Grana E, Zonta F, D'Agostino G, Dondi G
Arch Int Pharmacodyn Ther. 1980 Oct;247(2):306-19.
The actions of three local anesthetics (cocaine, procaine and tetracaine) on basal tone of isolated vas deferens from control and reserpinized rats were studied. The influence of these anesthetics on responses to norepinephrine and calcium was also examined. Cocaine, procaine and tetracaine, in the order, induced phasic and tonic contractions, the latter ones probably due to catecholamine release. The local anesthetics, at the lowest doses, produced an elevation of the maximum response to norepinephrine, as well as a leftward shift of the dose-response curve. The highest doses of local anesthetics inhibited the response to norepinephrine in a non-competitive way, while the response to calcium was competitively inhibited. In this connection, tetracaine proved to be the most active compound. The distinction between destabilizing and stabilizing effects on membrane is pointed out and discussed.
研究了三种局部麻醉药（可卡因、普鲁卡因和丁卡因）对来自对照大鼠和利血平化大鼠的离体输精管基础张力的作用。还考察了这些麻醉药对去甲肾上腺素和钙反应的影响。可卡因、普鲁卡因和丁卡因依次引起相性和强直性收缩，后者可能是由于儿茶酚胺释放所致。最低剂量的局部麻醉药使对去甲肾上腺素的最大反应升高，以及剂量反应曲线向左移动。局部麻醉药的最高剂量以非竞争性方式抑制对去甲肾上腺素的反应，而对钙的反应则被竞争性抑制。在这方面，丁卡因被证明是最具活性的化合物。指出并讨论了对膜的去稳定和稳定作用之间的区别。
