Moredopamine
Bluelighter
edit: oops. I meant to post in ADD!
There is indeed one thread regarding this interesting molecule but it's four years old and the purpose of this thread is more about its antidepressant activity as shown in a very recent trial.
The only problem is that this is an endogenous compound and to my understanding one can't patent it for this reason... not to mention rampant opiophobia within the antidepressant industry.
It may also be of use to non-depressed people as enkephalins are heavily implicated in basal hedonic tone.
Human opiorphin protects enkephalins from degradation by human neutral endopeptidase and aminopeptidase-N and inhibits pain perception in various behavioral rodent models of pain via endogenous enkephalin-related activation of opioidergic pathways. In addition to pain control, endogenous opioid pathways are also implicated in the modulation of emotion-related behaviors. Thus, we explored the dose-dependent motivational responses induced by opiorphin using the forced swim test, the standard rat model of depression. In addition, to further understand the endogenous events triggered by opiorphin, we investigated the specific involvement of mu- or delta-opioid receptor-dependent pathways. In parallel, the locomotor activity test was used to detect possible sedation or hyperactivity. Here, we report for the first time that at 1-2 mg/kg i.v. doses, opiorphin elicited antidepressant-like effects by activating endogenous delta-opioidergic pathways, since that activation was reversed by the selective delta-opioid antagonist naldrindole (10 mg/kg i.p.). The antidepressive behavioral responses exerted by opiorphin are specific at systemically active doses. Treated-rats did not develop either hypo- or hyper-active responses in a locomotor test or amnesic behavioral response in the passive avoidance rat model. In addition, opiorphin did not induce either anxiolytic-, or anxiogenic-like responses in the conditioned defensive burying test. Taking the data together, we conclude that opiorphin is able to elicit antidepressant-like effects, mediated via delta-opioid receptor-dependent pathways, by modulating the concentrations of endogenous enkephalin released in response to specific physical and/or psychological stimuli. Thus, opiorphin or optimized derivatives is a promising single candidate to treat disorders that include both pain and mood disorders, particularly depression."
http://www.jpp.krakow.pl/journal/archive/0610/pdf/355_0610_article.pdf
(Fully study linked)
Of particular interest within the full study:
"the analgesic response induced by opiorphin, which
requires activation of endogenous μ-opioid pathways, is
comparable to that induced by the morphine μ-opioid agonist, in
terms of effective doses as well as of analgesic response, delay
and intensity. In addition, in contrast to exogenous μ-opioid
agonists such as morphine, opiorphin did not develop significant
abuse liability or antinociceptive drug tolerance when
chronically administered at equi-effective analgesic doses
(Rougeot at al., unpublished data)." (page one, intro)
If only one could somehow coax one's saliva to make proper use of this substance.
There is indeed one thread regarding this interesting molecule but it's four years old and the purpose of this thread is more about its antidepressant activity as shown in a very recent trial.
The only problem is that this is an endogenous compound and to my understanding one can't patent it for this reason... not to mention rampant opiophobia within the antidepressant industry.
It may also be of use to non-depressed people as enkephalins are heavily implicated in basal hedonic tone.
Human opiorphin protects enkephalins from degradation by human neutral endopeptidase and aminopeptidase-N and inhibits pain perception in various behavioral rodent models of pain via endogenous enkephalin-related activation of opioidergic pathways. In addition to pain control, endogenous opioid pathways are also implicated in the modulation of emotion-related behaviors. Thus, we explored the dose-dependent motivational responses induced by opiorphin using the forced swim test, the standard rat model of depression. In addition, to further understand the endogenous events triggered by opiorphin, we investigated the specific involvement of mu- or delta-opioid receptor-dependent pathways. In parallel, the locomotor activity test was used to detect possible sedation or hyperactivity. Here, we report for the first time that at 1-2 mg/kg i.v. doses, opiorphin elicited antidepressant-like effects by activating endogenous delta-opioidergic pathways, since that activation was reversed by the selective delta-opioid antagonist naldrindole (10 mg/kg i.p.). The antidepressive behavioral responses exerted by opiorphin are specific at systemically active doses. Treated-rats did not develop either hypo- or hyper-active responses in a locomotor test or amnesic behavioral response in the passive avoidance rat model. In addition, opiorphin did not induce either anxiolytic-, or anxiogenic-like responses in the conditioned defensive burying test. Taking the data together, we conclude that opiorphin is able to elicit antidepressant-like effects, mediated via delta-opioid receptor-dependent pathways, by modulating the concentrations of endogenous enkephalin released in response to specific physical and/or psychological stimuli. Thus, opiorphin or optimized derivatives is a promising single candidate to treat disorders that include both pain and mood disorders, particularly depression."
http://www.jpp.krakow.pl/journal/archive/0610/pdf/355_0610_article.pdf
(Fully study linked)
Of particular interest within the full study:
"the analgesic response induced by opiorphin, which
requires activation of endogenous μ-opioid pathways, is
comparable to that induced by the morphine μ-opioid agonist, in
terms of effective doses as well as of analgesic response, delay
and intensity. In addition, in contrast to exogenous μ-opioid
agonists such as morphine, opiorphin did not develop significant
abuse liability or antinociceptive drug tolerance when
chronically administered at equi-effective analgesic doses
(Rougeot at al., unpublished data)." (page one, intro)
If only one could somehow coax one's saliva to make proper use of this substance.
