How is paraxanthine metabolized?

How is paraxanthine metabolized?

Paraxanthine is also a major metabolite of caffeine in humans and other animals, such as mice. Shortly after ingestion, caffeine is metabolized into paraxanthine by hepatic cytochrome P450, which removes a methyl group from the N3 position of caffeine.

What are theophylline theobromine and paraxanthine?

Theobromine is water insoluble and is an isomer of theophylline as well as paraxanthine. Theobromine is categorized as 3,7-dimethylxanthine while theophylline is 1,3-dimethyl-7H-purine-2,6-dione and paraxanthine is 1,7-dimethylxanthine. Theophylline is known to be a bitter-tasting principle of green tea.

What does paraxanthine?

Paraxanthine is a central nervous stimulant and exhibits higher potency at A1 and A2 receptors, but has lower toxicity and lesser anxiogenic effects than caffeine.

How is caffeine metabolized?

Caffeine is processed or metabolized in the liver by the cytochrome P450 oxidase enzyme system and broken down into three metabolic dimethylxanthines. These include: Paraxanthine (forms 84%), which breaks down fats and increases blood levels of glycerol and fats.

What is caffeine’s mechanism of action?

Caffeine increases energy metabolism throughout the brain but decreases at the same time cerebral blood flow, inducing a relative brain hypoperfusion. Caffeine activates noradrenaline neurons and seems to affect the local release of dopamine.

What does theobromine do to humans?

According to the National Hazardous Substances Database: “It has been stated that “in large doses” theobromine may cause nausea and anorexia and that daily intake of 50-100 g cocoa (0.8-1.5 g theobromine) by humans has been associated with sweating, trembling and severe headache.” Occasionally, people (mostly the …

What affects caffeine metabolism?

Caffeine metabolism is affected by many exogenous and endogenous factors such as genetic determinants, age, sex, pregnancy, diet, lifestyle, smoking, environmental factors, medications, and diseases.

Is caffeine neurotoxic?

7. Caffeine induces neurotoxicity effects. In addition to the beneficial effects, exposure to high dose of caffeine can lead to neurotoxicity (Gepdiremen et al., 1998, Kang et al., 2002). Neurotoxicity has been observed in cerebellar granular cell isolated from rat pups (Gepdiremen et al., 1998).

How is paraxanthine metabolized in the human body?

Moreover, it is noteworthy that caffeine is metabolized to paraxanthine and, partially, to theobromine and theophylline by the hepatic microsomal enzymes (Fredholm, Bättig, Holmén, Nehlig, & Zvartau, 1999 ). This suggests that the consumption of caffeine is itself sufficient to expose the individual to different methylxanthines.

How is paraxanthine related to caffeine in humans?

1, 7-dimethylxanthine (paraxanthine) is the preferential path of caffeine metabolism in humans. Paraxanthine is a dimethylxanthine compound structurally related to caffeine. Like caffeine, paraxanthine is a psychoactive central nervous system (CNS) stimulant.

Which is more teratogenic theophylline or paraxanthine?

As with other methylxanthines, paraxanthine is reported to be teratogenic when administered in high doses; but it is a less potent teratogen as compared to caffeine and theophylline.

Which is stronger for locomotor activation, caffeine or paraxanthine?

Paraxanthine was also reported to result in stronger locomotor activation than caffeine and the other major caffeine metabolites, theophylline and theobromine. There is evidence paraxanthine is less anxiogenic than caffeine.