Chen J, Woodward D F, Yuan Y D, Marshall K, Senior J
Department of Biological Sciences, Allergan, Inc., Irvine, CA 92612, USA.
Prostaglandins Other Lipid Mediat. 1998 Apr;55(5-6):387-94. doi: 10.1016/s0090-6980(98)00034-3.
Natural and synthetic prostanoid agonists were used to study the prostanoid receptors involved in contraction of the mature, isolated uterus of virgin rabbits. The prostanoids elicited contractile responses with a rank order of potency of PGF2 alpha, fluprostenol > PGD2 > U-46,619 > PGE2 > carbaprostacyclin with mean EC50 (nM) values of 4, 6, 34, 550, 1318 and > 10,000, respectively. Carbachol, a muscarinic agonist given after the prostanoids to elicit a reference contraction, had a mean EC50 value of 1.1 microM. The results show that the mature rabbit uterus is most sensitive to prostaglandin FP agonists and, thus, can be defined pharmacologically as an FP receptor preparation. These findings may facilitative investigations into the possibility of different prostanoid receptor populations. In the absence of useful competitive FP receptor antagonists, agonist potency data is particularly useful in systems where cross-species comparisons and tissue-related factors are not involved. The potent activities of the FP agonists, PGF2 alpha and fluprostenol, in the isolated jugular vein and uterus of the rabbit suggest that these tissues may be useful for intra-species comparisons.
使用天然和合成的前列腺素激动剂来研究参与未孕兔成熟离体子宫收缩的前列腺素受体。前列腺素引发收缩反应的效力顺序为：PGF2α、氟前列醇＞PGD2＞U - 46,619＞PGE2＞卡前列环素，其平均EC50（nM）值分别为4、6、34、550、1318和＞10,000。卡巴胆碱是一种毒蕈碱激动剂，在前列腺素给药后用于引发参照收缩，其平均EC50值为1.1微摩尔。结果表明，未孕兔子宫对前列腺素FP激动剂最为敏感，因此在药理学上可定义为一种FP受体制剂。这些发现可能有助于研究不同前列腺素受体群体的可能性。在缺乏有效的竞争性FP受体拮抗剂的情况下，激动剂效力数据在不涉及跨物种比较和组织相关因素的系统中特别有用。FP激动剂PGF2α和氟前列醇在兔离体颈静脉和子宫中的强效活性表明，这些组织可能有助于种内比较。
