Lebl M, Slaninová J, Johnson R L
Institute of Organic Chemistry and Biochemistry, Czechoslovak Academy of Sciences, Prague.
Int J Pept Protein Res. 1989 Jan;33(1):16-21. doi: 10.1111/j.1399-3011.1989.tb00678.x.
Analogs of deamino-oxytocin wherein the Leu-Gly peptide bond has been replaced by a tetrazole moiety or by a double bond of trans configuration were synthesized and their biological activities evaluated. Trans double bond was found to be the most appropriate substitution for the amide bond (uterotonic activity 24% of the deamino-oxytocin). In the case of all three analogs low but prolonged galactogogic activity was found and the ratio of uterotonic in vitro and in vivo activity was surprisingly high (ranging from 4.5 to 20).
合成了亮氨酸-甘氨酸肽键被四唑部分或反式构型的双键取代的脱氨基催产素类似物，并对其生物活性进行了评估。发现反式双键是酰胺键最合适的取代基（子宫收缩活性为脱氨基催产素的24%）。在所有三种类似物的情况下，均发现了较低但持久的催乳活性，且体外和体内子宫收缩活性的比值出奇地高（范围为4.5至20）。
