DAMGO (
small>D-Ala2, ''N''-MePhe4, Gly-olenkephalin) is a synthetic
opioid peptide 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 ...
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 opioi ...
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
*
DPDPE
DPDPE ( 2,-5nkephalin) is a synthetic opioid peptide and a selective agonist of the δ-opioid receptor (DOR) which is used in scientific research. It was developed in the early 1980s and was the first highly selective agonist of the DOR to be d ...
*
Morphiceptin
References
{{Opioid receptor modulators
Synthetic opioids
Opioid peptides
Mu-opioid receptor agonists