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从毒鲉(Synanceia trachynis)有毒皮肤分泌物中获得的一个组分对豚鼠回肠的抗痉挛作用。

The antispasmogenic action on guinea-pig ileum of a fraction obtained from the toxic skin secretion of the stonefish, Synanceia trachynis.

作者信息

Cameron A M, Lewis R J

出版信息

Toxicon. 1982;20(6):991-1000. doi: 10.1016/0041-0101(82)90101-5.

DOI:10.1016/0041-0101(82)90101-5
PMID:7164115
Abstract

The toxic skin tubercle gland secretion of the stonefish, Synanceia trachynis, contains a smooth muscle antispasmogen that is readily distinguished from papaverine, verapamil and both alpha and beta adrenoreceptor agonists. At 15 micrograms/ml, the toxin containing fraction markedly inhibited the phasic response and had a lesser inhibitory effect on the tonic response of acetylcholine-and KCl-induced contractures of guinea-pig ileum, while at 50 micrograms/ml, the toxin markedly inhibited both responses. Over the same dose range the toxin fraction markedly inhibited BaCl2-induced contractile responses but did not distinguish between the phasic and tonic components. Whereas the toxin fraction markedly reduced the tone of previously induced supramaximal KCl and acetylcholine responses of guinea-pig ileum, it had little effect on the tone of previously induced BaCl2 responses. The toxin non-competitively inhibited acetylcholine-induced contractions of guinea-pig ileum and similarly non-competitively inhibited the response induced by Ca2+ in high-[K+] Ringer. The toxin is not a chelating agent for Ca2+ or Mg2+ and it does not affect ATP-induced contracture of glycerinated guinea-pig ileum. The antispasmogenic effect of the toxin contained in the fraction does not result from inhibition of cAMP phosphodiesterase activity.

摘要

毒鲉(Synanceia trachynis)的有毒皮肤结节腺分泌物含有一种平滑肌抗痉挛原,它很容易与罂粟碱、维拉帕米以及α和β肾上腺素能受体激动剂区分开来。在15微克/毫升时,含毒素部分显著抑制了豚鼠回肠乙酰胆碱和氯化钾诱导的挛缩的相性反应,而对强直性反应的抑制作用较小;在50微克/毫升时,毒素显著抑制了两种反应。在相同剂量范围内,毒素部分显著抑制了氯化钡诱导的收缩反应,但未区分相性和强直性成分。虽然毒素部分显著降低了豚鼠回肠先前诱导的超最大氯化钾和乙酰胆碱反应的张力,但对先前诱导的氯化钡反应的张力影响很小。该毒素非竞争性抑制豚鼠回肠乙酰胆碱诱导的收缩,同样非竞争性抑制高钾任氏液中钙离子诱导的反应。该毒素不是钙或镁的螯合剂,也不影响甘油化豚鼠回肠ATP诱导的挛缩。该部分所含毒素的抗痉挛作用并非源于抑制环磷酸腺苷磷酸二酯酶活性。

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