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TL;DR: In patients with type 2 diabetes, near maximal glucose-lowering efficacy of sitagliptin after single oral doses was associated with inhibition of plasma DPP-4 activity of 80% or greater, corresponding to a plasma sitgliptin concentration of 100 nm or greater and an augmentation of active GLP-1 and GIP levels of 2-fold or higher after an OGTT.

TL;DR: Rofecoxib had no significant effect on urinary excretion of 11‐dehydro TXB2, a COX‐ 1‐derived product, and these data support the contention that rofecoxIB is the only drug of the regimens tested that uniquely inhibits COx‐2 without affectingCOX‐1.

TL;DR: Nonsteroidal anti‐inflammatory drugs such as aspirin, ibuprofen, and indomethacin (INN, indometacin) inhibit both the constitutive and inducible isoforms of cyclooxygenase, leading to the hypothesis that COX‐2 inhibition primarily accounts for the therapeutic properties of NSAIDs.

TL;DR: Autoradiographic studies in rhesus monkey brain showed that [18F]MK-9470 binding is aligned with the reported distribution of CB1 receptors with high specific binding in the cerebral cortex, cerebellum, caudate/putamen, globus pallidus, substantia nigra, and hippocampus, and PET imaging studies in human research subject demonstrated behavior very similar to that seen in monkeys.

TL;DR: Mechanism-of-action studies suggest that engagement of the CB1R by taranabant leads to weight loss by reducing food intake and increasing energy expenditure and fat oxidation.