Biology:Hypocretin (orexin) receptor 1

Short description: Protein-coding gene in the species Homo sapiens

Generic protein structure example

Orexin receptor type 1 (Ox1R or OX₁), also known as hypocretin receptor type 1 (HcrtR1), is a protein that in humans is encoded by the HCRTR1 gene.

Function

The orexin 1 receptor (OX₁), 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. OX₁ selectively binds the orexin-A neuropeptide. It shares 64% identity with OX₂.

Ligands

Agonists

• Orexin-A

Antagonists

• RTIOX-276 - Selective OX₁ antagonist
• ACT-335827 - Selective OX₁ antagonist
• Almorexant - Dual OX₁ and OX₂ antagonist
• Lemborexant - Dual OX₁ and OX₂ antagonist
• Nemorexant - Dual OX₁ and OX₂ antagonist
• SB-334,867 - Selective OX₁ antagonist
• SB-408,124 - Selective OX₁ antagonist
• SB-649,868 - Dual OX₁ and OX₂ antagonist
• Suvorexant - Dual OX₁ and OX₂ antagonist

See also

• Orexin receptor

External links

• "Orexin Receptors: OX₁". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. http://www.iuphar-db.org/GPCR/ReceptorDisplayForward?receptorID=3012. 

Further reading

• "Obesity and the hypothalamus: novel peptides for new pathways". Cell 92 (4): 437–40. Feb 1998. doi:10.1016/S0092-8674(00)80937-X. PMID 9491885. 
• "To eat or to sleep? Orexin in the regulation of feeding and wakefulness". Annual Review of Neuroscience 24: 429–58. 2001. doi:10.1146/annurev.neuro.24.1.429. PMID 11283317. 
• "Hypocretin/orexin, sleep and narcolepsy". BioEssays 23 (5): 397–408. May 2001. doi:10.1002/bies.1058. PMID 11340621. 
• "The hypocretins: hypothalamus-specific peptides with neuroexcitatory activity". Proceedings of the National Academy of Sciences of the United States of America 95 (1): 322–7. Jan 1998. doi:10.1073/pnas.95.1.322. PMID 9419374. Bibcode: 1998PNAS...95..322D. 
• "Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior". Cell 92 (4): 573–85. Feb 1998. doi:10.1016/S0092-8674(00)80949-6. PMID 9491897. 
• "Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior". Cell 92 (5): 1 page following 696. Mar 1998. doi:10.1016/S0092-8674(02)09256-5. PMID 9527442. 
• "A mutation in a case of early onset narcolepsy and a generalized absence of hypocretin peptides in human narcoleptic brains". Nature Medicine 6 (9): 991–7. Sep 2000. doi:10.1038/79690. PMID 10973318. 
• "Cellular localization of orexin receptors in human pituitary". The Journal of Clinical Endocrinology and Metabolism 86 (7): 1616–9. Jul 2001. doi:10.1210/jcem.86.7.7433. PMID 11443222. 
• "Polymorphisms in hypocretin/orexin pathway genes and narcolepsy". Neurology 57 (10): 1896–9. Nov 2001. doi:10.1212/wnl.57.10.1896. PMID 11723285. 
• "The SK-N-MC cell line expresses an orexin binding site different from recombinant orexin 1-type receptor". European Journal of Biochemistry 269 (4): 1128–35. Feb 2002. doi:10.1046/j.0014-2956.2001.02739.x. PMID 11856342. 
• "Hypersensitization of the Orexin 1 receptor by the CB1 receptor: evidence for cross-talk blocked by the specific CB1 antagonist, SR141716". The Journal of Biological Chemistry 278 (26): 23731–7. Jun 2003. doi:10.1074/jbc.M212369200. PMID 12690115. 
• "Expression of human prepro-orexin and signaling characteristics of orexin receptors in the male reproductive system". The Journal of Clinical Endocrinology and Metabolism 89 (4): 1957–62. Apr 2004. doi:10.1210/jc.2003-031778. PMID 15070969. 
• "OX1 orexin receptors couple to adenylyl cyclase regulation via multiple mechanisms". The Journal of Biological Chemistry 280 (8): 6570–9. Feb 2005. doi:10.1074/jbc.M407397200. PMID 15611118. 
• "Preproorexin and orexin receptors are expressed in cortisol-secreting adrenocortical adenomas, and orexins stimulate in vitro cortisol secretion and growth of tumor cells". The Journal of Clinical Endocrinology and Metabolism 90 (6): 3544–9. Jun 2005. doi:10.1210/jc.2004-2385. PMID 15797953. 
• "Association of an orexin 1 receptor 408Val variant with polydipsia-hyponatremia in schizophrenic subjects". Biological Psychiatry 58 (5): 401–7. Sep 2005. doi:10.1016/j.biopsych.2005.04.015. PMID 15978554. 
• "Orexins stimulate glucocorticoid secretion from cultured rat and human adrenocortical cells, exclusively acting via the OX1 receptor". The Journal of Steroid Biochemistry and Molecular Biology 96 (5): 423–9. Sep 2005. doi:10.1016/j.jsbmb.2005.05.003. PMID 16157481. 

This article incorporates text from the United States National Library of Medicine, which is in the public domain.