Amiloride derived inhibitors of acid-sensing ion channel-3 (ASIC3)

被引:37
|
作者
Kuduk, Scott D. [1 ]
Di Marco, Christina N. [1 ]
Chang, Ronald K. [1 ]
DiPardo, Robert M. [1 ]
Cook, Sean P. [2 ]
Cato, Matthew J. [2 ]
Jovanovska, Aneta [2 ]
Urban, Mark O. [2 ]
Leitl, Michael [2 ]
Spencer, Robert H. [2 ]
Kane, Stefanie A. [2 ]
Bilodeau, Mark T. [1 ]
Hartman, George D. [1 ]
Bock, Mark G. [1 ]
机构
[1] Merck Res Labs, Dept Med Chem, West Point, PA 19486 USA
[2] Pain Res Merck Res Labs, West Point, PA 19486 USA
关键词
Amiloride; Pain; ASIC3; Acidosis; RECEPTOR;
D O I
10.1016/j.bmcl.2009.03.029
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of amiloride derivatives modified at the 5-position of the pyrazine ring were evaluated as inhibitors of acid-sensing ion channel-3 (ASIC3), a novel target for the treatment of chronic pain. (C) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码:2514 / 2518
页数:5
相关论文
共 50 条
  • [31] Acid-sensing ion channel 3: An analgesic target
    Dulai, Jasdip Singh
    Smith, Ewan St John
    Rahman, Taufiq
    CHANNELS, 2021, 15 (01) : 94 - 127
  • [32] Analgesic Activity of Acid-Sensing Ion Channel 3 (ASIC3) Inhibitors: Sea Anemones Peptides Ugr9-1 and APETx2 versus Low Molecular Weight Compounds
    Andreev, Yaroslav A.
    Osmakov, Dmitry I.
    Koshelev, Sergey G.
    Maleeva, Ekaterina E.
    Logashina, Yulia A.
    Palikov, Victor A.
    Palikova, Yulia A.
    Dyachenko, Igor A.
    Kozlov, Sergey A.
    MARINE DRUGS, 2018, 16 (12):
  • [33] ASIC2b-dependent regulation of ASIC3, an essential acid-sensing ion channel subunit in sensory neurons via the partner protein PICK-1
    Deval, E
    Salinas, M
    Baron, A
    Lingueglia, E
    Lazdunski, M
    JOURNAL OF BIOLOGICAL CHEMISTRY, 2004, 279 (19) : 19531 - 19539
  • [34] Acidic pH promotes intervertebral disc degeneration: Acid-sensing ion channel-3 as a potential therapeutic target
    Gilbert, Hamish T. J.
    Hodson, Nathan
    Baird, Pauline
    Richardson, Stephen M.
    Hoyland, Judith A.
    SCIENTIFIC REPORTS, 2016, 6
  • [35] The expression profile of acid-sensing ion channel (ASIC) subunits ASIC1a, ASIC1b, ASIC2a, ASIC2b, and ASIC3 in the esophageal vagal afferent nerve subtypes
    Dusenkova, Svetlana
    Ru, Fei
    Surdenikova, Lenka
    Nassenstein, Christina
    Hatok, Jozef
    Dusenka, Robert
    Banovcin, Peter, Jr.
    Kliment, Jan
    Tatar, Milos
    Kollarik, Marian
    AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY, 2014, 307 (09): : G922 - G930
  • [36] ACID-SENSING ION CHANNEL 3 (ASIC3) INHIBITOR INCREASES FUNCTIONAL BLADDER CAPACITY WITH OR WITHOUT ACIDIC IRRITATION OF LOWER URINARY TRACT IN MICE WHEN ADMINISTERING INTRAPERITONEALLY BUT NOT INTRAVESICALLY
    Yoshiyama, M.
    Kobayashi, H.
    Araki, I
    Takeda, M.
    NEUROUROLOGY AND URODYNAMICS, 2020, 39 : S282 - S283
  • [37] INHIBITORY REGULATION OF ACID-SENSING ION CHANNEL 3 BY ZINC
    Jiang, Q.
    Papasian, C. J.
    Wang, J. Q.
    Xiong, Z. G.
    Chu, X. P.
    NEUROSCIENCE, 2010, 169 (02) : 574 - 583
  • [38] Acid-Sensing Ion Channel 3 in Retinal Function and Survival
    Ettaiche, Mohammed
    Deval, Emmanuel
    Pagnotta, Sophie
    Lazdunski, Michel
    Lingueglia, Eric
    INVESTIGATIVE OPHTHALMOLOGY & VISUAL SCIENCE, 2009, 50 (05) : 2417 - 2426
  • [39] DISTRIBUTION OF ACID-SENSING ION CHANNEL 3 IN THE RAT HYPOTHALAMUS
    Meng, Q. -Y.
    Wang, W.
    Chen, X. -N.
    Xu, T. -L.
    Zhou, J. -N.
    NEUROSCIENCE, 2009, 159 (03) : 1126 - 1134
  • [40] Coxsackievirus and adenovirus receptor (CAR) mediates trafficking of acid sensing ion channel 3 (ASIC3) via PSD-95
    Excoffon, Katherine J. D. A.
    Kolawole, Abimbola O.
    Kusama, Nobuyoshi
    Gansemer, Nicholas D.
    Sharma, Priyanka
    Hruska-Hageman, Alesia M.
    Petroff, Elena
    Benson, Christopher J.
    BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 2012, 425 (01) : 13 - 18