Ohnami Soichiro, Naito Megumi, Kawase Haruki, Higuchi Momoko, Hasebe Shigeru, Takasu Keiko, Kanemaru Ryo, Azuma Yuki, Yokoyama Rei, Kochi Takahiro, Imado Eiji, Tahara Takeru, Kotake Yaichiro, Asano Satoshi, Oishi Naoya, Takuma Kazuhiro, Hashimoto Hitoshi, Ogawa Koichi, Nakamura Atsushi, Yamakawa Hidekuni, Ago Yukio
Laboratory for Drug Discovery and Disease Research, Shionogi & Co. Ltd., Toyonaka, Osaka, Japan.
SK Project, Medical Innovation Center, Graduate School of Medicine, Kyoto University, Kyoto, Kyoto, Japan.
JCI Insight. 2024 Dec 6;9(23):e182060. doi: 10.1172/jci.insight.182060.
The opioid system plays crucial roles in modulating social behaviors in both humans and animals. However, the pharmacological profiles of opioids regarding social behavior and their therapeutic potential remain unclear. Multiple pharmacological, behavioral, and immunohistological c-Fos mapping approaches were used to characterize the effects of μ-opioid receptor agonists on social behavior and investigate the mechanisms in naive mice and autism spectrum disorder-like (ASD-like) mouse models, such as prenatally valproic acid-treated mice and Fmr1-KO mice. Here, we report that low-dose morphine, a μ-opioid receptor agonist, promoted social behavior by selectively activating neurons in prosocial brain regions, including the nucleus accumbens, but not those in the dorsomedial periaqueductal gray (dmPAG), which are only activated by analgesic high-dose morphine. Critically, intra-dmPAG morphine injection counteracted the prosocial effect of low-dose morphine, suggesting that dmPAG neural activation suppresses social behavior. Moreover, buprenorphine, a μ-opioid receptor partial agonist with less abuse liability and a well-established safety profile, ameliorated social behavior deficits in two mouse models recapitulating ASD symptoms by selectively activating prosocial brain regions without dmPAG neural activation. Our findings highlight the therapeutic potential of brain region-specific neural activation induced by low-dose opioids for social behavior deficits in ASD.
阿片类系统在调节人类和动物的社会行为中发挥着关键作用。然而,阿片类药物在社会行为方面的药理学特征及其治疗潜力仍不清楚。我们使用了多种药理学、行为学和免疫组织化学c-Fos图谱方法,来表征μ-阿片受体激动剂对社会行为的影响,并在未经处理的小鼠和自闭症谱系障碍样(ASD样)小鼠模型(如产前丙戊酸处理的小鼠和Fmr1基因敲除小鼠)中研究其机制。在此,我们报告低剂量吗啡(一种μ-阿片受体激动剂)通过选择性激活包括伏隔核在内的亲社会脑区中的神经元来促进社会行为,但不激活仅被镇痛高剂量吗啡激活的背内侧导水管周围灰质(dmPAG)中的神经元。至关重要的是,向dmPAG内注射吗啡可抵消低剂量吗啡的亲社会作用,这表明dmPAG神经激活会抑制社会行为。此外,丁丙诺啡是一种滥用可能性较小且安全性良好的μ-阿片受体部分激动剂,它通过选择性激活亲社会脑区而不激活dmPAG神经,改善了两种模拟ASD症状的小鼠模型中的社会行为缺陷。我们的研究结果突出了低剂量阿片类药物诱导的脑区特异性神经激活对ASD社会行为缺陷的治疗潜力。