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The Lack of Contribution of 7-Hydroxymitragynine to the Antinociceptive Effects of Mitragynine in Mice: A Pharmacokinetic and Pharmacodynamic Study
Erin C Berthold et al. Drug Metab Dispos. 2022 Feb.
“Concerns have been raised regarding the active metabolite of MTG, 7-hydroxymitragynine (7HMG), which has higher affinity and efficacy at µ-opioid receptors than MTG. Here we investigated the hotplate antinociception, pharmacokinetics, and tissue distribution of MTG and 7HMG at equianalgesic oral doses in male and female C57BL/6 mice to determine the extent to which 7HMG metabolized from MTG accounts for the antinociceptive effects of MTG and investigate any sex differences. The mechanism of action was examined by performing studies with the opioid receptor antagonist naltrexone. A population pharmacokinetic/pharmacodynamic model was developed to predict the behavioral effects after administration of various doses of MTG and 7HMG. When administered alone, 7HMG was 2.8-fold more potent than MTG to produce antinociception. At equivalent effective doses of MTG and 7HMG, there was a marked difference in the maximum brain concentration of 7HMG achieved, i.e., 11-fold lower as a metabolite of MTG. The brain concentration of 7HMG observed 4 hours post administration, producing an analgesic effect <10%, was still 1.5-fold higher than the maximum concentration of 7HMG as a metabolite of MTG. These results provide strong evidence that 7HMG has a negligible role in the antinociceptive effects of MTG in mice. SIGNIFICANCE STATEMENT: Mitragynine (MTG) is being investigated for its potential to aid in pain relief, opioid withdrawal syndrome, and opioid use disorder. The active metabolite of MTG, 7-hydroxymitragynine (7HMG), has been shown to have abuse potential and has been implicated in the opioid-like analgesic effect after MTG administration. The results of this study suggest a lack of involvement of 7HMG in the antinociceptive effects of MTG in mice.”
https://t.co/wrGVjmKg1U
https://t.co/k01T9wRhG8
@regulatecalnow Here is another one that contradicts that 7oh claim from 2022 from UF https://t.co/dZpYLoulP7
Great interview and important read. #KratomScience
Inteview with Pharmacokineticist and Kratom Researcher Dr. Abhisheak Sharma
“So everything, even we drink too much water, that is going to cause a problem. That same rule applies to here. So we have to control what we are taking, and how much should we take? Right? So that’s the concern. Up to a certain concentration, no problem. If you go beyond that concentration, in the long term, it is going to inhibit certain enzymes and if you have taken any other drug along with it, it will stay longer in your body…
I don’t remember if you have seen a news report on kratom in 2019 published in USA Today, with a broad headline written, “Herbal Drug Kratom Linked to Almost 100 Overdose Deaths, CDC States”. So if you read that, and you read the whole news, and you come down, and the last line written is “In most of the kratom-related deaths, fentanyl was also a cause of death.”
Now as a pharmacokineticist, if I look at what can happen, if I were to take mitragynine with fentanyl, what is going to happen? So according to the publications mitragynine is a PGP integrator. PGP [P-glycoprotein] is a transporter which cleans certain drugs out of our brain. It does the same thing with fentanyl. Right? So if I took fentanyl along with mitragynine, then what is going to happen? My brain is not going to clear that fentanyl. And it will stay there forever, and that’s the problem associated with this thing. So whenever we have been taking some herbs, it’s not always safe, so we always have to think about having drug interactions, and yes, mitragynine is prone to cause herbal drug interactions and we have to take it carefully if we are taking more than one drug.”
Read the entire interview-
https://t.co/dCQHIOcPq6
This isn't hype or marketing. The NIH, NIDA, NCATS, and University of Florida are scientifically researching mitragynine. Responsible advocates want science, facts, and transparency, not panic or prohibition. #KratomScience #Research
Kratom's complexity is often oversimplified. It's not just alkaloids; studies show over 80 compounds, including flavonoids and terpenoids, form its intricate chemical matrix. #KratomScience #Botanicals
Reducing kratom to a single molecule overlooks its complex function as a chemical system. Scientific evidence highlights its antioxidant and cell-protective properties, showing a broader biological role. #KratomScience #HerbalResearch
Missed last night? watch here
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#Johnshopkins is still looking for more participants. Go to https://t.co/FMyMpYJCAw
#kratomscience #science

https://t.co/PF60uCqlmK
#KratomScience Presentation at the UN CND
Thank you to everyone who participated and please watch and share!
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Watch the AKA kratom science presentation live at the UN CND this Friday 10 am CET (5am ET)
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https://t.co/h5apbXtFpx
Thank you to all #kratomadvocates who submitted testimonies in #northdakota You can watch the hearing online. The #AKA will be monitoring the bill closing and working hard to inform officials of #kratomscience and #kratomconsumerprotection
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Opportunity to participate in #KratomScience Research
Title: Johns Hopkins lab-based research study on kratom
The Johns Hopkins University School of Medicine is currently seeking volunteers for a research
study that will take place on our Baltimore, MD campus.
Adults who are using kratom on a regular basis may be eligible. The study is assessing the
effects from the kratom products that people use and any effects that may develop when kratom
use is discontinued. We are also assessing how kratom products are metabolized by the body.
People who may be eligible for this study are: 18 years of age or older, using kratom on a regular
basis, are willing to provide samples of the kratom product they regularly use.
Participation requires an in-person screening visit (about 3-5 hours) and a stay on our residential
research unit for 3 consecutive days and 2 nights.
This is not a treatment study.
Compensation of up to $1,000 will be provided for study completion.
If you are interested in seeing if you may be eligible for this study, you can complete online
screening questionnaire here: https://t.co/5SkDRfPGW0
To learn more, email us at [email protected]
The Principal Investigator for this study is Kirsten E. Smith, Ph.D.
Study Protocol: IRB00408134
One year ago- First #CongressionalBriefing on #kratomscience https://t.co/CaLrobl7Qh
#NIDA #keepkratomsafe #kratomsafe
Local bans are really scary. They're growing in #illinois #louisiana #ohio and elsewhere. Go to https://t.co/pP06XSrM2R to register to join us Sunday night #kratom #AKA #kratomscience #keepkratomsafe #kratomsafe
Watch full #CongressionalBriefing by Dr. Smith #kratomscience https://t.co/G9UjRNKI7E
#kratom #keepkratomsafe #kratomsafe #science #driving
Help pass the #Ohio #kratomconsumerprotectionact
Go to #Protectkratom Ohio page
#kratomscience #kratomsafe #keepkratomsafe
Share your story today https://t.co/5KxqdKP9rQ
#keepkratomsafe #kratomsafe #kratomscience #kratom #california

#congressionalbriefing on #kratomscience
Watch full brieing at https://t.co/RENP4cTdSX
#keepkratomsafe #kratomsafe #kratom
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