Cizmáriková R
Katedra chemickej teórie lieciv Farmaceutickej fakulty Univerzity Komenského, Bratislava.
Ceska Slov Farm. 2002 May;51(3):121-8.
The present review of beta-adrenergic receptor blockers deals with different pharmacodynamic, pharmacokinetic and toxicological effects of individual enantiomers in the group of arylaminoethanols and aryloxyaminopropanols. From the viewpoint of beta-adrenolytic activity, (-)-enantiomers in both groups are several times more effective and in many beta-blockers both enantiomers show different therapeutic indications. The absolute configuration in the sense of Cahn-Ingold-Prelog system exists in (-)-enantiomers in the group of arylaminoethanols (R) and in the group of aryloxyaminopropanols (S). Of the beta-blockers hitherto used in therapeutic practice, pure enantiomers are (S)-(-)-penbutolol, (S)-(-)-timolol, and (S)-(-)-levobunolol. The hitherto research in this field, however, does not unambiguously answer, as the experience with labetalol, sotalol, and timolol shows, the question of the advantages of therapeutic use of pure enantiomeric forms.
本对β-肾上腺素能受体阻滞剂的综述涉及芳基氨基乙醇和芳氧基氨基丙醇类中各对映体不同的药效学、药代动力学和毒理学效应。从β-肾上腺素能阻断活性的角度来看，两组中的（-）-对映体效力要高出数倍，并且在许多β受体阻滞剂中，两种对映体都显示出不同的治疗适应症。按照卡恩-英戈尔德-普雷洛格体系，绝对构型在芳基氨基乙醇组的（-）-对映体中为（R），在芳氧基氨基丙醇组中为（S）。在迄今治疗实践中使用的β受体阻滞剂中，纯对映体有（S）-（-）-喷布洛尔、（S）-（-）-噻吗洛尔和（S）-（-）-左布诺洛尔。然而，正如拉贝洛尔、索他洛尔和噻吗洛尔的经验所示，该领域迄今的研究并未明确回答使用纯对映体形式进行治疗的优势问题。
