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Biased versus Partial Agonism in the Search for Safer Opioid Analgesics.在寻找更安全的阿片类镇痛药时,偏倚与部分激动作用的比较。
Molecules. 2020 Aug 25;25(17):3870. doi: 10.3390/molecules25173870.
2
Oliceridine, a G protein-selective ligand at the μ-opioid receptor, for the management of moderate to severe acute pain.奥利替丁,一种μ-阿片受体的G蛋白选择性配体,用于治疗中重度急性疼痛。
Drugs Today (Barc). 2020 Apr;56(4):269-286. doi: 10.1358/dot.2020.56.4.3107707.
3
Pharmacological and non-pharmacological treatments for neuropathic pain: Systematic review and French recommendations.神经病理性疼痛的药物和非药物治疗:系统评价和法国建议。
Rev Neurol (Paris). 2020 May;176(5):325-352. doi: 10.1016/j.neurol.2020.01.361. Epub 2020 Apr 7.
4
Biased agonism of clinically approved μ-opioid receptor agonists and TRV130 is not controlled by binding and signaling kinetics.临床上批准的 μ 阿片受体激动剂和 TRV130 的偏性激动作用不受结合和信号转导动力学的控制。
Neuropharmacology. 2020 Apr;166:107718. doi: 10.1016/j.neuropharm.2019.107718. Epub 2019 Jul 24.
5
APOLLO-2: A Randomized, Placebo and Active-Controlled Phase III Study Investigating Oliceridine (TRV130), a G Protein-Biased Ligand at the μ-Opioid Receptor, for Management of Moderate to Severe Acute Pain Following Abdominoplasty.APOLLO-2 研究:一项随机、安慰剂和阳性对照的 III 期研究,旨在评估奥立哌啶(TRV130)治疗腹部整形术后中重度急性疼痛的疗效,奥立哌啶是一种作用于 μ 阿片受体的 G 蛋白偶联配体。
Pain Pract. 2019 Sep;19(7):715-731. doi: 10.1111/papr.12801. Epub 2019 Jun 24.
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Dexmedetomidine enhances glymphatic brain delivery of intrathecally administered drugs.右美托咪定增强鞘内给予药物的脑内给药。
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Buprenorphine Treatment for Opioid Use Disorder: An Overview.阿片类物质使用障碍的丁丙诺啡治疗:概述。
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APOLLO-1: a randomized placebo and active-controlled phase III study investigating oliceridine (TRV130), a G protein-biased ligand at the µ-opioid receptor, for management of moderate-to-severe acute pain following bunionectomy.APOLLO-1:一项随机、安慰剂对照和活性药物对照的III期研究,旨在研究μ-阿片受体的G蛋白偏向性配体oliceridine(TRV130)用于拇囊炎切除术后中重度急性疼痛的管理。
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Arrestin recruitment and signaling by G protein-coupled receptor heteromers.G 蛋白偶联受体异源二聚体的 arrestin 募集和信号转导。
Neuropharmacology. 2019 Jul 1;152:15-21. doi: 10.1016/j.neuropharm.2018.11.010. Epub 2018 Nov 9.
10
Transcranial optical imaging reveals a pathway for optimizing the delivery of immunotherapeutics to the brain.经颅光学成像是一种可以优化免疫疗法向大脑传递的途径。
JCI Insight. 2018 Oct 18;3(20):120922. doi: 10.1172/jci.insight.120922.

丁丙诺啡:远超“天花板”。

Buprenorphine: Far Beyond the "Ceiling".

机构信息

Department of Experimental Medicine, Division of Pharmacology, University of Campania "L. Vanvitelli", 80138 Naples, Italy.

Division of Anesthesiology, Intensive Care and Pain Medicine, ICOT Polo Pontino, Sapienza University of Rome, 04100 Rome, Italy.

出版信息

Biomolecules. 2021 May 31;11(6):816. doi: 10.3390/biom11060816.

DOI:10.3390/biom11060816
PMID:34072706
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8230089/
Abstract

Chronic pain, including neuropathic pain, represents an untreated disease with important repercussions on the quality of life and huge costs on the national health system. It is well known that opioids are the most powerful analgesic drugs, but they represent the second or third line in neuropathic pain, that remain difficult to manage. Moreover, these drugs show several side effects that limit their use. In addition, opioids possess addictive properties that are associated with misuse and drug abuse. Among available opioids compounds, buprenorphine has been suggested advantageous for a series of clinical reasons, including the effectiveness in neuropathic pain. Some properties are partly explained by its unique pharmacological characteristics. However, questions on the dynamic profile remain to be answered. Pharmacokinetics optimization strategies, and additional potentialities, are still to be explored. In this paper, we attempt to conceptualize the potential undiscovered dynamic profile of buprenorphine.

摘要

慢性疼痛,包括神经性疼痛,是一种未得到治疗的疾病,对生活质量有重要影响,给国家卫生系统带来巨大负担。众所周知,阿片类药物是最有效的镇痛药,但它们在神经性疼痛的治疗中仅处于二线或三线地位,仍然难以控制。此外,这些药物具有多种副作用,限制了它们的使用。此外,阿片类药物具有成瘾性,这与滥用和药物滥用有关。在可用的阿片类化合物中,丁丙诺啡因其一系列临床原因而被认为具有优势,包括对神经性疼痛的有效性。一些特性部分可以通过其独特的药理学特征来解释。然而,关于其动态特征仍存在一些问题有待回答。药代动力学优化策略以及其他潜在可能性仍有待探索。在本文中,我们试图从概念上理解丁丙诺啡潜在的未被发现的动态特征。