Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate

Escape from Flatland: Increasing Saturation as an Approach to Improving Clinical Success

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The influence of drug-like concepts on decision-making in medicinal chemistry

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Physiochemical drug properties associated with in vivo toxicological outcomes

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Extent and direction of ghrelin transport across the blood-brain barrier is determined by its unique primary structure

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New Perspectives into the Molecular Pathogenesis and Treatment of Type 2 Diabetes

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Probing the links between in vitro potency, ADMET and physicochemical parameters

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In Vitro P-glycoprotein Assays to Predict the in Vivo Interactions of P-glycoprotein with Drugs in the Central Nervous System

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The kinetics of competitive radioligand binding predicted by the law of mass action.

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Ghrelin Suppresses Glucose-Stimulated Insulin Secretion and Deteriorates Glucose Tolerance in Healthy Humans

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Dose-Dependent Inhibition by Ghrelin of Insulin Secretion in the Mouse

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Development of a new permeability assay using low‐efflux MDCKII cells

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Administration of acylated ghrelin reduces insulin sensitivity, whereas the combination of acylated plus unacylated ghrelin strongly improves insulin sensitivity.

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Structural Modifications that Alter the P-Glycoprotein Efflux Properties of Compounds

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Ghrelin Uses Gαi2 and Activates Voltage-Dependent K+ Channels to Attenuate Glucose-Induced Ca2+ Signaling and Insulin Release in Islet β-Cells

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Effects of an Oral Growth Hormone Secretagogue in Older Adults

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Ghrelin Infusion in Humans Induces Acute Insulin Resistance and Lipolysis Independent of Growth Hormone Signaling

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Ghrelin is a physiological regulator of insulin release in pancreatic islets and glucose homeostasis

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Role of Physicochemical Properties and Ligand Lipophilicity Efficiency in Addressing Drug Safety Risks

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Dose Selection Based on Physiologically Based Pharmacokinetic (PBPK) Approaches

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Constant intravenous ghrelin infusion in healthy young men: clinical pharmacokinetics and metabolic effects.

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The thermodynamic basis for the use of lipophilic efficiency (LipE) in enthalpic optimizations

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Acute Effects of Ghrelin Administration on Glucose and Lipid Metabolism

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Acute Effects of Ghrelin on Insulin Secretion and Glucose Disposal Rate in Gastrectomized Patients

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Metabolic and endocrine effects of physiological increments in plasma ghrelin concentrations

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Ghrelin Receptor

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GSK1614343, a Novel Ghrelin Receptor Antagonist, Produces an Unexpected Increase of Food Intake and Body Weight in Rodents and Dogs

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Final Answer: Ghrelin Can Suppress Insulin Secretion in Humans, but Is It Clinically Relevant?

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Identification of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor

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Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor

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Pharmacologic Inhibition of Ghrelin Receptor Signaling Is Insulin Sparing and Promotes Insulin Sensitivity

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Identification of piperazine-bisamide GHSR antagonists for the treatment of obesity

Yu, M., Lizarzaburu, M. E., Beckmann, H., Connors, R., Dai, K., Haller, K., Li, C., Liang, L., Lindström, M., Ma, J., et al. (2010) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2010.01.043 · Cited by 26 · see citing works

Pharmacological characterization of the ghrelin receptor antagonist, GSK1614343 in rat RC-4B/C cells natively expressing GHS type 1a receptors

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Identification of pyrazolo-pyrimidinones as GHS-R1a antagonists and inverse agonists for the treatment of obesity

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Synthesis and pharmacological evaluation of indolinone derivatives as novel ghrelin receptor antagonists

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Discovery of a new class of ghrelin receptor antagonists

Mihalic, J. T., Kim, Y., Lizarzaburu, M. E., et al. (2012) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2012.01.014 · Cited by 23 · see citing works

Discovery and optimization of novel 4-[(aminocarbonyl)amino]-N-[4-(2-aminoethyl)phenyl]benzenesulfonamide ghrelin receptor antagonists

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Ghrelin Receptor Modulators and Their Therapeutic Potential

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METABOLISM, PHARMACOKINETICS, TISSUE DISTRIBUTION, AND EXCRETION OF [14C]CP-424391 IN RATS

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Azabicyclo[3.1.0]hexane‐1‐carbohydrazides as Potent and Selective GHSR1a Ligands Presenting a Specific in vivo Behavior

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Current and emerging therapies for type 2 diabetes.

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The novel ghrelin receptor inverse agonist PF-5190457 administered with alcohol: Preclinical safety experiments and a phase 1b human laboratory study

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Molecular mechanism of agonism and inverse agonism in ghrelin receptor

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A Narrative Review of Current and Emerging Trends in the Treatment of Alcohol Use Disorder

Celik, M., Gold, M. S., & Fuehrlein, B. (2024) · Brain Sciences · doi:10.3390/brainsci14030294 · Cited by 25 · see citing works

1H NMR structural analysis of human ghrelin and its six truncated analogs

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Endocrinological activities of ghrelin: new insights

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A Novel Growth Hormone Secretagogue-1a Receptor Antagonist That Blocks Ghrelin-Induced Growth Hormone Secretion but Induces Increased Body Weight Gain

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The role of ghrelin in GH secretion and GH disorders

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[Ghrelin--peptide hormone that increases appetite. It opens new possibilities for the research on energy metabolism].

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