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Opioids Any stimulant opiates known?

Tapentadol and pethidine both act as inhibitors on SERT and NET. As well as tramadol. Tapentadol has been the most potent at these sites I believe though but I'll keep looking for you =). Mitragynine is another but I believe that it kratom as a whole is responsible for the stimulant and opioid effects. There are too many compounds that interact and work together to say that mitragynine is the sole contributor. Over 20 alkaloids are psychoactive and while most of the kratom is mitragynine, the other compounds that are not as present in the leaf may very well play an important part in its effects.

sekio said:
pethidine / meperidine has some activity at DAT/NET i thought
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You thought quite correctly!
 
Mr.Deeds said:
Tapentadol and pethidine both act as inhibitors on SERT and NET. As well as tramadol. Tapentadol has been the most potent at these sites I believe though but I'll keep looking for you =). Mitragynine is another but I believe that it kratom as a whole is responsible for the stimulant and opioid effects. There are too many compounds that interact and work together to say that mitragynine is the sole contributor. Over 20 alkaloids are psychoactive and while most of the kratom is mitragynine, the other compounds that are not as present in the leaf may very well play an important part in its effects.



You thought quite correctly!
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Sometimes I really wish we had access to the separate compounds in Kratom and could experiment with taking them individually or mixing and matching rather than just having to take whatever amounts or in each strain.

Some people sleep fine on Kratom but I can't sleep unless it has literally worn off like 6-8 hours before bed cause of the stimulant effects, and that goes for Red Strains too.

I wonder if it would be possible to still get pleasurable effects from only taking the downer-parts of the compound and yet no be kept up at night.

That being said, I am equally if not more in love with Kratom's stimulant effects as its' opioid/downer effects.

i guess I'd say I just love both and how they mix so well, but I'd rather not be kept up at night when I dose too late.
 
An ethanol extraction of kratom would yield a somewhat decent amount of mitragynine back. It is more sedating than pure leaf IMO and leads me to believe that there are other compounds that add to the stimulant effects of the plant. You could try this out yourself and report your experience. That being said, tapentadol seems to be the closest to a stimulating opioid that I can find. I bet there are other novel opioids that I havent heard of yet that have SNRI and/or NDRI actions that are very speedy.
 
Just saw Pethidine mentioned above... I had a script for pethidine tablets years ago and they could be quite stimulating although felt horribly toxic in large doses. It's not prescribed anymore over here. I believe one of its metabolites, nor-pethidine is toxic and can cause Serotonin syndrome? Which (although i didnt know it at the time) I'm almost certain occured with me once...
 
Are you from across the pond? I'm in USA and its Schedule 2. It's not common to see a script anymore though. Mostly used at the hospitals now I believe.
 
Mr.Deeds said:
Are you from across the pond? I'm in USA and its Schedule 2. It's not common to see a script anymore though. Mostly used at the hospitals now I believe.
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Yeah mate, I'm from the UK. It used to be fairly common in hospitals up until the late 90s and early 00s especially for women in labour pain (where it has been replaced by IV diamorphine)... When I was scripted the pills I was on MXL (24 hour ER morphine pill) 240mg day wirh 50-100mg pethidine for breakthrough pain. This was quite an odd combination even back then and as with in the US, isn't used much now if at all...

Can anyone possibly verify what i mentioned above regarding the toxicity of nor-pethidine and risk of serotonin syndrome in overdose?
 
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Mr.Deeds said:
An ethanol extraction of kratom would yield a somewhat decent amount of mitragynine back. It is more sedating than pure leaf IMO and leads me to believe that there are other compounds that add to the stimulant effects of the plant. You could try this out yourself and report your experience. That being said, tapentadol seems to be the closest to a stimulating opioid that I can find. I bet there are other novel opioids that I havent heard of yet that have SNRI and/or NDRI actions that are very speedy.
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I don't think I'd necessarily do it, but how would you even do an ethanol extract?

And what do they normally prescribe tapentadol for?

Is it scheduled?
 
apocalypse_when said:
Yeah mate, I'm from the UK. It used to be fairly common in hospitals up until the late 90s and early 00s especially for women in labour pain (where it has been replaced by IV diamorphine)... When I was scripted the pills I was on MXL (24 hour ER morphine pill) 240mg day wirh 50-100mg pethidine for breakthrough pain. This was quite an odd combination even back then and as with in the US, isn't used much now if at all...

Can anyone possibly verify what i mentioned above regarding the toxicity of nor-pethidine and risk of serotonin syndrome in overdose?
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13646
 
^its a pdf file of an extensive overview of pethidine. I just got a screenshot of the serotonin syndrome warning so you dont have to download it.

There are a few case studies out there on pethidine alone causing serotonin toxicity as well I believe.
 
even methadone can be stimulating but when it fully kicks in the nods/sedation does
usually oxy and trams are stimulating ones
 
Mr.Deeds said:
Methadone has SNRI actions as well IIRC. Good catch there Hezman.
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Really? I didn't know that mate.. I knew it had NMDA antagonist properties but I wasn't of it having SNRI properties....

You've been schooling me today in this thread brother :)
 
apocalypse_when said:
Really? I didn't know that mate.. I knew it had NMDA antagonist properties but I wasn't of it having SNRI properties....

You've been schooling me today in this thread brother :)
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Yeah it has quite an interesting profile if you have the time look into it.

Sometimes I can get into the zone and am able to put the thoughts in my head down on paper so to speak. Its difficult for me to write or say what I am thinking, everything moves so fast in my brain that it gets all jumbled up. So today I guess I'm just getting lucky bud ?
 
When my tolerance is particularly low, the Thebaine in oxy and bupe(norbupe) is very stimulating for me and causes insomnia.
 
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