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Orexin (/ ɒ ˈ r ɛ k s ɪ n /), also known as hypocretin, is a neuropeptide that regulates arousal, wakefulness, and appetite. [5] It exists in the forms of orexin-A and orexin-B.The most common form of narcolepsy, type 1, in which the individual experiences brief losses of muscle tone ("drop attacks" or cataplexy), is caused by a lack of orexin in the brain due to destruction of the cells ...
Once made, the orexin peptides can bind to the orexin receptor; which is a G protein-coupled receptor. This receptor senses molecules outside the cell and activates inside signal transduction pathways to elicit cellular responses. Research shows that an absence of orexin-A appears to cause narcolepsy. Deficit amounts of orexin-A will make ...
The lateral hypothalamus (LH), also called the lateral hypothalamic area (LHA), [1] contains the primary orexinergic nucleus within the hypothalamus that widely projects throughout the nervous system; [2] this system of neurons mediates an array of cognitive and physical processes, such as promoting feeding behavior and arousal, reducing pain perception, and regulating body temperature ...
The orexin 1 receptor (OX 1), is a G-protein coupled receptor that is heavily expressed in projections from the lateral hypothalamus and is involved in the regulation of feeding behaviour. OX 1 selectively binds the orexin-A neuropeptide. It shares 64% identity with OX 2. [5]
Orexin deficiency has been identified as responsible for narcolepsy. [ 10 ] Research suggests that orexin and histamine neurons play distinct, but complementary roles in controlling wakefulness with orexin being more involved with wakeful behavior and histamine with cognition and activation of cortical EEG .
SB-334867 is an orexin antagonist.It was the first non-peptide antagonist developed that is selective for the orexin receptor subtype OX 1, with around 50x selectivity for OX 1 over OX 2 receptors. [1]
Both orexin receptors exhibit a similar pharmacology – the 2 orexin peptides, orexin-A and orexin-B, bind to both receptors and, in each case, agonist binding results in an increase in intracellular calcium levels. However, orexin-B shows a 5- to 10-fold selectivity for orexin receptor type 2, whilst orexin-A is equipotent at both receptors ...
These results highlighted a highly specific anatomical and molecular substrate for ethanol intake; orexin receptor 2 signalling in the anterior PVT. [11] Since the PVT appeared to play a role in alcohol consumption behavior, Barson was interested in exploring the role of this area in emotional processing. [11]