Momma Kazuo, Toyoshima Katsuaki, Takeuchi Daiji, Imamura Shinichiro, Nakanishi Toshio
Section of Pediatric Cardiology, Tokyo Women's Medical University, Tokyo 162-8666, Japan.
Pediatr Res. 2005 Nov;58(5):971-5. doi: 10.1203/01.pdr.0000182182.49476.24.
Indomethacin is used to constrict the patent ductus arteriosus in premature infants. To clarify possible prostanoid receptor antagonists that can constrict the ductus, we studied in vivo constriction of the fetal and neonatal ductus arteriosus by AE3-208, a prostanoid EP4-receptor antagonist, in rats. Following quick cesarean section of near-term pregnant rats (21 d), neonates were incubated in room air at 33 degrees C. The inner diameter of the ductus was measured with a microscope and a micrometer following rapid whole-body freezing of the fetus and neonate, and sectioning of the thorax in the frontal plane on a freezing microtome. In the control, the ductus arteriosus constricted quickly after birth, and the inner diameter was 0.80 mm in the fetus and 0.06 mm at 90 min after birth. AE3-208, administered orogastrically to the dam, constricted the fetal ductus dose dependently. Maximal ductal constriction was observed 4 h after administration, and the ductal diameters were 0.06 mm and 0.26 mm after administration of 10 mg/kg and 10 ng/kg of AE3-208, respectively. In neonatal rats, AE3-208 injected subcutaneously at 30 min after birth, inhibited dilatation of the ductus by PGE1 dose dependently. PGE1 (10 microg/kg) was injected subcutaneously to the 1-h-old neonatal rat, and the ductal diameters were 0.53 mm and 0.19 mm without and with pretreatment of AE3-208 (10 microg/kg), respectively. These results indicate the major role of EP4 in the fetal and neonatal ductus and show that an EP4 antagonist can be used to constrict the patent ductus of premature infants.
吲哚美辛用于收缩早产儿的动脉导管。为了明确可能收缩动脉导管的前列腺素受体拮抗剂,我们在大鼠中研究了前列腺素EP4受体拮抗剂AE3 - 208对胎儿和新生动脉导管的体内收缩作用。对接近足月(21天)的妊娠大鼠进行快速剖宫产术后,将新生大鼠在33℃的室温空气中孵育。在对胎儿和新生大鼠进行快速全身冷冻,并在冷冻切片机上沿额平面切开胸部后,用显微镜和测微计测量动脉导管的内径。在对照组中,出生后动脉导管迅速收缩,胎儿期内径为0.80毫米,出生后90分钟时为0.06毫米。经口胃管给母鼠灌胃AE3 - 208可使胎儿动脉导管剂量依赖性收缩。给药后4小时观察到最大导管收缩,分别给予10毫克/千克和10纳克/千克的AE3 - 208后,导管直径分别为0.06毫米和0.26毫米。在新生大鼠中,出生后30分钟皮下注射AE3 - 208可剂量依赖性抑制PGE1引起的动脉导管扩张。对1小时龄的新生大鼠皮下注射PGE1(10微克/千克),未用AE3 - 208(10微克/千克)预处理和预处理后的动脉导管直径分别为0.53毫米和0.19毫米。这些结果表明EP4在胎儿和新生动脉导管中起主要作用,并表明EP4拮抗剂可用于收缩早产儿的动脉导管未闭。