Charles Willis Lugar

TL;DR: SERBA-1 in vivo demonstrates involution of the ventral prostate in CD-1 mice (ERβ effect), while having no effect on gonadal hormone levels (ERα effect) at 10× the efficacious dose, consistent with in vitro properties of this molecule.

TL;DR: Tissue distribution studies with radiolabelled metabolite indicate that conversion to raloxifene occurs readily in a variety of tissues including the liver, lung, spleen, kidney, bone and uterus, indicating that the origin of ral oxifene's pharmacology does not result from tissue-selective deconjugation of metabolite to parent.

TL;DR: In this paper, the authors present novel compounds which are useful in the modulation of endogenous growth hormone levels in a mammal, as well as novel intermediates for use in the synthesis of said compounds, and novel processes employed in these syntheses.

TL;DR: The findings revealed that the optimal stereochemical array was the same for both NMDA (32 and 61) and AMPA (9) antagonists identified in this series and that the tetrahydroisoquinoline (25) and the C-1 carboxy (30) analogs of 9 are inactive.

TL;DR: Novel 3-aryl indoles are reported as potent and efficacious progesterone receptor (PR) antagonists with potential for the treatment of uterine fibroids and demonstrated excellent selectivity over other steroid nuclear hormone receptors such as the mineralocorticoid receptors.