Regulation of ingestive behaviors in the rat by GSK1521498, a novel μ-opioid receptor-selective inverse agonist

DM Ignar, AS Goetz, KN Noble, LH Carballo… - … of Pharmacology and …, 2011 - ASPET
μ-Opioid receptor (MOR) agonism induces palatable food consumption principally through
modulation of the rewarding properties of food. N-{[3, 5-difluoro-3′-(1 H-1, 2, 4-triazol-3-yl) …

Opioid Receptor Modulation of Hedonic Taste Preference and Food Intake: A Single‐Dose Safety, Pharmacokinetic, and Pharmacodynamic Investigation With …

PJ Nathan, BV O'Neill, MA Bush, A Koch… - The Journal of …, 2012 - Wiley Online Library
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 …

The μ-opioid receptor subtype is required for the anorectic effect of an opioid receptor antagonist

J Zhang, A Frassetto, RRC Huang, JZ Lao… - European journal of …, 2006 - Elsevier
A diaryl ether derivative,(6-(4-{[(3-methylbutyl) amino] methyl} phenoxy) nicotinamide, was
prepared and investigated for its biochemical properties at cloned opioid receptors and its …

[HTML][HTML] Inhibition of opioid transmission at the μ-opioid receptor prevents both food seeking and binge-like eating

C Giuliano, TW Robbins, PJ Nathan… - …, 2012 - nature.com
Endogenous opioids, and in particular μ-opioid receptors, have been linked to hedonic and
rewarding mechanisms engaged during palatable food intake. The aim of this study was to …

Multiple‐Dose Safety, Pharmacokinetics, and Pharmacodynamics of the μ‐Opioid Receptor Inverse Agonist GSK1521498

PJ Nathan, MA Bush, WX Tao, A Koch… - The Journal of …, 2012 - Wiley Online Library
The endogenous opioid system and μ‐opioid receptors in particular have been
demonstrated to play a fundamental role in hedonic and motivational behaviors reinforced …

Activation of mesolimbic dopamine neurons during novel and daily limited access to palatable food is blocked by the opioid antagonist LY255582

AE Sahr, DK Sindelar… - American Journal …, 2008 - journals.physiology.org
An analog of the trans-3, 4-dimethyl-4-(3-hydroxyphenyl) piperidine series (LY255582)
exhibits high in vitro binding affinity and antagonist potency for the μ-, δ-, and κ-opioid …

[HTML][HTML] Effects of the mu-opioid receptor antagonist GSK1521498 on hedonic and consummatory eating behaviour: a proof of mechanism study in binge-eating obese …

H Ziauddeen, SR Chamberlain, PJ Nathan… - Molecular …, 2013 - nature.com
The opioid system is implicated in the hedonic and motivational processing of food, and in
binge eating, a behaviour strongly linked to obesity. The aim of this study was to evaluate …

Localization of opioid receptor antagonist [3H]-LY255582 binding sites in mouse brain: comparison with the distribution of mu, delta and kappa binding sites

SL Gackenheimer, TM Suter, JE Pintar, SJ Quimby… - Neuropeptides, 2005 - Elsevier
Agonist stimulation of opioid receptors increases feeding in rodents, while opioid
antagonists inhibit food intake. The pan-opioid antagonist, LY255582, produces a sustained …

Reduction by central ß-funaltrexamine of food intake in rats under freely-feeding, deprivation and glucoprivic conditions

D Arjune, KM Standifer, GW Pasternak, RJ Bodnar - Brain research, 1990 - Elsevier
The present study evaluated the central effects of ß-funaltrexamine (B-FNA), a non-
equilibrium antagonist of μ-opioid receptors and a reversible agonist of κ-opioid receptors …

Diet-induced obesity increases μ opioid receptor binding in specific regions of the rat brain

SL Smith, JA Harrold, G Williams - Brain research, 2002 - Elsevier
Mu (μ) opioid agonists preferentially increase the intake of highly palatable food. Here we
investigated changes in μ opioid binding in feeding-and reward-related brain regions in rats …