Characterization of mono- and diaminopyrimidine derivatives as novel, nonpeptide gonadotropin releasing hormone (GnRH) receptor antagonists

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• 作者：Luthin ; David R. ; Hong ; Yufeng ; Tompkins ; Eileen ; Anderes ; Kenna L. ; Paderes ; Genevieve ; Kraynov ; Eugenia A. ; et. al.
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2002
• 出版时间：December 16, 2002
• 年：2002
• 卷：12
• 期：2
• 页码：3635-3639
• 全文大小：176 K

文摘

A novel series of derivatives of mono- and diaminopyrimidines 1 potently displaced binding of a radiolabeled GnRH analogue to human and rat GnRH receptors. Analogues from these series competitively antagonized GnRH-stimulated increases in extracellular acidification in vitro and suppressed GnRH-mediated increases in circulating luteinizing hormone (LH) in castrated rats and testosterone in intact rats. These compounds or their analogues may be useful in treating sex hormone-dependent disease.