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Abstract The steroid SC17599 (17α-acetoxy-6-dimethylaminomethyl-21-fluoro-3-ethoxypregna-3,5-dien-20-one) has μ-opioid actions in vivo. The ability of SC17599 to interact with opioid receptors has been studied using radioligand and 35 Sguanosine-5′- O -(3-thio)triphosphate (GTPγS) binding...
Abstract Zopiclone is a cyclopyrrolone that is used clinically as a hypnotic. Although this drug is known to interact with neuronal γ-aminobutyric acid type A receptors, its binding site(s) within the receptor oligomer has been reported to be distinct from that of the classical benzodiazepines....
Abstract RNA encoding the human 5-HT 2C receptor undergoes adenosine-to-inosine RNA editing events at five positions in the putative second intracellular loop, with a corresponding reduction in receptor/G-protein coupling. Agonist-stimulated calcium release was examined in NIH-3T3 fibroblasts...
Abstract The aryl hydrocarbon receptor (AHR) is a ligand-activated transcription factor that mediates the biological responses to environmental contaminants such as 2,3,7,8-tetrachlorodibenzo- p -dioxin. Embryonic fibroblast (EF) isolated from AHR-null mice exhibited slow cell growth compared...
Abstract We previously demonstrated differential interactions of the methoxychlor metabolite 2,2-bis( p -hydroxyphenyl)-1,1,1-trichloroethane (HPTE) with estrogen receptor α (ERα), ERβ, and the androgen receptor (AR). In this study, we characterize the ERα, ERβ, and AR activity of...
Abstract The new olivacine derivative S16020-2 (NSC-659687) is a DNA topoisomerase II inhibitor endowed with a remarkable antitumor activity against various experimental tumors. In vitro physicochemical properties of this compound, in particular its interaction with DNA and DNA topoisomerase II,...
Abstract Neuromedin U (NmU) is a 25 amino acid peptide prominently expressed in the upper gastrointestinal (GI) tract and central nervous system. It is highly conserved throughout evolution and induces smooth muscle contraction in a variety of species. Our understanding of NmU biology has been...
Abstract Sequence analysis revealed a strong homology between the ligand-binding domain (LBD) of the human mineralocorticoid receptor (hMR) and glucocorticoid receptor (hGR). Nevertheless, steroids with bulky C11-substituents bind to hGR, unlike hMR. In this report, a mutant hMR, in which the...
Abstract R , S -α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor up-modulators of the benzamide type (“ampakines”) have previously been shown to enhance excitatory synaptic transmission in vivo and in vitro and AMPA receptor currents in excised patches. The present study...
Abstract The heterologous regulation of the α2C-adrenergic receptor (α2C-AR) was investigated in the HepG2 cell line. Binding of 3 HMK912 (α2-antagonist) to membranes from cells submitted to various treatments showed that exposure to insulin, phorbol 12-myristate 13-acetate, or dexamethasone...
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