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Opioid Receptor Modulation of Hedonic Taste Preference and Food Intake: A Single-Dose Safety, Pharmacokinetic, and Pharmacodynamic Investigation With GSK1521498, a Novel μ-Opioid Receptor Inverse Agonist
- Source :
- The Journal of Clinical Pharmacology. 52:464-474
- Publication Year :
- 2012
- Publisher :
- Wiley, 2012.
-
Abstract
- 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.
- Subjects :
- Adult
Male
Taste
Drug Inverse Agonism
medicine.drug_class
Receptors, Opioid, mu
Administration, Oral
Pharmacology
Eating
Food Preferences
Double-Blind Method
Opioid receptor
medicine
Humans
Inverse agonist
Single-Blind Method
Pharmacology (medical)
Overeating
Receptor
Endogenous opioid
Cross-Over Studies
Dose-Response Relationship, Drug
Chemistry
Area under the curve
Triazoles
Opioid
Area Under Curve
Indans
medicine.drug
Subjects
Details
- ISSN :
- 00912700
- Volume :
- 52
- Database :
- OpenAIRE
- Journal :
- The Journal of Clinical Pharmacology
- Accession number :
- edsair.doi.dedup.....0dbf10350851a4d07f26c65be02acda2