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A β3-AR antagonist in animal models; less selective for human β-AR subtypes (Kis = 16.4, 61.9, and 122 nM for β1-, β2-, and β3-AR, respectively); blocks MDMA-induced hyperthermia at low and high concentrations with some α1-AR antagonist properties
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A selective ligand of RORγ (IC50 = 1 μM); does not bind RORα, LXR, or FXR; acts as an inverse agonist of RORγ, inhibiting endogenous IL-17A gene expression and suppressing differentiation of TH17 cells; stimulates T regulatory development
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A STING agonist (EC50 = 2.1 µM in a reporter assay); selective for STING over a panel of 468 kinases; increases plasma IFN-β and IL-6 levels in mice at 30 mg/kg; increases the intratumor frequency of CD69+CD8+ T cells, reduces tumor growth, and increases survival in a B16/F10 murine melanoma model
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A derivative of GABA that acts as an antagonist of GABAA receptors (Ki = 74-150 nM); elicits seizures when administered intravenously in mice; effective against GABAA receptor isoforms from mice, rats, and humans
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