In a Rat Model of Opioid Maintenance, the G Protein-Biased Mu Opioid Receptor Agonist TRV130 Decreases Relapse to Oxycodone Seeking and Taking and Prevents Oxycodone-Induced Brain Hypoxia

Bossert Jennifer M.; Kiyatkin Eugene A.; Korah Hannah; Hoots Jennifer K.; Afzal Anum; Perekopskiy David; Thomas Shruthi; Fredriksson Ida; Blough Bruce E.; Negus S. Stevens; Epstein David H.; Shaham Yavin

首页> 外文期刊>Biological psychiatry >In a Rat Model of Opioid Maintenance, the G Protein-Biased Mu Opioid Receptor Agonist TRV130 Decreases Relapse to Oxycodone Seeking and Taking and Prevents Oxycodone-Induced Brain Hypoxia

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In a Rat Model of Opioid Maintenance, the G Protein-Biased Mu Opioid Receptor Agonist TRV130 Decreases Relapse to Oxycodone Seeking and Taking and Prevents Oxycodone-Induced Brain Hypoxia

机译：在阿片类药物维持的大鼠模型中，G蛋白质偏置的MU阿片类受体激动剂TRV130降低了羟考酮的复发，寻求和预防羟考酮诱导的脑缺氧

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BACKGROUND: Maintenance treatment with opioid agonists (buprenorphine, methadone) is effective for opioid addiction but does not eliminate opioid use in all patients. We modeled maintenance treatment in rats that self-administered the prescription opioid oxycodone. The maintenance medication was either buprenorphine or the G protein-biased mu opioid receptor agonist TRV130. We then tested prevention of oxycodone seeking and taking during abstinence using a modified context-induced reinstatement procedure, a rat relapse model.

机译：背景：用阿片类激动剂（Buprenorphine，美沙酮）的维持治疗对于阿片类药物是有效的，但不会消除所有患者的阿片类药物。我们在自我施用的大鼠进行维持治疗，以自我施用处方阿片羟基酮。维护药物是丁丙诺啡或G蛋白质偏置μOpiOd受体激动剂TRV130。然后，使用修改的上下文诱导的恢复程序，测试在禁止期间预防羟考酮寻找和服用戒断症。

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《Biological psychiatry》 |2020年第12期|共10页
作者
Bossert Jennifer M.; Kiyatkin Eugene A.; Korah Hannah; Hoots Jennifer K.; Afzal Anum; Perekopskiy David; Thomas Shruthi; Fredriksson Ida; Blough Bruce E.; Negus S. Stevens; Epstein David H.; Shaham Yavin;
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NIDA Behav Neurosci Branch Intramural Res Program NIH Baltimore MD 21224 USA;

NIDA Behav Neurosci Branch Intramural Res Program NIH Baltimore MD 21224 USA;

NIDA Behav Neurosci Branch Intramural Res Program NIH Baltimore MD 21224 USA;

NIDA Behav Neurosci Branch Intramural Res Program NIH Baltimore MD 21224 USA;

NIDA Behav Neurosci Branch Intramural Res Program NIH Baltimore MD 21224 USA;

NIDA Behav Neurosci Branch Intramural Res Program NIH Baltimore MD 21224 USA;

NIDA Behav Neurosci Branch Intramural Res Program NIH Baltimore MD 21224 USA;

NIDA Behav Neurosci Branch Intramural Res Program NIH Baltimore MD 21224 USA;

Res Triangle Inst Ctr Drug Discovery POB 12194 Res Triangle Pk NC 27709 USA;

Virginia Commonwealth Univ Dept Pharmacol &

Toxicol Richmond VA USA;

NIDA Clin Pharmacol &

Therapeut Res Branch Intramural Res Program NIH Baltimore MD USA;

NIDA Behav Neurosci Branch Intramural Res Program NIH Baltimore MD 21224 USA;

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正文语种 eng
中图分类神经病学与精神病学;
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1. Kappa-opioid receptor agonist U50448H protects against renal ischemia-reperfusion injury in rats via activating the PI3K/Akt signaling pathway [J] . Li-jie LIU, Jian-jun YU, Xiao-lin XU 中国药理学报：英文版 . 2018,第001期
2. RNA interference targeting mu-opioid receptors reverses the inhibition of fentanyl on glucose-evoked insulin release of rat islets [J] . QIAN Tao-lai, ZHANG Lei, WANG Xin-hua, 中华医学杂志：英文版 . 2010,第024期
3. RNA interference targeting mu-opioid receptors reverses the inhibition of fentanyl on glucose-evoked insulin release of rat islets [J] . QIAN Tao-lai, ZHANG Lei, WANG Xin-hua, 中华医学杂志（英文版） . 2010,第024期
4. Novel Application for G Protein-Biased Mu Opioid Receptor Agonists in Opioid Relapse Prevention [J] . Fakira Amanda K., Devi Lakshmi A., Kennedy Pamela J. Biological psychiatry . 2020,第12期

机译：对蛋白质偏置的穆阿片类受体激动剂在阿片类药物复发预防中的新施用
5. The G-protein biased mu-opioid agonist, TRV130, produces reinforcing and antinociceptive effects that are comparable to oxycodone in rats [J] . Zamarripa C. Austin, Edwards Shelley R., Qureshi Hina N., Drug and alcohol dependence . 2018,第期

机译：G蛋白偏置的Mu-阿片类激动剂TRV130产生与大鼠中羟考酮相当的增强和抗血质效果
6. TRV0109101, a G Protein-Biased Agonist of the mu-Opioid Receptor, Does Not Promote Opioid-Induced Mechanical Allodynia following Chronic Administration [J] . Koblish Michael, Carr Richard III, Siuda Edward R., The Journal of Pharmacology and Experimental Therapeutics: Official Publication of the American Society for Pharmacology and Experimental Therapeutics . 2017,第2期

机译：TRV0109101，MU-阿片受体的G蛋白质偏置激动剂，不促进慢性施用后诱导的阿片类药物异常疼痛
7. Identification of opioid receptor ligand interactions using structurally related delta-opioid receptor agonists and antagonists and molecular modeling. [C] . Sharon D.Bryant, Yunden Jinsmaa, Lawrence H.Lazarus International Peptide Symposium;European Peptide Symposium . 2005

机译：使用结构相关的δ-阿片类受体激动剂和拮抗剂和分子建模鉴定阿片受体配体的相互作用。
8. Bifunctional Mu Opioid and Nociceptin/Orphanin FQ Receptor Agonist BU08028 Selectively Decreases Alcohol Drinking in Rhesus Monkeys [D] . Flynn, Shawn M. 2019

机译：双功能Mu阿片类和Noceptin / Orphanin FQ受体激动剂BU08028选择性减少恒河猴的饮酒量
9. The G-protein biased mu-opioid agonist TRV130 produces reinforcing and antinociceptive effects that are comparable to oxycodone in rats. [O] . C. Austin Zamarripa, Shelley R. Edwards, Hina N. Qureshi, -1

机译：G蛋白偏向性阿片类激动剂TRV130在大鼠中产生与羟考酮相当的增强和镇痛作用。
10. The G-protein biased mu-opioid agonist, TRV130, produces reinforcing and antinociceptive effects that are comparable to oxycodone in rats [O] . C. Austin Zamarripa, Shelley R. Edwards, Hina N. Qureshi, 2018

机译：G-蛋白质偏向的MU-阿片类激动剂TRV130产生与大鼠中羟考酮相当的增强和抗血汗效应
11. Co-Expression of Regulator of G Protein Signaling 4 (RGS4) and the MU Opioid Receptor in Regions of Rat Brain: Evidence That RGS4 Attenuates MU Opioid Receptor Signaling [R] . Crowder, A. T. 2003

机译：G蛋白信号调节因子4（RGs4）和mU阿片受体在大鼠脑区域的共表达：RGs4减弱mU阿片受体信号的证据

In a Rat Model of Opioid Maintenance, the G Protein-Biased Mu Opioid Receptor Agonist TRV130 Decreases Relapse to Oxycodone Seeking and Taking and Prevents Oxycodone-Induced Brain Hypoxia

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