Stable dermorphin solution/solvent at room temp?

[MadWolfZX]

Just a quick question for those more familiar with the peptide dermorphin: Would it be probable that simple dissolvement of crystals into a 40-50 percent ethanol solution kept at room temp. would be stable for a length of time? I wanted an easy way to divide a 5mg crystalline form into oral doses of known quantity, however, storage of product is specified to be in -20C for 12 month stability, and in fact, item has to be overnighted and in a freeze pak for guaranteed stability. If I have to, of course, I will simply dissolve into distilled water, divide that into doses, and freeze them, but that is obviously not nearly as practical.

 

[MurphyClox]

1. This is a peptide; I'd strongly recommend storage at lower temperatures as labeled. Dissolve the solid in water, then divide the solutions into aliquots with each one containing enough for a single application, dry everything properly (high-tech would be lyophilisation; low-tech would be simple evaporation of the water and final drying over e.g. CaCl2) and then store in the freezer. Everything else will lead to a considerable loss of activity within short time.

2. As general rule of thumb, compounds are less stable in solution than as a solid. If you intend to store it in solution anyway, be sure to add sufficient EtOH (not denaturated one!!!) or you will have to face bacterial contamination soon.

3. ...errrrrr, did I read "oral doses"?


- Murphy

 

[MadWolfZX]

I very much appreciate your responses and will follow your advice. As for your no. 3 response...yes... oral dosing is what I intend. I prefer to avoid the needle when I can, as well, the instances I have read of IV use of this substance seem to result in very short duration compared to oral or sub-lingual usage. I am diabetic and require insulin injections, but again, I even hate this, so I'm not trying to expand on the things I inject.

I have two questions.

1. Is it suitable to use ordinary distilled water for my solution(such as the cheap distilled water from a local grocery)? Or do I need to use USP sterile water?

2. Can you recommend a cheap suitable small container that will not be damaged by expansion as the water solution freezes for my individual doses? I can only seem to find glass vials; I was looking for plastic as to minimize the chance of the container cracking, but seem to have a problem finding medical vials in plastic form. Or, do you think the glass vials would be okay(assuming say, only 5-10 percent filling of the vial)? I have to buy a large batch of them, and do not have any local sources to 'try/test' these medical vials beforehand... so I want to be sure what I buy is going to be suitable.

 

[atara]

2. As general rule of thumb, compounds are less stable in solution than as a solid. If you intend to store it in solution anyway, be sure to add sufficient EtOH (not denaturated one!!!) or you will have to face bacterial contamination soon.

Could one use bacteriostatic water (i.e. 0.9% benzyl alcohol) for this? As a corollary, is bacteriostatic water safe to ingest?

 

[Sturnam]

Oral doses won't work. Your stomach has peptidases to break apart peptides (read: dermorphin) very efficiently. Your saliva might too, but I can't remember my physiology on that.

Second: Are you completely sure dermorphin will dissolve in water? Most peptides are not soluble to any appreciable degree in water. Personally, I suggest DMSO. Dissolve in the pure DMSO first, then you can dilute it with water, saline, etc.

Glass vials can have liquid in them frozen and not crack I'm pretty sure. It's only a problem if it's 99% full, because then the liquid doesn't have anywhere to expand. But if you only fill 5-10%, it can just expand upwards. Why dont you test it out with some water? Tap is probably fine. But fill it up a little way, freeze it, and see if it's broken.

 

[MadWolfZX]

Oral doses won't work. Your stomach has peptidases to break apart peptides (read: dermorphin) very efficiently. Your saliva might too, but I can't remember my physiology on that.

I'm pretty sure most 'recreational' personal accounts of use were oral, with one or two being sub-lingual, and with the exception of one person, accounts were very positive.

I am all for discussion of potential superior ROAs except IV.

Second: Are you completely sure dermorphin will dissolve in water? Most peptides are not soluble to any appreciable degree in water. Personally, I suggest DMSO. Dissolve in the pure DMSO first, then you can dilute it with water, saline, etc.

The bio-research supply company I use lists the substance as water soluble in the material property sheet.

BTW, for other readers that might think trying dermorphin is a good idea, please realize this is ONLY a research substance at this point in the most literal meaning. Only animal studies have been tried so far, and nothing is known about negative side effects. Extended use by humans could cause neurological damage for all we know. I am a chronic pain patient that has great difficulty in obtaining needed meds from my doctor, so I am experimenting with this substance as a back up medication. Otherwise, I would not be considering this exercise.

 

[MurphyClox]

I asked about the oral route, because I share Sturnam's concerns about enzymatic breakdown. Peptides usually have a very low (if not zero) bioavailability orally for several reasons. In dermorphin's case, I read that BBB-passage was suggested to happen via active transport, because it enters the brain quite effectively despite its disadvantageous logP (clogP = -1.59; see Peptides 2010, 21, p.1390). Maybe something similar occurs in the intestines, too.

Bacteriostatic water could work for the preservation of the prepared solutions, but I'm no expert when it comes to sterility. I think as long as the samples are stored in the freezer, bacterial growth should be minimized to a sufficient extend. Glass vials are suitable for this job, too, just don't fill more than 50% and nothing will crack.

Could one use bacteriostatic water (i.e. 0.9% benzyl alcohol) for this? As a corollary, is bacteriostatic water safe to ingest?

In Europe it is an allowed food additive (E 1519), but also a known allergen. So, yes and no...


Peace! - Murphy

 

[MadWolfZX]

Now you have me worried I'm going to destroy my stuff.

I am not buying this from the standard cheap sources, as I only trust tried/true/credible bio-material supply companies used normally for research by credited institutions. So if prep this only for oral, and it turns out that oral DOES NOT work, I've wasted a healthy amount of dollars here folks!

So now I'm thinking the bacteriostatic water, disolving into many glass vials and freezing at -20C for storage. This way I have oral possibility and IV safe doses as well, if it is required ultimately to make this stuff do it's job. I have never tried to drink bacteriostatic water, so I have no idea if I have an allergy to it if used orally, though. Unfortunately this stuff comes in 5mg portion, and even though I have access to very sensitive scales, the supply company's material data sheet warns explicitly against weighing out from the supplied mass, and to only divide it AFTER dissolving completely into a solution.

So, folks, is the bacteriostatic water a sure bet here? Or is the benzyl alcohol have any potential to damage the peptide in extended storage?

 

[MurphyClox]

The benzylalcohol won't do any harm to this peptide. The only risk associated with that compound is allergenic potential (citing Wiki here).

- Murphy

 

[MadWolfZX]

Should subcutaneous injection, like I do or my insulin, be a feasible ROA for an opoid peptide? Or would one be required to use intravenous injection?

 

[MurphyClox]

Absolutely no idea.

 

[Sturnam]

Subcutaneous/Intramuscular should work well. It will bypass all the peptidases in the stomach. I've used a different opioid peptide SC/IM with success.

 

[MadWolfZX]

Thanks for the information everybody. I now have everything on order and will report back in a few weeks simply to let you know the ROAs that actually worked, if at all.

 

[raybeez]

If you put the sequence (YAFGYPS) into ExPASy PeptideCutter the results show that 2 out of the 3 major GI proteases (pepsin and chymotrypsin) will digest dermorphin. Interestingly the main salivary protease (endopeptidase) doesn't show up on the list.

I also ran it through a hydrophobicity calculator and it's slightly hydrophobic so solubility might be problematic

 

[jahh]

The posts i'v read on Dermorphin are very skeptical, some very dissapointed and others thought is was the greatest thing! How can these posts be so different?
makes me wonder how active this peptide really is!

Still waiting for more posts on this one.

 

[Sturnam]

I suspect the difference in opinion may be due to the strong selectivity for mu subtype. I have a few reasons to believe that mu agonism alone may not produce the kind of euphoria that a mixed mu/delta agonist can provide.

 

[MurphyClox]

Sounds much like the recent contradictory trip reports for 6-APB (...which were explained easily by the different batches that were sold, some actually containing the labeled drug, but in most cases not containing it but random bullshit instead).

- Murphy

 

[nuke]

I know someone who used to work with it and yes, you need to store the solutions at 4C or preferably -20C.

Ideally to make a sterile solution to inject from a stock you would autoclave a bottle of distilled water and then pour it and your product into a micron filter, solvate and strain it through into an autclaved injection vial, cap the vial with a sealing tool.

 

[MadWolfZX]

The posts i'v read on Dermorphin are very skeptical, some very dissapointed and others thought is was the greatest thing! How can these posts be so different?
makes me wonder how active this peptide really is!

Still waiting for more posts on this one.

I really feel bad reports are possibly the result of buying product from not-so-reliable sources. This is a fragile product and must be stored and transported under stringent conditions. This is why I used a more costly and difficult source; but it is a highly respected bio-supply company.

The material is stable at room temperate for at least 24 hours, so don't think it has to be frozen at all times. But it does need to be stored at -20C ideally.

I will report that so far, it is a very good painkiller with 4-6hours duration, comparable to hydrocodone and oxycodone in effect and duration used so far in both sublingual oral and subcutaneous injection methods. I still have yet to try IV, but will do so within the next week.

The material is completely soluble in water; it dissolves instantaneously upon contact.

Again, please do not assume this is a safe medication just because I have tried it. I could have already caused injury that has yet to show up; this is strictly an experimental exotic compound with virtually no human data and limited animal research data.

 

[MurphyClox]

I will report that so far, it is a very good painkiller with 4-6hours duration, comparable to hydrocodone and oxycodone in effect and duration used so far in both sublingual oral and subcutaneous injection methods. I still have yet to try IV, but will do so within the next week.

Would you be so kind and elaborate on the mentioned routes of application, please?
I'd like to read some details, in particular how the sublingual dosage was prepared and what time interval expended between application and feeling the first effects.

Thanks!

- Murphy