Pharmacokinetics and pharmacodynamics of PF-05190457: The first oral ghrelin receptor inverse agonist to be profiled in healthy subjects

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 secretionex vivo

(2016) J Kong et al.   BRITISH JOURNAL OF PHARMACOLOGY

The Concise Guide to PHARMACOLOGY 2015/16: G protein-coupled receptors

(2015) Stephen PH Alexander et al.   BRITISH JOURNAL OF PHARMACOLOGY

KATPchannels in the nodose ganglia mediate the orexigenic actions of ghrelin

(2015) Gintautas Grabauskas et al.   JOURNAL OF PHYSIOLOGY-LONDON

Anamorelin for patients with cancer cachexia: an integrated analysis of two phase 2, randomised, placebo-controlled, double-blind trials

(2015) José M Garcia et al.   LANCET ONCOLOGY

The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands

(2015) Christopher Southan et al.   NUCLEIC ACIDS RESEARCH

Blunted suppression of acyl-ghrelin in response to fructose ingestion in obese adolescents: The role of insulin resistance

(2015) Michelle Van Name et al.   Obesity

Ghrelin in psychiatric disorders – A review

(2015) Dirk Alexander Wittekind et al.   PSYCHONEUROENDOCRINOLOGY

Effect of ghrelin on autonomic activity in healthy volunteers

(2014) Takeshi Soeki et al.   PEPTIDES

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

(2014) Samit K. Bhattacharya et al.   ACS Medicinal Chemistry Letters

Effects of an Oral Ghrelin Mimetic on Body Composition and Clinical Outcomes in Healthy Older Adults

(2013) Ralf Nass et al.   ANNALS OF INTERNAL MEDICINE

Ghrelin and motilin receptor agonists: a long and winding misconception

(2013) G. J. Sanger   NEUROGASTROENTEROLOGY AND MOTILITY

Ghrelin increases vagally mediated gastric activity by central sites of action

(2013) E. M. Swartz et al.   NEUROGASTROENTEROLOGY AND MOTILITY

Differential Effects of Laparoscopic Sleeve Gastrectomy and Laparoscopic Gastric Bypass on Appetite, Circulating Acyl-ghrelin, Peptide YY3-36 and Active GLP-1 Levels in Non-diabetic Humans

(2013) Ahmed Yousseif et al.   OBESITY SURGERY

GHS-R1a constitutive activity and its physiological relevance

(2013) Yves Mear et al.   Frontiers in Neuroscience

GLP-1 based therapies: differential effects on fasting and postprandial glucose

(2012) M.S. Fineman et al.   DIABETES OBESITY & METABOLISM

Liraglutide: short-lived effect on gastric emptying-long lasting effects on body weight

(2012) J. Jelsing et al.   DIABETES OBESITY & METABOLISM

Exogenous and endogenous ghrelin counteracts GLP-1 action to stimulate cAMP signaling and insulin secretion in islet β-cells

(2012) Boldbaatar Damdindorj et al.   FEBS LETTERS

Ghrelin as a starvation signal

(2012) Yukari Date et al.   Obesity Research & Clinical Practice

Prandial ghrelin attenuation provides evidence that des-acyl ghrelin may be an artifact of sample handling in human plasma

(2012) Matthew Blatnik et al.   Bioanalysis

Centrally administered ghrelin activates cardiac vagal nerve in anesthetized rabbits

(2011) Shuji Shimizu et al.   AUTONOMIC NEUROSCIENCE-BASIC & CLINICAL

Guide to Receptors and Channels (GRAC), 5th edition

(2011) SPH Alexander et al.   BRITISH JOURNAL OF PHARMACOLOGY

Rapid Tachyphylaxis of the Glucagon-Like Peptide 1-Induced Deceleration of Gastric Emptying in Humans

(2011) M. A. Nauck et al.   DIABETES

Impaired wake-promoting mechanisms in ghrelin receptor-deficient mice

(2011) Matthew Esposito et al.   EUROPEAN JOURNAL OF NEUROSCIENCE

The orexin system: roles in sleep/wake regulation

(2010) Takeshi Sakurai et al.   Annals of the New York Academy of Sciences

Ghrelin inhibits autonomic function in healthy controls, but has no effect on obese and vagotomized subjects

(2010) M. S. B. Huda et al.   CLINICAL ENDOCRINOLOGY

A practical guide for the stabilization of acylghrelin in human blood collections

(2010) Matthew Blatnik et al.   CLINICAL ENDOCRINOLOGY

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

(2010) J. Tong et al.   DIABETES

Effects of ghrelin on psychopathology, sleep and secretion of cortisol and growth hormone in patients with major depression

(2010) Michael Kluge et al.   JOURNAL OF PSYCHIATRIC RESEARCH

Acylated and desacyl ghrelin stimulate lipid accumulation in human visceral adipocytes

(2009) A Rodríguez et al.   INTERNATIONAL JOURNAL OF OBESITY

Effects of an Oral Growth Hormone Secretagogue in Older Adults

(2009) Heidi K. White et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

Ghrelin increases slow wave sleep and stage 2 sleep and decreases stage 1 sleep and REM sleep in elderly men but does not affect sleep in elderly women

(2009) Michael Kluge et al.   PSYCHONEUROENDOCRINOLOGY

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

(2008) E. T. Vestergaard et al.   DIABETES

Ghrelin antagonizes MPTP-induced neurotoxicity to the dopaminergic neurons in mouse substantia nigra

(2008) Hong Jiang et al.   EXPERIMENTAL NEUROLOGY

Ghrelin and Obestatin Levels in Severely Obese Women Before and After Weight Loss After Roux-en-Y Gastric Bypass Surgery

(2008) Christian L. Roth et al.   OBESITY SURGERY

Ghrelin alone or co-administered with GHRH or CRH increases non-REM sleep and decreases REM sleep in young males

(2008) Michael Kluge et al.   PSYCHONEUROENDOCRINOLOGY

Nocturnal levels of ghrelin and leptin and sleep in chronic insomnia

(2008) Sarosh J. Motivala et al.   PSYCHONEUROENDOCRINOLOGY

Ghrelin and gastric acid secretion

(2008) Koji Yakabi et al.   WORLD JOURNAL OF GASTROENTEROLOGY

Ghrelin suppresses cardiac sympathetic activity and prevents early left ventricular remodeling in rats with myocardial infarction

(2007) Takeshi Soeki et al.   AMERICAN JOURNAL OF PHYSIOLOGY-HEART AND CIRCULATORY PHYSIOLOGY

Acute Effects of Ghrelin Administration on Glucose and Lipid Metabolism

(2007) Esben Thyssen Vestergaard et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

Ghrelin deficiency does not influence feeding performance

(2007) Takahiro Sato et al.   REGULATORY PEPTIDES