Reith M E, Meisler B E, Lajtha A
Pharmacol Biochem Behav. 1985 Nov;23(5):831-6. doi: 10.1016/0091-3057(85)90078-4.
Spontaneous locomotor activity of mice was stimulated by IP administration of cocaine and its closely related phenyltropane analogs. In contrast, locomotion was inhibited by IP administration of cocaine congeners such as norcocaine, (+)-pseudococaine, and tropacocaine, and of isomers of phenyltropane analogs. Also inhibitory were the local anesthetics procaine, tetracaine, benzocaine, lidocaine, and prilocaine. The locomotor inhibition induced by IP norcocaine or tetracaine could be reversed by subsequent treatment with cocaine. Both cocaine and norcocaine were centrally stimulatory when injected intracerebroventricularly. The rank order of potencies of cocaine congeners and local anesthetics in depressing locomotion was similar to that of their potencies in interacting with sodium channels. From these results we infer that the locomotor depression induced by systemic administration of cocaine congeners results from a local anesthetic action involving inhibition of the ion conductance of sodium channels.
通过腹腔注射可卡因及其密切相关的苯基托烷类似物可刺激小鼠的自发运动活性。相比之下，腹腔注射可卡因同系物（如去甲可卡因、(+)-假可卡因和托哌可卡因）以及苯基托烷类似物的异构体可抑制运动。局部麻醉药普鲁卡因、丁卡因、苯佐卡因、利多卡因和丙胺卡因也具有抑制作用。腹腔注射去甲可卡因或丁卡因所诱导的运动抑制可通过随后用可卡因治疗而逆转。当脑室内注射时，可卡因和去甲可卡因均具有中枢兴奋作用。可卡因同系物和局部麻醉药在抑制运动方面的效力顺序与其与钠通道相互作用的效力顺序相似。从这些结果我们推断，全身给予可卡因同系物所诱导的运动抑制是由涉及抑制钠通道离子电导的局部麻醉作用引起的。
