Highly potent delta antagonists?

[Sphinx (Afterlife)]

Highly meaning used in the nanograms/kilogram ratio.


No, not TIPP, or any of those others that are used at like 1-XX mcg/kg, talkin even more potent. Anyone?

TIPP is a peptide right, so preferably not a peptide delta antagonist, as im under the impression peptides are more sensitive to their environments and harder to deal with.


As for why delta antagonists? These have been shown to do good job of reversing fentanyl derivatives respiratory depressant effects, while not affecting antinociception.

 

[BilZ0r]

Well I don't know about dosings, but DMT-Tic is like a rediculously potent delta antagonist with a 10s of picomolar affinity... it's peptide-ey, but if you're IVing it, that shouldn't matter anway.

 

[Sphinx (Afterlife)]

Well I don't know about dosings, but DMT-Tic is like a rediculously potent delta antagonist with a 10s of picomolar affinity... it's peptide-ey, but if you're IVing it, that shouldn't matter anway.

Can peptides be dissolved in harsh solvents, and evapped out, without denaturing?

I know such a things prolly impossible to do with HGH or IGF-1 which are the sorts of peptides im used to working with, as they are extremely sensitive.

Is such true for ALL peptides? Or better yet, DMT-Tic?

Was more or less looking to cut such into such else personal use but material need be able to be dissolved in universal solvent that will also handle active and filler, both of which will not be peptides, and to my understanding peptides require much more maintained and controlled environments. So such a thing would seem impossible to do a with peptide unless I overestimate the fragility of such a peptide as Dimethyltyrosine.


Then onset of the delta anatagonist would also need be very rapid, so prolly very lipophilic. Otherwise be dead before the delta antag would even take effect, assuming the active was extremely fast onset.

 

[BilZ0r]

I don't have a clue, however HGH is a pretty big signalling peptide and IGF-1 isn't that small either... However I would have assumed that DMT-Tic, which in it's delta antagonist form is just a couple of amino acids, would be pretty fucking stable.

 

[edarrin]

Can peptides be dissolved in harsh solvents, and evapped out, without denaturing?

I doubt it just by the nature of denaturation. Likely very similar to the Hgh and IGF-1 mentioned.

 

[BilZ0r]

^ Yeah, but you can't really denature 3 amino acid peptides.

 

[Sphinx (Afterlife)]

Pardon the ignorance but what magnitude is picomoles?

Can such be converted to a weight? nanos? micros?


This DMT-Tic sounds interesting, especially this derivative H-Dmt-Tic-Gly-NH-CH(2)-Ph which says "whose spacer was longer by a single methylene group exhibited potent delta-antagonism (pA(2), 9.25) and very high mu-agonism (pEC(50), 8.57)"

What do those bolded values mean? Ive never seen such a value listing?

Taken from http://www.ncbi.nlm.nih.gov/entrez/...ve&db=PubMed&list_uids=11806723&dopt=Abstract


What the hells considered 'potent' and 'very high' to them?

 

[Smyth]

I'm more of a druggy myself, I dont hardly know of any peptides except for cyclosporin. Did you know that because an amino acid contains exactly that [an amino + an acid residue] that you have to use protecting groups to the max. It's all right in principle espcecially now that robots are actually being programmed to do the micro syntheses for you (no tedius labor). I'll have to skip on this since I have nothing to contribute, however the area looks quite fertile given that only a few AA's need to be linked to form bioactive residues.

 

[BilZ0r]

pico is 10 to the power of -12... so a 1000 times lower than nano (milli, micro, nano, pico, femto). A mole is a number of molecules. picomolar is talking about cencentrations as in moles a litre.

what does pA2 and pEC50 mean? p, means -log... so -log of the A2 value and the EC50 value... A2 is the apparent affinity, I forget how it's deduced... and EC50 is the concentration needed to get a 50 percent response. low p values mean high affinitie.s