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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >Lobeline attenuates locomotor stimulation induced by repeated nicotine administration in rats.
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Lobeline attenuates locomotor stimulation induced by repeated nicotine administration in rats.

机译：洛贝林可减轻大鼠反复尼古丁给药引起的运动刺激。

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Lobeline inhibits [3H]nicotine binding to rat brain membranes and nicotine-induced [3H]dopamine release from superfused rat striatal slices, indicating that lobeline acts as a nicotinic receptor antagonist. To determine whether lobeline also inhibits the effects of nicotine in vivo, the present study assessed the effect of lobeline pretreatment on nicotine-induced hyperactivity and sensitization. For 12 consecutive days, rats were injected subcutaneously with lobeline (3 mg/kg) or saline, followed 10 min later by nicotine (0.3 mg/kg) or saline injection, and activity was monitored. To determine if lobeline inhibits induction of sensitization to nicotine, 1 or 28 days later, rats were pretreated with saline followed by nicotine or saline. Lobeline attenuated nicotine-induced hyperactivity when both drugs were administered repeatedly. Although an initial injection of lobeline produced hypoactivity, tolerance to this effect developed. Importantly, tolerance did not develop to the lobeline-induced attenuation of nicotine hyperactivity. Lobeline attenuated the induction of sensitization to nicotine 1 day, but not 28 days, after the cessation of lobeline treatment. These results demonstrate that systemic administration of lobeline attenuates the locomotor-activating effects of repeated nicotine injection and the sensitization to nicotine, consistent with lobeline inhibition of nicotinic receptors and/or neurotransmitter transporters.
机译：肝胆碱抑制[3H]烟碱与大鼠脑膜的结合，以及尼古丁诱导的[3H]多巴胺从超融合大鼠纹状体切片的释放，表明肝胆碱可作为烟碱样受体拮抗剂。为了确定lobeline是否在体内也抑制尼古丁的作用，本研究评估了lobeline预处理对尼古丁引起的机能亢进和致敏作用的影响。连续12天，给大鼠皮下注射卵磷脂（3 mg / kg）或生理盐水，然后在10分钟后注射尼古丁（0.3 mg / kg）或生理盐水，并监测活性。为了确定卵磷脂是否抑制了对烟碱致敏的诱导，在1或28天后，先用生理盐水然后用烟碱或生理盐水对大鼠进行预处理。当两种药物重复给药时，Lobeline减弱了尼古丁引起的机能亢进。尽管初次注射肝胆碱会产生机能减退，但对这种作用产生了耐受性。重要的是，对烟碱诱导的尼古丁机能亢进减弱没有产生耐受性。 Lobeline治疗停止后1天（而非28天）减弱了对尼古丁的敏化诱导。这些结果表明，全身性给予肝油碱可减轻重复烟碱注射和对烟碱致敏的运动激活作用，这与肝碱对烟碱样受体和/或神经递质转运蛋白的抑制作用相一致。

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