Department of Neuroscience, The Scripps Research Institute, La Jolla, CA 92037.
eNeuro. 2018 Jul 2;5(3). doi: 10.1523/ENEURO.0153-18.2018. eCollection 2018 May-Jun.
GPR139 is an orphan G protein-coupled receptor (GPCR) that is expressed mainly in the brain, with the highest expression in the medial habenula. The modulation of GPR139 receptor function has been hypothesized to be beneficial in the treatment of some mental disorders, but behavioral studies have not yet provided causal evidence of the role of GPR139 in brain dysfunction. Because of the high expression of GPR139 in the habenula, a critical brain region in addiction, we hypothesized that GPR139 may play role in alcohol dependence. Thus, we tested the effect of GPR139 receptor activation using the selective, brain-penetrant receptor agonist JNJ-63533054 on addiction-like behaviors in alcohol-dependent male rats. Systemic administration of JNJ-63533054 (30 mg/kg but not 10 mg/kg, p.o.) reversed the escalation of alcohol self-administration in alcohol-dependent rats, without affecting water or saccharin intake in dependent rats or alcohol intake in nondependent rats. Moreover, systemic JNJ-63533054 administration decreased withdrawal-induced hyperalgesia, without affecting somatic signs of alcohol withdrawal. Further analysis demonstrated that JNJ-63533054 was effective only in a subgroup of dependent rats that exhibited compulsive-like alcohol drinking. Finally, site-specific microinjection of JNJ-63533054 in the habenula but not interpeduncular nucleus (IPN) reduced both alcohol self-administration and withdrawal-induced hyperalgesia in dependent rats. These results provide robust preclinical evidence that GPR139 receptor activation reverses key addiction-like behaviors in dependent animals, suggest that GPR139 may be a novel target for the treatment of alcohol use disorder, and demonstrate that GPR139 is functionally relevant in regulating mammalian behavior.
GPR139 是一种孤儿 G 蛋白偶联受体(GPCR),主要在大脑中表达,其中间苍白球表达最高。调节 GPR139 受体功能被假设对某些精神疾病的治疗有益,但行为研究尚未提供 GPR139 在大脑功能障碍中的作用的因果证据。由于 GPR139 在成瘾关键脑区缰核中高度表达,我们假设 GPR139 可能在酒精依赖中发挥作用。因此,我们使用选择性、脑穿透性受体激动剂 JNJ-63533054 测试了 GPR139 受体激活对酒精依赖雄性大鼠成瘾样行为的影响。系统给予 JNJ-63533054(30mg/kg,但 10mg/kg,po)可逆转酒精依赖大鼠酒精自我给药的增加,而不影响依赖大鼠的水或糖精摄入或非依赖大鼠的酒精摄入。此外,系统给予 JNJ-63533054 可降低戒断引起的痛觉过敏,而不影响酒精戒断的躯体症状。进一步分析表明,JNJ-63533054 仅在表现出强迫性饮酒的依赖大鼠亚组中有效。最后,JNJ-63533054 在缰核而非中脑脚间核(IPN)的特异性局部注射可减少依赖大鼠的酒精自我给药和戒断引起的痛觉过敏。这些结果提供了有力的临床前证据,表明 GPR139 受体激活可逆转依赖动物的关键成瘾样行为,表明 GPR139 可能是治疗酒精使用障碍的新靶点,并证明 GPR139 在调节哺乳动物行为方面具有功能相关性。