Kapa opioidni receptor
Kapa opioidni receptor 1 | |||||||||||
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Identifikatori | |||||||||||
Simboli | OPRK1; KOR; OPRK | ||||||||||
Vanjski ID |
OMIM: 165196 MGI: 97439 HomoloGene: 20253 IUPHAR: | ||||||||||
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Pregled RNK izražavanja | |||||||||||
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podaci | |||||||||||
Ortolozi | |||||||||||
Vrsta | Čovek | Miš | |||||||||
Entrez | 4986 | 18387 | |||||||||
Ensembl | ENSG00000082556 | ENSMUSG00000025905 | |||||||||
UniProt | P41145 | Q14AL5 | |||||||||
RefSeq (mRNA) | NM_000912 | NM_011011 | |||||||||
RefSeq (protein) | NP_000903 | NP_035141 | |||||||||
Lokacija (UCSC) |
Chr 8: 54.3 - 54.33 Mb |
Chr 1: 5.58 - 5.59 Mb | |||||||||
PubMed pretraga | [1] | [2] |
Tipovi
[уреди | уреди извор]Na osnovu istraživanja receptorskog vezivanja, tri varijante
Funkcija
[уреди | уреди извор]Dugo vremena je poznato da su agonisti
Prenos signala
[уреди | уреди извор]Aktivacija
Ligandi
[уреди | уреди извор]Sintetički alkaloid ketazocin[23] i terpenoidni prirodni proizvod salvinorin A[24] su potentni i selektivni agonisti
- Asimadolin
- Butorfanol
- BRL-52537
- Ciklazocin
- Dekstrometorfan
- Dinorfin (endogeni peptidni ligand)
- Enadolin
- GR-89696 - selektivan za
κ 2 tip - HZ-2
- ICI-204,448 - periferno selektivan
- ICI-199,441
- Ketazocin
- LPK-26 - visoko selektivan
- Mentol
- Nalbufin
- Nalfurafin
- Norbuprenorfin
- Oksikodon
- Pentazocin
- Salvinorin A
- 2-Metoksimetil Salvinorin B[26] i njegovi etoksimetil i fluoroetoksimetil homolozi[27][28]
- Spiradolin
- Tifluadom
- U-50488
- U-69593
Antagonisti
Prirodni agonist
[уреди | уреди извор]Menta
[уреди | уреди извор]Nađeno u brojnim vrstama minta (pepermint, Mentha spicata, i Mentha aquatica), prirodno jedinjenje mentol je slab agonist k-opioidnog receptora[29]. Mint isto tako može da desenzitiviše region putem aktivacije TRPM8 receptora ('hladnoća'/mentol receptor).[30]
Salvia divinorum
[уреди | уреди извор]Ključno jedinjenje u Salvia divinorum, Salvinorin A, je poznato kao netoksični i potentni agonist
Ibogain
[уреди | уреди извор]Ibogain se koristi se za lečenje adikcije u pojedinim zemljama. On je postao ikona menadžmenta adikcije u nekim krugovima. Uprkos toga što ne izaziva zavisnost, ibogain se tretira kao kontrolisana supstanca u SAD-u, i stoga je njegovo posedovanje ilegalno. Ibogain je agonist
Interakcije
[уреди | уреди извор]Za
Vidi još
[уреди | уреди извор]Reference
[уреди | уреди извор]- ^ James IF, Chavkin C, Goldstein A (1982). „Selectivity of dynorphin for kappa opioid receptors”. Life Sci. 31 (12-13): 1331—4. PMID 6128656. doi:10.1016/0024-3205(82)90374-5.
- ^ Fine, Perry G.; Russell K. Portenoy (2004). „Chapter 2: The Endogenous Opioid System” (PDF). A Clinical Guide to Opioid Analgesia (PDF). McGraw Hill. Архивирано из оригинала (PDF) 19. 07. 2011. г.
- ^ Mansour A, Fox CA, Akil H, Watson SJ (1995). „Opioid-receptor mRNA expression in the rat CNS: anatomical and functional implications”. Trends Neurosci. 18 (1): 22—9. PMID 7535487. doi:10.1016/0166-2236(95)93946-U.
- ^ de Costa BR, Rothman RB, Bykov V, Jacobson AE, Rice KC (1989). „Selective and enantiospecific acylation of kappa opioid receptors by (1S,2S)-trans-2-isothiocyanato-N-methyl-N-[2-(1-pyrrolidinyl) cyclohexy l] benzeneacetamide. Demonstration of kappa receptor heterogeneity”. J. Med. Chem. 32 (2): 281—3. PMID 2536435. doi:10.1021/jm00122a001.
- ^ Rothman RB, France CP, Bykov V, De Costa BR, Jacobson AE, Woods JH, Rice KC (1989). „Pharmacological activities of optically pure enantiomers of the kappa opioid agonist, U50,488, and its cis diastereomer: evidence for three kappa receptor subtypes”. Eur. J. Pharmacol. 167 (3): 345—53. PMID 2553442. doi:10.1016/0014-2999(89)90443-3.
- ^ Mansson E, Bare L, Yang D (1994). „Isolation of a human kappa opioid receptor cDNA from placenta”. Biochem. Biophys. Res. Commun. 202 (3): 1431—7. PMID 8060324. doi:10.1006/bbrc.1994.2091.
- ^ Jordan BA, Devi LA (1999). „G-protein-coupled receptor heterodimerization modulates receptor function”. Nature. 399 (6737): 697—700. PMID 10385123. doi:10.1038/21441.
- ^ Land BB, Bruchas MR, Lemos JC, Xu M, Melief EJ, Chavkin C (2008). „The dysphoric component of stress is encoded by activation of the dynorphin kappa-opioid system”. J. Neurosci. 28 (2): 407—14. PMC 2612708
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- ^ Lomas LM, Barrett AC, Terner JM, Lysle DT, Picker MJ (2007). „Sex differences in the potency of kappa opioids and mixed-action opioids administered systemically and at the site of inflammation against capsaicin-induced hyperalgesia in rats”. Psychopharmacology (Berl.). 191 (2): 273—85. PMID 17225166. doi:10.1007/s00213-006-0663-1.
- ^ Sershen H, Hashim A, Lajtha A (1998). „Gender differences in kappa-opioid modulation of cocaine-induced behavior and NMDA-evoked dopamine release”. Brain Res. 801 (1-2): 67—71. PMID 9729284. doi:10.1016/S0006-8993(98)00546-0.
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- ^ Lawrence DM, Bidlack JM (1993). „The kappa opioid receptor expressed on the mouse R1.1 thymoma cell line is coupled to adenylyl cyclase through a pertussis toxin-sensitive guanine nucleotide-binding regulatory protein”. J. Pharmacol. Exp. Ther. 266 (3): 1678—83. PMID 8103800.
- ^ Konkoy CS, Childers SR (1993). „Relationship between kappa 1 opioid receptor binding and inhibition of adenylyl cyclase in guinea pig brain membranes”. Biochem. Pharmacol. 45 (1): 207—16. PMID 8381004. doi:10.1016/0006-2952(93)90394-C.
- ^ Schoffelmeer, A. N.; Rice, K. C.; Jacobson AE; et al. (1988). „Mu-, delta- and kappa-opioid receptor-mediated inhibition of neurotransmitter release and adenylate cyclase activity in rat brain slices: studies with fentanyl isothiocyanate”. Eur. J. Pharmacol. 154 (2): 169—78. PMID 2906610. doi:10.1016/0014-2999(88)90094-5.
- ^ Henry DJ, Grandy DK, Lester HA, Davidson N, Chavkin C (1995). „Kappa-opioid receptors couple to inwardly rectifying potassium channels when coexpressed by Xenopus oocytes”. Mol. Pharmacol. 47 (3): 551—7. PMID 7700253.
- ^ Tallent M, Dichter MA, Bell GI, Reisine T (1994). „The cloned kappa opioid receptor couples to an N-type calcium current in undifferentiated PC-12 cells”. Neuroscience. 63 (4): 1033—40. PMID 7700508. doi:10.1016/0306-4522(94)90570-3.
- ^ Bohn LM, Belcheva MM, Coscia CJ (2000). „Mitogenic signaling via endogenous kappa-opioid receptors in C6 glioma cells: evidence for the involvement of protein kinase C and the mitogen-activated protein kinase signaling cascade.”. J Neurochem. 74 (2): 564—73. PMC 2504523
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- ^ Belcheva MM, Clark AL, Haas PD, Serna JS, Hahn JW, Kiss A, Coscia CJ (2005). „Mu and kappa opioid receptors activate ERK/MAPK via different protein kinase C isoforms and secondary messengers in astrocytes”. J. Biol. Chem. 280 (30): 27662—9. PMC 1400585
. PMID 15944153. doi:10.1074/jbc.M502593200.
- ^ Bruchas MR, Macey TA, Lowe JD, Chavkin C (2006). „Kappa opioid receptor activation of, pp. 38 MAPK is GRK3- and arrestin-dependent in neurons and astrocytes”. J. Biol. Chem. 281 (26): 18081—9. PMC 2096730
. PMID 16648139. doi:10.1074/jbc.M513640200.
- ^ Bruchas MR, Xu M, Chavkin C (2008). „Repeated swim stress induces kappa opioid-mediated activation of extracellular signal-regulated kinase 1/2”. Neuroreport. 19 (14): 1417—22. PMC 2641011
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- ^ Kam AY, Chan AS, Wong YH (2004). „Kappa-opioid receptor signals through Src and focal adhesion kinase to stimulate c-Jun N-terminal kinases in transfected COS-7 cells and human monocytic THP-1 cells”. J. Pharmacol. Exp. Ther. 310 (1): 301—10. PMID 14996948. doi:10.1124/jpet.104.065078.
- ^ Bruchas MR, Yang T, Schreiber S, Defino M, Kwan SC, Li S, Chavkin C (2007). „Long-acting kappa opioid antagonists disrupt receptor signaling and produce noncompetitive effects by activating c-Jun N-terminal kinase”. J. Biol. Chem. 282 (41): 29803—11. PMC 2096775
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- ^ Roth, B. L.; Baner, K.; Westkaemper R; et al. (2002). „Salvinorin A: a potent naturally occurring nonnitrogenous kappa opioid selective agonist”. Proc. Natl. Acad. Sci. U.S.A. 99 (18): 11934—9. PMC 129372
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- ^ Holtzman SG (1985). „Drug discrimination studies”. Drug Alcohol Depend. 14 (3-4): 263—82. PMID 2859972. doi:10.1016/0376-8716(85)90061-4.
- ^ Wang Y, Chen Y, Xu W, Lee DY, Ma Z, Rawls SM, Cowan A, Liu-Chen LY (2008). „2-Methoxymethyl-salvinorin B is a potent kappa opioid receptor agonist with longer lasting action in vivo than salvinorin A”. The Journal of Pharmacology and Experimental Therapeutics. 324 (3): 1073—83. PMC 2519046
. PMID 18089845. doi:10.1124/jpet.107.132142.
- ^ Munro TA, Duncan KK, Xu W, Wang Y, Liu-Chen LY, Carlezon WA, Cohen BM, Béguin C (2008). „Standard protecting groups create potent and selective kappa opioids: salvinorin B alkoxymethyl ethers”. Bioorganic & Medicinal Chemistry. 16 (3): 1279—86. PMC 2568987
. PMID 17981041. doi:10.1016/j.bmc.2007.10.067.
- ^ Baker LE, Panos JJ, Killinger BA, Peet MM, Bell LM, Haliw LA, Walker SL (2009). „Comparison of the discriminative stimulus effects of salvinorin A and its derivatives to U69,593 and U50,488 in rats”. Psychopharmacology. 203 (2): 203—11. PMID 19153716. doi:10.1007/s00213-008-1458-3.
- ^ Galeotti N, Di Cesare Mannelli L, Mazzanti G, Bartolini A, Ghelardini C (2002). „Menthol: a natural analgesic compound”. Neurosci. Lett. 322 (3): 145—8. PMID 11897159. doi:10.1016/S0304-3940(01)02527-7.
- ^ Werkheiser JL, Rawls SM, Cowan A (2006). „Mu and kappa opioid receptor agonists antagonize icilin-induced wet-dog shaking in rats”. Eur. J. Pharmacol. 547 (1-3): 101—5. PMID 16945367. doi:10.1016/j.ejphar.2006.07.026.
- ^ Butelman ER, Mandau M, Tidgewell K, Prisinzano TE, Yuferov V, Kreek MJ (2007). „Effects of salvinorin A, a kappa-opioid hallucinogen, on a neuroendocrine biomarker assay in nonhuman primates with high kappa-receptor homology to humans”. The Journal of pharmacology and experimental therapeutics. 320 (1): 300—6. PMID 17060493. doi:10.1124/jpet.106.112417.
- ^ Chavkin C, Sud S, Jin W, Stewart J, Zjawiony JK, Siebert DJ, Toth BA, Hufeisen SJ, Roth BL (2004). „Salvinorin A, an active component of the hallucinogenic sage salvia divinorum is a highly efficacious kappa-opioid receptor agonist: structural and functional considerations”. The Journal of pharmacology and experimental therapeutics. 308 (3): 1197—203. PMID 14718611. doi:10.1124/jpet.103.059394.
- ^ Glick SD, Maisonneuve IS (1998). „Mechanisms of antiaddictive actions of ibogaine”. Annals of the New York Academy of Sciences. 844: 214—26. PMID 9668680. doi:10.1111/j.1749-6632.1998.tb08237.x.
- ^ Huang, Peng; Deborah, Steplock; et al. (2004). „kappa Opioid receptor interacts with Na(+)/H(+)-exchanger regulatory factor-1/Ezrin-radixin-moesin-binding phosphoprotein-50 (NHERF-1/EBP50) to stimulate Na(+)/H(+) exchange independent of G(i)/G(o) proteins”. J. Biol. Chem. United States. 279 (24): 25002—9. ISSN 0021-9258. PMID 15070904. doi:10.1074/jbc.M313366200.
- ^ Li, Jian-Guo; Chongguang, Chen; Liu-Chen Lee-Yuan (2002). „Ezrin-radixin-moesin-binding phosphoprotein-50/Na+/H+ exchanger regulatory factor (EBP50/NHERF) blocks U50,488H-induced down-regulation of the human kappa opioid receptor by enhancing its recycling rate”. J. Biol. Chem. United States. 277 (30): 27545—52. ISSN 0021-9258. PMID 12004055. doi:10.1074/jbc.M200058200.
- ^ Li, Jian-Guo; Haines Dale S; Liu-Chen Lee-Yuan (2008). „Agonist-promoted Lys63-linked polyubiquitination of the human kappa-opioid receptor is involved in receptor down-regulation”. Mol. Pharmacol. United States. 73 (4): 1319—30. PMID 18212250. doi:10.1124/mol.107.042846.
Literatura
[уреди | уреди извор]- Fine, Perry G.; Russell K. Portenoy (2004). „Chapter 2: The Endogenous Opioid System” (PDF). A Clinical Guide to Opioid Analgesia (PDF). McGraw Hill. Архивирано из оригинала (PDF) 19. 07. 2011. г.
Spoljašnje veze
[уреди | уреди извор]- „Opioid Receptors:
κ ”. IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Архивирано из оригинала 23. 02. 2014. г. - kappa+Opioid+Receptor на US National Library of Medicine Medical Subject Headings (MeSH)