Central antinociceptive effects of mitragynine in mice: contribution of descending noradrenergic and serotonergic systems

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

doi:10.1016/s0014-2999(96)00714-5

Cited by 178 publications

(135 citation statements)

References 27 publications

Supporting

Mentioning

126

Contrasting

Unclassified

Order By: Relevance

“…Corynantheidine also binds at μ-receptors but acts as a functional antagonist since it does not activate this receptor [8]. In addition to the opioid receptor-mediated effects, there are conflicting data on the effect of mitragynine on α 2 and HT 2A receptors [12][13][14]. Kratom is often said to have coca-like effects (first described in 1932 [15]), but except the increased ability to work, there is little evidence for amphetamine-like effects and the possible pharmacological mechanisms remain unclear.…”

Section: Discussionmentioning

confidence: 99%

Intrahepatic Cholestasis Following Abuse of Powdered Kratom (Mitragyna speciosa)

et al. 2011

View full text Add to dashboard Cite

Section: Discussionmentioning

confidence: 99%

Intrahepatic Cholestasis Following Abuse of Powdered Kratom (Mitragyna speciosa)

et al. 2011

View full text Add to dashboard Cite

“…Thus, this simple indole alkaloid could also be derived from strictosidine or related compounds, such as common monoterpenoid indole alkaloids. 21) By fragmentation of the aglucone of strictosamide (33) or that of vincoside lactam (34), the C4 unit was eliminated and subsequent oxidation (aromatization) of the D-ring produced nauclefidine (31). To prove this structure, the total synthesis of 31 was carried out.…”

Section: )mentioning

confidence: 99%

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

2004

Self Cite

View full text Add to dashboard Cite

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.

show abstract

“…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%

“…In vitro characterization of mitragynine receptor binding in the central nervous system reveals the complexity with which Kratom acts (see Table 1) [10]. In regard to its antinociceptive actions, mitragynine is one third as potent as morphine and three times as potent as codeine [18,19].…”

Section: Introductionmentioning

confidence: 99%

Suspected Adulteration of Commercial Kratom Products with 7-Hydroxymitragynine

et al. 2016

View full text Add to dashboard Cite

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.

show abstract

Central antinociceptive effects of mitragynine in mice: contribution of descending noradrenergic and serotonergic systems

Cited by 178 publications

References 27 publications

Intrahepatic Cholestasis Following Abuse of Powdered Kratom (Mitragyna speciosa)

Intrahepatic Cholestasis Following Abuse of Powdered Kratom (Mitragyna speciosa)

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

Suspected Adulteration of Commercial Kratom Products with 7-Hydroxymitragynine

Contact Info

Product

Resources

About