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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.
The orexin receptor (also referred to as the hypocretin receptor) is a G-protein-coupled receptor that binds the neuropeptide orexin. There are two variants, OX 1 and OX 2 , each encoded by a different gene ( HCRTR1 , HCRTR2 ).
The orexin peptides bind to the two G-protein coupled orexin receptors, OX 1 and OX 2, with orexin-A binding to both OX 1 and OX 2 with approximately equal affinity while orexin-B binds mainly to OX 2 and is 5 times less potent at OX 1. [20] [21] The orexins are strongly conserved peptides, found in all major classes of vertebrates. [22]
BOSTON and LONDON, Aug. 27, 2024 (GLOBE NEWSWIRE) -- Centessa Pharmaceuticals plc (Nasdaq: CNTA), today announced that preclinical data from a non-human primate (NHP) study of ORX142, a highly potent and selective orexin receptor 2 (OX2R) agonist being developed to address excessive daytime sleepiness (EDS) in select neurological, neurodegenerative, and psychiatric disorders, has been accepted ...
The preclinical data were featured today in a late-breaking poster presentation entitled, “ORX142, an Oral, Highly Potent and Selective Orexin Receptor 2 Agonist, Promotes Wakefulness in Non-Human Primates,” by Sarah Wurts Black PhD, Head of Biology for Centessa’s Orexin Agonist Program, at the 27 th Congress of the European Sleep ...
ORX750 is an investigational, orally administered, highly potent and selective orexin receptor 2 (OX2R) agonist designed using Nxera technology to directly target the underlying pathophysiology of orexin neuron loss in narcolepsy type 1 (NT1), with potential applicability to narcolepsy type 2 (NT2), idiopathic hypersomnia, and other sleep-wake ...
[1] [2] Firazorexton was studied by Takeda for the treatment of narcolepsy. [3] [4] [5] It is a small-molecule and orally active compound and acts as a highly selective agonist of the orexin receptor 2 (OX 2) with >700-fold selectivity over the orexin receptor 1 (OX 1). [3] [4] [6] [7] Firazorexton is related to danavorexton (TAK-925). [8]
Type 2 diabetes. Stroke. Obesity. ... Hypocretin/orexin receptor antagonists like suvorexant (Belsomra) and lemborexant (Dayvigo) The melatonin receptor agonist ramelteon (Rozerem)