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Thread: Kanna and its alkaloids

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    Kanna and its alkaloids 
    #1
    Correct me if i am worng but i believe i have seen figures showing mesembrine as the major alkaloid in kanna and being about 80% of tota alkaloids...

    now i have also seen most reports note that the pure compound lacks the overall texture of the whole herb and then i assume some other minor and likely related alkaloids are active...but then they would have to be assumably extremely potent themselves due to their low concentration ...

    any thoughts...?
     

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    #2
    From Wikipedia,

    Mesembrine is an alkaloid present in Sceletium tortuosum.[1] It has been shown to be an extremely potent serotonin reuptake inhibitor, active at dosages as low as 100μg (micrograms).[2] It has also been shown to be a PDE4-inhibitor.[3] Mesembrine may contribute to the antidepressant effects of kanna.

    References:

    1. Smith M, Crouch N, Gericke N, Hirst M (1996). "Psychoactive constituents of the genus Sceletium N.E.Br. and other Mesembryanthemaceae: a review". J Ethnopharmacol 50 (3): 11930. PMID 8691846.
    2. Pharmaceutical compositions containing mesembrine and related compounds. U.S. Patent 6,288,104 (PDF)
    3. Mesembrine - an inhibitor of PDE4 that follows structure-activity relationship to rolipram. [1]
    Selective Phosphodiesterase inhibitor
    If they're roughly as potent as mesembrine itself, I don't think that's unlikely. Is it known if there are any active phytosterols in it? Some of them are quite potent.
     

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    #3
    It may be so for mesembrine being the most potent SSRI, but it seems like this doesn't correlate at all with the psychoactivity of the plant -- 50-100mg mesembrine orally didn't have any effect in one report. So, either it gets killed by first past metabolism, or the effect is from a many of the different compounds in the plant.
     

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    #4
    and for those that find mesembrine to be active as a pure substrate it is alluded to not be the same effect as the whole herb or extract...and remarks usually lean to be somewhat inferior in overall quality of experience for the monomer

    i doubt though there are any psychoactive compounds other than alkaloids as there are no substrates i have seen that at all seem to bear any notable psychoactive potential besides the alkaloids
     

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    #5
    I've put Kanna up my nose several times and found it to be the most effective method. For those of you whom have put MDMA or 2C-B up your nose and thought it was bad. You don't know nothing. Fuck... I thought my eye was going to bleed from Kanna. And then I did it again. I'm smart. What else can I say?

    Peace,
    PL
     

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    #6
    yeah consensus is insufflation is best effect overall but also not all too pleasant in regard to your nasal cavity

    assumably the pharmacodynamics are best expressed this way and it is pretty obvious i think from reading around that mesembrine itself has piss poor oral bioavailability though i have never seen a documentation of it in a research paper oddly enough considering there are a slew synth papers on it but no one can do a freakin oral bioavailability assessment
     

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    #7
    Bluelighter Kenaz's Avatar
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    Quote Originally Posted by Pimp Lazy
    I've put Kanna up my nose several times and found it to be the most effective method. For those of you whom have put MDMA or 2C-B up your nose and thought it was bad. You don't know nothing. Fuck... I thought my eye was going to bleed from Kanna. And then I did it again. I'm smart. What else can I say?

    Peace,
    PL
    I found kanna works best between the cheek and gums: a little pinch provides a nice mood lift and energy lift. Snorting it may be more effective, but I'm not sure the agony is worth the extra boost.
     

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    #8
    I think it's probably destroyed pretty quickly orally if 200mg didn't do anything.

    I don't think phytosterols are too likely, but if the minor alkaloids have a potency anywhere near that of mesembrine, they could certainly play a large role.
     

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    #9
    it appears via subL mesembrine indeed expresses an effect at as low as 100ug and strong effects up into 5-10mg range via this route

    orally it is obviously very poor and may it appears somewhat on an individual;s metabolism as some seem to do reasonably well witthat route while other seem to get no real effect (both pure monomer and extracts)

    the minor alkaloids definitely play some role, but exactly what/how and how much is hard to ascertain
     

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