DAMGO (
D-Ala2, ''N''-MePhe4, Gly-ol">small>D-Ala2, ''N''-MePhe4, Gly-olenkephalin) is a synthetic
opioid peptide
Opioid peptides are peptides that bind to opioid receptors in the brain; opiates and opioids mimic the effect of these peptides. Such peptides may be produced by the body itself, for example endorphins. The effects of these peptides vary, but th ...
with high
μ-opioid receptor
The μ-opioid receptors (MOR) are a class of opioid receptors with a high affinity for enkephalins and beta-endorphin, but a low affinity for dynorphins. They are also referred to as μ(''mu'')-opioid peptide (MOP) receptors. The prototypical Π...
specificity. It was synthesized as a biologically stable analog of
δ-opioid receptor
The δ-opioid receptor, also known as delta opioid receptor or simply delta receptor, abbreviated DOR or DOP, is an inhibitory 7-transmembrane G-protein coupled receptor coupled to the G protein Gi/G0 and has enkephalins as its endogenous lig ...
-preferring endogenous
opioid
Opioids are substances that act on opioid receptors to produce morphine-like effects. Medically they are primarily used for pain relief, including anesthesia. Other medical uses include suppression of diarrhea, replacement therapy for opioid us ...
s, leu- and met-
enkephalin
An enkephalin is a pentapeptide involved in regulating nociception in the body. The enkephalins are termed endogenous ligands, as they are internally derived and bind to the body's opioid receptors. Discovered in 1975, two forms of enkephalin ...
. Structures of DAMGO bound to the
µ opioid receptor reveal a very similar binding pose to
morphinans
Morphinan is the prototype chemical structure of a large chemical class of psychoactive drugs, consisting of opiate analgesics, cough suppressants, and dissociative hallucinogens, among others.
Structure
Morphinan has a phenanthrene core struct ...
.
Its structure is H-Tyr-
D-Ala-Gly-''N''-MePhe-Gly-ol.
DAMGO has been used in experimental settings for the possibility of alleviating or reducing opiate tolerance for patients under the treatment of an opioid. Such treatment on rats, adding DAMGO to morphine administration, showed that after seven days morphine had as much of an effect at the same dosage as the first day when administered together with DAMGO to the rats, whereas a separate control group of rats that were administered the same dosage of morphine over the course of the same week, but without DAMGO, displayed an increased tolerance and lessened analgesic efficacy toward the end of that week.
See also
*
DADLE
DADLE ( D-Ala2,_D-Leu5.html" ;"title="small>D-Ala2, D-Leu5">small>D-Ala2, D-Leu5Enkephalin) is a synthetic opioid peptide with analgesic properties. Although it is often considered a selective delta opioid receptor agonist, it also binds to the μ ...
*
DPDPE
*
Morphiceptin
Morphiceptin is a tetrapeptide (Tyr-Pro-Phe-Pro-NH2) that is a selective μ-opioid receptor agonist. It is derived from β-casomorphin and has over 1,000 times selectivity for μ- over δ-opioid receptors. When injected intracerebroventricular ...
References
{{Opioid receptor modulators
Synthetic opioids
Opioid peptides
Mu-opioid receptor agonists