Hypocretin (orexin) receptor 2

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Hypocretin (orexin) receptor 2
Identifiers
SymbolsHCRTR2; OX2R
External IDsOMIM: 602393 MGI: 2680765 HomoloGene: 1168 IUPHAR: OX2 GeneCards: HCRTR2 Gene
RNA expression pattern
250px
More reference expression data
Orthologs
SpeciesHumanMouse
Entrez3062387285
EnsemblENSG00000137252ENSMUSG00000032360
UniProtO43614Q8BV78
RefSeq (mRNA)NM_001526NM_198962
RefSeq (protein)NP_001517NP_945200
Location (UCSC)Chr 6:
55.15 - 55.26 Mb		Chr 9:
76.01 - 76.11 Mb
PubMed search[1][2]

Orexin receptor type 2 (Ox2R or OX2), also known as hypocretin receptor type 2, is a protein that in humans is encoded by the HCRTR2 gene.[1]

Function

OX2 is a G-protein coupled receptor expressed exclusively in the brain. It has 64% identity with OX1. OX2 binds both orexin A and orexin B neuropeptides. OX2 is involved in the central feedback mechanism that regulates feeding behaviour.[1]

Ligands

Agonists

Antagonists

  • Almorexant - mixed OX1/2 antagonist
  • SB-649,868 - mixed OX1/2 antagonist
  • TCS-OX2-29 - selective OX2 antagonist
  • 1-(2,4-dibromophenyl)-3-((4S,5S)-2,2-dimethyl-4-phenyl-[1,3]dioxan-5-yl)urea (600x selective for OX2 over OX1)[2]
  • (3,4-dimethoxyphenoxy)alkylamino acetamides [3]

See also

References

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External links

  • "Orexin Receptors: OX2". 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. 
  • Wright GJ, Puklavec MJ, Willis AC; et al. (2000). "Lymphoid/neuronal cell surface OX2 glycoprotein recognizes a novel receptor on macrophages implicated in the control of their function". Immunity. 13 (2): 233–42. doi:10.1016/S1074-7613(00)00023-6. PMID 10981966. 
  • Hartley JL, Temple GF, Brasch MA (2001). "DNA cloning using in vitro site-specific recombination". Genome Res. 10 (11): 1788–95. doi:10.1101/gr.143000. PMC 310948 Freely accessible. PMID 11076863. 
  • Mazzocchi G, Malendowicz LK, Gottardo L; et al. (2001). "Orexin A stimulates cortisol secretion from human adrenocortical cells through activation of the adenylate cyclase-dependent signaling cascade". J. Clin. Endocrinol. Metab. 86 (2): 778–82. doi:10.1210/jc.86.2.778. PMID 11158046. 
  • Blanco M, López M, García-Caballero T; et al. (2001). "Cellular localization of orexin receptors in human pituitary". J. Clin. Endocrinol. Metab. 86 (4): 1616–9. doi:10.1210/jc.86.4.1616. PMID 11297593. 
  • 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. 
  • Karteris E, Randeva HS, Grammatopoulos DK; et al. (2001). "Expression and coupling characteristics of the CRH and orexin type 2 receptors in human fetal adrenals". J. Clin. Endocrinol. Metab. 86 (9): 4512–9. doi:10.1210/jc.86.9.4512. PMID 11549701. 
  • Randeva HS, Karteris E, Grammatopoulos D, Hillhouse EW (2001). "Expression of orexin-A and functional orexin type 2 receptors in the human adult adrenals: implications for adrenal function and energy homeostasis". J. Clin. Endocrinol. Metab. 86 (10): 4808–13. doi:10.1210/jc.86.10.4808. PMID 11600545. 
  • Olafsdóttir BR, Rye DB, Scammell TE; et al. (2002). "Polymorphisms in hypocretin/orexin pathway genes and narcolepsy". Neurology. 57 (10): 1896–9. PMID 11723285. 
  • Blanco M, García-Caballero T, Fraga M; et al. (2002). "Cellular localization of orexin receptors in human adrenal gland, adrenocortical adenomas and pheochromocytomas". Regul. Pept. 104 (1-3): 161–5. doi:10.1016/S0167-0115(01)00359-7. PMID 11830291. 
  • 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. 
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This article incorporates text from the United States National Library of Medicine, which is in the public domain.

Class A: Rhodopsin like
α1 (A, B, D) · α2 (A, B, C) · β1 · β2 · β3
Adenosine (A1, A2A, A2B, A3) · P2Y (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)
(all but 5-HT3) 5-HT1 (A, B, D, E, F) · 5-HT2 (A, B, C) · 5-HT (4, 5A, 6, 7)
Other
Acetylcholine (M1, M2, M3, M4, M5) · Dopamine (D1, D2, D3, D4, D5) · Histamine (H1, H2, H3, H4) · Melatonin (1A, 1B, 1C) · TAAR (1, 2, 3, 5, 6, 8, 9)
Metabolites and
signaling molecules
CysLT (1, 2) · LTB4 (1, 2) · FPRL1 · OXE · Prostaglandin (DP (1, 2), EP (1, 2, 3, 4), FP) · Prostacyclin · Thromboxane
Other
Bile acid · Cannabinoid (CB1, CB2, GPR (18, 55, 119)) · EBI2 · Estrogen · Free fatty acid (1, 2, 3, 4) · Lactate  · Lysophosphatidic acid (1, 2, 3, 4, 5, 6)  · Lysophospholipid (1, 2, 3, 4, 5, 6, 7, 8) · Niacin (1, 2) · Oxoglutarate · PAF · Sphingosine-1-phosphate (1, 2, 3, 4, 5) · Succinate
Peptide
B/W (1, 2) · FF (1, 2) · S · Y (1, 2, 4, 5) · Neuromedin (B, U (1, 2)) · Neurotensin (1, 2)
Other
Miscellaneous
GPR (1, 3, 4, 6, 12, 15, 17, 18, 19, 20, 21, 22, 23, 25, 26, 27, 31, 32, 33, 34, 35, 37, 39, 42, 44, 45, 50, 52, 55, 61, 62, 63, 65, 68, 75, 77, 78, 81, 82, 83, 84, 85, 87, 88, 92, 101, 103, 109A, 109B, 119, 120, 132, 135, 137B, 139, 141, 142, 146, 148, 149, 150, 151, 152, 153, 160, 161, 162, 171, 173, 174, 176, 177, 182, 183)
Other
Class B: Secretin like
GPR (56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 155, 157)
Other
Class C: Metabotropic
glutamate / pheromone
TAS1R (1, 2, 3) · TAS2R (1, 3, 4, 5, 8, 9, 10, 12, 13, 14, 16, 19, 20, 30, 31, 38, 39, 40, 41, 42, 43, 45, 46, 50)
Other
Class F:
Frizzled / Smoothened
Frizzled
Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10)
Smoothened
  1. ↑ 1.0 1.1 "Entrez Gene: HCRTR2 hypocretin (orexin) receptor 2". 
  2. ↑ McAtee LC, Sutton SW, Rudolph DA, Li X, Aluisio LE, Phuong VK, Dvorak CA, Lovenberg TW, Carruthers NI, Jones TK. Novel substituted 4-phenyl-[1,3]dioxanes: potent and selective orexin receptor 2 (OX(2)R) antagonists. Bioorganic and Medicinal Chemistry Letters. 2004 Aug 16;14(16):4225-9. PMID 15261275
  3. ↑ Cole AG, Stroke IL, Qin LY, Hussain Z, Simhadri S, Brescia MR, Waksmunski FS, Strohl B, Tellew JE, Williams JP, Saunders J, Appell KC, Henderson I, Webb ML. Synthesis of (3,4-dimethoxyphenoxy)alkylamino acetamides as orexin-2 receptor antagonists. Bioorganic and Medicinal Chemistry Letters. 2008 Oct 15;18(20):5420-3. PMID 18815029
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