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Showing papers on "Theobromine published in 1980"


Journal ArticleDOI
TL;DR: In this article, commercial chocolate products were analyzed for theobromine and caffeine content by High Performance Liquid Chromatography, levels in 22 samples of chocolate liquor averaged 1.22% theobrome and 0.21% caffeine.
Abstract: Commercial chocolate products were analyzed for theobromine and caffeine content by High Performance Liquid Chromatography, Levels in 22 samples of chocolate liquor averaged 1.22% theobromine and 0.21% caffeine. Commercial cocoas contained, on the average, 1.89% theobromine and 0.21% caffeine. Sweet chocolate averaged 0.46% theobromine and 0.07% caffeine, while milk chocolate averaged 0.15% theobromine and 0.02% caffeine. Hot cocoa (chocolate) beverages averaged 65 mg of theobromine and 4 mg of caffeine per 5 ounce serving and chocolate milk prepared from a variety of cocoa-sugar mixes averaged 58 mg of theobromine and 5 mg of caffeine per 8 ounce serving. Theobromine and caffeine levels varied widely in individual samples within the product categories examined. Also, the ratio of theobromine to caffeine varied widely among different chocolate liquors ranging from a low of 2.5:1 to a high of 23.0:1.

74 citations


Journal Article
TL;DR: Assessment of the effects of acute, intraperitoneal administration of caffeine on serum thyrotropin, growth hormone, prolactin, thyroxine and 3,3',5-triiodothyronine in rats suggests that caffeine inhibits GH and TSH secretion by releasing hypothalamic somatostatin.
Abstract: We studied the effects of acute, intraperitoneal administration of caffeine on serum thyrotropin (TSH), growth hormone, prolactin, thyroxine and 3,3',5-triiodothyronine in rats. Caffeine lowered serum TSH and GH in a dose-dependent manner with ED50 values of 30 and approximately 50 mg/kg, respectively. TSH levels were depressed 1 to 6 hr after injection and correlated with serum caffeine levels greater than 20 micrograms/ml. The decrease in serum TSH was followed by decreases in serum 3,3',5-triiodothyroxine and thyroxine 4 hr after caffeine administration. Theophylline and theobromine had effects similar to those of caffeine on hormone levels. Caffeine did not significantly affect hormone secretion when incubated directly with rat pituitaries in vitro. Administration of antisomatostatin antiserum to rats blocked the inhibitory effects of caffeine on serum GH levels, suggesting that caffeine inhibits GH and TSH secretion by releasing hypothalamic somatostatin.

48 citations


Journal ArticleDOI
TL;DR: The results support the existence of adenosine receptors in the guinea‐pig trachea and caffeine and theophylline enhanced the non‐adrenergic inhibitory response to nerve stimulation (NAIR).
Abstract: 1 To test the possibility that adenosine receptors exist within the trachea of the guinea-pig, an attempt has been made to identify a compound with adenosine antagonist activity in this tissue. 2 Quinidine, phentolamine, phenoxybenzamine, 2-2′-pyridylisatogen tosylate (PIT) and caffeine were tested for antagonism of spasmolytic responses to adenosine, adenosine 5′-triphosphate (ATP) and adenine on the guinea-pig isolated trachea. 3 Quinidine (10 and 25 μg/ml), phentolamine (10 and 30 μg/ml) and phenoxybenzamine (10 μg/ml) had little or no effect on response to adenosine, ATP and adenine. PIT (21 μg/ml) potentiated responses to adenosine, ATP and adenine by an unexplained mechanism. 4 Caffeine (25 μg/ml) partially relaxed the trachea and inhibited spasmolytic responses to both adenosine and ATP, but not to adenine, isoprenaline, aminophylline or prostaglandin E2 (PGE2). 5 A number of compounds related to caffeine (xanthine, hypoxanthine, theophylline and theobromine) were tested for adenosine antagonist activity. Xanthine (300 μg/ml) and hypoxanthine (300 μg/ml) did not relax the trachea or antagonize spasmolytic responses to adenosine. Both theophylline (10 μg/ml) and theobromine (30 μg/ml) partially relaxed the trachea; theophylline, but not theobromine, antagonized spasmolytic responses to adenosine. 6 pA2 values for caffeine and theophylline as antagonists of adenosine were 4.3 and 4.7 respectively. However, the slopes of the Schild plot regressions were significantly less than 1.0 for both compounds. 7 Four compounds, adenine, AH 8883, M30966 and ICI 63197, which like caffeine and theophylline, have phosphodiesterase inhibitory activity were tested for adenosine antagonist activity in the trachea. Adenine and AH 8883 had no effect and M30966 and ICI 63197 caused significant potentiation. 8 The effects of caffeine and theophylline were also investigated on the non-adrenergic inhibitory response to nerve stimulation (NAIR). Both caffeine (100 μg/ml, n = 4) and theophylline (30 μg/ml, n = 4) enhanced the NAIR (20 Hz) while virtually abolishing matched responses to exogenous adenosine. 9 The results support the existence of adenosine receptors in the guinea-pig trachea.

37 citations


Journal ArticleDOI
TL;DR: The method is reproducible, correlates well with EMIT for plasma theophylline, and is applicable to the routine monitoring of both paediatric and adult patients as well as to metabolic studies.

36 citations


Journal ArticleDOI
TL;DR: A new metabolic pathway of theophylline has been investigated in premature human newborns using the ion cluster technique of stable isotope labelling combined with gas chromatography mass spectrometry.
Abstract: A new metabolic pathway of theophylline has been investigated in premature human newborns using the ion cluster technique of stable isotope labelling combined with gas chromatography mass spectrometry. Labelled caffeine, paraxanthine and theobromine have been found in plasma and urine of two preterm newborns receiving [1,3-15N], [2-13C] theophylline for the treatment of primitive apneas. Theophylline is converted to caffeine by N-7 methylation. In adults, the inverse process exists wherein caffeine is demethylated to give theophylline.

34 citations


Journal ArticleDOI
TL;DR: The in vivo administration of methylxanthines caused a significant inhibition of the xanthine oxidase activity in lungs, kidneys, heart and brain of rats and the level of uric acid in the tissues of the drug treated animals was also found to be reduced.

32 citations


Journal ArticleDOI
TL;DR: Theobromine, theophylline, paraxanthine and 1,3,7-trimethyluric acid were identified as caffeine metabolites after incubation of [2-14C]caffeine with rat liver microsomes and separation by high-pressure liquid chromatography (HPLC).

30 citations


Journal ArticleDOI
TL;DR: The sera of 30 healthy male beagles were analyzed by reversed-phase high-performance liquid chromatography and the chromatograms of each group were very reproducible; however, there were characteristic differences between the two groups.

21 citations


Journal ArticleDOI
TL;DR: Dibutyryl cyclic AMP (10(-10) to 10(-2)M) did not substitute for theophylline in increasing interferon production, and, if used together with theophylla, did not cause further enhancement.
Abstract: Summary Conditions are described for the production of 0.3 to 0.7 NIH mouse reference standard units of interferon per cell from Ehrlich ascites tumour cells cultured as monolayers and induced by infection with Newcastle disease virus (NDV). Inclusion of theophylline (6 mm) in the medium increased the interferon yield three to four times. Cells infected with NDV started to lyse at about 15 h p.i., but infected, theophylline-treated cells lysed only 24 h p.i. Several other methylxanthines (e.g. theobromine, caffeine and isobutylmethylxanthine), when tested at concentrations similar to that of theophylline, did not boost interferon production. Dibutyryl cyclic AMP (10-6 to 10-2 m) did not substitute for theophylline in increasing interferon production, and, if used together with theophylline, did not cause further enhancement.

20 citations


Journal ArticleDOI
TL;DR: It is suggested that the change in caffeine clearance seen during development of the beagle puppy is determined primarily by the rate of maturation of caffeine-7-N-demethylase.

14 citations


Journal ArticleDOI
TL;DR: In this paper, four duplicate samples of cocoa-containing materials, a practice sample, and standards were submitted to the collaborators for theobromine and caffeine analysis by HPLC.
Abstract: Four duplicate samples of cocoa-containing materials, a practice sample, and standards were submitted to the collaborators for theobromine and caffeine analysis by HPLC. In the method the samples are defatted with petroleum ether, and dried. The fat-free residue is then extracted with water and an aliquot is injected into the chromatograph. Compounds are quantitated by comparison with internal or external standards, either by peak height or peak area. Results for all the analyses showed that few of the values were more than 2 standard deviations from the mean. The method has been adopted as official first action.

Patent
20 Sep 1980
TL;DR: In this paper, the authors present a method for the synthesis of (5-oxohexyl)-theobromine having vasodilating activity using 1,3-dibromopropane.
Abstract: PURPOSE:To prepare the title compound in high yield, with one step, by reacting 1,3-dibromopropane with theobromine in an organic solvent which is a poor solvent of alkali metal salts of theobromine, in the presence of an alkali carbonate or an alkali hydroxide. CONSTITUTION:In the preparation of a theobromine derivative of formula [e.g. 1-(3-bromopropyl)theobromine] by reacting 1,3-dibromopropane which is available at a relatively low cost, with theobromine in the presence of an alkali carbonate or an alkali hydroxide, the reaction is carried out in an organic solvent which is a poor solvent of the alkali metal salt of theobromine (pref. ethanol, acetone, etc.). The amount of the solvent is >=4 parts, pref. 8-10 parts, per 1 part of theobromine. When an alkali metal salt of theobromine is used as a reactant in place of theobromine, the alkali carbonate or hydroxide is not necessary. USE:Important raw material for the synthesis of (5-oxohexyl)-theobromine having vasodilating activity.

Journal ArticleDOI
TL;DR: Bovine serum albumin conjugate of 1-methyl-3-(3'-carboxypropyl)xanthine elicits highly specific anti-theophylline antibodies when injected into sheep, and immunogens prepared from the C-8 functionalized drug afford antibodies which show more serious cross-reactivity to these compounds.
Abstract: Bovine serum albumin conjugate of 1-methyl-3-(3′-carboxypropyl)xanthine elicits highly specific anti-theophylline antibodies when injected into sheep. When used in a homogeneous enzyme immunoassay for theophylline these antibodies show insignificant cross-reactivity (< 1%) to 1-methyl-and 1,3-dimethyluric acid, 3-methylxanthine, caffeine, and theobromine. In contrast, immunogens prepared from the C-8 functionalized drug afford antibodies which show more serious cross-reactivity to these compounds. Plausible rationale for attachment of the drug to carrier proteins through its N-3 position which furnishes specific antibodies are given.

Journal ArticleDOI
TL;DR: In this article, the electron density and other indices of reactivity have been performed for N-methyl-substituted xanthines using the Huckel, Del Re, and CNDO/2 methods.
Abstract: Calculations of electron density and other indices of reactivity have been performed for N-methyl-substituted xanthines using the Huckel, Del Re, and CNDO/2 methods. The considerable difference in chemical reactivity of theophylline, theobromine, and caffeine is probably due either to steric repulsion of the van der Waals type or to the electrostatic effects of a positively charged methyl group in position 7.

Patent
17 Jul 1980
TL;DR: In this paper, the authors proposed a method to obtain a titled compound useful as a drug having vasodilating activity using the most economical, simple and safe process comprising the heating in a mineral acid, without using an expensive reagent.
Abstract: PURPOSE: To prepare the titled compound useful as a drug having vasodilating activity, etc., using the most economical, simple and safe process comprising the heating in a mineral acid, without using an expensive reagent, by hydrolyzing a theobromine derivative in the presence of an acid. CONSTITUTION: A theobromine derivative of formula I (R 1 and R 2 are H or group of formula II) is hydrolyzed in the presence of an acid (e.g. an aqueous solution of a mineral acid) at room temperature W200°C to obtain 1-(5'-oxohexyl)-3,7- dimethylxanthine of formula III. EFFECT: The use of a highly toxic heavy metal salt is not necessary. COPYRIGHT: (C)1982,JPO&Japio