Tatsumi M, Kajiwara A, Yasumoto T, Ohizumi Y
J Pharmacol Exp Ther. 1985 Dec;235(3):783-7.
Scaritoxin (STX), a potent toxic substance isolated from poisonous fish induced a dose-dependent contraction of the isolated guinea-pig vas deferens at concentrations of 10(-8) to 10(-6) g/ml. This contraction was abolished or inhibited by tetrodotoxin, low Na+ medium, phentolamine or reserpine, but not by atropine, chlorpheniramine or methysergide. STX shifted to the left the dose-contractile response curve for norepinephrine, KCI or acetylcholine in the vas deferens. STX caused a release of norepinephrine from the vas deferens, in a dose-dependent manner, which was blocked by tetrodotoxin, Mg++ or Ca++-free medium. In the guinea-pig taenia caeci or ileum, STX elicited a dose-dependent contraction. The contractions of both tissues were blocked completely by tetrodotoxin and were inhibited markedly by atropine but not by mecamylamine or chlorpheniramine. These results suggest that the STX-induced contraction is the result of an indirect action mediated through the norepinephrine release from adrenergic nerve terminals of the vas deferens and acetylcholine release from cholinergic nerve endings of the taenia caeci or the ileum. It is also suggested that STX causes an increase in Na+ permeability of the cell membrane of these tissues, which may play an important role in the release of chemical transmitters induced by STX.
石房蛤毒素(STX)是从有毒鱼类中分离出的一种强效有毒物质,在浓度为10⁻⁸至10⁻⁶克/毫升时,可使离体豚鼠输精管产生剂量依赖性收缩。这种收缩可被河豚毒素、低钠培养基、酚妥拉明或利血平消除或抑制,但不受阿托品、氯苯那敏或甲基麦角新碱的影响。STX使输精管中去甲肾上腺素、氯化钾或乙酰胆碱的剂量-收缩反应曲线向左移动。STX以剂量依赖性方式导致输精管释放去甲肾上腺素,这一过程被河豚毒素、无镁或无钙培养基阻断。在豚鼠盲肠带或回肠中,STX引起剂量依赖性收缩。两种组织的收缩均被河豚毒素完全阻断,并被阿托品显著抑制,但不受美加明或氯苯那敏的影响。这些结果表明,STX诱导的收缩是通过输精管肾上腺素能神经末梢释放去甲肾上腺素以及盲肠带或回肠胆碱能神经末梢释放乙酰胆碱介导的间接作用的结果。还表明,STX导致这些组织细胞膜的钠通透性增加,这可能在STX诱导的化学递质释放中起重要作用。