Discovery of SHR9352: A Highly Potent G Protein-Biased μ-Opioid Receptor Agonist

Xin Li; Wei He; Yang Chen; Guimei Yang; Hong Wan; Lei Zhang; Qiyue Hu; Jun Feng; Zhigao Zhang; Feng He; Chang Bai; Lianshan Zhang; Li You; Weikang Tao

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Discovery of SHR9352: A Highly Potent G Protein-Biased μ-Opioid Receptor Agonist

机译：SHR9352的发现：高强度G蛋白偏置的μ阿片受体激动剂

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Recently, targeting the G protein-biased signaling has emerged as an attractive therapeutic strategy for treating severe acute pain with the potential to reduce the side effect of the traditional opioid drug. Herein, we describe the discovery of a highly potent G protein-biased μ-opioid receptor (MOR) agonist, SHR9352. This novel molecule exhibited excellent MOR activity and limited β-arrestin recruitment, as well as a high selectivity over κ-opioid receptor and δ-opioid receptor demonstrated robust in vivo efficacy and displayed favorable pharmacokinetic properties across species.

机译：近来，靶向G蛋白偏向的信号已经成为一种有吸引力的治疗策略，用于治疗严重的急性疼痛，具有减轻传统阿片类药物副作用的潜力。在这里，我们描述了一种高度有效的G蛋白偏向μ阿片受体（MOR）激动剂SHR9352的发现。这种新型分子表现出出色的MOR活性和有限的β-arrestin募集，以及对κ阿片受体和δ阿片受体的高选择性，显示出强大的体内功效，并在整个物种中显示出良好的药代动力学特性。

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《ACS Omega》 |2017年第12期|共7页
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Xin Li; Wei He; Yang Chen; Guimei Yang; Hong Wan; Lei Zhang; Qiyue Hu; Jun Feng; Zhigao Zhang; Feng He; Chang Bai; Lianshan Zhang; Li You; Weikang Tao;
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1. Novel TIPP (H-Tyr-Tic-Phe-Phe-OH) analogues displaying a wide range of efficacies at the δ opioid receptor. Discovery of two highly potent and selective δ opioid agonists [J] . BerezowskaI., LemieuxC., ChungN.N., Bioorganic and Medicinal Chemistry Letters . 2012,第5期

机译：新型TIPP（H-Tyr-Tic-Phe-Phe-OH）类似物在δ阿片受体上显示出广泛的功效。发现了两种高效和选择性的δ阿片激动剂
2. Discovery of a Highly Selective and Potent kappa Opioid Receptor Agonist from N-Cyclopropylmethyl-7 alpha-phenyl-6,14-endoethanotetrahydronorthebaines with Reduced Central Nervous System (CNS) Side Effects Navigated by the Message-Address Concept [J] . Xiao Li, Wang Yujun, Zhang Mumei, Journal of Medicinal Chemistry . 2019,第24期

机译：从N-环丙基甲基-7α-苯基-6,14-内乙酸四氢乙烯雌激酶的发现，从N-环丙基甲基-6α-苯基-6,14-内乙酸异常效应的发现，通过消息地址概念导航的减少的中枢神经系统（CNS）副作用
3. Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist [J] . Spetea M., Berzetei-Gurske I.P., Guerrieri E., Journal of Medicinal Chemistry . 2012,第22期

机译：二苯乙胺衍生物（HS665）的发现和药理评估，这是一种高效且选择性的κ阿片受体激动剂
4. Synthesis and pharmacological activity of Dmt-Tic analogs with highly potent agonist and antagonist/agonist opioid activity [C] . Remo Guerrini, Gianfranco Balboni, Daniela Girolamo Calo, the International Peptide Symposium . 2001

机译：具有高效激动剂和拮抗剂/激动剂阿片类能活性DMT-TIC类似物的合成与药理活性
5. SAR studies on a weak delta opioid dipeptide antagonist (Tyr-Tic) and a potent mu opioid peptidomimetic agonist. [D] . Ma, Wenli. 2000

机译：SAR研究了一种弱δ阿片类二肽拮抗剂（Tyr-Tic）和一种有效的μ阿片类肽模拟激动剂。
6. Discovery of SHR9352: A Highly Potent G Protein-Biased μ-OpioidReceptor Agonist [O] . Xin Li, *, Wei He, 2017

机译：SHR9352的发现：高强度G蛋白偏置的μ阿片类药物受体激动剂
7. Discovery of SHR9352: A Highly Potent G Protein-Biased μ‑Opioid Receptor Agonist [O] . Xin Li, Wei He, Yang Chen, 2017

机译：发现sHR9352：一种高效G蛋白偏向的μ-阿片受体激动剂

Discovery of SHR9352: A Highly Potent G Protein-Biased μ-Opioid Receptor Agonist

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