Alkondon M, Ray A, Sen P
J Pharm Pharmacol. 1986 Nov;38(11):848-50. doi: 10.1111/j.2042-7158.1986.tb04509.x.
The effect of (+/-)-propranolol and some related drugs have been investigated on the cholinesterase (ChE) enzyme activity of heart and brain tissues of the rat. Brain homogenates hydrolysed more methacholine than benzoylcholine and the reverse was true for the heart tissue. In-vitro, (+/-)-, (+)- and (-)-propranolol, as well as its quaternary analogue, UM-272, all significantly inhibited heart and brain ChE. Timolol and sotalol, however, were less potent. In-vivo, (+/-)-propranolol (30 mumol kg-1) significantly inhibited brain ChE activity in rats when compared with saline controls. It is inferred that propranolol inhibits brain and heart ChE enzyme in a non-stereoselective manner and that this cholinomimetic action could be involved in the mediation of some of its therapeutic effects.
已研究了（±）-普萘洛尔及一些相关药物对大鼠心脏和脑组织胆碱酯酶（ChE）活性的影响。脑匀浆对乙酰甲胆碱的水解能力比对苯甲酰胆碱更强，而心脏组织则相反。在体外，（±）-、（+）-和（-）-普萘洛尔及其季铵类似物UM-272均能显著抑制心脏和脑ChE。然而，噻吗洛尔和索他洛尔的作用较弱。在体内，与生理盐水对照组相比，（±）-普萘洛尔（30 μmol·kg⁻¹）能显著抑制大鼠脑ChE活性。据推测，普萘洛尔以非立体选择性方式抑制脑和心脏ChE酶，且这种拟胆碱作用可能参与了其某些治疗作用的介导过程。
