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Drug info - Kratom alkaloids and their effects

Discussion in 'Kratom' started by Tripdisaster, Oct 7, 2012.

  1. Tripdisaster

    Tripdisaster Newbie

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    I found this very intresting article on Kratom.net which present the many alkaloids found in Kratom and their effects.




    List of alkaloids identified in Mitragyna speciosa Kratom, and their known or potential activity



    by Kratom Devotee

    Concentration percentages given come from different studies of alkaloid concentrations in Mitragyna speciosa- Kratom leaf. Some of the alkaloids given in this list still need to be studied more specifically in order to determine their potential activity.

    Ajmalicine (Raubasine): Cerebrocirculant, antiaggregant, anti-adrenergic (at alpha-1), sedative, anticonvulsant, smooth muscle relaxer. Also found in Rauwolfia serpentina.

    Akuammigine

    Ciliaphylline: antitussive, analgesic. < 1% of total alkaloid content found in Kratom leaf.

    Corynantheidine: μ -opioid antagonist, also found in Yohimbe. < 1% of total alkaloid content found in Kratom leaf.

    Corynoxeine: Calcium channel blocker. < 1% of total alkaloid content found in Kratom leaf.

    Corynoxine A and B: Dopamine mediating anti-locomotives. < 1% of total alkaloid content found in Kratom leaf.

    Epicatechin: Antioxidant, antiaggregant, antibacterial, antidiabetic,
    antihepatitic, anti-inflammatory, anti-leukemic, antimutagenic, antiperoxidant,
    antiviral, potential cancer preventative, alpha-amylase inhibitor. Also found in dark chocolate.

    9-Hydroxycorynantheidine: Partial opioid agonist

    7-hydroxymitragynine: Analgesic, antitussive, antidiarrheal; primary
    psychoactive in Kratom, Roughly 2% of total alkaloid content found in Kratom leaf.

    Isomitraphylline: Immunostimulant, anti-leukemic. < 1% of total alkaloid content found in Kratom leaf.

    Isomitrafoline: < 1% of total alkaloid content found in Kratom leaf.

    Isopteropodine: Immunostimulant

    Isorhynchophylline: Immunostimulant. < 1% of total alkaloid content found in Kratom leaf.

    Isospeciofoline: < 1% of total alkaloid content found in Kratom leaf.

    Mitraciliatine: < 1% of total alkaloid content found in Kratom leaf.

    Mitragynine: Indole alkaloid. Analgesic, antitussive, antidiarrheal, adrenergic, antimalarial,
    possible psychedelic (5-HT2A) antagonist. Roughly 66% of total alkaloid content found in Kratom leaf.

    Mitragynine oxindole B. < 1% of total alkaloid content found in Kratom leaf.

    Mitrafoline: < 1% of total alkaloid content found in Kratom leaf.

    Mitraphylline: Oxindole alkaloid. Vasodilator, antihypertensive, muscle relaxer, diuretic, antiamnesic, anti-leukemic, possible immunostimulant. <1% of total alkaloid contents in Kratom leaf.

    Mitraversine

    Paynantheine: Indole alkaloid. Smooth muscle relaxer. 8.6% to 9% of total alkaloid contents in Kratom leaf.

    Rhynchophylline: Vasodilator, antihypertensive, calcium channel blocker,
    antiaggregant, anti-inflammatory, antipyretic, anti-arrhythmic, antithelmintic. < 1% of total alkaloid content found in Kratom leaf.

    Speciociliatine: Weak opioid agonist. 0.8% to 1% of total alkaloid content of Kratom leaf, unique to Kratom.

    Speciofoline

    Speciogynine: Smooth muscle relaxer. 6.6% to 7% of total alkaloid contents of Kratom leaf.

    Speciophylline: Indole alkaloid. Anti-leukemic. <1% of total alkaloid contents of Kratom leaf.

    Stipulatine

    Tetrahydroalstonine: Hypoglycemic, anti-adrenergic (at alpha-2)
     
    Last edited by a moderator: Oct 26, 2012
  2. seaturtle

    seaturtle Titanium Member

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    The diverse spectra of alkaloids in Kratom is fascinating, and I wonder how many of the alkaloids are analogous to those found in opium and which are exclusive to Kratom. I feel like there must be some relationship between the 2 plants, and if that's the case their activity profiles should have similarities.

    The presence of alkaloids that act as immunostimulants, antioxidants, antileukemics, anti-inflammatory, antihypertensive, antiviral, etc may give Kratom medicinal uses far beyond opioid pain management, and may make Kratom a far better alternative to opium. Can't forget the stimulating effects of Kratom either, you get all the analgesic effects of opium but feel stimulated for 2-3 hours instead of passing out immediately and being useless. I hope research on Kratom continues to push forward, the world needs an opium alternative and Kratom seems like the prime candidate.
     
  3. Tripdisaster

    Tripdisaster Newbie

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    I is a good idea but if they use it medicinally, they will probably schedule it and everybody who currently use if for pain relief or anti-depressant, will need a prescription, also pharmaceutical company will create synthetic version of mytragynine and analogue of it and honestly even if synthetic product are more effective, they are also more addictive and create tolerance faster and I prefere taking a natural remedy rather than a synthetic product.

    But yes, Kratom is a very promising alternative to opium and opioids.
     
    Last edited by a moderator: Oct 26, 2012
  4. AMKR

    AMKR Newbie

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    25+ Kratom Alkaloids Identified; mechanisms of action for almost all of them

    [FONT=&amp]The alkaloid content of Kratom, Mitragyna speciosa leaves is about 0.5%, about half of which is mitragynine. An average leaf weighs about 1.7 grams fresh or 0.43 grams dried. Twenty leaves contain approximately 17mg of mitragynine. All leaves appear to contain mitragynine, speciogynine, paynanthine, and small quantities of speciociliatine. Oxindole alkaloids usually occur only in small or trace amounts.

    Kratom alkaloid content varies from place to place and at different times. Within each location, there is a quantitative variation in alkaloid content from month to month. While indole content seems to be fairly stable, oxindole content shows tremendous variation.

    Ajmalicine (Raubasine): Cerebrocirculant, antiaggregant, anti-adrenergic (at alpha-1),
    sedative, anticonvulsant, smooth muscle relaxer. Also found in Rauwolfia serpentina.

    Akuammigine: action, receptor site or percentage of total alkaloid content as of yet
    unknown.

    Ciliaphylline: antitussive, analgesic. < 1% of total alkaloid content found in Kratom
    leaf.

    Corynantheidine: μ -opioid antagonist, also found in Yohimbe. < 1% of total alkaloid
    content found in Kratom leaf.

    Corynoxeine: Calcium channel blocker. < 1% of total alkaloid content found in Kratom leaf.

    Corynoxine A and B: Dopamine mediating anti-locomotives. (I believe this means dopamine
    agonist, like miraplex or requip - or carbolevodopa, correct me if I'm wrong) < 1% of
    total alkaloid content found in Kratom leaf.

    (-)-Epicatechin: Antioxidant, antiaggregant, antibacterial, antidiabetic, antihepatitic,
    anti-inflammatory, anti-leukemic, antimutagenic, antiperoxidant, antiviral, potential
    cancer preventative, alpha-amylase inhibitor, Also found in dark chocolate.

    9-Hydroxycorynantheidine: Partial opioid agonist

    7-Hydroxymitragynine: Analgesic, antitussive, antidiarrheal; primary psychoactive in
    kratom; Roughly 2% of total alkaloid content found in Kratom leaf.

    Isomitraphylline: Immunostimulant, anti-leukemic. < 1% of total alkaloid content found in
    Kratom leaf.

    Isopteropodine: Immunostimulant.

    Isorhynchophylline: Immunostimulant. < 1% of total alkaloid content found in Kratom leaf.

    Isospeciofoline: < 1% of total alkaloid content found in Kratom leaf.

    Mitraciliatine: unknown mechanism of action and binding site. < 1% of total alkaloid
    content found in Kratom leaf.

    Mitragynine: Indole Alkaloid. Analgesic, antitussive, antidiarrheal, adrenergic,
    antimalarial, possible psychedelic (5-HT2A) antagonist. Roughly 66% of total alkaloid
    content found in Kratom leaf. (Could be the reason Kratom is very nice on the comedown of
    5-HT2A agonist psychedelics)

    Mitragynine oxindole B. < 1% of total alkaloid content found in Kratom leaf.

    Mitrafoline: < 1% of total alkaloid content found in Kratom leaf.

    Mitraphylline: Oxindole alkaloid. Vasodilator, antihypertensive, muscle relaxer, diuretic,
    anti-amnesic, anti-leukemic, possible immunostimulant. <1% of total alkaloid contents in
    Kratom leaf.

    Mitraversine: % of alkaloid content unknown as is the mechanism of action, and binding
    site.

    Paynantheine: Indole alkaloid. Smooth muscle relaxer. 8.6% to 9% of total alkaloid
    contents in Kratom leaf.

    Rhynchophylline: Vasodilator, antihypertensive, calcium channel blocker, antiaggregant,
    anti-inflammatory, antipyretic (fever reducer?), anti-arrhythmic, antithelmintic. < 1% of
    total alkaloid content found in Kratom

    Speciociliatine: Weak opioid agonist. 0.8% to 1% of total alkaloid content of Kratom leaf,
    also it's unique to Kratom.

    Speciofoline: % of alkaloid content unknown as is the mechanism of action, and binding
    site.

    Speciogynine: Smooth muscle relaxer. 6.6% to 7% of total alkaloid contents of Kratom leaf.

    Speciophylline: Indole alkaloid. Anti-leukemic. <1% of total alkaloid contents of Kratom leaf.

    Stipulatine: % of alkaloid content unknown as is the mechanism of action, and binding site.

    Tetrahydroalstonine: Hypoglycemic, anti-adrenergic (at alpha-2)

    Mitragyna speciosa Kratom alkaloid content varies quantitatively from geographical location, and from month to month, at different leaf harvest times, which has lead some teams (Shellard et al. in the 1970s) to conclude that there may be different geographical variants within the same species.

    [FONT=&amp]The Chelsea College Pharmacognosy Research Laboratories collected thirty samples of Kratom from Thailand, Malaysia, and Papua New Guinea between 1961 and 1970. All contained mitragynine, but also proved to have considerable variation in the alkaloid makeup. For red and green/ white leaved plants of Thailand, the most common alkaloidal profile was mitragynine, speciogynine, speciociliatine, paynantheine, traces of ajmalicine, traces of (C9) methoxy-oxindoles, and traces of other indoles.
    [FONT=&amp]
    Yet other Thai plants contained distinct alkaloidal profiles, some with many more alkaloids. In the Malay specimens, one contained mitragynine, speciofoline, and other indoles and oxindoles, while others contained mitragynine, ajmalicine, speciogynine, speciociliatine, paynantheine, traces of indoles, and (C9) methoxy-oxindoles. Specimens from Papua New Guinea contained mitragynine, speciogynine, speciociliatine, paynantheine, specionoxeine, and isospecionoxeine.
    [FONT=&amp]
    Prior to the late 1990’s, nearly all chemical studies of Kratom activity focused on mitragynine with the assumption that mitragynine was the main active alkaloid. With [FONT=&amp]7-hydroxymitragynine[FONT=&amp] now clearly identified out as the principal psychoactive alkaloid in Kratom, many elements of these studies need[FONT=&amp] to be revised.

    [FONT=&amp]Takayama et al. also found that Thai and Malay Kratom had the alkaloids mitragynine, speciogynine, speciociliatine, paynantheine and 7-hydroxymitragynine in common. In both Thai and Malay samples, mitragynine was the most abundant alkaloid, yet it made up 66% of the total alkaloid in the Thai Kratom sample, while it made up only 12% of the alkaloids from the Malaysian sample. The Malay Kratom sample had mitragynaline and pinoresinol as major components, as well as mitralactonal, mitrasulgynine and 3,4,5,6-tetradehydromitragynine.

    [FONT=&amp]Working with the leaves of Malay Mitragyna Kratom plants, the Houghton and Said team found 4 new types of indole alkaloids (corynantheidaline, corynantheidalinic acid, mitragynaline and mitragynalinic acid), in very young leaves.

    [FONT=&amp]These new alkaloids were reported as having an unusual skeleton, with a carbon function at the C14 position (in comparison with previously known monoterpenoid indoles), but another research team, lead by Pr. Takayama, later revised the structure of the mitragynaline and corynantheidaline alkaloids, showing that there was actually no substitution on the 14 position.

    [FONT=&amp]The variety of alkaloids discovered in diverse Kratom samples to this day still calls for further studies and experimentation, investigating their specific activity, effects and potential applications.
    [FONT=&amp]Through its makeup and tradition of use, it is clear [FONT=&amp]Mitragyna speciosa [FONT=&amp][FONT=&amp](Kratom) is much more than a simple opioid-like narcotic and mild stimulant. Many of the secondary chemicals found in [FONT=&amp]Mitragyna speciosa[FONT=&amp] (Kratom) are present in small yet appreciable quantities, and their synergetic role and activity in the general pharmacology of [FONT=&amp]Mitragyna speciosa[FONT=&amp] (Kratom)[FONT=&amp] is not yet fully understood, as thorough research has only just begun.
    ---------------

    This was just taken and reformatted from two websites - but I found it highly interesting and in-depth look into some of the lesser effects of the non-analgesic alkaloids. Had never seen them broken down like this. Kratom has a veritable treasure trove of positive effects - that Ive noticed but now can point to a specific alkaloid :cool:
     
    Last edited by a moderator: Apr 30, 2017
  5. Guppe

    Guppe Silver Member

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    Re: 25+ Kratom Alkaloids Identified; mechanisms of action for almost all of them

    Good post, lots of good info on the alkaloids in Kratom! Would you mind incluiding the source/s for your research? Thank you
     
  6. Impure157

    Impure157 Silver Member

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    Re: 25+ Kratom Alkaloids Identified; mechanisms of action for almost all of them


    While this is the first time I've ever heard the term 'anti-locomotive' I believe it's referring to dopamine antagonist action like antipsychotics. That's because dopamine agonists, as with other stimulants, commonly cause a dramatic increase activity and movement even to the point of dysfunction, known as psychomotor agitation so they would definitely not be 'anti-locomotive' under normal circumstances.
     
    Last edited by a moderator: Apr 30, 2017
  7. DiabolicScheme

    DiabolicScheme Titanium Member

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    The term anti-locomotive is a weasle word. It's confusing because we're not sure what exactly it refers to. Parkinson's disease (which involves uncontrolled movements) is caused by inadequate dopamine production in a specific region of the brain and is treated with l-dopa and agonists to control the symptoms. So in this case anti-locomotive could be referring to dopamine agonist activity.

    However your general dopamine agonists are generally stimulants which can induce activity in people so if it's anti-locomotive as it refers to stimulants then it would be an antagonist.

    This information here does explain blood pressure drops some people experience with Kratom (me). Would like to know the mechanism of action for why Kratom turns sedative in larger doses and is a stimulant in lower though.