clin Pharmacol 1985 Apr;7(4):195-201.PMID:2862314doi
Three tests were utilized to determine and compare the toxicity of timolol, propranolol and two new aliphatic and alicyclic oxime ethers with beta-blocking activity (falintolol and compound POS 7). Effects on the electrical potential difference across the in vitro bovine corneal epithelium. Local anaesthesia on in vivo rabbit cornea. Antimicrobial activity on bacterial and fungal suspensions. In addition, partition coefficients were determined as physicochemical properties of the drugs. Falintolol, as well as timolol produced a minor change in electrophysiology at clinical concentration. They had neither local anaesthetic, nor antimicrobial effects. Conversely, propranolol and compound POS 7 showed acute corneal toxicity in the present models. It was concluded that changes in the potential difference across a perfused cornea in vitro, local anaesthesia and bacterial inhibition, might be a demonstration of the cytotoxicity of certain topical agents in terms of acute eye tissue reaction. They might represent a valuable model for the acute corneal toxicity evaluation of topical beta-blockers.