Low Dose Oxytocin Antagonists Pre-bed For Receptor Upregulation

[Quality]

WARNING: THIS IDEA IS FOR PEOPLE WITH AUTISM SPECTRUM DISORDERS/ASPERGERS/AUTISM
WARNING: THIS IDEA IS NOT FOR PREGNANT WOMEN NOR DO I ADVICE IT

Theres been alot of interest these days in LDN (low dose naltrexone) to upregulate opioid receptors, given its mechanism I am wondering if this would also be possible with different type of receptor such as the title states above.
The idea would be similar to that of LDN (taken pre-bed) to cause upregulation/rebound while sleeping so you can profit of it the next day.

Im unsure which meds/chemicals are out there these days that have affinity for oxytocin receptors IN THE BRAIN.
Injections and pill form of agonists barely(if any at all) reach the brain.

All input welcome

 

[LeeLemonoil]

http://press.endocrine.org/doi/10.1210/en.2012-2253

http://press.endocrine.org/doi/10.1210/en.2011-1002

5α-androstane-3β,17β-diol positively regulates oxytocin neurons and signaling in the paraventricular nucleus of hypothalamus

It is a metabolite of both DHEA and DHT (via two different enzymes) - Androsterone and Pansterone sem very likely to me to increase it, along with supplemets taht increase the two required enzymes.
Also, Androsterone, Oxytocin or 3ß-Andiol (hard to source though) can possibly be used as an ethnaolic solution and used as an aerosol / inhalation agent ot reach the brain

 

[Quality]

Thanks for the input bud, appreciate it, however Im not interested in using pro-hormones.
Besides there are other hormones that increase oxytocin expression aswell, such as T3:
Thyroid hormone regulates the oxytocin gene. - PubMed - NCBI

Have to say its a pretty good find that you got there, especially since it states that it basically increases oxytocin in the hypothalamus, which is definatly the right area.

 

[LeeLemonoil]

And thak you for the T3 study provided which I id not know. Pls keep us updated on this idea of yours and if you identfy viable substances

 

[Quality]

Peripherally Administered Non-peptide Oxytocin Antagonist, L368,899®, Accumulates in Limbic Brain Areas: A New Pharmacological Tool for the Study of Social Motivation in Non-Human Primates
......... Therefore, the significance of endogenous OT in primate social behavior remains uncertain. Unfortunately peptide OT antagonists used successfully in rodent studies have two major disadvantages in primates: they are much less selective for OT than for vasopressin V1a receptors (Toloczko et al., 1997) and they must be administered intracerebrally because their penetration through the blood brain barrier is quite limited.

Peripherally Administered Non-peptide Oxytocin Antagonist, L368,899®, Accumulates in Limbic Brain Areas: A New Pharmacological Tool for the Study of Social Motivation in Non-Human Primates
watch this graph closely:

figure b.
males have LESS incomplete mount time on 1mg/kg of this oxytocin antagonist, less than the saline!
3mg/kg increases incomplete mount time though

same thing happens with female sexual behaviour figure b.
females have LESS refuse mount duration on 1mg/kg of this oxytocin antagonist, less than the saline!
3mg/kg increases refuse mount duration by basically doubling it compared to the saline

Seems not much hope by reading these few lines in an article, Im guess blood-brain-barrier penetration would be hard with oral route of any antagonist.


Regarding to melatonin (exogenous):

Melatonin - Scientific Review on Usage, Dosage, Side Effects | Examine.com

A 500mcg dose of melatonin appears to be able to increase secretion of oxytocin and vasopressin within 40-60 minutes of oral ingestion. However, 5mg has no significant influence on its own, yet it is able to suppress an increase in vasopressin normally seen with exercise.[113] Another study using 50mcg as well as 500mcg and 5mg noted that, in roughly the same population, 50mcg was not significantly different than placebo in regards to vasopressin and barely more significant in increasing oxytocin, while 500mcg significantly increased both neurohormones by 40 minutes after dosing, levels of which appeared to normalize by 150 minutes. A 5mg dose showed a suppressive effect once again.[114] This suppression was noted in a third study using 5mg nightly for 4 days.[115]



Low oxytocin and melatonin levels and their possible role in the diagnosis and prognosis in Iraqi autistic children. - PubMed - NCBI

Low oxytocin and melatonin levels and their possible role in the diagnosis and prognosis in Iraqi autistic children.

Dose dependant curve it seems, currently ordered Metergoline, once ive used that for a week or 4 I will try melatonin 500mcg DURING DAYTIME/LATE AFTERNOON.

 

[Such_Saturation]

I don't know that "antagonism for receptor upregulation" is very peatish...

 

[Quality]

I don't know that "antagonism for receptor upregulation" is very peatish...

errr and?

 

[Such_Saturation]

THIS IDEA IS FOR PEOPLE WITH AUTISM SPECTRUM DISORDERS/ASPERGERS/AUTISM

I don't know, it just seemed like a pretty generic intro. Just my input, though.

 

[Quality]

What are you trying to say with all this? does everything i post have to have a peat certified sticker on it.
Im looking for positive contributions.

 

[Such_Saturation]

Well it said all input welcome, but anyway oxytocin is very complex... I'd be wary of anyone who claims "antagonism of oxytocin receptor" because it sure as hell won't be just that. There's a reason why Ray Peat approaches things upstream where the molecules are more simple...

 

[Quality]

Well it said all input welcome, but anyway oxytocin is very complex... I'd be wary of anyone who claims "antagonism of oxytocin receptor" because it sure as hell won't be just that. There's a reason why Ray Peat approaches things upstream where the molecules are more simple...

Ok first of all, it is an IDEA as stated
Second of all, I gave warnings

And guess what, we live in a chemical world full of health disruptors and not everything can be fixed the simple way.
Thinking outside of the box has led to revolutions, following like a sheep certainly hasnt. my 2c.

 

[Such_Saturation]

Ok first of all, it is an IDEA as stated
Second of all, I gave warnings

And guess what, we live in a chemical world full of health disruptors and not everything can be fixed the simple way.
Thinking outside of the box has led to revolutions, following like a sheep certainly hasnt. my 2c.

Receptor theory is thinking outside the box?

 

[Quality]

Besides critisism do you have anything better to do with your life...?

 

[Such_Saturation]

Besides critisism do you have anything better to do with your life...?

I really want to see how it works out... I just wanted to give some warning...

 

[Dragon]

I don't know that "antagonism for receptor upregulation" is very peatish...

nor likely to last very long either.