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Cannabidiol inhibits transient receptor potential canonical 4 and modulates excitability of pyramidal neurons in mPFC

文献类型：期刊论文

作者Han, Yujun1; Wang, Shuting2,3; Xiang, Yu1; Chang, Liuliu2,3; Wang, Xian1; Ren, Shimin1; Guo, Fei3; Li, Tianyu3,4,5; Liu, Zhiqiang6; Li, Yang1,2,3,7
刊名FRONTIERS IN PHARMACOLOGY
出版日期2024-11-13
卷号15页码:12
关键词TRPC4 cannabidiol epinephrine inhibitor medial prefrontal cortex
DOI10.3389/fphar.2024.1431758
通讯作者Li, Tianyu(litianyu_94@qq.com) ; Liu, Zhiqiang(drliuzhiqiang@163.com) ; Li, Yang(liyang@simm.ac.cn)
英文摘要Cannabidiol (CBD), a non-psychoactive compound derived from the cannabis plant, has been extensively studied for its potential therapeutic effects on various central nervous system (CNS) disorders, including epilepsy, chronic pain, Parkinson's disease, and stress-related neuropsychiatric disorders. However, the pharmacological mechanisms of CBD have not been fully elucidated due to the complexity of their targets. In this study, we reported that the transient receptor potential canonical 4 (TRPC4) channel, a calcium-permeable, non-selective cation channel, could be inhibited by CBD. TRPC4 is highly abundant in the central nervous system and plays a critical role in regulating axonal regeneration, neurotransmitter release, and neuronal network activity. Here, we used whole-cell electrophysiology and intracellular calcium measurements to identify the inhibitory effects of CBD on TRPC4, in which CBD was found to inhibit TRPC4 channel with an IC50 value of 1.52 mu M TRPC4 channels function as receptor-operated channels (ROC) and could be activated by epinephrine (EP) via G proteins. We show that CBD can inhibit EP-evoked TRPC4 current in vitro and EP-evoked neuronal excitability in the medial prefrontal cortex (mPFC). These results are consistent with the action of TRPC4-specific inhibitor Pico145, suggesting that TRPC4 works as a functional ionotropic receptor of CBD. This study identified TRPC4 as a novel target for CBD in the CNS and suggested that CBD could reduce the pyramidal neuron excitability by inhibiting TRPC4-containing channels in the mPFC.
WOS关键词ANXIETY-LIKE BEHAVIOR ; ADRENERGIC-RECEPTORS ; MICE BRAIN ; CHANNEL ; TRPC4 ; RAT ; INVOLVEMENT ; NEUROTRANSMISSION ; AMYGDALA ; C57BL/6
资助项目National Natural Science Foundation[32371005] ; National Natural Science Foundation[82371533] ; Natural Science Foundation of Shanghai[22ZR1449300] ; Program of Shanghai Academic/Technology Research Leader[22XD1402400]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:001363196300001
出版者FRONTIERS MEDIA SA
源URL[http://119.78.100.183/handle/2S10ELR8/314698]  
专题中国科学院上海药物研究所
通讯作者Li, Tianyu; Liu, Zhiqiang; Li, Yang
作者单位1.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing, Peoples R China
2.Univ Chinese Acad Sci, Beijing, Peoples R China
3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai, Peoples R China
4.Tongji Univ, Shanghai Matern & Infant Hosp 1, Shanghai Inst Maternal Fetal Med & Gynecol Oncol, Sch Med, Shanghai, Peoples R China
5.Tongji Univ, Anesthesia & Brain Funct Res Inst, Sch Med, Shanghai, Peoples R China
6.Fudan Univ, Obstet & Gynecol Hosp, Dept Anesthesiol, Shanghai, Peoples R China
7.Fudan Univ, Huashan Hosp, Natl Clin Res Ctr Aging & Med, Shanghai, Peoples R China
推荐引用方式
GB/T 7714		 Han, Yujun,Wang, Shuting,Xiang, Yu,et al. Cannabidiol inhibits transient receptor potential canonical 4 and modulates excitability of pyramidal neurons in mPFC[J]. FRONTIERS IN PHARMACOLOGY,2024,15:12.
APA Han, Yujun.,Wang, Shuting.,Xiang, Yu.,Chang, Liuliu.,Wang, Xian.,...&Li, Yang.(2024).Cannabidiol inhibits transient receptor potential canonical 4 and modulates excitability of pyramidal neurons in mPFC.FRONTIERS IN PHARMACOLOGY,15,12.
MLA Han, Yujun,et al."Cannabidiol inhibits transient receptor potential canonical 4 and modulates excitability of pyramidal neurons in mPFC".FRONTIERS IN PHARMACOLOGY 15(2024):12.

入库方式： OAI收割

来源：上海药物研究所

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