Hypocretin (orexin) receptor 1
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Hypocretin (orexin) receptor 1 | |||||||||||||
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Identifiers | |||||||||||||
Symbols | HCRTR1; OX1R | ||||||||||||
External IDs | OMIM: 602392 MGI: 2385650 HomoloGene: 37492 IUPHAR: OX1 GeneCards: HCRTR1 Gene | ||||||||||||
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RNA expression pattern | |||||||||||||
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More reference expression data | |||||||||||||
Orthologs | |||||||||||||
Species | Human | Mouse | |||||||||||
Entrez | 3061 | 230777 | |||||||||||
Ensembl | ENSG00000121764 | ENSMUSG00000028778 | |||||||||||
UniProt | O43613 | Q0VDP5 | |||||||||||
RefSeq (mRNA) | NM_001525 | XM_983697 | |||||||||||
RefSeq (protein) | NP_001516 | XP_988791 | |||||||||||
Location (UCSC) | Chr 1: 31.86 - 31.87 Mb | Chr 4: 129.63 - 129.64 Mb | |||||||||||
PubMed search | [1] | [2] |
Orexin receptor type 1 (Ox1R or OX1), also known as hypocretin receptor type 1, is a protein that in humans is encoded by the HCRTR1 gene.[1]
Contents
Function
The orexin 1 receptor (OX1), is a G-protein coupled receptor expressed in the hypothalamus and involved in the regulation of feeding behaviour. OX1 selectively binds the orexin-A neuropeptide. It shares 64% identity with OX2.[1]
Ligands
Agonists
Antagonists
- Almorexant - mixed OX1/2 antagonist
- SB-334,867 - selective OX1 antagonist
- SB-408,124 - selective OX1 antagonist
- SB-649,868 - mixed OX1/2 antagonist
See also
References
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External links
- "Orexin Receptors: OX1". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.
Further reading
- Flier JS, Maratos-Flier E (1998). "Obesity and the hypothalamus: novel peptides for new pathways". Cell. 92 (4): 437–40. doi:10.1016/S0092-8674(00)80937-X. PMID 9491885.
- Willie JT, Chemelli RM, Sinton CM, Yanagisawa M (2001). "To eat or to sleep? Orexin in the regulation of feeding and wakefulness". Annu. Rev. Neurosci. 24: 429–58. doi:10.1146/annurev.neuro.24.1.429. PMID 11283317.
- Hungs M, Mignot E (2001). "Hypocretin/orexin, sleep and narcolepsy". Bioessays. 23 (5): 397–408. doi:10.1002/bies.1058. PMID 11340621.
- de Lecea L, Kilduff TS, Peyron C; et al. (1998). "The hypocretins: hypothalamus-specific peptides with neuroexcitatory activity". Proc. Natl. Acad. Sci. U.S.A. 95 (1): 322–7. doi:10.1073/pnas.95.1.322. PMC 18213 Freely accessible. PMID 9419374.
- Sakurai T, Amemiya A, Ishii M; et al. (1998). "Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior". Cell. 92 (4): 573–85. doi:10.1016/S0092-8674(00)80949-6. PMID 9491897.
- Sakurai T, Amemiya A, Ishii M; et al. (1998). "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. doi:10.1016/S0092-8674(00)80949-6. PMID 9527442.
- Peyron C, Faraco J, Rogers W; et al. (2000). "A mutation in a case of early onset narcolepsy and a generalized absence of hypocretin peptides in human narcoleptic brains". Nat. Med. 6 (9): 991–7. doi:10.1038/79690. PMID 10973318.
- Blanco M, López M, GarcIa-Caballero T; et al. (2001). "Cellular localization of orexin receptors in human pituitary". J. Clin. Endocrinol. Metab. 86 (7): 1616–9. doi:10.1210/jc.86.4.1616. PMID 11443222.
- Olafsdóttir BR, Rye DB, Scammell TE; et al. (2002). "Polymorphisms in hypocretin/orexin pathway genes and narcolepsy". Neurology. 57 (10): 1896–9. PMID 11723285.
- Wieland HA, Söll RM, Doods HN; et al. (2002). "The SK-N-MC cell line expresses an orexin binding site different from recombinant orexin 1-type receptor". Eur. J. Biochem. 269 (4): 1128–35. doi:10.1046/j.0014-2956.2001.02739.x. PMID 11856342.
- Strausberg RL, Feingold EA, Grouse LH; et al. (2003). "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences". Proc. Natl. Acad. Sci. U.S.A. 99 (26): 16899–903. doi:10.1073/pnas.242603899. PMC 139241 Freely accessible. PMID 12477932.
- Hilairet S, Bouaboula M, Carrière D; et al. (2003). "Hypersensitization of the Orexin 1 receptor by the CB1 receptor: evidence for cross-talk blocked by the specific CB1 antagonist, SR141716". J. Biol. Chem. 278 (26): 23731–7. doi:10.1074/jbc.M212369200. PMID 12690115.
- Karteris E, Chen J, Randeva HS (2004). "Expression of human prepro-orexin and signaling characteristics of orexin receptors in the male reproductive system". J. Clin. Endocrinol. Metab. 89 (4): 1957–62. doi:10.1210/jc.2003-031778. PMID 15070969.
- Holmqvist T, Johansson L, Ostman M; et al. (2005). "OX1 orexin receptors couple to adenylyl cyclase regulation via multiple mechanisms". J. Biol. Chem. 280 (8): 6570–9. doi:10.1074/jbc.M407397200. PMID 15611118.
- Spinazzi R, Rucinski M, Neri G; et al. (2005). "Preproorexin and orexin receptors are expressed in cortisol-secreting adrenocortical adenomas, and orexins stimulate in vitro cortisol secretion and growth of tumor cells". J. Clin. Endocrinol. Metab. 90 (6): 3544–9. doi:10.1210/jc.2004-2385. PMID 15797953.
- Meerabux J, Iwayama Y, Sakurai T; et al. (2005). "Association of an orexin 1 receptor 408Val variant with polydipsia-hyponatremia in schizophrenic subjects". Biol. Psychiatry. 58 (5): 401–7. doi:10.1016/j.biopsych.2005.04.015. PMID 15978554.
- Ziolkowska A, Spinazzi R, Albertin G; et al. (2006). "Orexins stimulate glucocorticoid secretion from cultured rat and human adrenocortical cells, exclusively acting via the OX1 receptor". J. Steroid Biochem. Mol. Biol. 96 (5): 423–9. doi:10.1016/j.jsbmb.2005.05.003. PMID 16157481.
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This article incorporates text from the United States National Library of Medicine, which is in the public domain.