Literature DB >> 18829333

Design, synthesis, and structure-activity relationship of novel opioid kappa-agonists.

Koji Kawai1, Jun Hayakawa, Toru Miyamoto, Yoshifumi Imamura, Shinichi Yamane, Hisanori Wakita, Hideaki Fujii, Kuniaki Kawamura, Hirotoshi Matsuura, Naoki Izumimoto, Ryosuke Kobayashi, Takashi Endo, Hiroshi Nagase.   

Abstract

By focusing on 4,5-epoxymorphinan, a traditional opioid skeleton but a new structure in the opioid kappa-agonist research field, and by rationally applying the 'message-address concept' and 'accessory site hypothesis,' we discovered a new chemical class opioid kappa-agonist, TRK-820 (1). Its development as an antipruritus is now in the final stage. Here, the full scope of its design, synthesis, and structure-activity relationship are described.

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Year:  2008        PMID： 18829333     DOI： 10.1016/j.bmc.2008.09.011

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  8 in total

1.  Opioid activity of spinally selective analogues of N-naphthoyl-β-naltrexamine in HEK-293 cells and mice.

Authors:  Morgan Le Naour; Mary M Lunzer; Mike D Powers; Philip S Portoghese
Journal:  J Med Chem       Date:  2012-01-05       Impact factor: 7.446

Review 2.  Kappa-opioid ligands in the study and treatment of mood disorders.

Authors:  William A Carlezon; Cécile Béguin; Allison T Knoll; Bruce M Cohen
Journal:  Pharmacol Ther       Date:  2009-06-02       Impact factor: 12.310

3.  Verifying the role of 3-hydroxy of 17-cyclopropylmethyl-4,5α-epoxy-3,14β-dihydroxy-6β-[(4'-pyridyl) carboxamido]morphinan derivatives via their binding affinity and selectivity profiles on opioid receptors.

Authors:  Boshi Huang; Rama Gunta; Huiqun Wang; Mengchu Li; Danni Cao; Rolando E Mendez; James C Gillespie; Chongguang Chen; Lan-Hsuan M Huang; Lee-Yuan Liu-Chen; Dana E Selley; Yan Zhang
Journal:  Bioorg Chem       Date:  2021-02-09       Impact factor: 5.275

4.  Exploring the putative mechanism of allosteric modulations by mixed-action kappa/mu opioid receptor bitopic modulators.

Authors:  Huiqun Wang; Danni Cao; James C Gillespie; Rolando E Mendez; Dana E Selley; Lee-Yuan Liu-Chen; Yan Zhang
Journal:  Future Med Chem       Date:  2021-02-16       Impact factor: 3.808

5.  Synthesis and pharmacological activities of 6-glycine substituted 14-phenylpropoxymorphinans, a novel class of opioids with high opioid receptor affinities and antinociceptive potencies.

Authors:  Mariana Spetea; Petra Windisch; Yan Guo; Indre Bileviciute-Ljungar; Johannes Schütz; Muhammad Faheem Asim; Ilona P Berzetei-Gurske; Pal Riba; Kornel Kiraly; Susanna Fürst; Mahmoud Al-Khrasani; Helmut Schmidhammer
Journal:  J Med Chem       Date:  2011-01-14       Impact factor: 7.446

6.  Topical administration of the kappa opioid receptor agonist nalfurafine suppresses corneal neovascularization and inflammation.

Authors:  Hurramhon Shokirova; Takenori Inomata; Tsuyoshi Saitoh; Jun Zhu; Kenta Fujio; Yuichi Okumura; Ai Yanagawa; Keiichi Fujimoto; Jaemyoung Sung; Atsuko Eguchi; Maria Miura; Ken Nagino; Kunihiko Hirosawa; Mizu Kuwahara; Yasutsugu Akasaki; Hiroshi Nagase; Akira Murakami
Journal:  Sci Rep       Date:  2021-04-21       Impact factor: 4.379

7.  Post-Marketing Surveillance Study of the Safety and Efficacy of Nalfurafine (Capsules 2.5 μg, Oral Dispersing Tablets 2.5 μg) in 1186 Patients with Chronic Liver Disease and Intractable Pruritus.

Authors:  Hiroshi Yoshitani; Junko Ito; Hideki Kozono
Journal:  Hepat Med       Date:  2022-05-02

8.  Post-marketing surveillance study of the safety and efficacy of nalfurafine hydrochloride (Remitch® capsules 2.5 μg) in 3,762 hemodialysis patients with intractable pruritus.

Authors:  Hideki Kozono; Hiroshi Yoshitani; Ryoko Nakano
Journal:  Int J Nephrol Renovasc Dis       Date:  2018-01-15
  8 in total

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