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PROGRESS IN NEURO-PSYCHOPHARMACOLOGY & BIOLOGICAL PSYCHIATRY · 2022 · IF 5.201

Baicalein exerts anxiolytic and antinociceptive effects in a mouse model of posttraumatic stress disorder: Involvement of the serotonergic system and spinal delta-opioid receptors

Lina Ruan,Kaiyu Guan,Yue Wang,Ming Gu,Yue Chen,Lisha Cai,Ruixuan Ye,Zhengwei Huang,Anqi Guo,Zhengkang Su,Xi Li,Jianchun Pan

Post-traumatic stress disorder (PTSD) is a serious mental disease featured by a stress dysfunction that occurs after an individual has faced intense mental stress, often accompanied by anxiety and chronic pain. Currently, the mainstream drug for PTSD is serotonin reuptake inhibitors (SSRIs), however, their pain management for patients is limited. Baicalein , a Chinese traditional herbal medicine, has shown promising results in treating anxiety, depression, and pain. In this study, we found that baicalein may alleviate single prolonged stress (SPS)-induced PTSD-like behaviors in mice without altering baseline nociceptive sensitivity or activity. Meanwhile, baicalein increased the noradrenaline (NE) and serotonin (5-HT) content and decreased the ratio of 5-hydroxyindoleacetic acid (5-HIAA)/5-HT by inhibiting the activity of monoamine oxidase A (MAO-A) in SPS-induce mice. The anxiolytic and antinociceptive effects induced by baicalein were totally abolished by 5-HT depleting agents. Moreover, the anxiolytic effects of baicalein could be abolished by the 5-HT 1A receptor antagonist WAY-100635, and the analgesic effects could be abolished by delta-opioid receptor antagonists in the spinal. Taken together, our study provides compelling evidence that baicalein reversed anxiety-like behaviors and neuropathic pain in PTSD through serotonergic system and spinal delta-opioid receptors.

研究领域: 药理学 · 神经科学 · 精神病学 · 传统中药
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ENVIRONMENTAL SCIENCE & TECHNOLOGY · 2025 · IF 11.3

Developmental and Neurobehavioral Toxicity of Hexaphenoxycyclotriphosphazene: Implications for Its Safety as a Flame-Retardant Alternative to Triphenyl Phosphate

Ruobing Bai,Hongyi Xian,Yu Feng,Xiyun Huang,Shiyue Tang,Zhiming Li,Long Zhang,Yizhou Zhong,Wanyan Wu,Jiangpeng Tang,Chudan Gao,Li Yan,Xinguang Zhong,Da Chen,Zhenlie Huang

Hexaphenoxycyclotriphosphazene (HPCTP) has been introduced as a halogen-free replacement for the flame-retardant triphenyl phosphate (TPhP); however, its environmental behavior and toxicological safety remain poorly defined. Here, using zebrafish larvae with TPhP as a benchmark, we systematically evaluated the developmental and neurobehavioral toxicity of HPCTP at environmentally relevant concentrations (50–5000 ng/L) from 6 to 120 h postfertilization. HPCTP showed greater bioaccumulation potential than TPhP, suggesting the risk of long-term ecological persistence. Despite lower acute toxicity, HPCTP induced pronounced developmental defects, including reduced body length and cardiac malformations. Strikingly, HPCTP and TPhP produced divergent neurobehavioral outcomes. HPCTP caused dose-dependent depression-like behaviors (hypoactivity, light-zone avoidance) through suppression of serotonin 1A (5-HT1A) signaling, supported by decreased htr1aa expression and serotonin levels and partially rescued by the 5-HT1A receptor agonist 8-OH-DPAT. By contrast, TPhP elicited anxiety-like phenotypes (hyperactivity, thigmotaxis) via CD83-dependent neuroinflammation, evidenced by decreased cd83 expression and microglial activation, which were reversed by cd83 overexpression. Taken together, these findings demonstrate that HPCTP, though marketed as a safer alternative, poses distinct developmental and neurobehavioral hazards, underscoring the urgent need for comprehensive risk evaluation prior to its widespread application.

研究领域: 环境毒理学 · 发育生物学 · 神经科学 · 分子药理学 · 生态风险评估
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COMPARATIVE BIOCHEMISTRY AND PHYSIOLOGY A-MOLECULAR & INTEGRATIVE PHYSIOLOGY · 2019 · IF 2.142

Pharmacological characterization of the 5-HT1A receptor of Bombyx mori and its role in locomotion

Rong Xiong,Wei Zhao,Xi Chen,Tian Li,Haiyin Li,Yan Li,Wangshang Shen,Ping Chen

Serotonin is involved in the regulation of many physiological and behavioral processes in vertebrates and invertebrates. The effects of serotonin are mediated through interactions of several 5-HT receptor types. The expression and pharmacological properties of 5-HT1 have received more attention than other serotonin receptors, but its functions at the individual level are little studied in arthropods. Silkworm , a Lepidoptera model, almost has no reports about serotonin receptors. To analyze the function of Bm5-HT1A receptor in vitro , the ORF of Bm5-HT1A was cloned into the pcDNA3.1 vector and expressed in HEK 293 cells . Serotonin activation of Bm5-HT1A -expressing cells decreased forskolin-stimulated cAMP synthesis and had the most potent effect compared to other biogenic amines. Serotonin reduced cAMP synthesis in a dose-dependent manner, and half-maximal activation (EC50) occurred at a concentration of 1.17 × 10 −7  M (117 nM). The pharmacological analysis demonstrated that the rank potency of agonists was pimozide >8-OH-DPAT >5-MeOT ~ αm-5-HT, and antagonists was WAY-100635 >  prazosin > SB-269970 > methiothepin at the Bm5-HT1A receptor. Injecting the antagonist of Bm5-HT1A receptor into larvae caused slow or weak motility, and adults lowered courtship vitality or moving speed. Injecting dsRNA of Bm5-HT1A into adults also dropped locomotivity in courtship. These results show that the Bm5-HT1A receptor is related to locomotor activity. This study provides the first information of serotonin receptor on pharmacological in silkworm and on individual functions in arthropods.

CAS / MDL: 162760-96-5
研究领域: 神经生物学 · 药理学 · 昆虫生理学 · 分子生物学
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