العربية
中国
Français
Deutsch
Ελληνική
हिन्दी
Italiano
日本語
Português
Русский
EspañolOPIOID RECEPTOR
(Redirected from Opiate receptor)
'Opioid receptors' are a group of G-protein coupled receptors with opioids as ligands. The endogenous opioids are dynorphins, enkephalins and endorphins. The opioid receptors are ~40% identical to somatostatin receptors (SSTRs).
There are three major subtypes of opioid receptors: [1]
Sigma receptors (σ) were once considered to be opioid receptors, but are not usually currently classified as such.
The receptors were named using the first letter of the first ligand that was found to bind to them. Morphine was the first chemical shown to bind to mu receptors. The first letter of the drug morphine is `m'. But in biochemistry there is a tendency to use Greek letters so they converted the 'm' to μ. Similarly a drug known as ketocyclazocine was first shown to attach itself to kappa receptors.[2]
The opioid receptor types are ~70% identical with differences located at N and C termini. The μ receptor (the μ represents morphine) is perhaps the most important. It is thought that the G protein binds to the third intracellular loop of the opioid receptors. Both in mice and humans the genes for the various receptor subtypes are located on different chromosomes.
Separate subtypes have been identified in human tissue. Research has so far failed to identify the genetic evidence of the subtypes, and it is thought that they arise from post-translational modification of cloned receptor types.[3]
An additional opioid receptor has been identified and cloned based on homology with the cDNA. This receptor is known as the nociceptin receptor or ORL 1 receptor.
1. Corbett AD, Henderson G, McKnight AT, Paterson SJ (2006).75 years of opioid research: the exciting but vain quest for the Holy Grail. Brit. J. Pharmacol.'147,' S153–S162
2. http://opioids.com/narcotic-drugs/chapter-3.html
3. Fries, DS (2002). Opioid Analgesics. In Williams DA, Lemke TL. ''Foye's Principles of Medicinal Chemistry'' (5 ed.). Philadelphia: Lippincott Williams & Wilkins. ISBN 0-683-30737-1.
★ Opioid antagonist
★ http://opioids.com/receptors/index.html
★ IUPHAR GPCR Database - Opioid Receptors
★
★ Calculated spatial position of mu-opioid receptor in the lipid bilayer, inactive state with antagonist and active state with agonist
'Opioid receptors' are a group of G-protein coupled receptors with opioids as ligands. The endogenous opioids are dynorphins, enkephalins and endorphins. The opioid receptors are ~40% identical to somatostatin receptors (SSTRs).
| Contents |
| Types of receptors |
| References |
| See also |
| External links |
Types of receptors
There are three major subtypes of opioid receptors: [1]
| 'Greek letter name' | 'Name based on order of discovery' | 'Subtypes' |
| delta opioid receptor (δ) | OP1 | δ1, δ2 |
| kappa opioid receptor (κ) | OP2 | κ1, κ2, κ3 |
| mu opioid receptor (μ) | OP3 | μ1, μ2, μ3 |
Sigma receptors (σ) were once considered to be opioid receptors, but are not usually currently classified as such.
The receptors were named using the first letter of the first ligand that was found to bind to them. Morphine was the first chemical shown to bind to mu receptors. The first letter of the drug morphine is `m'. But in biochemistry there is a tendency to use Greek letters so they converted the 'm' to μ. Similarly a drug known as ketocyclazocine was first shown to attach itself to kappa receptors.[2]
The opioid receptor types are ~70% identical with differences located at N and C termini. The μ receptor (the μ represents morphine) is perhaps the most important. It is thought that the G protein binds to the third intracellular loop of the opioid receptors. Both in mice and humans the genes for the various receptor subtypes are located on different chromosomes.
Separate subtypes have been identified in human tissue. Research has so far failed to identify the genetic evidence of the subtypes, and it is thought that they arise from post-translational modification of cloned receptor types.[3]
An additional opioid receptor has been identified and cloned based on homology with the cDNA. This receptor is known as the nociceptin receptor or ORL 1 receptor.
References
1. Corbett AD, Henderson G, McKnight AT, Paterson SJ (2006).75 years of opioid research: the exciting but vain quest for the Holy Grail. Brit. J. Pharmacol.'147,' S153–S162
2. http://opioids.com/narcotic-drugs/chapter-3.html
3. Fries, DS (2002). Opioid Analgesics. In Williams DA, Lemke TL. ''Foye's Principles of Medicinal Chemistry'' (5 ed.). Philadelphia: Lippincott Williams & Wilkins. ISBN 0-683-30737-1.
See also
★ Opioid antagonist
★ http://opioids.com/receptors/index.html
External links
★ IUPHAR GPCR Database - Opioid Receptors
★
★ Calculated spatial position of mu-opioid receptor in the lipid bilayer, inactive state with antagonist and active state with agonist
This article provided by Wikipedia. To edit the contents of this article, click here for original source.
psst.. try this: add to faves
