Извор странице Opioidni receptor

{{Infobox Proteinska Familija-lat
| Symbol = 7tm_1
| Name = GPCR
| image = 4DJH.png
| width = 
| caption = Dimerna struktura ljudskog [[Kapa opioidni receptor|k opioidnog G protein spregnutog receptora]] u kompleksu sa -{[[JDTic]]}-<ref>{{cite journal |title=Structure of the human k-opioid receptor in complex with JDTic |author=Huixian Wu |display-authors=etal | doi=10.1038/nature10939 |year=2012 |journal=Nature |url=http://www.nature.com/nature/journal/vaop/ncurrent/full/nature10939.html}}</ref>
| Pfam = PF00001 
| Pfam_clan = 
| InterPro = IPR000276
| SMART = 
| PROSITE = PDOC00210 
| MEROPS =
| SCOP = 
| TCDB = 
| OPM family = 
| OPM protein = 
| CAZy = 
| CDD =
}}
'''Opioidni receptori''' su grupa [[G protein spregnuti receptori|G protein-spregnutih receptora]] sa [[opioid]]ima kao [[Ligand (biohemija)|ligandima]]. [[Endogen]]i [[opioid]]i su [[dinorfin]]i, [[enkefalin]]i, [[endorfin]]i, [[endomorfin]]i i [[nociceptin]]. Opioidni receptori su ~40% identični sa [[somatostatin]]skim [[receptor (biohemija)|receptorima]] (SSTR).

== Otkriće ==

Sredinom [[1960e|1960]]-tih, postalo je očevidno iz farmakoloških studija da [[Opijati|opijatni]] lekovi deluju na specifičnim receptorskim mestima, i da je verovatno da postoji više takvih mesta.<ref name="pmid4867058">{{cite journal | author = Martin WR | title = Opioid antagonists | journal = Pharmacol. Rev. | volume = 19 | issue = 4 | pages = 463-521 | year = 1967 | pmid = 4867058 | doi =  |url= | issn =  }}</ref> Ti receptori su prvo identifikovani kao specifični molekuli putem upotrebe studija vezivanja liganda, u kojima je za opijate obeležene sa [[radioizotop]]ima nađeno da se vezuju za moždane [[biološka membrana|membranske]] homogenate. Prva takva studija je objavljena [[1971]], koristeći [[Tricijum|<sup>3</sup>-{H}-]]-[[levorfanol]].<ref name="pmid5288759">{{cite journal |vauthors=Goldstein A, Lowney LI, Pal BK | title = Stereospecific and nonspecific interactions of the morphine congener levorphanol in subcellular fractions of mouse brain | journal = Proc. Natl. Acad. Sci. U.S.A. | volume = 68 | issue = 8 | pages=1742-7 | year = 1971 | pmid = 5288759 | pmc = 389284 | doi = 10.1073/pnas.68.8.1742| url =  }}</ref> Kandas Pert i Solomon H. Snider su [[1973]]. objavili prvu detaljnu studiju μ opioidnog receptora, koristeći [[Tricijum|<sup>3</sup>-{H}-]]-[[nalokson]].<ref name="pmid4687585">{{cite journal |vauthors=Pert CB, Snyder SH | title = Opiate receptor: demonstration in nervous tissue | journal = Science (journal) | volume = 179 | issue = 77 | pages=1011-4 | year = 1973 | pmid = 4687585 | doi = 10.1126/science.179.4077.1011 | url =  | issn = }}</ref> Ta studija se smatra prvim definitivnom potvrdom postojanja opioidnog receptora, mada su dve druge studije objavljene kratko posle toga.<ref name="pmid4801733">{{cite journal |last=Terenius|first=L.| title = Stereospecific interaction between narcotic analgesics and a synaptic plasm a membrane fraction of rat cerebral cortex | journal = Acta Pharmacol. Toxicol. (Copenh.) | volume = 32 | issue = 3 | pages=317-20 | year = 1973 | pmid = 4801733 | doi = | url = | issn = }}</ref><ref name="pmid4516196">{{cite journal |vauthors=Simon EJ, Hiller JM, Edelman I | title = Stereospecific binding of the potent narcotic analgesic (3H) Etorphine to rat-brain homogenate | journal = Proc. Natl. Acad. Sci. U.S.A. | volume = 70 | issue = 7 | pages=1947-9 | year = 1973 | pmid = 4516196 | pmc = 433639 | doi = 10.1073/pnas.70.7.1947| url =  }}</ref>

== Prečišćavanje ==

Prečišćavanje receptora je proizvelo dodatne potvrde o njegovom postojanju. Prvi pokušaj da se prečisti receptor se sastojao od upotrebe novog antagonista opioidnog receptora, hlornaltreksamina, za koji je bilo pokazano da se vezuje za opioidni receptor.<ref name="pmid86208">{{cite journal |last1=Caruso|first1=T. P.|last2=Takemori|first2=AE|last3=Larson|first3=DL|last4=Portoghese|first4=PS| title = Chloroxymorphamine, an opioid receptor site-directed alkylating agent having narcotic [[Agonist (farmakologija)|agonist]] activity | journal = Science | volume = 204 | issue = 4390 | pages=316-8 | year = 1979 | pmid = 86208 | pmc = | doi = 10.1126/science.86208 }}</ref> Karuso et al.<ref name="pmid6259471">{{cite journal |last1=Caruso|first1=T. P.|last2=Larson|first2=DL|last3=Portoghese|first3=PS|last4=Takemori|first4=AE| title = Isolation of selective 3H-chlornaltrexamine-bound complexes, possible opioid receptor components in brains of mice.  | journal = Life Sciences | volume = 27 | issue = 22 | pages=2063-9 | year = 1980 | pmid = 6259471 | pmc = | doi = 10.1016/0024-3205(80)90485-3| url = http://www.ncbi.nlm.nih.gov/pubmed/6259471?itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsPanel.Pubmed_RVDocSum&ordinalpos=2 }}</ref> su [[1980]]. prečistili deterdžentom-ekstraktovanu komponentu membrane mozga pacova koja se ispira sa specifično vezanim [[tricijum|<sup>3</sup>-{H}-]]-[[hlornaltreksamin]]om.

== Glavni podtipovi ==

Postoje četiri glavna podtipa opioidnog receptora:<ref name="pmid16402099">{{cite journal |vauthors=Corbett AD, Henderson G, McKnight AT, Paterson SJ | title = 75 years of opioid research: the exciting but vain quest for the Holy Grail | journal = Br. J. Pharmacol. | volume = 147 Suppl 1 | issue = | pages = S153–62 | year = 2006 | pmid = 16402099 | doi = 10.1038/sj.bjp.0706435 | pmc = 1760732 }}</ref>

{| class="wikitable"
|-
! Receptor
! Podtipovi 
! Lokacija<ref name="stoppain">{{Cite book | last = Fine | first = Perry G. | author2 = Russell K. Portenoy | title = A Clinical Guide to Opioid Analgesia | url = http://www.stoppain.org/pcd/_pdf/OpioidChapter2.pdf | format =  | accessdate =  | edition =  | series =  | volume =  | date =  | year = 2004 | month =  | publisher = McGraw Hill | location =  | language =  | oclc =  | doi =  | pages =  | chapter = Chapter 2: The Endogenous Opioid System | chapterurl = http://www.stoppain.org/pcd/_pdf/OpioidChapter2.pdf | archive-date = 19. 07. 2011 | archive-url = https://web.archive.org/web/20110719072413/http://www.stoppain.org/pcd/_pdf/OpioidChapter2.pdf | url-status =  }}</ref>

! Funkcija<ref name="stoppain"/>
 |- 
 | [[Delta opioidni receptor|delta (δ)]] <br /> OP<sub>1</sub> <sup>(I)</sup> || δ<sub>1</sub>, δ<sub>2</sub> ||
* [[mozak]]
** [[Varolijev most]] 
** [[amigdala]]
** [[mirisni mozak]]
** duboki [[cerebralni korteks|korteks]]
||
* [[Analgetik|analgezija]]
* [[Antidepresivi|antidepresivni]] efekti
* [[fizička zavisnost]]
 |- 
 | [[kapa opioidni receptor|kapa (κ)]] <br /> OP<sub>2</sub> <sup>(I)</sup>  || κ<sub>1</sub>, κ<sub>2</sub>, κ<sub>3</sub> ||
* [[mozak]]
** [[hipotalamus]]
** [[centralna siva masa]]
** [[klaustrum]]
* [[kičmena moždina]]
** -{[[substantia gelatinosa]]}-
||
* kičmena analgezija
* [[sedacija]]
* [[mioza]]
* inhibicija [[Antidiuretski hormon|ADH]] oslobađanja 
* [[disforija]]
 |- 
 | [[Mi opioidni receptor|Mi (μ)]] <br /> OP<sub>3</sub> <sup>(I)</sup> || μ<sub>1</sub>, μ<sub>2</sub>, μ<sub>3</sub> ||
* [[mozak]]
** [[cerebralni korteks|korteks]] (lamine III i IV)
** [[talamus]]
** [[centralna siva masa]]
* [[kičmena moždina]]
** -{[[substantia gelatinosa]]}-
* [[систем органа за варење|intestinalni trakt]]
|| '''μ<sub>1</sub>''':
* [[supraspinalni]] [[Analgetik|analgezija]]
* [[fizička zavisnost]]
'''μ<sub>2</sub>''':
* [[Hipoventilacija|respiratorna depresija]]
* [[mioza]]
* [[euforija]]
* umanjena [[Систем органа за варење|GI]] motilnost
* [[fizička zavisnost]]
'''μ<sub>3</sub>''':
* nepoznato
 |- 
 | [[Nociceptinski receptor|Nociceptinski]] <br />receptor<br /> OP<sub>4</sub> || ORL<sub>1</sub> ||
* [[mozak]]
** [[Cerebralni korteks|korteks]]
** [[amigdala]] 
** [[hipokampus]]
** [[septal nuclei]]
** [[habenula]]
** [[hipotalamus]]
* [[kičmena moždina]]
||
* anksioznost
* depresija
* apetit
* razvoj tolerancije na μ agoniste
|}

<small>(I). Ime je bazirano na redosledu otkrivanja. </small>

== Vidi još ==
* [[Opioidni antagonist]]

== Reference ==
{{reflist|2}}

== Literatura ==
{{Литература|2}}
* {{cite web | url = http://www.iuphar-db.org/GPCR/ChapterMenuForward?chapterID=1295 | title = Opioid Receptors | accessdate =  | date =  | format =  | work = IUPHAR Database of Receptors and Ion Channels | publisher = International Union of Basic and Clinical Pharmacology | pages =  | language =  | archiveurl = https://web.archive.org/web/20210118045402/https://www.iuphar-db.org/GPCR/ChapterMenuForward?chapterID=1295 | archivedate = 18. 01. 2021 | quote =  | url-status =  }}
* {{cite web | url = http://opioids.com/receptors/index.html | title = Opioid Receptors | accessdate = 21. 3. 2008. | vauthors = Corbett A, McKnight S, Henderson G | date =  | work =  | publisher = BLTC Research | pages =  | language =  | archiveurl = https://web.archive.org/web/20210314162355/https://www.opioids.com/receptors/index.html | archivedate = 14. 03. 2021 | quote =  | url-status =  }}
* {{cite web | url = http://opm.phar.umich.edu/ | title = Orientations of Proteins in Membranes (OPM) database | accessdate = 21. 3. 2008. | vauthors = Lomize A, Lomize M, Pogozheva I | date =  | format =  | work =  | publisher = University of Michigan | pages =  | language =  | archiveurl = https://web.archive.org/web/20140103112750/http://opm.phar.umich.edu/ | archivedate = 03. 01. 2014 | quote =  | url-status = dead }}
** {{cite web | url = http://opm.phar.umich.edu/protein.php?pdbid=2iql | title = Mu-opioid receptor model (inactive state) with antagonist | accessdate = 21. 3. 2008. | date = | format = | work = | publisher =  | pages = | language = | archiveurl = | archivedate = | quote = }}
** {{cite web | url = http://opm.phar.umich.edu/protein.php?pdbid=2iqo | title = Mu-opioid receptor model in active state with agonist | accessdate = 21. 3. 2008. | date = | format = | work = | publisher = | pages = | language = | archiveurl = | archivedate = | quote = }}
{{Литература крај}}

== Spoljašnje veze ==
* {{MeshName|Opioid+Receptors}}
{{-}}
{{G protein spregnuti receptori-lat}}
{{Neuropeptidni receptori-lat}}
{{Opioidi-lat}}
{{Neuropeptidni ligandi-lat}}

{{normativna kontrola}}

[[Категорија:Опиоидни рецептори]]