Ichida S, Oka H, Masada A, Fujisue T, Hata T, Matsuda N
Department of Biological Chemistry, Faculty of Pharmacy, Kinki University, Higashi-Osaka, Japan.
Jpn J Pharmacol. 1988 Dec;48(4):395-405. doi: 10.1254/jjp.48.395.
The effect of synthetic omega-conotoxin (omega-CgTX) on the contractile responses of segments of rat ileum, stomach fundus and uterus and guinea pig taenia coli were investigated. Omega-CgTX (10(-9)-5 x 10(-6) M) did not inhibit the contractile responses of all smooth muscle segments to high KCl and/or ACh. However, unexpectedly, omega-CgTX (3 x 10(-7)-10(-5) M) alone caused dose-dependent contraction of segments of the stomach fundus and uterus. These contractile responses to omega-CgTX alone depended upon the presence and/or the influx of extracellular Ca2+; and they were inhibited by calcium antagonists such as diltiazem, nitrendipine and verapamil, with the exception that the segments of stomach fundus was not inhibited by verapamil. With the segments of uterus, but not those of other tissues, omega-CgTX (10(-7)-5 x 10(-6) M) significantly enhanced the contractile responses to various concentrations of ACh and high KCl. With rat ileum and guinea pig taenia coli segments, omega-CgTX (10(-9)-5 x 10(-6) M) did not induce a contractile response or have an enhancing effect. These findings suggest that omega-CgTX may have a calcium agonist-like effect on smooth muscles such as the stomach fundus and uterus of rats.
研究了合成ω-芋螺毒素(ω-CgTX)对大鼠回肠、胃底和子宫以及豚鼠结肠带节段收缩反应的影响。ω-CgTX(10⁻⁹ - 5×10⁻⁶ M)不抑制所有平滑肌节段对高钾和/或乙酰胆碱的收缩反应。然而,出乎意料的是,ω-CgTX(3×10⁻⁷ - 10⁻⁵ M)单独引起胃底和子宫节段的剂量依赖性收缩。这些对单独ω-CgTX的收缩反应依赖于细胞外Ca²⁺的存在和/或内流;并且它们被钙拮抗剂如地尔硫卓、尼群地平和维拉帕米抑制,但胃底节段不受维拉帕米抑制。对于子宫节段,而不是其他组织的节段,ω-CgTX(10⁻⁷ - 5×10⁻⁶ M)显著增强了对各种浓度乙酰胆碱和高钾的收缩反应。对于大鼠回肠和豚鼠结肠带节段,ω-CgTX(10⁻⁹ - 5×10⁻⁶ M)未诱导收缩反应或产生增强作用。这些发现表明,ω-CgTX可能对大鼠胃底和子宫等平滑肌具有钙激动剂样作用。