Antinociceptive action of mitragynine in mice: Evidence for the involvement of supraspinal opioid receptors

Matsumoto, Kinzo; Mizowaki, Maho; Suchitra, Thongpradichote; Takayama, Hiromitsu; Sakai, Shin‐ichiro; Aimi, Norio; Watanabe, Hiroshi

doi:10.1016/0024-3205(96)00432-8

Cited by 138 publications

(110 citation statements)

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“…Kratom has been utilized for thousands of years to enhance work productivity, cultural ceremonies, for medicinal purposes, and as a substitute for ethanol or opium [1][2][3][4]. Kratom contains a multitude of alkaloids, many of which are responsible for the biological effects of the plant [5]. Despite being criminalized in foreign countries with punishments of up to 70 years or more [1,6], Kratom use has become increasingly popular in the USA, where it is still legal to possess and consume in most states [7][8][9][10][11].…”

Section: Introductionmentioning

confidence: 99%

“…Mitragynine, a major indolecontaining constituent similar in structure to yohimbine [13], accounts for up to 66 % of the plant's alkaloid content [15,16]. It produces opioid-like effects predominantly via mu-and delta-opioid receptor agonism [5,13,17] in addition to modulation of the descending serotonergic and noradrenergic pathways [18]. In vitro characterization of mitragynine receptor binding in the central nervous system reveals the complexity with which Kratom acts (see Table 1) [10].…”

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: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Suspected Adulteration of Commercial Kratom Products with 7-Hydroxymitragynine

et al. 2016

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“…injection into mice was investigated. 30) Mitragynine (5.0-30 mg/kg, i.p. and 1.0-10 mg/mouse, i.c.v.)…”

Section: )mentioning

confidence: 99%

Chemistry and Pharmacology of Analgesic Indole Alkaloids from the Rubiaceous Plant, Mitragyna speciosa

2004

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The leaves of a tropical plant, Mitragyna speciosa KORTH (Rubiaceae), have been traditionally used as a substitute for opium. Phytochemical studies of the constituents of the plant growing in Thailand and Malaysia have led to the isolation of several 9-methoxy-Corynanthe-type monoterpenoid indole alkaloids, including new natural products. The structures of the new compounds were elucidated by spectroscopic and/or synthetic methods. The potent opioid agonistic activities of mitragynine, the major constituent of this plant, and its analogues were found in in vitro and in vivo experiments and the mechanisms underlying the analgesic activity were clarified. The essential structural features of mitragynines, which differ from those of morphine and are responsible for the analgesic activity, were elucidated by pharmacological evaluation of the natural and synthetic derivatives. Among the mitragynine derivatives, 7-hydroxymitragynine, a minor constituent of M. speciosa, was found to exhibit potent antinociceptive activity in mice.

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“…Mitragyna speciose preparations have been used by Malay and Thai natives for their opium and coca-like effects to enhance tolerance for hard work under the hot sun [Grewal 1932a,b;Suwanlert 1975;Tanguay 2011]. Studies have found this drug to have similar analgesic and antitussive properties as codeine [Matsumoto et al 1996]. …”

Section: Mitragyninementioning

confidence: 99%

Health hazard evaluation report: evaluation of law enforcement agents' potential exposures during a raid of a clandestine "spice" lab.

2016

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Antinociceptive action of mitragynine in mice: Evidence for the involvement of supraspinal opioid receptors

Cited by 138 publications

References 7 publications

Suspected Adulteration of Commercial Kratom Products with 7-Hydroxymitragynine

Suspected Adulteration of Commercial Kratom Products with 7-Hydroxymitragynine

Chemistry and Pharmacology of Analgesic Indole Alkaloids from the Rubiaceous Plant, Mitragyna speciosa

Health hazard evaluation report: evaluation of law enforcement agents' potential exposures during a raid of a clandestine "spice" lab.

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