Document Detail


Opioid Receptor Modulation of Hedonic Taste Preference and Food Intake: A Single-Dose Safety, Pharmacokinetic, and Pharmacodynamic Investigation With GSK1521498, a Novel {micro}-Opioid Receptor Inverse Agonist.
MedLine Citation:
PMID:  21610207     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
Endogenous opioids and μ-opioid receptors have been linked to hedonic and rewarding aspects of palatable food intake. The authors examined the safety, pharmacokinetic, and pharmacodynamic profile of GSK1521498, a μ-opioid receptor inverse agonist that is being investigated primarily for the treatment of overeating behavior in obesity. In healthy participants, GSK1521498 oral solution and capsule formulations were well tolerated up to a dose of 100 mg. After single doses (10-150 mg), the maximum concentration (C(max)) and area under the curve (AUC) in plasma increased in a dose-proportional manner. GSK1521498 selectively reduced sensory hedonic ratings of high-sugar and high-fat dairy products and caloric intake of high-fat/high-sucrose snack foods. These findings provide encouraging data in support of the development of GSK1521498 for the treatment of disorders of maladaptive ingestive behavior or compulsive consumption.
Authors:
Pradeep J Nathan; Barry V O'Neill; Mark A Bush; Annelize Koch; Wenli X Tao; Kay Maltby; Antonella Napolitano; Allison C Brooke; Andrew L Skeggs; Craig S Herman; Andrew L Larkin; Diane M Ignar; Duncan B Richards; Pauline M Williams; Edward T Bullmore
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-5-24
Journal Detail:
Title:  Journal of clinical pharmacology     Volume:  -     ISSN:  1552-4604     ISO Abbreviation:  -     Publication Date:  2011 May 
Date Detail:
Created Date:  2011-5-25     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0366372     Medline TA:  J Clin Pharmacol     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Affiliation:
GlaxoSmithKline Pharmaceuticals.
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