硫代甘油与不含二硫键的催产素类似物之间不存在拮抗作用。
Lack of antagonism between thioglycerol and an oxytocin analogue not containing a disulphide bond.
作者信息
Schild H O
出版信息
Br J Pharmacol. 1970 May;39(1):69-72.
Abstract
- The antagonistic effect of thioglycerol against oxytocin and an analogue of oxytocin not containing a disulphide bridge (desamino-1-carba-oxytocin) has been compared in the rat isolated depolarized uterus.2. Thioglycerol clearly differentiated between the two compounds, 40 mM producing a dose ratio of 12 with oxytocin but only 1.5 with the carba compound.3. It was confirmed that thioglycerol produces no appreciable destruction of oxytocin in vitro.4. The mode of action of thiols in antagonizing specifically S-S polypeptides is discussed. It is concluded that they probably do not produce their effect either by inactivating receptors or by inactivating S-S polypeptides in solution. A possible mechanism is that thiols potentiate the destruction of S-S polypeptides at the receptor site.
摘要
在大鼠离体去极化子宫中比较了硫代甘油对催产素和一种不含二硫键的催产素类似物（脱氨基-1-碳-催产素）的拮抗作用。
硫代甘油能明确区分这两种化合物，40 mM的硫代甘油与催产素产生的剂量比为12，但与碳化合物仅为1.5。
已证实硫代甘油在体外不会对催产素造成明显破坏。
讨论了硫醇特异性拮抗S-S多肽的作用方式。得出的结论是，它们可能既不是通过使受体失活，也不是通过使溶液中的S-S多肽失活来产生作用。一种可能的机制是硫醇增强了受体部位S-S多肽的破坏。
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本文引用的文献
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[Mechanism of the inactivation of oxytocin by uterine tissue].[子宫组织使催产素失活的机制]
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The antagonism of disulphide polypeptides by thiols.硫醇对二硫键多肽的拮抗作用。
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The effect of metals on the S-S polypeptide receptor in depolarized rat uterus.金属对去极化大鼠子宫中S-S多肽受体的影响。
Br J Pharmacol. 1969 Jun;36(2):329-49. doi: 10.1111/j.1476-5381.1969.tb09509.x.
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