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The neurosteroid allopregnanolone sulfate inhibits Nav1.3 α subunit-containing voltage-gated sodium channels, expressed in Xenopus oocytes.
Horishita, Takafumi; Yanagihara, Nobuyuki; Ueno, Susumu; Okura, Dan; Horishita, Reiko; Minami, Tomoko; Ogata, Yuichi; Sudo, Yuka; Uezono, Yasuhito; Kawasaki, Takashi.
Afiliação
  • Horishita T; Department of Anesthesiology, School of Medicine, University of Occupational and Environmental Health, 1-1 Iseigaoka, Yahatanishiku, Kitakyushu, Fukuoka, 807-8555, Japan. Electronic address: thori@med.uoeh-u.ac.jp.
  • Yanagihara N; School of Medicine, University of Occupational and Environmental Health, 1-1 Iseigaoka, Yahatanishiku, Kitakyushu, Fukuoka, 807-8555, Japan.
  • Ueno S; Department of Occupational Toxicology, Institute of Industrial Ecological Sciences, University of Occupational and Environmental Health, 1-1 Iseigaoka, Yahatanishiku, Kitakyushu, Fukuoka, 807-8555, Japan.
  • Okura D; Department of Anesthesiology, School of Medicine, University of Occupational and Environmental Health, 1-1 Iseigaoka, Yahatanishiku, Kitakyushu, Fukuoka, 807-8555, Japan.
  • Horishita R; Department of Anesthesiology, School of Medicine, University of Occupational and Environmental Health, 1-1 Iseigaoka, Yahatanishiku, Kitakyushu, Fukuoka, 807-8555, Japan.
  • Minami T; Department of Anesthesiology, School of Medicine, University of Occupational and Environmental Health, 1-1 Iseigaoka, Yahatanishiku, Kitakyushu, Fukuoka, 807-8555, Japan.
  • Ogata Y; Department of Anesthesiology, School of Medicine, University of Occupational and Environmental Health, 1-1 Iseigaoka, Yahatanishiku, Kitakyushu, Fukuoka, 807-8555, Japan.
  • Sudo Y; Department of Molecular Pathology & Metabolic Disease, Faculty of Pharmaceutical Sciences, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba, 278-8510, Japan.
  • Uezono Y; Cancer Pathophysiology Division, National Cancer Center Research Institute, 5-1-1 Tsukiji, Chuouku, Tokyo, 104-0045, Japan.
  • Kawasaki T; Department of Anesthesiology, School of Medicine, University of Occupational and Environmental Health, 1-1 Iseigaoka, Yahatanishiku, Kitakyushu, Fukuoka, 807-8555, Japan.
J Pharmacol Sci ; 137(1): 93-97, 2018 May.
Article em En | MEDLINE | ID: mdl-29773519
ABSTRACT
The neurosteroid allopregnanolone has potent analgesic effects, and its potential use for neuropathic pain is supported by recent reports. However, the analgesic mechanisms are obscure. The voltage-gated sodium channels (Nav) α subunit Nav1.3 is thought to play an essential role in neuropathic pain. Here, we report the effects of allopregnanolone sulfate (APAS) on sodium currents (INa) in Xenopus oocytes expressing Nav1.3 with ß1 or ß3 subunits. APAS suppressed INa of Nav1.3 with ß1 and ß3 in a concentration-dependent manner (IC50 values; 75 and 26 µmol/L). These results suggest the possible importance of Nav1.3 inhibition for the analgesic mechanisms of allopregnanolone.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Oócitos / Pregnanolona / Neurotransmissores / Canal de Sódio Disparado por Voltagem NAV1.3 / Bloqueadores do Canal de Sódio Disparado por Voltagem / Analgésicos Limite: Animals Idioma: En Revista: J Pharmacol Sci Assunto da revista: FARMACOLOGIA Ano de publicação: 2018 Tipo de documento: Article
Texto completo
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Oócitos / Pregnanolona / Neurotransmissores / Canal de Sódio Disparado por Voltagem NAV1.3 / Bloqueadores do Canal de Sódio Disparado por Voltagem / Analgésicos Limite: Animals Idioma: En Revista: J Pharmacol Sci Assunto da revista: FARMACOLOGIA Ano de publicação: 2018 Tipo de documento: Article