Author Topic: Re: Mesembrine (the active alkaloid of the Kanna plant-Sceletium)  (Read 123 times)

fresh1

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Re: Mesembrine (the active alkaloid of the Kanna plant-Sceletium)
« on: April 29, 2012, 04:31:33 AM »

   Mesembrine is an alkaloid present in Sceletium tortuosum (kanna). Mesembrine acts as a serotonin reuptake inhibitor. Mesembrine may contribute to the antidepressant effects of kanna.  A study found it to be a potent inhibitor of phosphodiesterase 4 (PDE4)   
 
      Active ingredient: the indole alkaloid 'Mesembrine'      http://www.freebase.com/view/en/mesembrine
   
      IUPAC name
                       (3aS,7aR)-3a- (3,4-dimethoxyphenyl)- 1-methyl-2,3,4,5,7,7a- hexahydroindol-6-one           
         
                           http://www.sceletium.org/sceletium-review-article.html

                           many folks say the same thing  'it's a keeper and worth doing again'
                            http://www.erowid.org/experiences/exp.php?ID=87706 . .
       
               apparently its  a bit like low dose mdma and seems to go very well with grass
                           http://www.erowid.org/experiences/exp.php?ID=65389
   
  My partner and I have both noted some similarities between Kanna and MDMA: in many ways, the Kanna high is like a very small dose of extremely clean MDMA. The empathogenic connection isn't nearly so strong, but neither is the tooth-grinding
       
 Conclusion:
    It may be concluded from the evidence presented that 'kougoed' and the Sceletium alkaloids show no hallucinogenic properties, but rather are narcotic-anxiolytic. This and their strongly synergistic interaction with other psychomimetics indicates a serious need for thorough pharmacological investigations. Foremost amongst these would be toxicity and mode of action, such as receptor binding. A recent study has shown that although mesembrenone was considerably less toxic to mouse fibroblasts that twenty-one amaryllidaceous alkaloids tested in vitro, it was moderately effective against cancer cells (Weniger et al., 1995).

According to the observations of plant gatherers, plants of Sceletium tortuosum and Sceletium strictum are becoming increasingly scarce. Dwindling natural populations point to possible overexploitation. A resurgence of interest in Sceletium alkaloids will serve to encourage cultivation of these plants, either in the natural habitat, botanical gardens, or elsewhere, especially as these taxa are reputedly easily grow

 enjoy

 f1  ;)
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Sydenhams chorea

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Re: Re: Mesembrine (the active alkaloid of the Kanna plant-Sceletium)
« Reply #1 on: April 29, 2012, 01:46:47 PM »
I have a three year old Sceletium joubertii plant that was grown from seed. Very beautiful and easy to grow, but the kougoed I've prepared from some of the fermented plant material isn't very potent. I think S. tortuosum is to be preferred.
It is perhaps the narcotic. Hyoscine affects certain people very oddly. One cannot be sure. Sometimes, these cases take strange forms. The victim becomes in a sense, 'mediumistic', a vehicle for all the intangible forces in operation around her.

Vesp

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Re: Re: Mesembrine (the active alkaloid of the Kanna plant-Sceletium)
« Reply #2 on: April 30, 2012, 03:04:49 AM »
Also lets not forget that varieties of Ice plant (Delosperma) contain this compound as well as DMT related alkaloids and oxalates - and this plant is often easier to grow and easier to get.
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myCH3

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Re: Mesembrine (the active alkaloid of the Kanna plant-Sceletium)
« Reply #3 on: April 30, 2012, 05:08:12 PM »
I've heard Delosperma cooperi is a good one that grows like a weed and contains some o that good stuff  8).   Vesp do you know any species that contain both mesembrine and dmt?  bet that would be quite the addition to an ayahuasca brew. 

I've really enjoyed kanna the times I have tried it, I found it to be the loveliest of marijuana potentiators and on top of that It gets rid of  any tired groggy feelings leaving you with just a relaxed energetic high when their mixed and that sweet taste so good.  Its sad to hear that it may be being over exploited but I could believe it what with the legal highs industry having found out about it.  Cool to hear their easy to grow, gonna go find my self some Sceletium tortuosum seeds and see if I cant have myself another little nice addition to my indoor garden. 

Tsathoggua

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Re: Re: Mesembrine (the active alkaloid of the Kanna plant-Sceletium)
« Reply #4 on: April 30, 2012, 06:08:54 PM »
Tsathoggua found S.tortuosum absolutely worthless, if not utterly so, then close to. Tastes like salty shit (
not that toady has ever tasted shite, salted or otherwise, nor has he ever any plans to. He is perfectly content to leave the diarrhea-gargling to politicians :P), noxious beyond belief to insufflate. He would bioassay the purified, recrystallized alkaloid fraction from S.tortuosum, working his way up from 1mg etc. Otherwise, he would sure enough add the plant to an entheogen garden, but the chances of him taking any are about the same as him taking a HNO3 enema, whilst sticking his cock into a wasps nest, pouring petrol over the entire thing, and flicking matches at random.

His experience was slightly unpleasant, he doesn't recall the dose, it was years ago. He would be happy to add it to an entheogen garden, and cultivate it,as he said, but the same goes for belladonna (which he just planted actually, along with some apple of peru)

Pretty useless stuff IMO. And do NOT insufflate it!!!!!!!!!!!!!!!!!!!
Its like having a welding torch rammed up your japs' eye, twisted sideways and ripped the fuck right out.       

IIRC it contains an SSRI component, so adding it to an aya brew could lead to a hypertensive crisis, or 5HT syndrome. Serotonin syndrome is NASTY, happened to my stalker/(sadly)ex-GF...she literally thought she was going to die that night.
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Vesp

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Re: Mesembrine (the active alkaloid of the Kanna plant-Sceletium)
« Reply #5 on: April 30, 2012, 08:58:48 PM »
Quote
Vesp do you know any species that contain both mesembrine and dmt?  bet that would be quite the addition to an ayahuasca brew. 

It would be a quote the addition indeed - likely hurting you very badly and maybe leading to death.  Mixing a MAOI with an SSRI (mesembrine) leads to serotonin syndrome and I am sure other issues as well.
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fresh1

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Re: Re: Mesembrine (the active alkaloid of the Kanna plant-Sceletium)
« Reply #6 on: May 01, 2012, 08:41:52 AM »
 Sceletium extracts may also contain quite high levels of  'oxalates' also,  and although they are a common compound occurring in many plants, it can cause some health issues if overdone, i.e kidney stones :P

"Although unusual, consumption of oxalates (for example, the grazing of animals on oxalate-containing plants such as greasewood or human consumption of Sorrel) may result in kidney disease or even death due to oxalate poisoning. The presence of Oxalobacter formigenes in the gut flora can prevent this. Cadmium catalyzes the transformation of vitamin C into oxalic acid and can result from smoking heavily, ingesting produce tainted with Cd or from industrial exposure to Cd."
 
       wiki   http://en.wikipedia.org/wiki/Oxalate
« Last Edit: May 01, 2012, 08:47:39 AM by fresh1 »
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myCH3

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Re: Mesembrine (the active alkaloid of the Kanna plant-Sceletium)
« Reply #7 on: May 01, 2012, 06:46:38 PM »
Quote
Vesp do you know any species that contain both mesembrine and dmt?  bet that would be quite the addition to an ayahuasca brew. 

It would be a quote the addition indeed - likely hurting you very badly and maybe leading to death.  Mixing a MAOI with an SSRI (mesembrine) leads to serotonin syndrome and I am sure other issues as well.

Oh snap I had completely forgotten that it was an ssri Yeah definitely would be a horrible idea to mix with an MAOI.  super dumb statement on my part.  What effects would an SSRI have on smoking dmt? would a "jungle spice" (full alkaloid extract) made from a plant that contains both be any good?  mesembrine has that super nice PDE4 inhibitor that keeps you from feeling tired.  or am I being dumb again and don't ssri's cancel out hallucinogens?
« Last Edit: May 01, 2012, 06:57:09 PM by myCH3 »

fresh1

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Re: Mesembrine (the active alkaloid of the Kanna plant-Sceletium)
« Reply #8 on: May 03, 2012, 05:35:21 AM »
Quote
What effects would an SSRI have on smoking dmt? would a "jungle spice" (full alkaloid extract) made from a plant that contains both be any good?  mesembrine has that super nice PDE4 inhibitor that keeps you from feeling tired.  or am I being dumb again and don't ssri's cancel out hallucinogens?

 In a word "yes"  :o   with "most definitely" added for caution  :P

   Most hallucinogens have a large effect on the "seretonergic pathways"--  MOAI's inhibit the enzyme which breaks down the amongst other things, the tryptophans in DMT,
 
   MOAI's  virtually stop the 'first pass' (and then later) metabolizing and degredation several substances (including seretonin and tryptophans)  which basically means that when you eat the alkaloid containing substance, its not so readily destroyed by this enzyme in your gut, but also once it's inside you it will take longer to be metabolized

    Most MOAI's are "irreversible" meaning once they 'knock out' the enzyme it stays depleted, until the body replaces it which takes a few weeks.  So once you have taken some MOAI's, even just one dose, your system will no longer break down these substances, including seretonin, as quickly as before
   
    This is how they potentiate drugs like DMT and Psylocin/cybin (both of which have major seretonergic effects)

  Taking a MOAI an hour or more before smoking DMT will make the trip last ime about 30-40mins with a good hit/dose rather than the standard 5-10mins -- and will continue to do so for a few weeks :)
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Tsathoggua

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Re: Re: Mesembrine (the active alkaloid of the Kanna plant-Sceletium)
« Reply #9 on: May 03, 2012, 12:14:44 PM »
Depends on the MAOI, plenty are reversible, such as the harmala alkaloids and moclobemide, they are what is known in the pharmacology trade as 'RIMAs' I.e 'reversible inhibitors of monoamine oxidase (type) a

There are two forms of MAO in humans, MAOa and MAOb, MAO-a is present in the periphery, and preferentially guzzles up (nor)adrenaline and serotonin, whilst the one present in the brain is MAOb, which has a bit more in the way of good taste, and prefers to munch up dopamine. (although on reading the wiki article, which contradicts what I have learned elsewhere, both types attack DA equally, and MAO-b preferentially trashes phenethylamine and trace amines, the endogenous ligands for the TAARs (such as for instance, the iodothyronamines, and quite possibly DMT) I thought I should include this to make sure no misinformation is given. Although of course, wiki isn't the best source in the world...but that info should not go unposted IMO.

Although in the same article, it then goes on to state, that MAO-b DOES preferentially chomp up DA and phenethylamine (and of course it still deaminates trace amines)



An example of the former (noncompetitive, I.e irreversible, competitive inhibitors compete with the enzyme's substrate, when it is 'really needed' to put it in simplistic terms, the subsrate can kick off the inhibitor to be broken down, noncompetitive inhibitors, also sometimes known as suicide inhibitors bind, and stay bound, meaning that when for instance, acetylcholine encounters the pharmaceutical drug galantamine, a competitive acetylcholinesterase inhibitor, to some degree, it gets pushed off AChE allowing the acetylcholine to be broken down and then recycled, whereas with a noncompetitive inhibitor such as tabun (early nerve agent, development wise, sarin (a G-series nerve agent), VX (a V-series nerve agent), GV, a hybrid between the G and V series, and the oh-so-bastardly new novichok (meaning 'newcomer' in russian, and pronounced 'no-wee-shok'), newer, 4th generation binary agents that are at least 10x the lethality of VX, and are solids, dispersed as powder, possibly as suspensions in volatile solvents, etc. depending on what kind of battle tactics those vicious russki buggers are using at the time, those are all noncompetitive, irreversible acetylcholinesterase inhibitors, and are highly toxic (no shit sherlock, thats the entire point of most chemical weapons :P:D:P)

As an overall, general rule of thumb, although I am sure there are exceptions, enzyme inhibitors containing reactive functional groups are likely to turn out to be noncompetitive. such as that nasty looking hydrazine in phenelzine, and isoniazide for example or that rather strained cyclopropane  ring in tranylcypromine. If such a reactive functional group is present in an enzyme inhibitor, that can end up forming a covalent bond with its target enzyme, an irreversible, noncompetitive inhibitor is pretty likely. And these are also likely of far greater toxicity in vivo than are competitive (reversible) inhibitors. With such a covalently bonding inhibitor the body has to synthesize new enzyme before the work of said enzyme can begin again. This takes time, explaining the long washout period between taking something like isoniazid and either being put on other antidepressants, or eating certain foods, I.e those are high in the dietary pressor amine tyramine, normally chopped a new arsehole by MAO.
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fresh1

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Re: Mesembrine (the active alkaloid of the Kanna plant-Sceletium)
« Reply #10 on: May 05, 2012, 06:09:22 AM »
 thanx toady that's some interesting stuff. 8) quite complex but  :P

I was led to believe the preponderance of Rxd  MOAI's are the 'non-competitive' type, possibly becoz IIRC this type were the first to be made and also becoz their effects are meant to be maintained it's not a bad thing as such :-\

   fresh has only had MAOI's twice both times with DMT but was wondering if anyone had ever experienced taking MDx after an MAOI? 
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Tsathoggua

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Re: Re: Mesembrine (the active alkaloid of the Kanna plant-Sceletium)
« Reply #11 on: May 06, 2012, 07:26:21 PM »
seretonin syndrome. gag. puke. twitch, die.
Nomen mihi Legio est, quia multi sumus

I'm hyperbolic, hypergolic, viral, chiral. So motherfucking twisted my laevo is on the right side.