New effective gonadotropin releasing hormone antagonists with minimal potency for histamine release in vitro

…, J Porter, CL Rivier, M Perrin, A Corrigan…

文献索引：Rivier, Jean E.; Porter, John; Rivier, Catherine L.; Perrin, Marylin; Corrigan, Anne; et al. Journal of Medicinal Chemistry, 1986 , vol. 29, # 10 p. 1846 - 1851

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被引用次数: 146

摘要

In order to minimize the adverse effect of histamine release in the rat of some gonadotropin releasing hormone (GnRH) antagonists, such as [A~-D~ N~~', D~ FP~~~, DT~~~, DA~~~]- G~ RH, new structures with modifications at positions 1, 2, 3, 5, 6, 7, and 10 were synthesized and tested in several biological systems. In vitro: the affinity for the pituitary GnRH receptor was measured as was the ability of the analogues to inhibit GnRH- ...