Antinociceptive effect of 7-hydroxymitragynine in mice: Discovery of an orally active opioid analgesic from the Thai medicinal herb Mitragyna speciosa

Matsumoto, Kenjiro; Horie, Syunji; Ishikawa, Hayato; Takayama, Hiromitsu; Aimi, Norio; Ponglux, Dhavadee; Watanabe, Kazuo

doi:10.1016/j.lfs.2003.09.054

Cited by 195 publications

(179 citation statements)

References 23 publications

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“…We have found multiple packaged commercial Kratom products to contain artificially elevated concentrations of 7-hydroxymitragynine, the alkaloid responsible for M. speciosa's concerning mechanistic and side effect profile [20][21][22]. The amount of 7-hydroxymitragynine exceeded that found in naturally occurring material by up to 500 %.…”

Section: Resultsmentioning

confidence: 99%

“…Accounting for roughly 2 % of the plant's alkaloid content [16], 7-hydroxymitragynine is an opioid receptor agonist (like mitragynine) but demonstrates potent mu and kappa receptor selectivity [12]. This alkaloid is the major contributing factor for Kratom's analgesic properties, demonstrating opioid receptor affinity up to 17 times that of morphine [20][21][22]. It may also contribute to problematic Kratom use, which has been reported numerous times in the literature [10,[23][24][25][26].…”

Section: Introductionmentioning

confidence: 99%

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Suspected Adulteration of Commercial Kratom Products with 7-Hydroxymitragynine

et al. 2016

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Introduction Kratom (Mitragyna speciosa), a plant native to Southeast Asia, has been used for centuries for its stimulant and opium-like effects. Mitragynine and 7-hydroxymitragynine, exclusive to M. speciosa, are the alkaloids primary responsible for Kratom's biologic and psychoactive profile, and likely contribute to its problematic use. We purchased several commercially available Kratom analogs for analysis and through our results, present evidence of probable adulteration with the highly potent and addictive plant alkaloid, 7-hydroxymitragynine. Methods A simple and sensitive LC-MS/MS method was developed for simultaneous quantification of mitragynine and 7-hydroxymitragynine in methanol extract of marketed Kratom supplements. Results We found multiple commercial Kratom products to have concentrations of 7-hydroxymitragynine that are substantially higher than those found in raw M. speciosa leaves. Conclusions We have found multiple packaged commercial Kratom products likely to contain artificially elevated concentrations of 7-hydroxymitragynine, the alkaloid responsible for M. speciosa's concerning mechanistic and side effect profile. This study describes a unique form of product adulteration, which stresses the importance of increased dietary supplement oversight of Kratom-containing supplements.

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Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Suspected Adulteration of Commercial Kratom Products with 7-Hydroxymitragynine

et al. 2016

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“…The opioid-like effects of analgesia [8] and reduced gastrointestinal motility [1,10] are attributed to mitragynine, which acts at μ-and δ-opioid receptors [8]. 7-Hydroxymitragynine shows a potent analgesic effect in rats even superior to morphine [11] and acts mainly at μ-opioid receptors and to a lesser extent at κ-opioid receptors. Corynantheidine also binds at μ-receptors but acts as a functional antagonist since it does not activate this receptor [8].…”

Section: Discussionmentioning

confidence: 99%

Intrahepatic Cholestasis Following Abuse of Powdered Kratom (Mitragyna speciosa)

et al. 2011

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“…Mitragynine is a known agonist of multiple receptors including the opioid receptors μ, κ, δ, as well as adenosine2a, postsynaptic alpha-2, dopamine-2s, and various serotonin receptors [2,5]. Additionally, 7-α-hydroxymitragynine, a minor constituent of the plant, has been found to be a more potent opioid agonist than both mitragynine and morphine and is thought to contribute substantially to the clinical effects of kratom when ingested orally [6]. The modulation of opioid receptors and/or presynaptic adrenergic receptors may explain decreased mental status as observed in our case, although the mechanism for seizure activity remains undefined.…”

Section: Discussionmentioning

confidence: 99%

Seizure and Coma Following Kratom (Mitragynina speciosa Korth) Exposure

Nelsen

Lapoint

Hodgman³

et al. 2010

J. Med. Toxicol.

143

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Reports of toxicity secondary to Kratom are rare and lack of diagnostic testing in human specimens has prevented confirmatory explanation of observed clinical effects. We present a novel case of serious human toxicity following Kratom use confirmed via quantitative analysis of urine by high performance liquid chromatography coupled to electrospray tandem mass spectrometry. A 64 year-old male was witnessed to have a seizure at home following kratom consumption. Upon arrival to the emergency department (ED), the patient was unresponsive. While in the ED, the patient sustained a second seizure. He was intubated to protect his airway. The remainder of his hospital course was uneventful. A urine specimen was collected shortly after admission and sent for analysis. The mitragynine concentration in the urine was 167±15 ng/ml. We report a rare case of Kratom toxicity characterized by a seizure and coma confirmed by urinary analysis of mitragynine by high performance liquid chromatography coupled to electrospray tandem mass spectrometry. The proposed mechanism for this reaction is unclear but suggested mechanisms include adenosine binding or stimulation of adrenergic and/or serotonergic receptors similar to tramadol.

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Antinociceptive effect of 7-hydroxymitragynine in mice: Discovery of an orally active opioid analgesic from the Thai medicinal herb Mitragyna speciosa

Cited by 195 publications

References 23 publications

Suspected Adulteration of Commercial Kratom Products with 7-Hydroxymitragynine

Suspected Adulteration of Commercial Kratom Products with 7-Hydroxymitragynine

Intrahepatic Cholestasis Following Abuse of Powdered Kratom (Mitragyna speciosa)

Seizure and Coma Following Kratom (Mitragynina speciosa Korth) Exposure

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