Theobromine

About: Theobromine is a research topic. Over the lifetime, 1137 publications have been published within this topic receiving 29723 citations. The topic is also known as: 3,7-Dimethylxanthine & Theobromin.

Structure Determination and Anti-Inflammatory Activity of some Purine Complexes.

Abstract: Organomercury(II)-purine derivatives of the type, p-MeOC6H4HgL1 (I), p-NO2C6H4HgCl(L2)(II), p-MeC6H4HgCl(L3)(III) and p-NO2C6H4HgCl(L3)(IV) [ HL1 = theophylline, L2 = theobromine, L3 = caffeine] have been synthesised and characterised on the basis of spectral studies (IR, UV, 1H & 13C NMR). The complexes have been screened for anti-inflammatory activity.

Population Pharmacokinetics of Caffeine and its Metabolites Theobromine, Paraxanthine and Theophylline after Inhalation in Combination with Diacetylmorphine

Abstract: The stimulant effect of caffeine, as an additive in diacetylmorphine preparations for study purposes, may interfere with the pharmacodynamic effects of diacetylmorphine. In order to obtain insight into the pharmacology of caffeine after inhalation in heroin users, the pharmacokinetics of caffeine and its dimethylxanthine metabolites were studied. The objectives were to establish the population pharmacokinetics under these exceptional circumstances and to compare the results to published data regarding intravenous and oral administration in healthy volunteers. Diacetylmorphine preparations containing 100 mg of caffeine were used by 10 persons by inhalation. Plasma concentrations of caffeine, theobromine, paraxanthine and theophylline were measured by high performance liquid chromatography. Non-linear mixed effects modelling was used to estimate population pharmacokinetic parameters. The model was evaluated by the jack-knife procedure. Caffeine was rapidly and effectively absorbed after inhalation. Population pharmacokinetics of caffeine and its dimethylxanthine metabolites could adequately and simultaneously be described by a linear multi-compartment model. The volume of distribution for the central compartment was estimated to be 45.7 l and the apparent elimination rate constant of caffeine at 8 hr after inhalation was 0.150 hr(-1) for a typical individual. The bioavailability was approximately 60%. The presented model adequately describes the population pharmacokinetics of caffeine and its dimethylxanthine metabolites after inhalation of the caffeine sublimate of a 100 mg tablet. Validation proved the stability of the model. Pharmacokinetics of caffeine after inhalation and intravenous administration are to a large extent similar. The bioavailability of inhaled caffeine is approximately 60% in experienced smokers.

Role of Theobromine in Cocoa's Metabolic Properties in Healthy Rats.

Abstract: Cocoa is rich in polyphenols and methylxanthines, and it has been reported that its consumption, among other properties, has beneficial effects on metabolism. This study aimed to investigate the role of theobromine in cocoa’s metabolic properties in healthy rats. In addition to morphometric measurements, biochemical markers of lipids and glucose metabolism and gene expression of molecules related to immune cells in adipose and hepatic tissues were assessed after 7 or 18 days of diet. Additionally, a metabolomic analysis was carried out at day 7. This study revealed the presence of six discriminant metabolites in plasma due to the diets. Moreover, the results showed that theobromine is the main responsible factor for cocoa’s effects on body weight gain as well as on lipid and glucose metabolism. The effects on body weight and lipids appeared as early as after 7 days of diet, whereas those affecting glucose metabolism required a longer intervention.

A comparison of the relative toxic, emetic and convulsive actions of a series of methylated xanthine derivatives.

Abstract: The acute intraperitoneal and oral toxicity in terms of LD50 mgm./kgm. was determined in the mouse for a series of 1 and 7 substituted xanthines. The values calculated for the LD50 by the intraperitoneal route in terms of mgm./kgm. varied from 100 to 1800. 1-Allyl theobromine was the most toxic derivative while 7-β-γ-dihydroxypropyl theophylline was the least toxic. By the oral route, the values for the LD50 in terms of mgm./kgm. varied from 190 to 2700. Again 1-allyl theobromine was the most toxic while 7-acetic acid theophylline was the least toxic. 7-Diethylaminoethyl theophylline was the most active derivative in producing convulsions in the mouse. Convulsions were also observed with 7-isoamyl theophylline, 7-butyl theophylline, caffeine, theophylline, aminophyffine, 1-butyl theobromine and 7-chloroethyl theophylline. By oral administration theophylline and aminophylline were well tolerated in both the dog and the cat. In both species, 1-butyl, 1-isoamyl theobromine, 7-acetic acid and 7-isoamyl theophyffine were the most active of these derivatives in producing emesis. 7-Diethylaminoethyl theophylline caused fatalities in both the dog and the cat.

Purine alkaloid formation and CO2 gas exchange in dependence of development and of environmental factors in leaves of Coffea arabica L.

Abstract: In the leaves of Coffea arabica L., purine alkaloid formation was estimated by analyzing the theobromine and caffeine content and by measuring the methylation rate of [2-14C]theobromine to [2-14C]caffeine in short-term experiments (6–24 h). At the same time, growth (in terms of dry weight and area), net photosynthesis (NPS), and dark respiration were determined. During leaf development, which was considered to be terminated when NPS was at a maximum (60–80 μmol g-1 s-1) and dark respiration at a minimum (5–7.5 μmol g-1 s-1), the content of theobromine and the velocity of caffeine formation were both found to decrease by a factor of more than 100. The close correlation between the theobromine content and the methylation rate is suspended when purine alkaloid formation is influenced by factors other than leaf development. Among these factors, temperature is the most effective: the velocity of caffeine biosynthesis is increased by raising the temperature and vice versa. Although the plants were well irrigated, a drastic decrease of NPS in the afternoon was observed under all environmental conditions tested. Light saturation was reached between 170–360 μmol m-2 s-1. The temperature optimum of NPS was shown to be very broad (24–33°C)m provided the adaptation time was sufficiently long.