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Psychotridine

L

LuxEtVeritas

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Interesting structure...any thoughts if it may act in a similar manner to you know what...???

Psychotridine

doi:10.1078/0944-7113-00025 How to Cite or Link Using DOI (Opens New Window)
Copyright © 2001 Urban & Fischer Verlag Published by Elsevier GmbH

Involvement of NMDA receptors in the analgesicproperties of psychotridine

T.A. Amadora, b, L. Verottac, D.S. Nunesd and E. Elisabetskya,

Available online 10 November 2004.

We have previously reported that the alkaloid extract of Psychotria colorata (Willd. ex R. & S.) Muell. Arg., had marked dose-dependent, opioid-like activity. Phytochemical analyses of P. colorata flowers and leaves identified several pyrrolidinoindoline alkaloids, including psychotridine. To further investigate the activity and mechanism of action of Psychotria alkaloids, we studied the effects of psychotridine on thermal and chemical models of analgesia. In the tail-flick model, psychotridine presents a dose-dependent analgesic effect; the effect is not reversed by prior treatment with naloxone. Psychotridine dose-dependently decreased capsaicin-induced pain. Performance in the rota-rod test showed that psychotridine does not induce motor deficits at doses effective in analgesia models. Psychotridine inhibited [3H]MK-801 (dizocilpine) binding to cortex membranes in a dose-dependent manner. Binding is completely abolished at 300 nM. The data rule out opioid activity, and the inhibition of capsaicin-induced pain and of radioligand binding strongly suggest the participation of NMDA receptors in psychotridine-induced analgesia.
 
This???
52617-25-1.png


Definitely a sweet structure. I never would have guessed it was active, much less as an NMDA antagonist
 
Whoa, what a trippy molecule (this guy is the jumbo shrimp of small molecules). I am guessing that it binds to the polypeptide (spermidine) site on the NMDA receptor, due to its pentameric structure, but I'm just pulling that out of my ass (since it did inhibit dizocilpine radioligand binding, it may very well just bind to the typical Mg++/PCP pore site).

I love the name of the molecule too--psychotridine...it has a nice ring to it.
 
If I read that paper correctly, it seems to say that it has a very short halflife (no significant effects after 40-60 minutes). If it's euphoric at all, and I suspect it might be as it's so short acting, it may be a decent legal replacement for ketamine. Tell ya what, though, I'd be nervous as hell being the first person to taste it!

Would love to be the third, though ;)
 
Ham-milton said:
If I read that paper correctly, it seems to say that it has a very short halflife (no significant effects after 40-60 minutes). If it's euphoric at all, and I suspect it might be as it's so short acting, it may be a decent legal replacement for ketamine. Tell ya what, though, I'd be nervous as hell being the first person to taste it!

Would love to be the third, though ;)
Click to expand...


i had you first on the list =D 8o
 
as may I. I wouldn't necessarily say its an incredible deal considering no one has used this substance and as such no one even knows if it is euphoric or not

Im confused. The study that the OP posted says that the analgesia was not reversed by naloxone. And then this study says it was:

http://www.informapharmascience.com/doi/abs/10.1076/phbi.34.4.267.13221?cookieSet=1&journalCode=phb

Strong opioid-like analgesic activity has been detected in alkaloids from Psychotria colorata (Willd ex R. & S.) Muell. Arg., used by Amazonian caboclos of Brazil as a pain killer. The present work was undertaken to study Psychotria brachypoda (Muell. Arg.) Britton in regard to the presence of alkaloids and potential analgesic activity. The leaf ethanol extract is rich in alkaloids and was evaluated for analgesia (mouse tail-flick), effects on body temperature and acute toxicity. In the tail-flick test the extract was active in a dose-effect pattern (i.p. 350 mg/kg comparable to 6 mg/kg of morphine) and the activity was reversed by naloxone. The body temperature decreased significantly. Sedation, blepharoptosis, but not loss of righting reflex were observed in acute toxicity test. These results show that the ethanol extract of P. brachypoda is rich in alkaloids with opioid-like analgesic activity. These data indicate the pertinence of isolating these alkaloids and further characterizing their pharmacological profile. Psychotria alkaloids can be regarded as potential templates for new analgesic compounds.
Click to expand...
 
I felt possibly placebo sedation when I tried it at night, and I definitely had muscle fatigue and a mild afterglow of some sort the day after taking it no matter what dose. But really no psychoactive effects ever showed themselves. Tried over 1000mg of isolate in one day, after feeling 'something' from as little as 15mg snorted.

This was all orally except for the 15mg snorted. It burns, so unless it has dramatic dissociative effects via the insufflated route it's really going to suck to snort high doses.
 
Smoke anyone?

Maybe adding some quinine/quercetin, harmala not sure how this is metabolized
 
Adding MAOIs to barely studied drugs is beyond stupid. I can't believe anyone with over 5 posts would suggest anything so stupid.
 
thats a sweet molecule, thanks for resurrecting this thread.

coolio probably didn't feel many effects from all his oral dosing due to first pass metabolism, of course. i bet IV is the way to go with this stuff!
 
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