Paulus Martin P, Stein Murray B, Simmons Alan N, Risbrough Victoria B, Halter Robin, Chaplan Sandra R
Department of Psychiatry, University of California San Diego, La Jolla, CA, USA.
Laureate Institute for Brain Research, Tulsa, OK, USA.
Neuropsychopharmacology. 2021 Apr;46(5):1011-1019. doi: 10.1038/s41386-020-00936-w. Epub 2020 Dec 17.
Acute pharmacological inhibition of the anandamide-degrading enzyme, fatty acid amide hydrolase (FAAH), prolongs the regulatory effects of endocannabinoids and reverses the stress-induced anxiety state in a cannabinoid receptor-dependent manner. However, the neural systems underlying this modulation are poorly understood. A single site, randomized, double-blind, placebo-controlled, parallel study was conducted with 43 subjects assigned to receive once daily dosing of either placebo (n = 21) or JNJ-42165279 (100 mg) (n = 22) for 4 consecutive days. Pharmacodynamic effects were assessed on the last day of dosing and included evaluation of brain activation patterns using BOLD fMRI during an (1) emotion face-processing task, (2) inspiratory breathing load task, and (3) fear conditioning and extinction task. JNJ-42165279 attenuated activation in the amygdala, bilateral anterior cingulate, and bilateral insula during the emotion face-processing task consistent with effects previously observed with anxiolytic agents. Higher levels of anandamide were associated with greater attenuation in bilateral anterior cingulate and left insula. JNJ-42165279 increased the activation during anticipation of an aversive interoceptive event in the anterior cingulate and bilateral anterior insula and right inferior frontal cortex. JNJ-42165279 did not affect fear conditioning or within-session extinction learning as evidenced by a lack of differences on a subjective and neural circuit level. Taken together, these results support the hypothesis that JNJ-42165279 at this dose shares some effects with existing anxiolytic agents in dampening response to emotional stimuli but not responses to conditioned fear.
急性药理学抑制花生四烯乙醇胺降解酶——脂肪酸酰胺水解酶(FAAH),可延长内源性大麻素的调节作用,并以大麻素受体依赖的方式逆转应激诱导的焦虑状态。然而,这种调节作用背后的神经系统却鲜为人知。本研究进行了一项单中心、随机、双盲、安慰剂对照的平行研究,43名受试者被分配为连续4天每日服用一次安慰剂(n = 21)或JNJ - 42165279(100 mg)(n = 22)。在给药的最后一天评估药效学效应,包括在以下任务中使用血氧水平依赖性功能磁共振成像(BOLD fMRI)评估大脑激活模式:(1)情绪面孔加工任务;(2)吸气呼吸负荷任务;(3)恐惧条件化和消退任务。在情绪面孔加工任务中,JNJ - 42165279减弱了杏仁核、双侧前扣带回和双侧脑岛的激活,这与先前在抗焦虑药物中观察到的效应一致。更高水平的花生四烯乙醇胺与双侧前扣带回和左侧脑岛的更大程度减弱相关。JNJ - 42165279增加了前扣带回、双侧前脑岛和右下额叶皮质在预期厌恶内感受性事件期间的激活。JNJ - 42165279不影响恐惧条件化或会话内消退学习,这在主观和神经回路水平上均无差异得到了证实。综上所述,这些结果支持以下假设:该剂量的JNJ - 42165279与现有的抗焦虑药物在减轻对情绪刺激的反应方面具有一些共同作用,但对条件性恐惧的反应则不然。