Oxytocin Nasal Spray synthetic vasopressin and a heap of questions

[f13nd]

Ok, first off, I am not a highly skilled biochemist or neuropsychopharmacologist. I am here to ask questions so some of what I may say may be incorrect, thats the point, so constructive criticism is more than welcome, I'd like to understand what I may be missing/wrong about!

What I know is both from areas in my psych education, independent research, and I worked as a volunteer research assistant in the bio-psychology labs doing a study with Pitocin (oxytocin precursor) subcutaneously injected into pregnant rats. The lab I worked at was primarily a 5ht focused lab. In this study we were actually doing tests with prenatal variables that can correlate with pups being born with autism. From what I helped work on, the results showed positive that there is a correlation between oxytocin levels in a pregnant mother and the occurence of autism/autism related disorders in the offspring. The study was done examining the behaviors of the rats and then later we did protein stains and examined the hippocampus.

While doing these studies, I remember one of the Doctors saying that changes in levels of Vasopressin can effect levels of Oxytocin (I can't specifically remember if he said increases/decreases in one has a direct or indirect effect in increase/decrease of the other so I had to leave that vague maybe someone can correct me?)

One specific thing I remember him saying about Vasopressin was its levels were affected by alcohol consumption, which also can cause changes in levels of oxytocin, which could explain the sometimes more trusting and bonding feeling alcohol will give, alongside the lowered inhibition, I do notice that theres a significant difference between sedative/anxiolytic medication inhibition lowering and alcohols inhibition lowering. As I said in the beginning, I'm not an expert so please don't flame me to hell for not knowing things I realize alcohol has a different mechanism of action and altho it can be a gaba agonist its effects can be caused in a much different way while still having properties similar to for example, a benzo. Also, I heard MDMA causes some oxytocin release??? Is that true?

Heres the less biochemistry related question and more drug question

I recently have seen certain websites advertising "Oxytocin Nasal Sprays" as a supplement that is a cure for social anxiety and shyness, relationship and sexual problems, even as a medical treatment for such serious handicaps as autism
The deficits we found in the autistic group in the experiment had altered brain chemistry, damage, deficits, whatever you want to call it. It was prenatal problems that INVOLVED oxytocin during the developmental stages of their lives, but the changes/damage caused by the oxytocin levels in the mother...well...it could be that the pups produce too much and have no biological need for bonding, their bodies tell them they have met all needs. Or perhaps flooding of the mother with this caused a low/non functioning part of the brain that either makes or regulates oxytocin production/release? There are many factors that seem like they could contribute to the problems that lead to autism, not simply a single cause and effect... Also, problems with oxytocin levels during prenatal development may not have had any effect on the oxytocin levels, production, or parts of the brain that solely are responsible for oxytocin, but what about the indirect stimuli that can control it? Maybe damage to the thalamus or problems with 5ht or DA transmission basically just screwed up the entire neural networking that controls the connections between oxytocins release and the natural stimuli that would provoke it? Indirect alterations or damage to the oxytocin system may have occured due to changes in the way other neurotransmitters/peptides/nonpeptides interact.

So....Does anyone know of studies/have any thoughts on this as to whether merely introducing oxytocin into someones bloodstream or mucous membrane will cure shyness, anxiety, increase the bonding people feel, and really be a help with autisms effects on those who display its characteristics? I didn't think that increasing oxytocin by an external source would have any effect on anything, I thought it was moreso about the endogenous release or production of it and the stimuli that evoke it to be release, where its released, and its connection to the other neurotransmitters, basically a global effect that is more complex than simply increasing plasma levels of it....


Another site that is more of a nootropic type vendor was selling some type of Vasopressin drug that is synthesized and claims to significantly increase the formation and retention of memories for a certain amount of time after using it. The drug is called Desmopressin, and its used normally to remind your body to retain water and regulate body temperature, however when used in the way its being marketed apparently it has a short term effect on creating a more vivid and retainable capacity for memory formation. Anyone have any experience with this or know if its actually effective in any way? It seems interesting that theres a hormone that could make events you want to remember for lets say the next half hour become your brains #1 priority towards retaining, focusing on, etc.

 

[Hammilton]

Just to point out: Pitocin is not an oxytocin precursor. It's a brand name for oxytocin, as is Syntocinon. Generic is available as oxytocin, too, though.

 

[PsychedelicPeptide]

check PM f13nd.

Oxytocin can give an effect, and some people believe it to be enhanced on MDMA or perhaps other substances as you now mention, but it is short-lasting at best. Administration is hard to do effectively and a concentrated solution needs to be used. Many commercial nasal sprays are probably not concentrated enough (or perhaps have bad product, although oxytocin is supposed to be really stable if kept sterile) to really give you a good taste of what it can do. Some say it works best if you "get a lot up there real fast all at once" sort of like DMT.

However I doubt its use in the things you suggest. It has a very short half-life in vivo. That doesn't mean a longer-acting analog with greater specificity wouldn't have some potential though. =P

It's a strange peptide though that's for sure.

I'd look towards racetams and other small molecule nootropics (esp. vinpocetine) for memory enhancement if you want that.

Also many labs seem to have been focusing a lot on oxytocin receptor antagonists as of late (based on the patent literature) versus agonists. I kind of wonder what use they will have, if any. To me it sounds like they would have bad side effects and the agonists are what could potentially be utilized...

 

[Hammilton]

However I doubt its use in the things you suggest. It has a very short half-life in vivo. That doesn't mean a longer-acting analog with greater specificity wouldn't have some potential though. =P

I wouldn't expect any analogue of oxytocin to be very valuable. It's either gonna have problems with penetrability or short half life, both or, more likely, total ineffectiveness. IIRC, Vasopressin is very, very similar, but ineffective.

There are small molecule agonists of oxytocin receptors that are definitely better choices.

I actually see lots on the subject of oxytocin receptor agonists, especially small molecules. Antagonists are of more obvious benefit, though, for preventing pre-term labor and other obstetrical uses.

 

[PsychedelicPeptide]

LOL dude the reason you "make an analog" in the first place is to design it with properties that allow you to overcome the problems we speak of, ie, the short half-life, low bioavailability issues, non-specificity, etc.

Peptide chemists are becoming very good these days. I highly suggest that you not underestimate what their minds and the technical capabilities of solid phase synthesis will present. You will see what the future holds...

True there may be small molecule agonists with certain capabilities as well, however, small molecules often bring with them off-target actions and thus may not represent a better alternative to a peptide-based agonist. This is something I cannot speak much more of though as most of the small molecule data to this point remains locked behind the doors of certain pharm companies who are either holding on to it until the time is right to show it to everyone, or holding on to it in a desk under a stack of papers because they know it is junk. =P

 

[Hammilton]

Um... no. There is publised data on selective oxytocin receptor agonists, hell, it's been posted to this site. Actually, you've even posted in this thread. Nothing is locked up. Well, I'm certain there is more known but not yet public, but the same could be said about just about everything. Google turns up a good deal of information on the subject.

I'm not super familiar with peptides, but I'm not aware of any that have substantial half-lives or useful oral BAs. It seems that the only way to get it into the body efficiently requires special delivery mechanisms, on which there is lots of research.

The problem with analogues of oxytocin is that even slight modifications result in massive changes in effect. (one example). I don't doubt the ability of the synthesis. Finding a peptide that has high oral BA, decent half life AND maintains selectivity is incredibly unlikely considering this.

 

[Tsukasa]

http://www.bluelight.ru/vb/showthread.php?t=421810&highlight=oxytocin - This thread has some interesting info. Check out my post (second post in thread) on oxytocin.

If alcohol did release OXT, then it would probably be because of the ADH inhibition. Generally, when vasopressin levels tend to be low, oxytocin levels then to be high and vice versa. But then caffeine would also do this, because it also blocks vasopressin. I remember I used to get this strange feeling, often when a little caffeinated. I would imagine a soothing or reassuring stimuli, and suddenly get the urge to use the bathroom (vasopressin inhibition), but also came along with it positive feelings of love, belongingness, connectedness, and calmness. I haven't experienced it in a long time, because of all the drugs I do now, but that's how I remember it. It was probably from subsequent oxytocin release.

MDMA causes OXT release from stimulation of 5-HT1A and 5-HT2A stimulation from the serotonin release.

 

[Black]

But then caffeine would also do this, because it also blocks vasopressin. I remember I used to get this strange feeling, often when a little caffeinated. I would imagine a soothing or reassuring stimuli, and suddenly get the urge to use the bathroom (vasopressin inhibition), but also came along with it positive feelings of love, belongingness, connectedness, and calmness. I haven't experienced it in a long time, because of all the drugs I do now, but that's how I remember it. It was probably from subsequent oxytocin release.

sounds quite plausible. i know that feeling from caffeine and was wondering 'this must be a watered down version of the feeling mdma gives people' before i had tried the latter. there are indeed similarities and oxytocin could be responsible for that.

caffeine inhibiting vasopressine would also explain why some people experience a drop in blood pressure after drinking coffee...