Pharmacological characterization of the first in class clinical candidate PF-05190457: a selective ghrelin receptor competitive antagonist with inverse agonism that increases vagal afferent firing and glucose-dependent insulin secretion ex vivo.

@article{Kong2016PharmacologicalCO,
  title={Pharmacological characterization of the first in class clinical candidate PF-05190457: a selective ghrelin receptor competitive antagonist with inverse agonism that increases vagal afferent firing and glucose-dependent insulin secretion ex vivo.},
  author={Jimmy X Kong and J Chuddy and Ingrid A. Stock and Paula M. Loria and Stephen V. Straub and Chandra Vage and Kimberly O'Keefe Groton Cameron and Samit K. Bhattacharya and Kimberly Lapham and Kim F McClure and Yan-ling Zhang and Vivienne Margaret Jackson},
  journal={British journal of pharmacology},
  year={2016},
  volume={173 9},
  pages={
          1452-64
        }
}
BACKGROUND AND PURPOSE Ghrelin increases growth hormone secretion, gastric acid secretion, gastric motility and hunger but decreases glucose-dependent insulin secretion and insulin sensitivity in humans. Antagonizing the ghrelin receptor has potential as a therapeutic approach in the treatment of obesity and type 2 diabetes. Therefore, the aim was to pharmacologically characterize the novel small-molecule antagonist PF-05190457 and assess translational pharmacology ex vivo. EXPERIMENTAL… CONTINUE READING
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