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Bioorg Med Chem Lett. 2002 Dec 16;12(24):3635-9.

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

Author information

1
Pfizer Global Research and Development-La Jolla/Agouron Pharmaceuticals, Inc., 10724 Science Center Drive, San Diego, CA 92121, USA. david.luthin@pfizer.com

Abstract

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.

PMID:
12443792
DOI:
10.1016/s0960-894x(02)00756-4
[Indexed for MEDLINE]

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