Schillinger E, Prior G, Speckenbach A, Wellershoff S
Prostaglandins. 1979 Aug;18(2):292-302. doi: 10.1016/0090-6980(79)90116-3.
Sulprostone is a tissue-specific PGE2-derivative with high abortifacient activity in various species including man. The dissociation constant KD of the receptor binding of this compound was compared with PGE2 and PGF2 alpha in various tissue preparations of different species. A structure-binding relationship was developed from competition curves after a logit/log transformation. It is demonstrated that the relative affinities of Sulprostone, PGE2 and PGF2 alpha remain essentially constant in all the tissues investigated. It is concluded that the tissue-specificity of Sulprostone cannot be ascribed to structural differences of the receptor molecule.
舒前列素是一种组织特异性的PGE2衍生物,在包括人类在内的多种物种中具有高堕胎活性。在不同物种的各种组织制剂中,将该化合物的受体结合解离常数KD与PGE2和PGF2α进行了比较。通过logit/log转换后的竞争曲线建立了结构-结合关系。结果表明,舒前列素、PGE2和PGF2α在所有研究的组织中的相对亲和力基本保持恒定。结论是,舒前列素的组织特异性不能归因于受体分子的结构差异。