Chimura T
Nihon Sanka Fujinka Gakkai Zasshi. 1985 Nov;37(11):2309-14.
The stimulating action of uterine contractions of cyclooxygenase products and 5-lipoxygenase products in an arachidonic acid cascade and the role of the inhibitors of both pathways have recently been the subject of much attention. We studied the influences of these drugs using the myometriums of pregnant rats. The inhibitory effects on pregnant uterine contractions (in vitro) were in the order beta 2-stimulants (procaterol, pirbuterol) greater than AA-861 greater than flurbiprofen greater than indomethacin greater than BW-755C. The inhibitory potency was reinforced by concurrent administration of AA-861 and flurbiprofen. Stimulation of the uterine contractions by Leukotriene (LT) was LTD4 greater than LTC4, and also the inhibition of the LT strain was AA-861 greater than flurbiprofen. The stimulation of PGE1 analog (ONO-802) revealed the reaction of LT + AA-861 (-) and LT + flurbiprofen (+/-). As to the changes in c-AMP and c-GMP in the bath medium before and after the administration of each drug, the change in the administration of the LT strain was slight, and an increase in c-AMP and a decrease of c-GMP were noted following the administration of contraction inhibitory substances. Its variation ratios were noted, in the order: increase in c-AMP of AA-861 + flurbiprofen greater than pirbuterol AA-861 greater than BW-755C, and decrease in c-GMP of pirbuterol greater than AA-861 + flurbiprofen greater than A-861 greater than BW-755C.
环氧化酶产物和5-脂氧合酶产物在花生四烯酸级联反应中对子宫收缩的刺激作用以及这两条途径抑制剂的作用,近来备受关注。我们使用妊娠大鼠的子宫肌层研究了这些药物的影响。对妊娠子宫收缩(体外)的抑制作用顺序为:β2激动剂(丙卡特罗、吡布特罗)大于AA-861大于氟比洛芬大于吲哚美辛大于BW-755C。同时给予AA-861和氟比洛芬可增强抑制效力。白三烯(LT)对子宫收缩的刺激作用为LTD4大于LTC4,对LT收缩的抑制作用也是AA-861大于氟比洛芬。PGE1类似物(ONO-802)的刺激显示出LT + AA-861(-)和LT + 氟比洛芬(+/-)的反应。关于每种药物给药前后浴液中c-AMP和c-GMP的变化,LT收缩给药后的变化轻微,给予收缩抑制物质后c-AMP增加而c-GMP减少。其变化率顺序为:AA-861 + 氟比洛芬的c-AMP增加大于吡布特罗、AA-861大于BW-755C,吡布特罗的c-GMP减少大于AA-861 + 氟比洛芬大于A-861大于BW-755C。