Mansner R, Mattila M J
Med Biol. 1975 Jun;53(3):169-76.
Injection of rats with 14C-labelled nicotine (3 mg/kg sc) resulted in tremor measured by an electronic device during the first minutes after the injection. The animals were decapitated immediately afterwards and tissue was removed for the measurement of nicotine and cotinine. In another set of experiments nicotine (2 mg/kg sc) was injected into alcohol anaesthetized rats, their urinary excretion was measured up to 40 min, and they were decapitated as above. Pretreatment with mecamylamine prevented nicotine-induced tremor and antidiuresis. It also lowered the brain and blood nicotine levels in tremor experiments but not in antidiuresis experiments. Restoration of tremor by arecoline did not modify the mecamylamine effects on the nicotine levels. The 2 mg/kg sc nicotine dose did not produce tremor although the brain nicotine levels at 10 min exceeded those measured at 2 min after 3 mg/kg of nicotine. It is concluded that the rate of receptor occupation is important in the nicotine tremor. Both tremor and antidiuresis correlate fairly well with brain nicotine levels whereas mecamylamine-nicotine antagonism is less clearly reflected in brain nicotine levels.
给大鼠皮下注射14C标记的尼古丁(3毫克/千克)后,在注射后的最初几分钟内,通过电子设备测量发现大鼠出现震颤。之后立即将动物断头,并取出组织用于测量尼古丁和可替宁。在另一组实验中,将尼古丁(2毫克/千克皮下注射)注入酒精麻醉的大鼠体内,测量其长达40分钟的尿液排泄情况,然后按上述方法将其断头。用美加明预处理可预防尼古丁引起的震颤和抗利尿作用。在震颤实验中,它还降低了大脑和血液中的尼古丁水平,但在抗利尿实验中则没有。槟榔碱恢复震颤并未改变美加明对尼古丁水平的影响。2毫克/千克皮下注射的尼古丁剂量未产生震颤,尽管10分钟时大脑中的尼古丁水平超过了3毫克/千克尼古丁注射后2分钟时测量的水平。得出的结论是,受体占据率在尼古丁震颤中很重要。震颤和抗利尿作用都与大脑中的尼古丁水平有相当好的相关性,而美加明 - 尼古丁拮抗作用在大脑尼古丁水平中反映得不太明显。