Engin Elif, Bakhurin Konstantin I, Smith Kiersten S, Hines Rochelle M, Reynolds Lauren M, Tang Wannan, Sprengel Rolf, Moss Stephen J, Rudolph Uwe
1] Laboratory of Genetic Neuropharmacology, McLean Hospital, Belmont, MA, USA [2] Department of Psychiatry, Harvard Medical School, Boston, MA, USA.
Tufts University School of Medicine, Department of Neuroscience, Boston, MA, USA.
Neuropsychopharmacology. 2014 Jul;39(8):1805-15. doi: 10.1038/npp.2014.41. Epub 2014 Feb 19.
Despite long-standing concerns regarding the abuse liability of benzodiazepines, the mechanisms underlying properties of benzodiazepines that may be relevant to abuse are still poorly understood. Earlier studies showed that compounds selective for α1-containing GABAA receptors (α1GABAARs) are abused by humans and self-administered by animals, and that these receptors may underlie a preference for benzodiazepines as well as neuroplastic changes observed in the ventral tegmental area following benzodiazepine administration. There is some evidence, however, that even L-838, 417, a compound with antagonistic properties at α1GABAARs and agonistic properties at the other three benzodiazepine-sensitive GABAA receptor subtypes, is self-administered, and that the α2GABAARs may have a role in benzodiazepine-induced reward enhancement. Using a two-bottle choice drinking paradigm to evaluate midazolam preference and an intracranial self-stimulation (ICSS) paradigm to evaluate the impact of midazolam on reward enhancement, we demonstrated that mice carrying a histidine-to-arginine point mutation in the α2 subunit which renders it insensitive to benzodiazepines (α2(H101R) mice) did not prefer midazolam and did not show midazolam-induced reward enhancement in ICSS, in contrast to wild-type controls, suggesting that α2GABAARs are necessary for the reward enhancing effects and preference for oral benzodiazepines. Through a viral-mediated knockdown of α2GABAARs in the nucleus accumbens (NAc), we demonstrated that α2 in the NAc is necessary for the preference for midazolam. Findings imply that α2GABAARs in the NAc are involved in at least some reward-related properties of benzodiazepines, which might partially underlie repeated drug-taking behavior.
尽管长期以来人们一直担心苯二氮䓬类药物的滥用可能性,但与滥用可能相关的苯二氮䓬类药物特性背后的机制仍未得到充分理解。早期研究表明,对含α1的GABAA受体(α1GABAA受体)具有选择性的化合物会被人类滥用并被动物自我给药,并且这些受体可能是对苯二氮䓬类药物产生偏好以及苯二氮䓬类药物给药后腹侧被盖区观察到的神经可塑性变化的基础。然而,有一些证据表明,即使是L-838,417这种在α1GABAA受体上具有拮抗特性且在其他三种对苯二氮䓬敏感的GABAA受体亚型上具有激动特性的化合物,也会被自我给药,并且α2GABAA受体可能在苯二氮䓬诱导的奖赏增强中起作用。我们使用双瓶选择饮水范式评估咪达唑仑偏好,并使用颅内自我刺激(ICSS)范式评估咪达唑仑对奖赏增强的影响,结果表明,α2亚基中携带组氨酸到精氨酸点突变从而使其对苯二氮䓬不敏感的小鼠(α2(H101R)小鼠)不偏好咪达唑仑,并且在ICSS中未表现出咪达唑仑诱导的奖赏增强,这与野生型对照相反,表明α2GABAA受体对于奖赏增强作用和口服苯二氮䓬类药物的偏好是必需的。通过病毒介导的伏隔核(NAc)中α2GABAA受体的敲低,我们证明NAc中的α2对于咪达唑仑偏好是必需的。研究结果表明,NAc中的α2GABAA受体至少参与了苯二氮䓬类药物的一些与奖赏相关的特性,这可能部分解释了重复用药行为。