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What is 1,7-dimethylxanthine?
From a chemical perspective, paraxanthine is 1,7-dimethylxanthine with two methyl groups at positions 1 and 7.
Caffeine enters the body through a process of "absorption → metabolic decomposition". Caffeine is mainly broken down into three metabolites: theophylline, paraxanthine and theobromine °, and the proportions and effects of these three metabolites vary. The largest component is paraxanthine.
Paraxanthine accounts for about 80% of the caffeine ingested, with a smaller proportion of caffeine metabolized into theobromine and theophylline. 11J Studies have shown that 11% of caffeine is eventually converted into theobromine and 4% into theophylline.
Paraxanthine vS Paraxanthine
Science is beginning to prove that there are huge differences in the way different people metabolize caffeine, and it all depends on whether you can convert caffeine into paraxanthine, the main active ingredient that produces the positive benefits of caffeine.
This may explain why some people get great results from pre-workouts or fat burners, while others do not.
Paraxanthine is the most desirable of the three metabolites. As an adenosine antagonist, it acts similarly to caffeine, but is more potent, less toxic, and has fewer side effects than caffeine itself.
Paraxanthine is a natural plant compound found in coffee, cocoa fruit, sinomenine, and the stamens of citrus flowers. It is also the primary metabolite of caffeine. In the body, caffeine is demethylated to dimethylxanthines in the liver by the cytochrome P450 enzyme system, specifically the CYP1A2 isoenzyme.
Pharmacokinetics of Paraxanthine
Compared to theobromine, theophylline, and caffeine, paraxanthine has the shortest half-life and the greatest plasma clearance. The half-life of paraxanthine is 3.1 hours, while the half-life of caffeine is 4.1 hours, which is significantly different from the 6.2 hours of theophylline and 7.2 hours of theobromine.
The total plasma clearance of paraxanthine (2.20 mL/min/kg) is greater than that of caffeine (2.07 mL/min/kg), and significantly greater than that of theobromine (1.20 mL/min/kg) and theophylline (0.93 mL/min/kg).
In addition, paraxanthine has low toxicity and is the least harmful of the caffeine-derived metabolites. Paraxanthine is also less anxiogenic (causing anxious palpitations) than caffeine.
Unlike other caffeine metabolites, paraxanthine does not cause nausea, diarrhea, tachycardia, and arrhythmias.
Paraxanthine has been tested in multiple toxicology studies to evaluate mutagenicity, genotoxicity, and acute and repeated-dose oral toxicity in rats, but no reports of toxic effects were observed.
Clinical Human Trial Results
Paraxanthine has been tested in clinical trials for its ability to increase cognitive flexibility, maintain attention, improve working memory, and inhibitory control.
In a clinical trial, acute ingestion of paraxanthine was observed to improve cognition and short-term memory, and help maintain attention.
The trial used a randomized, double-blind, placebo-controlled, crossover, and counterbalanced method and included 12 healthy male and female subjects (24±5 years, 170.0±12 cm, 72.9±19 kg, 24.8±4 kg/m2) who were randomly assigned to take placebo (PL) or 200 mg of Paraxanthine.
Participants completed a stimulant sensitivity and side effects questionnaire and then took a battery of standard cognitive function tests, including the Berg-Kad sorting task test (BCST), an executive function test that assesses long-term thinking, including reasoning, learning, executive control, and attention shifting; the go/no-go test (GNG), which assesses sustained attention and response control through reaction time and accuracy to visual stimuli; the Sternberg task test (STT), which uses reaction time and accuracy to assess short-term/working memory involving cognitive control processes; and the psychomotor vigilance task test (PVTT), which assesses sustained attention reaction time through response to visual stimuli.
Participants then took either a placebo or paraxanthine with 8 ounces of water and then completed an identical set of side effects questionnaires and cognitive function tests every hour for 6 hours. Seven days later, participants repeated the experiment while taking the alternative treatment.
The results of this study showed that paraxanthine supplementation resulted in faster response times, less mental fatigue, higher percentage of correct answers, and fewer errors, while the placebo group experienced a significant decrease in correct answers.
Paraxanthine supplementation also improved the ability to sustain attention (i.e., maintain reaction time and prevent mental fatigue), while the placebo group had significantly shorter reaction times.
The study also found that paraxanthine improved cognitive flexibility and reduced average reaction time by 33.9% compared to placebo (placebo only 2.7%).
Mechanism of Action of Paraxanthine
1,7-Dimethylxanthine is a central nervous system stimulant that induces locomotor activation through its ability to block adenosine receptors. However, paraxanthine appears to have a higher binding potency for adenosine A1 and A2a receptors.
In fact, paraxanthine has a stronger locomotor-activating effect than caffeine, theobromine, and theophylline.
The difference in the locomotor-activating effects of paraxanthine and caffeine is related to the difference in their ability to inhibit cGMP (cyclic guanosine monophosphate), preferentially inhibiting phosphodiesterases (PDEs).
Paraxanthine, but not caffeine, has been shown to induce a significant increase in striatal cGMP concentrations.
The results strongly suggest that there is an interaction between the two major mechanisms (A1 receptor antagonism and PDE inhibition) that contribute to the locomotor-activating effects of paraxanthine, increasing the release of the neurotransmitters glutamate and dopamine by enhancing nitric oxide signaling.
In addition, paraxanthine enhances neurotransmission by enhancing nitric oxide (NO) neurotransmitter signaling. PDE9 terminates NO neurotransmission by metabolizing cGMP back to GMP.
Paraxanthine inhibits PDE9, enhancing NO transmission and promoting dopamine release. Caffeine does not have this effect.
Paraxanthine's competitive PDE inhibition also increases intracellular cAMP/PKA (cAMP-dependent protein kinase) pathways and inhibits TNF-α and leukotriene synthesis.
Company Introduction And Certificates Obtained
YTBIO supplies 1,7-Dimethylxanthine has advantages.Professional 1,7-Dimethylxanthine Powder 99% suppliers.The company was established in 2014 and has many years of experience in R&D and production. We are committed to the R&D, production and sales of raw materials for the health industry in the 21st century. The certificates obtained so far include ISO9001, ISO22000, HALAL, KOSHER, HACCP, FDA, etc. We always maintain the highest demands on product quality.
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