Section on Clinical Psychoneuroendocrinology and Neuropsychopharmacology, National Institute on Alcohol Abuse and Alcoholism and National Institute on Drug Abuse, National Institutes of Health, Bethesda, MD, USA.
Clinical Core Laboratory, National Institute on Alcohol Abuse and Alcoholism, National Institutes of Health, Bethesda, MD, USA.
Neuropharmacology. 2018 Jul 15;137:230-239. doi: 10.1016/j.neuropharm.2018.04.011. Epub 2018 Apr 14.
Gamma-aminobutyric acid (GABA), the main inhibitory neurotransmitter in the nervous system, plays an important role in biobehavioral processes that regulate alcohol seeking, food intake, and stress response. The metabotropic GABA-B receptor has been investigated as a potential therapeutic target for alcohol use disorder, by using orthosteric agonists (e.g., baclofen) and positive allosteric modulators. Whether and how pharmacological manipulation of the GABA-B receptor, in combination with alcohol intake, may affect feeding- and stress-related neuroendocrine pathways remains unknown. In the present randomized, double-blind, placebo-controlled study, thirty-four alcohol-dependent individuals received baclofen (30 mg/day) or placebo in a naturalistic outpatient setting for one week, and then performed a controlled laboratory experiment which included alcohol cue-reactivity, fixed-dose priming, and self-administration procedures. Blood samples were collected, and the following neuroendocrine markers were measured: ghrelin, leptin, amylin, glucagon-like peptide-1 (GLP-1), insulin, prolactin, thyroid-stimulating hormone, growth hormone, cortisol, and adrenocorticotropic hormone (ACTH). During the outpatient phase, baclofen significantly increased blood concentrations of acyl-ghrelin (p = 0.01), leptin (p = 0.01), amylin (p = 0.004), and GLP-1 (p = 0.02). Significant drug × time-point interaction effects for amylin (p = 0.001) and insulin (p = 0.03), and trend-level interaction effects for GLP-1 (p = 0.06) and ACTH (p = 0.10) were found during the laboratory experiment. Baclofen, compared to placebo, had no effect on alcohol drinking in this study (p's ≥ 0.05). Together with previous studies, these findings shed light on the role of the GABAergic system and GABA-B receptors in the shared neurobiology of alcohol-, feeding-, and stress-related behaviors.
γ-氨基丁酸(GABA)是神经系统中的主要抑制性神经递质,在调节酒精寻求、食物摄入和应激反应的生物行为过程中发挥重要作用。代谢型 GABA-B 受体已被研究为治疗酒精使用障碍的潜在治疗靶点,通过使用正位激动剂(例如,巴氯芬)和正变构调节剂。在自然环境下的门诊设置中,34 名酒精依赖个体接受巴氯芬(30mg/天)或安慰剂治疗一周,然后进行对照实验室实验,其中包括酒精线索反应性、固定剂量启动和自我给药程序。采集血液样本,并测量以下神经内分泌标志物:胃饥饿素、瘦素、胰淀素、胰高血糖素样肽-1(GLP-1)、胰岛素、催乳素、促甲状腺激素、生长激素、皮质醇和促肾上腺皮质激素(ACTH)。在门诊阶段,巴氯芬显著增加了酰基胃饥饿素(p=0.01)、瘦素(p=0.01)、胰淀素(p=0.004)和 GLP-1(p=0.02)的血液浓度。在实验室实验中,发现了药物与时间点之间的显著相互作用效应,对胰淀素(p=0.001)和胰岛素(p=0.03),以及对 GLP-1(p=0.06)和 ACTH(p=0.10)的趋势水平相互作用效应。与安慰剂相比,在这项研究中,巴氯芬对饮酒没有影响(p's≥0.05)。结合以前的研究,这些发现揭示了 GABA 能系统和 GABA-B 受体在酒精、进食和应激相关行为的共同神经生物学中的作用。