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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 ...
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 ...
Orexin receptor type 2 (Ox2R or OX 2), also known as hypocretin receptor type 2 (HcrtR2), is a protein that in humans is encoded by the HCRTR2 gene. [5] It should not be confused for the protein CD200R1 which shares the alias OX2R but is a distinct, unrelated gene located on the human chromosome 3.
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]
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]
An orexin receptor antagonist, or orexin antagonist, is a drug that inhibits the effect of orexin by acting as a receptor antagonist of one (selective orexin receptor antagonist or SORA) or both (dual orexin receptor antagonis or DORA) of the orexin receptors, OX 1 and OX 2. [1] Medical applications include treatment of sleep disorders such as ...
SB-408124 is a drug which is a non-peptide antagonist selective for the orexin receptor subtype OX 1, with around 70x selectivity for OX 1 over OX 2 receptors, and improved oral bioavailability compared to the older OX 1 antagonist SB-334867. It is used in scientific research into the function of orexinergic neurons in the body. [1] [2]
Lemborexant is a dual antagonist of the orexin OX 1 and OX 2 receptors. [18] [19] [20] It associates and dissociates from the orexin receptors more rapidly than certain other orexin receptor antagonists, such as suvorexant, and this may cause it to have a shorter duration of action. [12]