Výsledky vyhledávání - "Mu opioid receptor (MOR)"

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Chronic tianeptine induces tolerance in analgesia and hyperlocomotion via mu-opioid receptor activation in mice

Autor: Florence Allain, Aliza T. Ehrlich, Michael McNicholas, Florence Gross, Weiya Ma, Brigitte L. Kieffer, Emmanuel Darcq

Publikováno v: Frontiers in Psychiatry, Vol 14 (2023)

IntroductionTianeptine is approved in some countries to treat depression and anxiety. In addition to its activity on serotonin and glutamate neurotransmission, tianeptine has been proven to be a mu-opioid receptor (MOR) agonist, but only a few precli

Externí odkaz: https://doaj.org/article/fbc1e78565a6457984f10478c201776d

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Modulation of G-protein activation, calcium currents and opioid receptor phosphorylation by the pH-dependent antinociceptive agonist NFEPP

Autor: Melih Özgür Celik, Viola Seitz, Fatih Yergöz, Sandeep Dembla, Nina Kathleen Blum, Stefan Schulz, Christoph Stein

Publikováno v: Frontiers in Molecular Neuroscience, Vol 16 (2023)

N-(3-fluoro-1-phenethylpiperidine-4-yl)-N-phenyl propionamide is a newly-designed pain killer selectively activating G-protein-coupled mu-opioid receptors (MOR) in acidic injured tissues, and therefore devoid of central side effects which are typical

Externí odkaz: https://doaj.org/article/d24edb3270114fefa997af4d5bc07964

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Discovery of a Potent Highly Biased MOR Partial Agonist among Diastereomeric C9-Hydroxyalkyl-5-phenylmorphans

Autor: Joshua A. Lutz, Agnieszka Sulima, Eugene S. Gutman, Eric W. Bow, Dan Luo, Sophia Kaska, Thomas E. Prisinzano, Carol A. Paronis, Jack Bergman, Gregory H. Imler, Andrew T. Kerr, Arthur E. Jacobson, Kenner C. Rice

Publikováno v: Molecules, Vol 28, Iss 12, p 4795 (2023)

All possible diastereomeric C9-hydroxymethyl-, hydroxyethyl-, and hydroxypropyl-substituted 5-phenylmorphans were synthesized to explore the three-dimensional space around the C9 substituent in our search for potent MOR partial agonists. These compou

Externí odkaz: https://doaj.org/article/d4aecd3b74884423a75e5b6fc1efb0c0

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Chronic morphine regulates TRPM8 channels via MOR-PKCβ signaling

Autor: Mircea Iftinca, Lilian Basso, Robyn Flynn, Charlie Kwok, Corinne Roland, Ahmed Hassan, Manon Defaye, Rithwik Ramachandran, Tuan Trang, Christophe Altier

Publikováno v: Molecular Brain, Vol 13, Iss 1, Pp 1-14 (2020)

Abstract Postoperative shivering and cold hypersensitivity are major side effects of acute and chronic opioid treatments respectively. TRPM8 is a cold and menthol-sensitive channel found in a subset of dorsal root ganglion (DRG) nociceptors. Deletion

Externí odkaz: https://doaj.org/article/f0704a57a3d34ea38724d49347c09a79

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Optimized synthesis of enantiomeric C9-keto-5-phenylmorphans, essential intermediates for novel MOR agonists and antagonists

Autor: Agnieszka Sulima, Jason A. Deck, Muneaki Kurimura, Arthur E. Jacobson, Kenner C. Rice

Publikováno v: Results in Chemistry, Vol 4, Iss , Pp 100390- (2022)

Two modifications of previous procedures enabled the high-yield scalable synthesis of the pharmacologically important enantiomers of a C9-keto-5-phenylmorphan ((1R,5R)- and (1S,5S)-5-(3-methoxyphenyl)-2-methyl-2-azabicyclo[3.3.1]nonan-9-one). The use

Externí odkaz: https://doaj.org/article/73dd035c57744f8aaacb06c43321a873

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Thymosin Beta 4 Is Involved in the Development of Electroacupuncture Tolerance

Autor: Juan Wan, Yi Ding, Sha Nan, Qiulin Zhang, Jinrui Sun, Chuanguang Suo, Mingxing Ding

Publikováno v: Frontiers in Cellular Neuroscience, Vol 13 (2019)

Background: Electroacupuncture (EA) tolerance, a negative therapeutic effect, is a gradual decline in antinociception because of its repeated or prolonged use. This study aims to explore the role of thymosin beta 4 (Tβ4), having neuro-protection pro

Externí odkaz: https://doaj.org/article/0d13accdbe2b43fa9d863bd0f633d07b

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