Cornely M, Rimpler M
Z Geburtshilfe Perinatol. 1985 May-Jun;189(3):103-11.
An improved bioassay for the testing of oxytocic compounds by the use of myometrium layer preparations has been developed and proved with synthetic oxytocin. The oxytocic activity of synthetic analogues was testes with this bioassay and compared to oxytocin. The myometrial layer preparation was demonstrated to be reliable, the vitality of the tissue is found for more than 8 hours. The sensitivity of the bioassay is found in the region of 10(-11) Mol/l oxytocin, the maximum of the stimulation of muscle strips varied from 5 X 10(-5) IU/ml to 10(-4) IU/ml oxytocin in the organ-bath. The concentration of the myometrium strips showed two different phases. Only the initial phase can be used for this bioassay. The calculation of the results was afforded planimetrically and by measuring of the concentration-maximum during the testing period. The synthetic hormone analogues [1-desamino-4-alpha-aminobutyric acid] lysine-vasotocin (2) and [4 alpha-aminobutyric acid] lysine-vasotocin had oxytocic activity and the myometrium was activated to contractions at 10(-8) Mol/1. The analogue 2 was 5-10 more active than 3. The contraction maximum for both analogues was found between 5 X 10(-6) and 5 X 10(-5) Mol/l. The induction of the concentration for both analogues varied with the factor 10(5).
已开发出一种改进的生物测定法,用于通过使用子宫肌层制剂来检测催产化合物,并已用合成催产素进行了验证。用这种生物测定法测试了合成类似物的催产活性,并与催产素进行了比较。结果表明子宫肌层制剂是可靠的,组织活力可维持8小时以上。该生物测定法的灵敏度在10^(-11)摩尔/升催产素范围内,在器官浴中,肌肉条的最大刺激范围为5×10^(-5)国际单位/毫升至10^(-4)国际单位/毫升催产素。子宫肌层条的浓度显示出两个不同阶段。只有初始阶段可用于此生物测定法。结果的计算通过平面测量法以及在测试期间测量浓度最大值来进行。合成激素类似物[1-去氨基-4-α-氨基丁酸]赖氨酸-血管升压素(2)和[4-α-氨基丁酸]赖氨酸-血管升压素具有催产活性,子宫肌层在10^(-8)摩尔/升时被激活收缩。类似物2比3的活性高5至10倍。两种类似物的最大收缩出现在5×10^(-6)至5×10^(-5)摩尔/升之间。两种类似物浓度的诱导变化因子为10^5。