Background:

WAY 207024 dihydrochloride is a potent gonadotropin releasing hormone receptor (GnRH-R) antagonist with IC50 values of 12 and 71 nM for human and rat GnRH receptors, respectively [1].
GnRH-R is a member of the G-protein coupled receptor (GPCR) family. Activation of the receptor by binding of gonadotropin-releasing hormone causes the release of leuteinizing hormone (LH) and follicle stimulating hormone (FSH) from the anterior pituitary gland and they in turn stimulate sex hormone synthesis and release into the general circulation [1].
WAY 207024 dihydrochloride displayed moderate membrane permeability properties and rat liver microsome stability [1].
In castrated rats, WAY 207024 dihydrochloride was absorbed well following oral administration with a bioavailability of 74%. Also, WAY 207024 dihydrochloride (30 mg/kg, oral gavage) reduced serum LH levels starting at 1 h post dosing and LH levels had returned to the vehicle treated group levels after 24h [1].
参考文献:
[1]. Pelletier JC, Chengalvala MV, Cottom JE, et al. Discovery of 6-({4-[2-(4-tert-butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl}methyl)quinoxaline (WAY-207024): an orally active antagonist of the gonadotropin releasing hormone receptor (GnRH-R). J Med Chem, 2009, 52(7): 2148-2152.