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神经降压素受体1的偏向性变构调节剂可减少啮齿动物的乙醇摄入量及对乙醇给药的反应。

Biased allosteric modulator of neurotensin receptor 1 reduces ethanol drinking and responses to ethanol administration in rodents.

作者信息

Gereau Graydon B, Zhou Diana, Voorhies Kalynn Van, Tyler Ryan E, Campbell Jeffrey, Murray Jackson G, Alvarez-Pamir Ali, Wykoff Luke A, Companion Michel A, Jackson Michael R, Olson Steven H, Barak Lawrence S, Slosky Lauren M, Vetreno Ryan P, Besheer Joyce, McElligott Zoe A

机构信息

Bowles Center for Alcohol Studies, University of North Carolina at Chapel Hill, USA.

Department of Pharmacology, University of North Carolina at Chapel Hill, USA.

出版信息

Addict Neurosci. 2024 Dec;13. doi: 10.1016/j.addicn.2024.100185. Epub 2024 Nov 2.

DOI:10.1016/j.addicn.2024.100185
PMID:40909094
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12407176/
Abstract

Alcohol use disorders (AUDs) impose an enormous societal and financial burden, and world-wide, alcohol misuse is the 7th leading cause of premature death [1]. Despite this, there are currently only 3 FDA approved pharmacological approaches for the treatment of AUDs in the United States. The neurotensin (Nts) system has long been implicated in modulating behaviors associated with alcohol misuse. Recently, a novel compound, SBI-553, that biases the action of Nts receptor 1 (NTSR1) activation, has shown promise in preclinical models of psychostimulant use. Here we investigate the efficacy of this compound to alter ethanol-mediated behaviors in a comprehensive battery of experiments assessing ethanol consumption, behavioral responses to ethanol, physiological sensitivity to ethanol, and ethanol metabolism. Additionally, we investigated behavior in avoidance and cognitive assays to monitor potential side effects of SBI-553. We find that SBI-553 reduces ethanol consumption in mice without altering avoidance behavior or novel object recognition. We also observe sex-dependent differences in physiological responses to sequential ethanol injections in mice. In rats, we show that SBI-553 attenuates sensitivity to the interoceptive effects of ethanol (using a Pavlovian drug discrimination task). Our data suggest that targeting NTSR1 signaling may be promising to attenuate alcohol misuse, and adds to a body of literature that suggests NTSR1 may be a common downstream target involved in the psychoactive effects of multiple reinforcing substances.

摘要

酒精使用障碍(AUDs)给社会和经济带来了巨大负担,在全球范围内,酒精滥用是过早死亡的第七大主要原因[1]。尽管如此,目前在美国仅有3种经美国食品药品监督管理局(FDA)批准的用于治疗酒精使用障碍的药物治疗方法。长期以来,神经降压素(Nts)系统一直被认为与调节酒精滥用相关行为有关。最近,一种新型化合物SBI - 553,它能使神经降压素受体1(NTSR1)激活的作用产生偏向性,在精神兴奋剂使用的临床前模型中显示出了前景。在此,我们通过一系列全面的实验来研究该化合物改变乙醇介导行为的功效,这些实验评估乙醇消耗、对乙醇的行为反应、对乙醇的生理敏感性以及乙醇代谢。此外,我们还研究了在回避和认知试验中的行为,以监测SBI - 553的潜在副作用。我们发现SBI - 553可减少小鼠的乙醇消耗,而不改变回避行为或新物体识别能力。我们还观察到小鼠对连续乙醇注射的生理反应存在性别差异。在大鼠中,我们表明SBI - 553可减弱对乙醇内感受效应的敏感性(使用巴甫洛夫药物辨别任务)。我们的数据表明,靶向NTSR1信号通路可能有望减轻酒精滥用,并为表明NTSR1可能是多种强化物质精神活性作用所涉及的共同下游靶点的文献增添了内容。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/59e0/12407176/257692580c2a/nihms-2101737-f0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/59e0/12407176/d08045382d13/nihms-2101737-f0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/59e0/12407176/95ae41212a50/nihms-2101737-f0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/59e0/12407176/d006adcdd486/nihms-2101737-f0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/59e0/12407176/d0b1f18d462c/nihms-2101737-f0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/59e0/12407176/257692580c2a/nihms-2101737-f0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/59e0/12407176/d08045382d13/nihms-2101737-f0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/59e0/12407176/95ae41212a50/nihms-2101737-f0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/59e0/12407176/d006adcdd486/nihms-2101737-f0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/59e0/12407176/d0b1f18d462c/nihms-2101737-f0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/59e0/12407176/257692580c2a/nihms-2101737-f0005.jpg

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