Akerman K E, Järvisalo J O
Acta Pharmacol Toxicol (Copenh). 1977 Apr;40(4):497-504. doi: 10.1111/j.1600-0773.1977.tb03550.x.
Propranolol (1-isopropylamino-3-(1-naphtoloxy)-propan-2-ol) a beta-adrenergic receptor blocking agent was found to cause changes of transmembraneous pH in liposomes prepared from Soy-lecithin and cardiolipin. When the external pH was neutral and the internum of the liposomes acidic, the drug decreased the pH gradient. When the externum was acidic and the internum neutral, the gradient was increased by the drug. The effect of butacaine was similar to that of propranolol, while procaine, timolol and practolol were ineffective. It is suggested that the charged form of propranolol is bound to the membrane and dislocates protons from binding sites in the membrane and that the uncharged form of propranolol penetrates the membrane. After penetration it could associate with protons in the intraliposomal compartment and hence increase the pH of the interior. Depending on the direction of the pre-existing proton gradient propranolol would thus be able to increase or decrease the pH difference across the liposomal membrane.
普萘洛尔（1 - 异丙氨基 - 3 -（1 - 萘氧基）- 丙 - 2 - 醇），一种β - 肾上腺素能受体阻滞剂，被发现会导致由大豆卵磷脂和心磷脂制备的脂质体跨膜pH值发生变化。当外部pH值为中性且脂质体内部为酸性时，该药物会降低pH梯度。当外部为酸性且内部为中性时，该药物会增加梯度。布他卡因的作用与普萘洛尔相似，而普鲁卡因、噻吗洛尔和美多心安则无效。有人提出，普萘洛尔的带电形式与膜结合，并使质子从膜中的结合位点移位，而普萘洛尔的不带电形式穿透膜。穿透后，它可能与脂质体内腔中的质子结合，从而增加内部的pH值。因此，根据预先存在的质子梯度方向，普萘洛尔能够增加或降低跨脂质体膜的pH差异。
