Schauer I, Schauer U J, Thielmann K
Int J Clin Pharmacol Ther Toxicol. 1984 Nov;22(11):608-10.
In vitro effects of DL-propranolol (a therapeutically used beta-blocker with local anesthetic properties), L-propranolol (having both beta-blocking and unspecific local anesthetic properties), D-propranolol (having local anesthetic, but much less beta-blocking properties), and talinolol (a therapeutically used beta-1-blocker with much less local anesthetic properties) on lecithin: cholesterol acyl transferase (LCAT) activity in human plasma were compared. Both D-propranolol and L-propranolol inhibited LCAT activity, the former being a little more effective. The racemic mixture showed intermediate dose-effect curves. In no case could a complete inhibition be achieved. Talinolol exhibited no effect on LCAT activity. Therefore, the inhibition of LCAT activity by beta-blocking drugs may be connected with their local anesthetic properties. Because LCAT inhibition is followed by a decrease of HDL cholesterol and an increase of triglycerides in plasma, it is recommended to use only beta-blockers without such side effects on lipoprotein metabolism for therapeutical purposes.
比较了DL-普萘洛尔（一种具有局部麻醉特性的治疗用β受体阻滞剂）、L-普萘洛尔（兼具β受体阻滞和非特异性局部麻醉特性）、D-普萘洛尔（具有局部麻醉特性，但β受体阻滞特性弱得多）和他林洛尔（一种治疗用β1受体阻滞剂，局部麻醉特性弱得多）对人血浆中卵磷脂胆固醇酰基转移酶（LCAT）活性的体外作用。D-普萘洛尔和L-普萘洛尔均抑制LCAT活性，前者的效果稍强。消旋混合物呈现出中间剂量效应曲线。在任何情况下都无法实现完全抑制。他林洛尔对LCAT活性无影响。因此，β受体阻滞剂对LCAT活性的抑制可能与其局部麻醉特性有关。由于LCAT抑制之后会出现血浆中高密度脂蛋白胆固醇降低和甘油三酯升高的情况，因此建议仅将对脂蛋白代谢无此类副作用的β受体阻滞剂用于治疗目的。
