Spilman C H, Bergstrom K K, Forbes A D
Prostaglandins. 1977 Apr;13(4):795-805. doi: 10.1016/0090-6980(77)90253-2.
The effects of 19-hydroxyprostaglandins (19-OH-PGs) were tested in vivo on the rabbit oviduct and uterus and on the rhesus monkey (Macaca mulatta) uterus. The 19-OH-PGEs suppressed spontaneous oviductal and uterine activity in the rabbit. The qualitative effect on the rabbit oviduct of 19-OH-PGEs was similar to that of PGE2. However, the typical response of the rabbit uterus to PGE2 was an increase in muscle activity. With regard to the rabbit oviduct, 19(R)-OH-PGE2 was as potent as PGE2, but 19(S)-OH-PGE2 was approximately 1/2 as potent as PGE2. Based on the dose of 19-OH-PGEs usually required to cause a minimal suppression and the dose of PGE2 required to cause a minimal stimulation of rabbit uterine activity, 19(R)-OH-PGE2 was twice as potent as PGE2 while 19(S)-OH-PGE2 was 1/2 as potent as PGE2. Stimulatory effects on the rabbit oviduct and uterus were observed following administration of 19-OH-PGFs and PGF2alpha. The potency on the rabbit oviduct of 19(S)-OH-PGF2alpha was about 1/5 to 1/10 that of PGF2alpha; the potency of 19(R)-OH-PGF2alpha was about 1/10 to 1/20 that of PGF2alpha. Both 19-OH-PGFs were approximately 1/5 to 1/10 as potent as PGF2alpha on the rabbit uterus. At the doses tested 19-OH-PGFs were inactive on the monkey uterus. Thus, these compounds are at least 1/5 as active as PGF2alpha. In contrast, 19(R)-OH-PGE2 had approximately the same potency as PGE2 in stimulating monkey uterine activity; but 19(S)-OH-PGE2 was approximately 1/3 as potent as PGE2.
对19-羟基前列腺素(19-OH-PGs)在兔输卵管和子宫以及恒河猴(猕猴)子宫上进行了体内试验。19-OH-PGEs抑制了兔输卵管和子宫的自发活动。19-OH-PGEs对兔输卵管的定性作用与PGE2相似。然而,兔子宫对PGE2的典型反应是肌肉活动增加。就兔输卵管而言,19(R)-OH-PGE2与PGE2的效力相当,但19(S)-OH-PGE2的效力约为PGE2的1/2。根据通常引起最小抑制所需的19-OH-PGEs剂量以及引起兔子宫活动最小刺激所需的PGE2剂量,19(R)-OH-PGE2的效力是PGE2的两倍,而19(S)-OH-PGE2的效力是PGE2的1/2。给予19-OH-PGFs和PGF2α后,观察到对兔输卵管和子宫有刺激作用。19(S)-OH-PGF2α对兔输卵管的效力约为PGF2α的1/5至1/10;19(R)-OH-PGF2α的效力约为PGF2α的1/10至1/20。两种19-OH-PGFs对兔子宫的效力约为PGF2α的1/5至1/10。在所测试的剂量下,19-OH-PGFs对猴子宫无活性。因此,这些化合物的活性至少是PGF2α的1/5。相比之下,19(R)-OH-PGE2在刺激猴子宫活动方面的效力与PGE2大致相同;但19(S)-OH-PGE2的效力约为PGE2的1/3。