Literature DB >> 28729057

Neuropathic pain-alleviating effects of pyrazole-conjugated arylsulfonamides as 5-HT6 receptor antagonists.

Jin Ri Hong1, Hyunah Choo2, Ghilsoo Nam3.   

Abstract

A novel series of arylsulfonylaminomethyl-3-(1-phenyl-5-isopropyl)pyrazoles was evaluated for serotonin receptor subtype 6 (5-HT6R) antagonistic effects in vitro. We also investigated their neuropathic pain-alleviating effects in vivo using a rat spinal nerve ligation (SNL) model. Bicyclic aromatic sulfonamino groups, such as naphthalene and quinolin-substituted derivatives, showed good 5-HT6 inhibitory activity in vitro. Among them, selected compounds, 12 and 13, having 8-quinoylsulfonamino groups, showed potent neuropathic pain-alleviating effects in the rat model.
Copyright © 2017 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  5-HT(6) receptor antagonist; Arylsulfonylaminomethylpyrazole; Neuropathic pain

Mesh：

Substances：

Year:  2017        PMID： 28729057     DOI： 10.1016/j.bmcl.2017.07.031

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  4 in total

1.  Peripheral 5-HT3 Receptors Are Involved in the Antinociceptive Effect of Bunodosine 391.

Authors:  Wilson Alves Ferreira Junior; Andre Junqueira Zaharenko; Kohei Kazuma; Gisele Picolo; Vanessa Pacciari Gutierrez; Jose Carlos de Freitas; Katsuhiro Konno; Yara Cury
Journal:  Toxins (Basel)       Date:  2017-12-27       Impact factor: 4.546

Review 2.  The Role of Descending Pain Modulation in Chronic Primary Pain: Potential Application of Drugs Targeting Serotonergic System.

Authors:  Zhuo-Ying Tao; Pei-Xing Wang; Si-Qi Wei; Richard J Traub; Jin-Feng Li; Dong-Yuan Cao
Journal:  Neural Plast       Date:  2019-12-17       Impact factor: 3.599

3.  Identification of a Potent and Selective 5-HT1A Receptor Agonist with In Vitro and In Vivo Antinociceptive Activity.

Authors:  Pasquale Linciano; Claudia Sorbi; Antonella Comitato; Anna Lesniak; Magdalena Bujalska-Zadrożny; Agata Pawłowska; Anna Bielenica; Jolanta Orzelska-Górka; Ewa Kędzierska; Grażyna Biała; Simone Ronsisvalle; Silvia Limoncella; Livio Casarini; Elena Cichero; Paola Fossa; Grzegorz Satała; Andrzej J Bojarski; Livio Brasili; Rita Bardoni; Silvia Franchini
Journal:  ACS Chem Neurosci       Date:  2020-12-02       Impact factor: 4.418

4.  Correlation of 5-HTR6 gene polymorphism with vestibular migraine.

Authors:  Xia Wu; Feng Qiu; Zhiwei Wang; Bing Liu; Xiaokun Qi
Journal:  J Clin Lab Anal       Date:  2019-10-06       Impact factor: 2.352
  4 in total

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