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戒烟药物伐尼克兰可改善 DBA/2 小鼠的 P20-N40 抑制不足。

The smoking cessation drug varenicline improves deficient P20-N40 inhibition in DBA/2 mice.

机构信息

Medical Research, Veterans Affairs Medical Center, Denver, CO 80220, USA.

出版信息

Pharmacol Biochem Behav. 2011 Nov;100(1):17-24. doi: 10.1016/j.pbb.2011.07.001. Epub 2011 Jul 7.

Abstract

Varenicline, an FDA approved smoking cessation pharmacotherapy, is an α4β2* nicotinic acetylcholine receptor (nAChR) partial agonist and an α7* nAChR full agonist. Both subtypes of nAChR are involved in modulating auditory evoked responses in rodents. In DBA/2 mice, an inbred strain, auditory evoked responses to paired auditory stimuli fail to inhibit to the second stimulus. This mouse strain replicates the auditory evoked response inhibition deficit experienced by the majority of schizophrenia patients. In this current study, we examined the effects of five different doses of varenicline (0.06, 0.3, 0.6, 3 and 6mg/kg) on auditory evoked responses in anesthetized DBA/2 mice. We also administered α4β2* and α7* nAChR selective antagonists prior to varenicline administration to determine which nAChR subtypes mediate the effects of varenicline. Four of the five doses of varenicline produced improvements in auditory evoked response inhibition deficits. Selective blockade of either the α4β2* or α7* nAChR in competition with 0.6mg/kg varenicline prevented varenicline induced improvements. In competition with a higher dose of varenicline (3mg/kg) only blockade of the α4β2* nAChR prevented varenicline induced improvement in auditory evoked response inhibition. These data indicate the importance of α4β2* nAChRs and the potential involvement of the α7* subtype in varenicline's effects on auditory evoked responses in DBA/2 mice.

摘要

伐伦克林,一种经 FDA 批准的戒烟药物治疗方法,是一种α4β2烟碱型乙酰胆碱受体(nAChR)部分激动剂和α7 nAChR 完全激动剂。这两种 nAChR 亚型都参与调节啮齿动物的听觉诱发电位。在 DBA/2 小鼠中,一种近交系,对成对听觉刺激的听觉诱发电位不能抑制到第二个刺激。这种小鼠品系复制了大多数精神分裂症患者所经历的听觉诱发电位抑制缺陷。在目前的研究中,我们检查了五种不同剂量的伐伦克林(0.06、0.3、0.6、3 和 6mg/kg)对麻醉 DBA/2 小鼠听觉诱发电位的影响。我们还在给予伐伦克林之前给予α4β2和α7 nAChR 选择性拮抗剂,以确定哪种 nAChR 亚型介导伐伦克林的作用。五种剂量中的四种都改善了听觉诱发电位抑制缺陷。与 0.6mg/kg 伐伦克林竞争时,选择性阻断α4β2或α7 nAChR 可防止伐伦克林诱导的改善。与更高剂量的伐伦克林(3mg/kg)竞争时,只有阻断α4β2* nAChR 可防止伐伦克林诱导的听觉诱发电位抑制改善。这些数据表明,α4β2* nAChR 的重要性和α7*亚型在伐伦克林对 DBA/2 小鼠听觉诱发电位的影响中的潜在作用。

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