A new type of Ca2+ channel blocker, NC-1100, inhibits the low- and high-threshold Ca2+ currents in the rat CNS neurons

Norihisa Miyake, Minoru Wakamori, Norio Akaike

研究成果: Article査読

9 被引用数 (Scopus)

抄録

The effect of a new type of organic Ca2+ channel blocker, NC-1100 [(±)-1-(3,4-dimethoxyphenyl)-2-(4-diphenylmethylpiperazinyl)ethanol dihydrochloride], on both low- and high-threshold Ca2+ currents was studied in the whole-cell mode of the pyramidal neurons freshly dissociated from rat hippocampal CA1 region under voltage-clamp condition. The NC-1100 reversibly reduced the high-threshold Ca2+ current (HVA ICa) in a concentration-dependent manner without affecting the current-voltage relationship. The values of half-inhibition (IC50) were 1.3 × 10-5 and 9.1 × 10-6 M in external solution containing 10 and 2.5 mM Ca2+, respectively. The NC-1100 also decreased the low-threshold Ca2+ current (LVA ICa) in a concentration-dependent manner. The inhibitory potency was augmented by increasing the stimulation frequency and / or decreasing the extracellular Ca2+ concentration to a physiological range (2.5 mM). The IC50 value decreased to 7.7 × 10-7 M in external solution containing 2.5 mM Ca2+ at a stimulation frequency of 1 Hz. The NC-1100 delayed the reactivation of LVA Ca2+ channel and enhanced voltage-dependently the steady-state inactivation, suggesting that this drug bound not only the resting LVA Ca2+ channel but also the inactivated one.

本文言語English
ページ(範囲)215-220
ページ数6
ジャーナルBrain research
598
1-2
DOI
出版ステータスPublished - 1992 12 11

ASJC Scopus subject areas

  • 神経科学(全般)
  • 分子生物学
  • 臨床神経学
  • 発生生物学

フィンガープリント

「A new type of Ca<sup>2+</sup> channel blocker, NC-1100, inhibits the low- and high-threshold Ca<sup>2+</sup> currents in the rat CNS neurons」の研究トピックを掘り下げます。これらがまとまってユニークなフィンガープリントを構成します。

引用スタイル