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This paper. This paper right here. Yeah. Read it. Options
 
cy6nu5
#1 Posted : 2/17/2019 12:00:21 AM
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Just gonna leave this here:

Psychedelic 5-Methoxy-N,N-dimethyltryptamine: Metabolism, Pharmacokinetics, Drug Interactions, and Pharmacological Actions
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https://www.ncbi.nlm.nih...pmc/articles/PMC3028383/
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ABSTRACT
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Quote:
5-Methoxy-N,N-dimethyltryptamine (5-MeO-DMT) belongs to a group of naturally-occurring psychoactive indolealkylamine drugs. It acts as a nonselective serotonin (5-HT) agonist and causes many physiological and behavioral changes. 5-MeO-DMT is O-demethylated by polymorphic cytochrome P450 2D6 (CYP2D6) to an active metabolite, bufotenine, while it is mainly inactivated through the deamination pathway mediated by monoamine oxidase A (MAO-A). 5-MeO-DMT is often used with MAO-A inhibitors such as harmaline. Concurrent use of harmaline reduces 5-MeO-DMT deamination metabolism and leads to a prolonged and increased exposure to the parent drug 5-MeO-DMT, as well as the active metabolite bufotenine. Harmaline, 5-MeO-DMT and bufotenine act agonistically on serotonergic systems and may result in hyperserotonergic effects or serotonin toxicity. Interestingly, CYP2D6 also has important contribution to harmaline metabolism, and CYP2D6 genetic polymorphism may cause considerable variability in the metabolism, pharmacokinetics and dynamics of harmaline and its interaction with 5-MeO-DMT. Therefore, this review summarizes recent findings on biotransformation, pharmacokinetics, and pharmacological actions of 5-MeO-DMT. In addition, the pharmacokinetic and pharmacodynamic drug-drug interactions between harmaline and 5-MeO-DMT, potential involvement of CYP2D6 pharmacogenetics, and risks of 5-MeO-DMT intoxication are discussed.

Keywords: 5-MeO-DMT, harmaline, metabolism, drug interaction, pharmacokinetics, pharmacogenetics, CYP2D6, serotonin toxicity



This paper, as I've been reading it is tremendously important for the understanding of DMT, 5-MEO, Harmaline/lol, THHL, and other pharmacologically significant alkaloids present in Ayahuasca and other preparations using chemically similar tryptamines.

It discusses the affinities for 5HT-[], SRT receptors, bindings, and other medically significant interactions caused by the drugs.Shocked Shocked
I’m Nobody! Who are you?
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Then there’s a pair of us!
Don’t tell! they’d advertise – you know!
I am the Walrus. Goo goo g'joob.
 

STS is a community for people interested in growing, preserving and researching botanical species, particularly those with remarkable therapeutic and/or psychoactive properties.
 
cy6nu5
#2 Posted : 2/17/2019 12:23:24 AM
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Quote:
5-MeO-DMT is regarded as an endogenous psychotoxin, and elevated concentrations of 5-MeO-DMT and its analogs in body fluids might be associated with psychotic disorders such as schizophrenic psychosis [12-19].


This is pretty significant. This is an endogenous psychotoxin, and this has often been said for N,N but to hear the same thing about the toad "venom" of the b. alvarius spp. is important. It's an interaction between the minds of various plants and animals, which is actually amazing.

Strassman's works on the topic often rave about this sort of thing in a rather woo-woo kind of way, but I mean when you dip into this stuff, you get kind of excited about it. It's an amazing chemical.

It calls it a neurotoxin and it is in the strictest sense. It causes extreme levels of serotonin in the brain which causes all sorts of hallucinations and visual effects because it plays rough with all kinds of neuro-electrical systems that are responsible for the impulses that handle visual data, cause respiration and many other regulated processes. This is rather obvious by analyzing the effects of the drug qualitatively.

Quantitatively, tryptamines and other indolamines (of which all of the -DMTs are), these drugs have high affinities for sigma receptors like 5HTP-1,2A/B receptors.

Quote:
5-MeO-DMT has high affinity for the serotonin 5-HT1A receptor, and it is 4- to 10-fold more potent than N,N-dimethyltryptamine (DMT) in human subjects [25, 26]. Unlike its chemically and pharmacologically related drugs, such as 5-hydroxy-N,N-dimethyltryptamine (bufotenine), DMT, 5-methoxy-N,N-diisopropyltryptamine (5-MeO-DiPT) and α-methyltryptamine (AMT) that all have been Schedule I controlled drugs for years, 5-MeO-DMT was not a federally controlled substance in United States until August 2009 when the Drug Enforcement Administration issued a notice intending to place 5-MeO-DMT into Schedule I of the Controlled Substances Act [20].


Incidentally, this 5HT agonism is the key mechanism of action in SSRI-class serotonergic psychoactives, and is responsible for its medical use. Why this indole ring structure has been outlawed everywhere seems obvious-- serotonin toxicity is a malady that shouldn't be tampered with lightly. And yet some of us do at our own risk and often our own detriment because we play with madness, hallucination and psychosis until we literally lose our minds.

I'm interested to find out more on the topic of other herbal 5HT-[] agonists like St. John's Wort which as I've learned today contains hypericin. It's proposed that it is responsible for its 5HT-1A agonism, I think.

I'm still reading. More on this to come.
I’m Nobody! Who are you?
Are you Nobody too?
Then there’s a pair of us!
Don’t tell! they’d advertise – you know!
I am the Walrus. Goo goo g'joob.
 
332211
#3 Posted : 2/17/2019 5:43:44 PM

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subed.

no need to feel pressured into working reading fast Pleased
 
 
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