Hayashi E, Yamada S
Br J Pharmacol. 1975 Feb;53(2):207-15. doi: 10.1111/j.1476-5381.1975.tb07350.x.
1 Some pharmacological properties of surugatoxin (SGTX), a purified toxic substance from the Japanese ivory mollusc (Babylonia japonica), have been investigated. SGTX (50 nmol/kg i.v.) produced a prolonged fall of blood pressure in anaesthetized cats. This hypotensive effect was neither blocked by atropine and propranolol nor by spinal cord transection. 2 SGTX (37-50 nmol/kg i.v.) inhibited the hypertensive and hypotensive response to 1,1-dimethyl-4-phenylpiperazinium iodide (DMPP) and to electrical stimulation of the splanchnic and vagal nerve, whereas it usually augmented the hypertensive response to adrenaline and to 4-(m-chlorophenylcarbamoyloxy)-2-butynyltrimethylammonium chloride (McN-A-343) in anaesthetized cats. 3 Close intra-arterial injection of SGTX (6.2-12.3 nmol/kg) to the superior cervical ganglion blocked the contractile response of the nictitating membrane to preganglionic stimulation of cervical sympathetic nerve or injected DMPP, but not to postganglionic stimulation or to injected adrenaline and McN-A-343. 4 SGTX affected neither the indirectly nor the directly stimulated response of the rat isolated phrenic nerve-diaphragm at concentrations less than 12.3 mum. 5 The effect of SGTX on the contractile response to some agonists and on the twitch response to transmural stimulation in the guinea-pig isolated ileum was investigated. At less than 12.3 mumSGTX did not depress responses to acetylcholine or histamine. The curves for nicotine- and DMPP-induced contractions were shifted to the right and depressed gradually as the concentration of SGTX was increased (12.3 nm-1.23 mum). SGTX partially inhibited the contraction induced by 5-hyroxytryptamine and the transmurally-stimulated twitch response. 6 These results suggest that SGTX has a ganglion-blocking action. The mode of anti-nicotinic action of SGTX in the guinea-pig isolated ileum seems to differ from that of hexamethonium and tetraethylammonium and to resemble more closely that of mecamylamine.
1 对从日本象牙贝(日本宝贝)中提纯得到的有毒物质蝾螺毒素(SGTX)的一些药理特性进行了研究。静脉注射SGTX(50 nmol/kg)可使麻醉猫的血压出现长时间下降。这种降压作用既不被阿托品、普萘洛尔阻断,也不受脊髓横断影响。2 静脉注射SGTX(37 - 50 nmol/kg)可抑制麻醉猫对1,1 - 二甲基 - 4 - 苯基哌嗪碘化物(DMPP)以及对内脏神经和迷走神经电刺激所产生的升压和降压反应,而它通常会增强麻醉猫对肾上腺素和4 - (间氯苯基氨甲酰氧基) - 2 - 丁炔基三甲基氯化铵(McN - A - 343)的升压反应。3 向上颈神经节动脉内近距离注射SGTX(6.2 - 12.3 nmol/kg)可阻断颈交感神经节前刺激或注射DMPP时瞬膜的收缩反应,但不影响节后刺激或注射肾上腺素及McN - A - 343时瞬膜的收缩反应。4 浓度低于12.3 μmol时,SGTX对大鼠离体膈神经 - 膈肌的间接或直接刺激反应均无影响。5 研究了SGTX对豚鼠离体回肠对某些激动剂的收缩反应以及对跨壁刺激的抽搐反应的影响。浓度低于12.3 μmol时,SGTX不会抑制对乙酰胆碱或组胺的反应。随着SGTX浓度增加(12.3 nmol - 1.23 μmol),尼古丁和DMPP诱导的收缩曲线右移并逐渐降低。SGTX部分抑制5 - 羟色胺诱导的收缩和跨壁刺激的抽搐反应。6 这些结果表明SGTX具有神经节阻断作用。SGTX在豚鼠离体回肠中的抗烟碱作用方式似乎不同于六甲铵和四乙铵,更类似于美加明。