Orexin receptors: pharmacology and therapeutic opportunities

TE Scammell, CJ Winrow - Annual review of pharmacology and …, 2011 - annualreviews.org
Orexin-A and-B (also known as hypocretin-1 and-2) are neuropeptides produced in the
lateral hypothalamus that promote many aspects of arousal through the OX1 and OX2 …

The lateral hypothalamus as integrator of metabolic and environmental needs: from electrical self-stimulation to opto-genetics

HR Berthoud, H Münzberg - Physiology & behavior, 2011 - Elsevier
As one of the evolutionary oldest parts of the brain, the diencephalon evolved to harmonize
changing environmental conditions with the internal state for survival of the individual and …

[PDF][PDF] Orexin is required for brown adipose tissue development, differentiation, and function

D Sellayah, P Bharaj, D Sikder - Cell metabolism, 2011 - cell.com
Orexin (OX) neuropeptides stimulate feeding and arousal. Deficiency of orexin is implicated
in narcolepsy, a disease associated with obesity, paradoxically in the face of reduced food …

Connectomics of orexin-producing neurons: interface of systems of emotion, energy homeostasis and arousal

T Sakurai, M Mieda - Trends in pharmacological sciences, 2011 - cell.com
Avoiding danger and finding food, which are life-sustaining activities that are regulated by
emotion, reward and energy balance, require proper wakefulness. The orexin system …

[HTML][HTML] Activation of central orexin/hypocretin neurons by dietary amino acids

MM Karnani, J Apergis-Schoute, A Adamantidis… - Neuron, 2011 - cell.com
Hypothalamic orexin/hypocretin (orx/hcrt) neurons regulate energy balance, wakefulness,
and reward; their loss produces narcolepsy and weight gain. Glucose can lower the activity …

Neurobiology of overeating and obesity: the role of melanocortins and beyond

R Pandit, JW de Jong, LJMJ Vanderschuren… - European journal of …, 2011 - Elsevier
The alarming increase in the incidence of obesity and obesity-associated disorders makes
the etiology of obesity a widely studied topic today. As opposed to 'homeostatic feeding' …

Evidence for the role of hindbrain orexin-1 receptors in the control of meal size

EM Parise, N Lilly, K Kay, AM Dossat… - American Journal …, 2011 - journals.physiology.org
Hypothalamic orexin neurons project to the hindbrain, and 4th-ventricle
intracerebroventricular (4th-icv) injection of orexin-A treatment increases food intake. We …

Dimorphic effects of leptin on the circadian and hypocretinergic systems of mice

J Mendoza, C Lopez‐Lopez, FG Revel… - Journal of …, 2011 - Wiley Online Library
The hormone leptin controls food intake and body weight through its receptor in the
hypothalamus, and may modulate physiological functions such as reproduction, sleep or …

A role for ΔFosB in calorie restriction-induced metabolic changes

V Vialou, H Cui, M Perello, M Mahgoub, GY Hana… - Biological …, 2011 - Elsevier
BACKGROUND: Calorie restriction (CR) induces long-term changes in motivation to eat
highly palatable food and, in body weight regulation, through an unknown mechanism …

Discovery of spiropiperidine-based potent and selective Orexin-2 receptor antagonists

T Fujimoto, Y Tomata, J Kunitomo, M Hirozane… - Bioorganic & medicinal …, 2011 - Elsevier
To generate novel human Orexin-2 Receptor (OX2R) antagonists, a spiropiperidine based
scaffold was designed and a SAR study was carried out. Compound 4f possessed the …