α-Conotoxin TxIB Reversed Nicotine-Induced Locomotor Sensitization and Nicotine-Enhanced Dopaminergic Activity in Mice

Nicotine addiction is a serious global public health problem, so there is an urgent necessity to develop novel effective smoking cessation treatments with fewer adverse effects. Spontaneous behavioral sensitization induced by repeated intermittent exposure to the addictive substance represents a cla...

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Main Authors: Weifeng Xu, Meiting Wang, Xiaodan Li, Rongyan He, Ren-Bo Ding, Jiaolin Bao, Dongting Zhangsun, Sulan Luo
Format: Article
Language:English
Published: MDPI AG 2025-03-01
Series:Marine Drugs
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Online Access:https://www.mdpi.com/1660-3397/23/3/109
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author Weifeng Xu
Meiting Wang
Xiaodan Li
Rongyan He
Ren-Bo Ding
Jiaolin Bao
Dongting Zhangsun
Sulan Luo
author_facet Weifeng Xu
Meiting Wang
Xiaodan Li
Rongyan He
Ren-Bo Ding
Jiaolin Bao
Dongting Zhangsun
Sulan Luo
author_sort Weifeng Xu
collection DOAJ
description Nicotine addiction is a serious global public health problem, so there is an urgent necessity to develop novel effective smoking cessation treatments with fewer adverse effects. Spontaneous behavioral sensitization induced by repeated intermittent exposure to the addictive substance represents a classical animal model of addiction research. A significant contributor to nicotine addiction is its interaction with α6β2* nAChRs located on midbrain dopaminergic neurons, which leads to an increase in dopamine (DA) release. α-Conotoxin (α-CTx) TxIB is a novel potent antagonist of the α6/α3β2β3* nAChRs, with an IC50 value of 28.4 nM developed by our group. In this study, we aimed to investigate the effectiveness of α-CTx TxIB in countering nicotine-induced behavioral sensitization and moderating the impact of nicotine on dopamine accumulation in the midbrain. Our results demonstrated that repeated nicotine administration remarkably elevated the locomotor activity of mice, including the number of entries, average speed, and total distance traveled, which could be effectively attenuated by α-CTx TxIB intervention in a dose-dependent manner (1 nmol and 5 nmol TxIB per mouse). Furthermore, 5 nmol α-CTx TxIB significantly reduced the nicotine-elevated DA and norepinephrine (NE) levels in the ventral tegmental area (VTA) and nucleus accumbens (NAc) of mice. 5 nmol α-CTx TxIB also markedly decreased the expression of critical proteins such as the dopamine transporter (DAT), N-methyl-D-aspartic acid receptor (NMDAR), and c-Fos in the NAc and prefrontal cortex (PFC) of the nicotine-exposed mice. This research provided the first compelling evidence that α-CTx TxIB attenuated nicotine-induced locomotor sensitization and inhibited the nicotine-induced dopamine elevation in mice. These results open up new avenues for exploring the therapeutic potential of α-CTx TxIB in the treatment of nicotine addiction.
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spelling doaj-art-75d96a98631841f689dbf6bf67b9b0792025-08-20T02:11:11ZengMDPI AGMarine Drugs1660-33972025-03-0123310910.3390/md23030109α-Conotoxin TxIB Reversed Nicotine-Induced Locomotor Sensitization and Nicotine-Enhanced Dopaminergic Activity in MiceWeifeng Xu0Meiting Wang1Xiaodan Li2Rongyan He3Ren-Bo Ding4Jiaolin Bao5Dongting Zhangsun6Sulan Luo7Key Laboratory of Tropical Biological Resources of Ministry of Education, Hainan University, Haikou 570228, ChinaGuangxi Key Laboratory of Special Biomedicine, School of Medicine, Guangxi University, Nanning 530004, ChinaKey Laboratory of Tropical Biological Resources of Ministry of Education, Hainan University, Haikou 570228, ChinaGuangxi Key Laboratory of Special Biomedicine, School of Medicine, Guangxi University, Nanning 530004, ChinaKey Laboratory of Tropical Biological Resources of Ministry of Education, Hainan University, Haikou 570228, ChinaKey Laboratory of Tropical Biological Resources of Ministry of Education, Hainan University, Haikou 570228, ChinaKey Laboratory of Tropical Biological Resources of Ministry of Education, Hainan University, Haikou 570228, ChinaKey Laboratory of Tropical Biological Resources of Ministry of Education, Hainan University, Haikou 570228, ChinaNicotine addiction is a serious global public health problem, so there is an urgent necessity to develop novel effective smoking cessation treatments with fewer adverse effects. Spontaneous behavioral sensitization induced by repeated intermittent exposure to the addictive substance represents a classical animal model of addiction research. A significant contributor to nicotine addiction is its interaction with α6β2* nAChRs located on midbrain dopaminergic neurons, which leads to an increase in dopamine (DA) release. α-Conotoxin (α-CTx) TxIB is a novel potent antagonist of the α6/α3β2β3* nAChRs, with an IC50 value of 28.4 nM developed by our group. In this study, we aimed to investigate the effectiveness of α-CTx TxIB in countering nicotine-induced behavioral sensitization and moderating the impact of nicotine on dopamine accumulation in the midbrain. Our results demonstrated that repeated nicotine administration remarkably elevated the locomotor activity of mice, including the number of entries, average speed, and total distance traveled, which could be effectively attenuated by α-CTx TxIB intervention in a dose-dependent manner (1 nmol and 5 nmol TxIB per mouse). Furthermore, 5 nmol α-CTx TxIB significantly reduced the nicotine-elevated DA and norepinephrine (NE) levels in the ventral tegmental area (VTA) and nucleus accumbens (NAc) of mice. 5 nmol α-CTx TxIB also markedly decreased the expression of critical proteins such as the dopamine transporter (DAT), N-methyl-D-aspartic acid receptor (NMDAR), and c-Fos in the NAc and prefrontal cortex (PFC) of the nicotine-exposed mice. This research provided the first compelling evidence that α-CTx TxIB attenuated nicotine-induced locomotor sensitization and inhibited the nicotine-induced dopamine elevation in mice. These results open up new avenues for exploring the therapeutic potential of α-CTx TxIB in the treatment of nicotine addiction.https://www.mdpi.com/1660-3397/23/3/109α-CTx TxIBα6β2* nAChRsnicotine addictionlocomotor sensitizationdopamine
spellingShingle Weifeng Xu
Meiting Wang
Xiaodan Li
Rongyan He
Ren-Bo Ding
Jiaolin Bao
Dongting Zhangsun
Sulan Luo
α-Conotoxin TxIB Reversed Nicotine-Induced Locomotor Sensitization and Nicotine-Enhanced Dopaminergic Activity in Mice
Marine Drugs
α-CTx TxIB
α6β2* nAChRs
nicotine addiction
locomotor sensitization
dopamine
title α-Conotoxin TxIB Reversed Nicotine-Induced Locomotor Sensitization and Nicotine-Enhanced Dopaminergic Activity in Mice
title_full α-Conotoxin TxIB Reversed Nicotine-Induced Locomotor Sensitization and Nicotine-Enhanced Dopaminergic Activity in Mice
title_fullStr α-Conotoxin TxIB Reversed Nicotine-Induced Locomotor Sensitization and Nicotine-Enhanced Dopaminergic Activity in Mice
title_full_unstemmed α-Conotoxin TxIB Reversed Nicotine-Induced Locomotor Sensitization and Nicotine-Enhanced Dopaminergic Activity in Mice
title_short α-Conotoxin TxIB Reversed Nicotine-Induced Locomotor Sensitization and Nicotine-Enhanced Dopaminergic Activity in Mice
title_sort α conotoxin txib reversed nicotine induced locomotor sensitization and nicotine enhanced dopaminergic activity in mice
topic α-CTx TxIB
α6β2* nAChRs
nicotine addiction
locomotor sensitization
dopamine
url https://www.mdpi.com/1660-3397/23/3/109
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