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3C-PEP - powerful & selective DA stim, v. close to opioids

Well, it's up in the air whether cinnamoyl-cocaine is active or not; but things lean to it having gone under the radar being another active coca plant alkaloid:

i.e.

226px-Cinnamoylcocaine.svg.png


The styrene is definitely active, and more potent than cocaine by more than forty-fold

220px-Cocaine_analog_224e_alt.svg.png


I'd say highly possible, the naphthyl is your best bet just because of how long the linkage is getting.

As for the forward nitrogen, it's in a bit of a no-mans-land from previous SAR I've seen tested, but this for example:

254px-Cocaine_analog_223a.svg.png


...is a functional ligand.

Makes me think of the SoRI-20041 phenyltropane hybrid, if that nitrogen works:

PSvyIO.jpg
 
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Just a point-If something i 10000x as potent as cocaine, who CARES about crap solubility. Poor solubility only matters if the dose required takes some dissolving. Mere 100s of micrograms, solubility is beside the point is it not.

And for other examples of combined opioid/monoaminergics, how about diphenidine and methoxphenidine? those are definitely opioids, from bioassay alone. And being so close to lefetamine I find it highly unlikely that they will not have MAT or releaser activity. I'm very sensitive to presence/absence of opioids by now, considering how long I've had to be on pain meds. Could definitely feel an opioid 'signature' from those, especially if I''d taken some without my usual morphine/oxy.
 
Limpet_Chicken said:
Just a point-If something i 10000x as potent as cocaine, who CARES about crap solubility. Poor solubility only matters if the dose required takes some dissolving. Mere 100s of micrograms, solubility is beside the point is it not.

And for other examples of combined opioid/monoaminergics, how about diphenidine and methoxphenidine? those are definitely opioids, from bioassay alone. And being so close to lefetamine I find it highly unlikely that they will not have MAT or releaser activity. I'm very sensitive to presence/absence of opioids by now, considering how long I've had to be on pain meds. Could definitely feel an opioid 'signature' from those, especially if I''d taken some without my usual morphine/oxy.
Click to expand...

Not necessarily true. Many drugs have poor solubilities meaning that they are required to be bound to a counterion to improve solubility, otherwise they will suffer from ADME issues. For example, diclofenac freebase has a solubility of 2.37mg/L. If taken as a free base at normal dosage (50-100mg), it will take ages to be absorbed from the gut, which is why it is complexed with sodium to form a salt. Diclofenac has some polar groups on it, and even so it is this insoluble. It would not come as a surprise to me if some of these lipophilic compounds would have much lower solubilities. Then, even in dosages within the microgram range, absorption and solubility becomes an issue.
 
Limpet_Chicken said:
Just a point-If something i 10000x as potent as cocaine, who CARES about crap solubility.
Click to expand...

As aced said. With poor solubility it won't cross the BBB fast enough to get a *rush* no matter the amount of the dose taken and its respective in vitro potency.
 
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