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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >Oral sazetidine-A, a selective alpha 4 beta 2(star) nicotinic receptor desensitizing agent, reduces nicotine self-administration in rats
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Oral sazetidine-A, a selective alpha 4 beta 2(star) nicotinic receptor desensitizing agent, reduces nicotine self-administration in rats

机译：口服Sazetidine-A，一种选择性α4β2（星）烟碱受体脱敏剂，降低了大鼠的尼古丁自我给药

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Sazetidine-A selectively desensitizes alpha 4 beta 2 nicotinic receptors and also has partial agonist effects. We have shown that subcutaneous acute and repeated injections as well as chronic infusions of sazetidine-A significantly reduce intravenous (IV) nicotine self-administration in rats. To further investigate the promise of sazetidine-A as a smoking cessation aid, it is important to determine sazetidine-A effects with oral administration and the time-effect function for its action on nicotine self administration. Young adult female Sprague-Dawley rats were trained to self-administer IV nicotine at the benchmark dose of 0.03 mg/kg/infusion dose in an operant FR1 schedule in 45-min sessions. After five sessions of training, they were tested for the effects of acute oral doses of sazetidine-A (0, 0.3, 1 and 3 mg/kg) given 30 min before testing. To determine the time-effect function, these rats were administered 0 or 3 mg/kg of sazetidine-A 1, 2, 4 or 23 h before the onset of testing. Our previous study showed that with subcutaneous injections, only 3 mg/kg of sazetidine-A significantly reduced nicotine self-administration, however, with oral administration of sazetidine-A lower dose of 1 mg/kg was also effective in reducing nicotine intake. A similar effect was seen in the time-effect study with 3 mg/kg of oral sazetidine-A causing a significant reduction in nicotine self-administration across all the time points of 1, 2, 4 or 23 h after oral administration. These results advance the development of sazetidine-A as a possible aid for smoking cessation by showing effectiveness with oral administration and persistence of the effect over the course of a day.
机译：Sazetidine-A选择性地脱敏α4β2烟碱受体，并且还具有部分激动剂效应。我们已经表明，皮下急性和重复的注射以及Sazetidine-A的慢性输注显着降低了大鼠静脉内（IV）尼古丁自我给药。为了进一步调查Sazetidine-A作为吸烟戒烟助剂的承诺，重要的是测定与口服给药的肌菌和时间效应对尼古丁自我施用的作用。年轻成年女性Sprague-Dawley大鼠在45分钟的课程中，在操作员FR1时间表的基准剂量为0.03mg / kg / kg / kg / kg / kg / kg / kg的基准剂量。经过五届培训后，在试验前30分钟进行急性口服剂量的急性口服剂量-A（0,0.3,1和3mg / kg）的影响。为了确定时间效应函数，在测试开始之前施用0或3mg / kg的Sazetidine-a 1,2,4或23h的大鼠。我们之前的研究表明，随着皮下注射，仅3毫克/千克萨齐齐汀-A显着降低的尼古丁自我给药，然而，用口服施用Sazetidine-较低剂量的1mg / kg也有效减少尼古丁的摄入量。用3mg / kg口服撒辛丁啶-A在时间效应研究中看到了类似的效果，导致口服给药后1,2,4或23h的所有时间点的尼古丁自我给药显着降低。这些结果通过表现出与每天效果的效果的有效性提高了Sazetidine-A作为吸烟的可能援助。

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    Rezvani Amir H.; Wells Corinne; Slade Susan; Xiao Yingxian; Kellar Kenneth J.; Levin Edward D.;

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    Duke Univ Dept Psychiat &

    Behav Sci Med Ctr POB 104790 Durham NC 27710 USA;

    Duke Univ Dept Psychiat &

    Behav Sci Med Ctr POB 104790 Durham NC 27710 USA;

    Duke Univ Dept Psychiat &

    Behav Sci Med Ctr POB 104790 Durham NC 27710 USA;

    Georgetown Univ Dept Physiol &

    Pharmacol Sch Med Washington DC 20057 USA;

    Georgetown Univ Dept Physiol &

    Pharmacol Sch Med Washington DC 20057 USA;

    Duke Univ Dept Psychiat &

    Behav Sci Med Ctr POB 104790 Durham NC 27710 USA;

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  • 正文语种 eng
  • 中图分类 药理学;
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