Opioid receptor: Difference between revisions

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imported>Robert Badgett
(New page: {{subpages}} '''Opiod receptors''' are "cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid ...)
 
imported>Robert Badgett
(→‎mu receptor: Added Alvimopan)
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Mu receptors are a "class of opioid receptors recognized by its pharmacological profile. Mu opioid receptors bind, in decreasing order of affinity, endorphins, dynorphins, met-enkephalin, and leu-enkephalin. They have also been shown to be molecular receptors for morphine."<ref>{{MeSH|mu receptor}}</ref>
Mu receptors are a "class of opioid receptors recognized by its pharmacological profile. Mu opioid receptors bind, in decreasing order of affinity, endorphins, dynorphins, met-enkephalin, and leu-enkephalin. They have also been shown to be molecular receptors for morphine."<ref>{{MeSH|mu receptor}}</ref>


Methylnaltrexone, an investigational drug for treating [[constipation]] due to [[opioid analgesic]]s, is an example of a mu receptor antagonist.<ref name="pmid18509120">{{cite journal |author=Thomas J, Karver S, Cooney GA, ''et al'' |title=Methylnaltrexone for opioid-induced constipation in advanced illness |journal=N. Engl. J. Med. |volume=358 |issue=22 |pages=2332–43 |year=2008 |month=May |pmid=18509120 |doi=10.1056/NEJMoa0707377 |url=http://content.nejm.org/cgi/pmidlookup?view=short&pmid=18509120&promo=ONFLNS19 |issn=}}</ref>
[[Alvimopan]] is a selective mu receptor antagonist used for treatment of postoperative
ileus after bowel resection.<ref name="pmidpending">{{cite journal |author=Anonymous |title=Alvimopan (Entereg) for Postoperative Ileus |journal=Medical Letter |volume=50 |issue=1300 |pages=93 |year=2008 |month=December |pmid= |doi= |url=http://www.medicalletter.org/restricted/articles/w1300a.pdf |issn=}}</ref> [[Methylnaltrexone]], is approved by the [[United States]] [[Food and Drug Administration]] for the treatment of [[constipation]] due to [[opioid analgesic]]s, is anotjher example of a mu receptor antagonist.<ref name="pmid18509120">{{cite journal |author=Thomas J, Karver S, Cooney GA, ''et al'' |title=Methylnaltrexone for opioid-induced constipation in advanced illness |journal=N. Engl. J. Med. |volume=358 |issue=22 |pages=2332–43 |year=2008 |month=May |pmid=18509120 |doi=10.1056/NEJMoa0707377 |url=http://content.nejm.org/cgi/pmidlookup?view=short&pmid=18509120&promo=ONFLNS19 |issn=}}</ref>


===delta receptor===
===delta receptor===

Revision as of 13:47, 26 November 2008

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Opiod receptors are "cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known."[1]

Classification

There a several cell surface receptors for opioids. All are are G-protein-coupled receptors.

kappa receptor

Kappa receptors are a "class of opioid receptors recognized by its pharmacological profile. Kappa opioid receptors bind dynorphins with a higher affinity than endorphins which are themselves preferred to enkephalins."[2]

mu receptor

Mu receptors are a "class of opioid receptors recognized by its pharmacological profile. Mu opioid receptors bind, in decreasing order of affinity, endorphins, dynorphins, met-enkephalin, and leu-enkephalin. They have also been shown to be molecular receptors for morphine."[3]

Alvimopan is a selective mu receptor antagonist used for treatment of postoperative ileus after bowel resection.[4] Methylnaltrexone, is approved by the United States Food and Drug Administration for the treatment of constipation due to opioid analgesics, is anotjher example of a mu receptor antagonist.[5]

delta receptor

Delta receptors are a "class of opioid receptors recognized by its pharmacological profile. Delta opioid receptors bind endorphins and enkephalins with approximately equal affinity and have less affinity for dynorphins."[6]

References