Oreksinski receptor 1

edit
Hipokretinski (oreksinski) receptor 1
Identifikatori
SimboliHCRTR1; OX1R
Vanjski IDOMIM: 602392 MGI: 2385650 HomoloGene: 37492 IUPHAR: OX1 GeneCards: HCRTR1 Gene
Ontologija gena
Molekularna funkcija aktivnost rodopsinu-sličnog receptora
receptorska aktivnost
aktivnost neuropeptidnog receptora
aktivnost oreksinskog receptora
Celularna komponenta integralno sa ćelijskom membranom
membrana
Biološki proces prenos signala
neuropeptidni signalni put
sinapsna transmisija
ishrana
Pregled RNK izražavanja
podaci
Ortolozi
VrstaČovekMiš
Entrez3061230777
EnsemblENSG00000121764ENSMUSG00000028778
UniProtO43613Q0VDP5
RefSeq (mRNA)NM_001525XM_983697
RefSeq (protein)NP_001516XP_988791
Lokacija (UCSC)Chr 1:
31.86 - 31.87 Mb
Chr 4:
129.63 - 129.64 Mb
PubMed pretraga[1][2]

Oreksinski receptor tip 1 (OX1R, OX1, ili hipokretinski receptor tip 1), je protein koji je kod ljudi kodiran HCRTR1 genom.[1]

Funkcija

OX1 je G-protein spregnuti receptor koji je izražen u hipotalamusu i učestvuje u regulaciji ishrane. OX1 selektivno vezuje neuropeptid oreksin-A. On je 64% identičan sa OX2.[1]

Ligandi

Agonisti

  • Oreksin-A

Antagonisti

  • Almoreksant - neselektivni OX1/2 antagonist
  • SB-334,867 - selektivni OX1 antagonist
  • SB-408,124 - selektivni OX1 antagonist
  • SB-649,868 - neselektivni OX1/2 antagonist

Vidi još

Reference

  1. 1,0 1,1 „Entrez Gene: HCRTR1 hypocretin (orexin) receptor 1”. 

Literatura

  • 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. 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.” (PDF). Cell 92 (4): 573–85. DOI:10.1016/S0092-8674(00)80949-6. PMID 9491897. Arhivirano iz originala na datum 2011-07-11. Pristupljeno 2014-05-08. 
  • 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): 697. DOI:10.1016/S0092-8674(02)09256-5. 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): 3444–7. DOI:10.1210/jc.86.7.3444. 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. 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. 

Spoljašnje veze

  • „Orexin Receptors: OX1”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Arhivirano iz originala na datum 2016-02-06. 
  • p
  • r
  • u
Klasa A: Rodopsinu slični
α1 (A, B, D) • α2 (A, B, C) • β1 • β2 • β3
Adenozinski (A1, A2A, A2B, A3) • P2Y (1, 2, 4, 5, 6, 8, 9, 10, 11, 12, 13, 14)
(svi osim 5-HT3) 5-HT1 (A, B, D, E, F) • 5-HT2 (A, B, C) • 5-HT (4, 5A, 6, 7)
Drugi
Acetilholin (M1, M2, M3, M4, M5) • Dopamin (D1, D2, D3, D4, D5) • Histamin (H1, H2, H3, H4) • Melatonin (1A, 1B, 1C) • TAAR (1, 2, 3, 5, 6, 8, 9)
Metaboliti i
signalni molekuli
CysLT (1, 2) • LTB4 (1, 2) • FPRL1 • OXE • Prostaglandin (DP (1, 2), EP (1, 2, 3, 4), FP) • Prostaciklin • Tromboksan
Drugi
Žučna kiselina • Kanabinoidni (CB1, CB2, GPR (18, 55, 119)) • EBI2 • Estrogen • Slobodna masna kiselina (1, 2, 3, 4) • Laktat  • Lizofosfatidna kiselina (1, 2, 3, 4, 5, 6)  • Lizofosfolipid (1, 2, 3, 4, 5, 6, 7, 8) • Niacin (1, 2) • Oksoglutarat • PAF • Sfingozin-1-fosfat (1, 2, 3, 4, 5) • Sukcinat
Peptid
B/W (1, 2) • FF (1, 2) • S • Y (1, 2, 4, 5) • Neuromedin (B, U (1, 2)) • Neurotenzin (1, 2)
Drugi
Anafilatoksin (C3a, C5a) • Angiotenzin (1, 2) • Apelin • Bombezin (BRS3, GRPR, NMBR) • Bradikinin (B1, B2) • Hemokin • Holecistokinin (A, B) • Endotelin (A, B) • Formil peptid (1, 2, 3) • FSH • Galanin (1, 2, 3) • GHB receptor • Gonadotropin-oslobađajući hormon (1, 2) • Grelin • Kispeptin • Luteinizirajući hormon/horiogonadotropin • MAS (1, 1L, D, E, F, G, X1, X2, X3, X4) • Melanokortin (1, 2, 3, 4, 5) • MCHR (1, 2) • Motilin • Opioidni (δ, κ, μ, Nociceptin & ζ, ali ne σ) • Oreksin (1, 2) • Oksitocin • Prokineticin (1, 2) • Prolaktin-oslobađajući peptid • Relaksin (1, 2, 3, 4) • Somatostatin (1, 2, 3, 4, 5) • Tahikinin (1, 2, 3) • Tirotropin • Tirotropin-oslobađajući hormon • Urotenzin-II • Vazopresin (1A, 1B, 2)
Razno
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)
Drugi
Adrenomedulin • Mirisni • Opsin (3, 4, 5, 1LW, 1MW, 1SW, RGR, RRH) • Proteazom-aktivirani (1, 2, 3, 4) • SREB (1, 2, 3)
Klasa B: Sekretinu slični
GPR (56, 64, 97, 98, 110, 111, 112, 113, 114, 115, 116, 123, 124, 125, 126, 128, 133, 143, 144, 155, 157)
Drugi
Klasa C: Metabotropni
glutamat / feromon
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)
Drugi
Klasa F:
Frizzled / Zaglađeni
Uvojiti
Frizzled (1, 2, 3, 4, 5, 6, 7, 8, 9, 10)
Zaglađeni
B trdu: peptidi (nrpl/grfl/cytl/horl), receptori (lgic, enzr, gprc, igsr, intg, nrpr/grfr/cytr), itra (adap, gbpr, mapk), calc, lipd, signalni putevi (hedp, wntp, tgfp+mapp, notp, jakp, fsap, hipp, tlrp)
  • p
  • r
  • u
Neuropeptidni receptori
Hormonski receptori
Drugi
Opioidni receptori
Drugi neuropeptidni receptori
B trdu: peptidi (nrpl/grfl/cytl/horl), receptori (lgic, enzr, gprc, igsr, intg, nrpr/grfr/cytr), itra (adap, gbpr, mapk), calc, lipd, signalni putevi (hedp, wntp, tgfp+mapp, notp, jakp, fsap, hipp, tlrp)
  • p
  • r
  • u
Holecistokinin
CCKA
Agonisti: Holecistokinin • CCK-4
Antagonisti: Asperlicin • Proglumid • Lorglumid • Devazepid • Deksloksiglumid
CCKB
Agonisti: Holecistokinin • CCK-4 • Gastrin
Antagonisti: Proglumid • CI-988
CRH
CRF1
CRF2
Galanin
GAL1
Agonisti: Galanin • Galaninu-sličan peptid • Galmic • Galnon
GAL2
Agonisti: Galanin • Galaninu-sličan peptid • Galmic • Galnon
GAL3
Agonisti: Galanin • Galmic • Galnon
Grelin
Agonisti: Grelin • Kapromorelin • MK-677 • Sermorelin • SM-130,686 • Tabimorelin
MCH
MCH1
MCH2
Melanokortin
MC1
MC2
Agonisti: ACTH • Kosintropin • Tetrakosaktid
MC3
Agonisti: alfa-MSH • Bremelanotid • Melanotan II
MC4
Agonisti: alfa-MSH • Bremelanotid • Melanotan II • THIQ
Antagonisti: Agutiju srodni peptid
MC5
Agonisti: alfa-MSH • Melanotan II
Neuropeptid S
Agonisti: Neuropeptid S
Antagonisti: SHA-68
Neuropeptid Y
Y1
Agonisti: Neuropeptid Y • Peptid YY
Antagonisti: BIBP-3226
Y2
Agonisti: Neuropeptid Y • Peptid YY
Antagonisti: BIIE-0246
Y4
Agonisti: Neuropeptid Y • Pankreasni polipeptid • Peptid YY
Antagonisti: UR-AK49
Y5
Agonisti: Neuropeptid Y • Peptid YY
Antagonisti: Lu AA-33810
Neurotenzin
NTS1
Agonisti: Neurotenzin • Neuromedin N
Antagonisti: SR-48692 • SR-142,948
NTS2
Agonisti: Neurotenzin
Antagonisti: Levokabastin • SR-142,948
Opioid
vidi Opioidi
Oreksin
OX1
Agonisti: Oreksin-A
Antagonisti: Almoreksant • SB-334,867 • SB-408,124 • SB-649,868
OX2
Agonisti: Oreksin-A
Antagonisti: Almoreksant • SB-649,868 • TCS-OX2-29
Oksitocin
Agonisti: Karbetocin • Demoksitocin • Oksitocin • WAY-267,464
Antagonisti: Atosiban • L-371,257 • L-368,899
Tahikinin
NK1
Agonisti: Supstanca P
Antagonisti: Aprepitant • Befetupitant • Kasopitant • CI-1021 • CP-96,345 • CP-99,994 • CP-122,721 • Dapitant • Ezlopitant • FK-888 • Fosaprepitant • GR-203,040 • GW-597,599 • HSP-117 • L-733,060 • L-741,671 • L-743,310 • L-758,298 • Lanepitant • LY-306,740 • Maropitant • Netupitant • NKP-608 • Nolpitantium • Orvepitant • RP-67,580 • SDZ NKT 343 • Vestipitant • Vofopitant
NK2
Agonisti: Neurokinin A
Antagonisti: GR-159897 • Ibodutant • Saredutant
NK3
Agonisti: Neurokinin B
Antagonisti: Osanetant • Talnetant
Vazopresin
V1A
Agonisti: Dezmopresin • Felipresin • Ornipresin • Terlipresin • Vazopresin
Antagonisti: Konivaptan • Demeklociklin • Relkovaptan
V1B
Agonisti: Felipresin • Ornipresin • Terlipresin • Vazopresin
Antagonisti: Demeklociklin • Nelivaptan
V2
Agonisti: Dezmopresin • Ornipresin • Vazopresin
Antagonisti: Konivaptan • Demeklociklin • Liksivaptan • Mozavaptan • Satavaptan • Tolvaptan