A pyrazolone with analgesic, anti-inflammatory, and antipyretic properties but has risk of AGRANULOCYTOSIS. A breath test with 13C-labeled aminopyrine has been used as a non-invasive measure of CYTOCHROME P-450 metabolic activity in LIVER FUNCTION TESTS.
Aminopyrine N-Demethylase is an enzyme, specifically a cytochrome P450 isoform, involved in the metabolism of drugs and xenobiotics, responsible for catalyzing the N-demethylation reaction.
A drug-metabolizing, cytochrome P-450 enzyme which catalyzes the hydroxylation of aniline to hydroxyaniline in the presence of reduced flavoprotein and molecular oxygen. EC 1.14.14.-.
Rounded or pyramidal cells of the GASTRIC GLANDS. They secrete HYDROCHLORIC ACID and produce gastric intrinsic factor, a glycoprotein that binds VITAMIN B12.
Closed vesicles of fragmented endoplasmic reticulum created when liver cells or tissue are disrupted by homogenization. They may be smooth or rough.
Hydrochloric acid present in GASTRIC JUICE.
An analgesic and antipyretic that has been given by mouth and as ear drops. Antipyrine is often used in testing the effects of other drugs or diseases on drug-metabolizing enzymes in the liver. (From Martindale, The Extra Pharmacopoeia, 30th ed, p29)
A drug that has analgesic, anti-inflammatory, and antipyretic properties. It is the sodium sulfonate of AMINOPYRINE.
An inhibitor of drug metabolism and CYTOCHROME P-450 ENZYME SYSTEM activity.
A superfamily of hundreds of closely related HEMEPROTEINS found throughout the phylogenetic spectrum, from animals, plants, fungi, to bacteria. They include numerous complex monooxygenases (MIXED FUNCTION OXYGENASES). In animals, these P-450 enzymes serve two major functions: (1) biosynthesis of steroids, fatty acids, and bile acids; (2) metabolism of endogenous and a wide variety of exogenous substrates, such as toxins and drugs (BIOTRANSFORMATION). They are classified, according to their sequence similarities rather than functions, into CYP gene families (>40% homology) and subfamilies (>59% homology). For example, enzymes from the CYP1, CYP2, and CYP3 gene families are responsible for most drug metabolism.
A barbiturate that is effective as a hypnotic and sedative.
A group of compounds that contain a bivalent O-O group, i.e., the oxygen atoms are univalent. They can either be inorganic or organic in nature. Such compounds release atomic (nascent) oxygen readily. Thus they are strong oxidizing agents and fire hazards when in contact with combustible materials, especially under high-temperature conditions. The chief industrial uses of peroxides are as oxidizing agents, bleaching agents, and initiators of polymerization. (From Hawley's Condensed Chemical Dictionary, 11th ed)
Compounds with a five-membered heterocyclic ring with two nitrogens and a keto OXYGEN. Some are inhibitors of TNF-ALPHA production.
A barbiturate that is used as a sedative. Secobarbital is reported to have no anti-anxiety activity.
A hypnotic and sedative. Its use has been largely superseded by other drugs.
A saclike, glandular diverticulum on each ductus deferens in male vertebrates. It is united with the excretory duct and serves for temporary storage of semen. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
A barbituric acid derivative that acts as a nonselective central nervous system depressant. It potentiates GAMMA-AMINOBUTYRIC ACID action on GABA-A RECEPTORS, and modulates chloride currents through receptor channels. It also inhibits glutamate induced depolarizations.
The removing of alkyl groups from a compound. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)
Oxidative enzyme which transforms p-nitroanisole into p-nitrophenol.
Lining of the STOMACH, consisting of an inner EPITHELIUM, a middle LAMINA PROPRIA, and an outer MUSCULARIS MUCOSAE. The surface cells produce MUCUS that protects the stomach from attack by digestive acid and enzymes. When the epithelium invaginates into the LAMINA PROPRIA at various region of the stomach (CARDIA; GASTRIC FUNDUS; and PYLORUS), different tubular gastric glands are formed. These glands consist of cells that secrete mucus, enzymes, HYDROCHLORIC ACID, or hormones.
A flavoprotein that catalyzes the reduction of heme-thiolate-dependent monooxygenases and is part of the microsomal hydroxylating system. EC 1.6.2.4.
Any tests done on exhaled air.
An amine derived by enzymatic decarboxylation of HISTIDINE. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and also a centrally acting neurotransmitter.
Aniline compounds, also known as aromatic amines, are organic chemicals derived from aniline (aminobenzene), characterized by the substitution of hydrogen atoms in the benzene ring with amino groups (-NH2).
Artifactual vesicles formed from the endoplasmic reticulum when cells are disrupted. They are isolated by differential centrifugation and are composed of three structural features: rough vesicles, smooth vesicles, and ribosomes. Numerous enzyme activities are associated with the microsomal fraction. (Glick, Glossary of Biochemistry and Molecular Biology, 1990; from Rieger et al., Glossary of Genetics: Classical and Molecular, 5th ed)
Widely distributed enzymes that carry out oxidation-reduction reactions in which one atom of the oxygen molecule is incorporated into the organic substrate; the other oxygen atom is reduced and combined with hydrogen ions to form water. They are also known as monooxygenases or hydroxylases. These reactions require two substrates as reductants for each of the two oxygen atoms. There are different classes of monooxygenases depending on the type of hydrogen-providing cosubstrate (COENZYMES) required in the mixed-function oxidation.
Semicarbazides are organic compounds containing a functional group with the structure NH2-NH-CO-NH2, which are commonly used as reagents in chemical reactions to form semicarbazones, and can also be found in some pharmaceuticals and industrial chemicals.
Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding.
A sympathomimetic agent with properties similar to DEXTROAMPHETAMINE. It is used in the treatment of obesity. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1222)
Cytochrome reductases are enzymes that catalyze the transfer of electrons from donor molecules to cytochromes in electron transport chains, playing a crucial role in cellular respiration and energy production within cells.
A large lobed glandular organ in the abdomen of vertebrates that is responsible for detoxification, metabolism, synthesis and storage of various substances.
A megaloblastic anemia occurring in children but more commonly in later life, characterized by histamine-fast achlorhydria, in which the laboratory and clinical manifestations are based on malabsorption of vitamin B 12 due to a failure of the gastric mucosa to secrete adequate and potent intrinsic factor. (Dorland, 27th ed)
Peroxides produced in the presence of a free radical by the oxidation of unsaturated fatty acids in the cell in the presence of molecular oxygen. The formation of lipid peroxides results in the destruction of the original lipid leading to the loss of integrity of the membranes. They therefore cause a variety of toxic effects in vivo and their formation is considered a pathological process in biological systems. Their formation can be inhibited by antioxidants, such as vitamin E, structural separation or low oxygen tension.

Effect of cyclosporine A on cytochrome P-450-mediated drug metabolism in the partially hepatectomized rat. (1/181)

Despite its hepatotoxic potential, cyclosporine A (CsA) has been reported to positively influence compensatory liver growth. To probe the physiological consequences of CsA on the recovery of liver function, studies were initiated in the 2/3 partially hepatectomized (PHx) rat, taking the recovery of cytochromes P-450-dependent drug metabolism as primary outcome. CsA was administered at a dose of 3. 33 mg/kg/day for 10 days. Drug metabolism was evaluated by the recovery of 14CO2 after administration of isotopically labeled model drugs and by studying the expression of the P-450 transcripts involved in their biotransformation before and 24 to 96 h after PHx. Before PHx, neither the steady-state mRNA nor the in vivo disposition of caffeine (CYP1A2), erythromycin (CYP3A2 and 3A1), or aminopyrine (CYP2B1 and 2C11) were influenced by CsA. Studies 24 h after PHx revealed a 29 to 39% reduction in the elimination of [14C]aminopyrine and [14C]erythromycin, which was unaffected by CsA. Their metabolism at 48 to 96 h after PHx also remained unaffected by CsA. By contrast, postPHx, [14C]caffeine elimination decreased to a level closely proportional to the loss in liver mass. In addition, CsA accelerated the recovery and/or prevented the decrease of caffeine elimination 24 h after PHx but not at later time points, indicating an early, but unsustained, beneficial effect of CsA on the recovery of CYP1A2-mediated activities. These data show that at the critical time of greatest loss in liver mass, CsA has only a selective influence on the biotransformation of cytochrome P-450 protein-dependent activities and that its effect on the regeneration process does not translate into an overall accelerated recovery of the hepatic drug-metabolizing function.  (+info)

L-365,260 inhibits in vitro acid secretion by interacting with a PKA pathway. (2/181)

The aim of this study was to analyse the antisecretory mechanism of L-365,260 in vitro in isolated rabbit gastric glands. We showed that compound L-365,260, described as a non-peptide specific competitive CCK-B receptor antagonist, was able to dose-dependently inhibit [14C]-aminopyrine accumulation induced by histamine (10(-4) M), carbachol (5x10(-5) M), 3-isobutyl-1-methyl-xanthine (IBMX) (5x10(-6) M) and forskolin (5x10(-7) M) with similar IC50 values respectively of 1.1+/-0.6x10(-7) M, 1.9+/-1.2x10(-7) M, 4.2+/-2.0x10(-7) M and 4.0+/-2.8x10(-7) M. We showed that L-365,260 acted beyond receptor activation and production of intracellular second messengers and that it had no action on the H+/K+ -ATPase. We found that L-365,260 inhibited cyclic AMP-induced [14C]-aminopyrine accumulation in digitonin-permeabilized rabbit gastric glands, suggesting that this compound acted, at least in part, as an inhibitor of the cyclic AMP-dependent protein kinase (PKA) pathway.  (+info)

Demethylation capacity of human fetal adrenal mitochondrial cytochrome P-450 in vitro. (3/181)

AIM: To explore the capacity and characteristics of adrenal mitochondria to metabolize xenobiotics in vitro in human fetus. METHODS: Subcellular fractions of fetal adrenal were prepared by differential centrifugation. Mitochondrial P-450 system was proved by spectral analyses and SDS-PAGE. The formaldehyde formation contents were measured with Nash reagent. RESULTS: The erythromycin N-demethylation linearly increased in the protein concentration (1-4 mg)- and incubation time (10-30 min)-dependent manners. A typical concentration-effect relationship appeared with erythromycin 0.067-1 mmol.L-1 and a positive correlation (r = 0.641, P < 0.05) existed between erythromycin N-demethylation and gestation months. The N-demethylation values (nmol.s-1/g protein) of erythromycin (2.7 +/- 0.8), benzfetamine (1.1 +/- 0.5), and aminophenazone (0.9 +/- 0.4) in mitochondria were 89% (P > 0.05), 162% (P < 0.01), and 62% (P < 0.01), respectively, of those in microsomes. There was correlation between mitochondria and microsomes in the N-demethylation of erythromycin (r = 0.708, P < 0.05) and benzfetamine (r = 0.707, P < 0.05). Troleandomycin stimulated erythromycin N-demethylation in adrenal mitochondria as well as in adrenal and liver microsomes in vitro. CONCLUSION: Fetal adrenal mitochondria, with multiple P-450 isoforms and greater capacity of demethylation, play a role in drug-metabolism during fetal development.  (+info)

Expression of rab11a N124I in gastric parietal cells inhibits stimulatory recruitment of the H+-K+-ATPase. (4/181)

Stimulation of the gastric parietal cell results in a massive redistribution of H+-K+-ATPase from cytoplasmic tubulovesicles to the apical plasma membrane. Previous studies have implicated the small GTPase rab11 in this process. Using matrix-assisted laser desorption mass spectrometry, we confirmed that rab11 is associated with H+-K+-ATPase-enriched gastric microsomes. A stoichiometry of one rab11 per six copies of H+-K+-ATPase was estimated. Furthermore, rab11 exists in at least three forms on rabbit gastric microsomes: the two most prominent resemble rab11a, whereas the third resembles rab11b. Using an adenoviral expression system, we expressed the dominant negative mutant rab11a N124I in primary cultures of rabbit parietal cells under the control of the tetracycline transactivator protein (tTA). The mutant was well expressed with a distribution similar to that of the H+-K+-ATPase. Stimulation of these cultures with histamine and IBMX was assessed by measuring the aminopyrine (AP) uptake relative to resting cells (AP index). In experiments on six culture preparations, stimulated uninfected cells gave an AP index of 10.0 +/- 2.9, whereas parallel cultures expressing rab11a N124I were poorly responsive to stimulation, with a mean AP index of 3.2 +/- 0. 9. Control cultures expressing tTA alone or tTA plus actin responded equally well to stimulation, giving AP index values of 9.0 +/- 3.1 and 9.6 +/- 0.9, respectively. Thus inhibition by rab11a N124I is not simply due to adenoviral infection. The AP uptake data were confirmed by immunocytochemistry. In uninfected cells, H+-K+-ATPase demonstrated a broad cytoplasmic distribution, but it was cleared from the cytoplasm and associated with apically derived membranes on stimulation. In cells expressing rab11a N124I, H+-K+-ATPase maintained its resting localization on stimulation. Furthermore, this effect could be alleviated by culturing infected cells in the presence of tetracycline, which prevents expression of the mutant rab11. We therefore conclude that rab11a is the prominent GTPase associated with gastric microsomes and that it plays a role in parietal cell activation.  (+info)

Responsiveness of beta-escin-permeabilized rabbit gastric gland model: effects of functional peptide fragments. (5/181)

We established a beta-escin-permeabilized gland model with the use of rabbit isolated gastric glands. The glands retained an ability to secrete acid, monitored by [14C]aminopyrine accumulation, in response to cAMP, forskolin, and histamine. These responses were all inhibited by cAMP-dependent protein kinase inhibitory peptide. Myosin light-chain kinase inhibitory peptide also suppressed aminopyrine accumulation, whereas the inhibitory peptide of protein kinase C or that of calmodulin kinase II was without effect. Guanosine-5'-O-(3-thiotriphosphate) (GTPgammaS) abolished cAMP-stimulated acid secretion concomitantly, interfering with the redistribution of H+-K+-ATPase from tubulovesicles to the apical membrane. To identify the targets of GTPgammaS, effects of peptide fragments of certain GTP-binding proteins were examined. Although none of the peptides related to Rab proteins showed any effect, the inhibitory peptide of Arf protein inhibited cAMP-stimulated secretion. These results demonstrate that our new model, the beta-escin-permeabilized gland, allows the introduction of relatively large molecules, e.g., peptides, into the cell, and will be quite useful for analyzing signal transduction of parietal cell function.  (+info)

Regulation and function of p38 protein kinase in isolated canine gastric parietal cells. (6/181)

We examined the regulation and functional role of p38 kinase in gastric acid secretion. p38 kinase was immunoprecipitated from cell lysates of highly purified gastric parietal cells in primary culture, and its activity was quantitated by in vitro kinase assay. Carbachol effects were dose- and time-dependent, with a maximal 10-fold stimulatory effect detected after 30 min of incubation. SB-203580, a highly selective inhibitor of p38 kinase, blocked carbachol induction of p38 kinase activity, with maximal inhibition at 10 microM. Stimulation by carbachol was unaffected by preincubation of parietal cells with the intracellular Ca(2+) chelator BAPTA-AM, but incubation of cells in Ca(2+)-free medium led to a 50% inhibition of carbachol induction of p38 kinase activity. Because some of the effects of carbachol are mediated by the small GTP-binding protein Rho, we examined the role of Rho in carbachol induction of p38 kinase activity. We tested the effect of exoenzyme C3 from Clostridium botulinum (C3), a toxin known to ADP-ribosylate and specifically inactivate Rho. C3 led to complete ADP-ribosylation of Rho, and it inhibited carbachol induction of p38 kinase by 50%. We then tested the effect of SB-203580 and C3 on carbachol-stimulated uptake of [(14)C]aminopyrine (AP). Inhibition of p38 kinase by SB-203580 led to a dose-dependent increase in AP uptake induced by carbachol, with maximal (threefold) effect at 10 microM SB-203580. Similarly, preincubation of parietal cells with C3 led to a twofold increase in AP uptake induced by carbachol. Thus carbachol induces a cascade of events in parietal cells that results in activation of p38 kinase through signaling pathways that are at least in part dependent on Rho activation and on the presence of extracellular Ca(2+). p38 kinase appears to inhibit gastric acid secretion.  (+info)

Tryptophan operon read-through. Isolation and characterization of an abnormally long tryptophan synthetase alpha subunit from a frame-shift mutant of Escherichia coli. (7/181)

A new mutant strain of Escherichia coli, strain ICR-47, contains a frame-shift mutation in the trpA gene, the gene most distal to the operator in the trp operon. Mapping experiments indicate that the lesion is located at a site within 10 to 15% of the end of this gene. The mutation results in "out-of-phase" translation of the distal portion of the trp mRNA; normal translational termination signal(s) are not encountered and a trpA gene product longer than the wild type protein is produced. As with the other enzymes produced from this operon, the in vivo level of the altered protein (the alpha subunit of the tryptophan synthetase enzyme complex) is controlled by exogenous L-tryptophan. The altered alpha subunit from the strain ICR-47 has been isolated and characterized. Molecular weight estimations indicate a molecular weight of approximately 37,000, an increase beyond the wild type enzyme corresponding to an additional 50 to 70 amino acid residues. The protein has a new COOH-terminal amino acid sequence. Results of preliminary hybridization experiments suggest that the ICR-47 mRNA, which is necessarily longer than that needed to code for wild type enzyme, is not detectably different in size from wild type mRNA. The enzymatic properties of the ICR-47 alpha subunit indicates a greatly reduced ability of the mutant subunit to combine functionally with wild type beta2 subunit, the second protein component in the tryptophan synthetase enzyme complex. In contrast, only 40 to 50% of the intrinsic enzymatic activity of the alpha subunit is lost.  (+info)

A proposed mechanism for the potentiation of cAMP-mediated acid secretion by carbachol. (8/181)

Acid secretion in isolated rabbit gastric glands was monitored by the accumulation of [(14)C]aminopyrine. Stimulation of the glands with carbachol synergistically augmented the response to dibutyryl cAMP. The augmentation persisted even after carbachol was washed out and was resistant to chelated extracellular Ca(2+) and to inhibitors of either protein kinase C or calmodulin kinase II. Cytochalasin D at 10 microM preferentially blocked the secretory effect of carbachol and its synergism with cAMP, whereas it had no effect on histamine- or cAMP-stimulated acid secretion within 15 min. Cytochalasin D inhibited the carbachol-stimulated intracellular Ca(2+) concentration ([Ca(2+)](i)) increase due to release from the Ca(2+) store. Treatment of the glands with cytochalasin D redistributed type 3 inositol 1,4,5-trisphosphate receptor (the major subtype in the parietal cell) from the fraction containing membranes of large size to the microsomal fraction, suggesting a dissociation of the store from the plasma membrane. These findings suggest that intracellular Ca(2+) release by cholinergic stimulation is critical for determining synergism with cAMP in parietal cell activation and that functional coupling between the Ca(2+) store and the receptor is maintained by actin microfilaments.  (+info)

Aminopyrine is a type of medication known as a non-opioid analgesic, which is used to relieve pain and reduce fever. It is an antipyretic and analgesic drug that was widely used in the past, but its use has been limited or discontinued in many countries due to the risk of rare but serious side effects such as agranulocytosis (a severe decrease in white blood cells), which can make individuals more susceptible to infections.

Chemically, aminopyrine is an aromatic heterocyclic compound containing a pyridine ring substituted with an amino group and a phenyl group. It works by inhibiting the enzyme cyclooxygenase (COX), which is involved in the production of prostaglandins, chemicals that mediate pain and inflammation. By reducing prostaglandin levels, aminopyrine helps to alleviate pain and reduce fever.

It's important to note that due to its potential side effects, aminopyrine is not commonly used in modern medical practice, and other safer and more effective medications are available for pain relief and fever reduction.

Aminopyrine N-demethylase is an enzyme that plays a role in the metabolism of drugs and other xenobiotics. It is primarily found in the liver and is responsible for catalyzing the N-demethylation of aminopyrine, a compound with analgesic and anti-inflammatory properties.

The enzyme works by transferring a methyl group from the aminopyrine molecule to a cofactor called NADPH, resulting in the formation of formaldehyde and dimethylaniline as products. This reaction is an important step in the biotransformation of many drugs and other foreign substances, allowing them to be more easily excreted from the body.

Aminopyrine N-demethylase is classified as a cytochrome P450 enzyme, which is a group of heme-containing proteins that are involved in oxidative metabolism. The activity of this enzyme can be influenced by various factors, including genetic polymorphisms, age, sex, and exposure to certain drugs or chemicals.

In addition to its role in drug metabolism, aminopyrine N-demethylase has also been used as a marker of liver function and as a tool for studying the regulation of cytochrome P450 enzymes.

Aniline hydroxylase is an enzyme that is involved in the metabolism of aromatic compounds, including aniline and other related substances. The enzyme catalyzes the addition of a hydroxyl group (-OH) to the aromatic ring of these compounds, which helps to make them more water-soluble and facilitates their excretion from the body.

Aniline hydroxylase is found in various tissues throughout the body, including the liver, lung, and kidney. It is a member of the cytochrome P450 family of enzymes, which are known for their role in drug metabolism and other xenobiotic-metabolizing reactions.

It's important to note that exposure to aniline and its derivatives can be harmful and may cause various health effects, including damage to the liver and other organs. Therefore, it is essential to handle these substances with care and follow appropriate safety precautions.

Parietal cells, also known as oxyntic cells, are a type of cell found in the gastric glands of the stomach lining. They play a crucial role in digestion by releasing hydrochloric acid and intrinsic factor into the stomach lumen. Hydrochloric acid is essential for breaking down food particles and creating an acidic environment that kills most bacteria, while intrinsic factor is necessary for the absorption of vitamin B12 in the small intestine. Parietal cells are stimulated by histamine, acetylcholine, and gastrin to release their secretory products.

Microsomes, liver refers to a subcellular fraction of liver cells (hepatocytes) that are obtained during tissue homogenization and subsequent centrifugation. These microsomal fractions are rich in membranous structures known as the endoplasmic reticulum (ER), particularly the rough ER. They are involved in various important cellular processes, most notably the metabolism of xenobiotics (foreign substances) including drugs, toxins, and carcinogens.

The liver microsomes contain a variety of enzymes, such as cytochrome P450 monooxygenases, that are crucial for phase I drug metabolism. These enzymes help in the oxidation, reduction, or hydrolysis of xenobiotics, making them more water-soluble and facilitating their excretion from the body. Additionally, liver microsomes also host other enzymes involved in phase II conjugation reactions, where the metabolites from phase I are further modified by adding polar molecules like glucuronic acid, sulfate, or acetyl groups.

In summary, liver microsomes are a subcellular fraction of liver cells that play a significant role in the metabolism and detoxification of xenobiotics, contributing to the overall protection and maintenance of cellular homeostasis within the body.

Gastric acid, also known as stomach acid, is a digestive fluid produced in the stomach. It's primarily composed of hydrochloric acid (HCl), potassium chloride (KCl), and sodium chloride (NaCl). The pH of gastric acid is typically between 1.5 and 3.5, making it a strong acid that helps to break down food by denaturing proteins and activating digestive enzymes.

The production of gastric acid is regulated by the enteric nervous system and several hormones. The primary function of gastric acid is to initiate protein digestion, activate pepsinogen into the active enzyme pepsin, and kill most ingested microorganisms. However, an excess or deficiency in gastric acid secretion can lead to various gastrointestinal disorders such as gastritis, ulcers, and gastroesophageal reflux disease (GERD).

Antipyrine is a chemical compound that was commonly used as a fever reducer and pain reliever in the past. It is a type of phenylpyrazole antipyretic and analgesic. However, due to its potential for causing liver damage and other side effects, it has largely been replaced by other medications and is not widely used in modern medicine.

The medical definition of Antipyrine refers to this specific chemical compound with the formula C11H13N3O2, and not to any broader category of drugs or substances. It is a white crystalline powder that is soluble in alcohol, chloroform, and ether, but insoluble in water.

Antipyrine was first synthesized in 1883 and was widely used as a fever reducer and pain reliever until the mid-20th century. However, its use declined due to concerns about its safety profile, including the potential for liver damage, skin reactions, and other side effects.

Today, Antipyrine is still used in some medical applications, such as in the measurement of earwax conductivity as a way to assess hearing function. It may also be used in some topical creams and ointments for pain relief. However, its use as a systemic medication is generally not recommended due to its potential for causing harm.

Dipyrone is a medication that belongs to the class of drugs known as non-opioid analgesics. It is primarily used for its analgesic and antipyretic effects, which means it helps to relieve pain and reduce fever. Dipyrone works by inhibiting the production of prostaglandins, chemicals in the body that cause inflammation and sensitivity to pain.

Dipyrone is available in various forms, including tablets, suppositories, and intravenous solutions. It is commonly used to treat mild to moderate pain, such as headaches, menstrual cramps, and muscle aches. However, it is important to note that dipyrone has been banned in several countries, including the United States, due to its potential to cause agranulocytosis, a serious blood disorder that can lead to infection and other complications.

The medical definition of dipyrone is as follows:

Dipyrone (INN, BAN, USAN), also known as metamizole or novaminsulfon, is a non-opioid analgesic, antipyretic, and anti-inflammatory drug. It is used for the treatment of mild to moderate pain, fever, and inflammation. Dipyrone works by inhibiting the activity of cyclooxygenase (COX) enzymes, which are involved in the production of prostaglandins, chemicals that contribute to pain, fever, and inflammation. However, due to its potential to cause agranulocytosis, a serious blood disorder, dipyrone has been banned in several countries, including the United States.

Proadifen is not typically referred to as a medical term or definition in modern medicine. However, it is an old antihistamine drug that was used in the past for its properties as a monoamine oxidase inhibitor (MAOI). MAOIs were used primarily in the treatment of depression but have largely been replaced by newer classes of drugs due to their potential for serious side effects.

Here is a brief medical definition of Proadifen as an MAOI:

Proadifen (SKF-525A): An older, nonselective and irreversible monoamine oxidase inhibitor (MAOI) that was used in the past for its antidepressant effects. Its use has been largely discontinued due to the risk of serious adverse reactions, such as hypertensive crises, when combined with certain foods or medications containing tyramine.

The Cytochrome P-450 (CYP450) enzyme system is a group of enzymes found primarily in the liver, but also in other organs such as the intestines, lungs, and skin. These enzymes play a crucial role in the metabolism and biotransformation of various substances, including drugs, environmental toxins, and endogenous compounds like hormones and fatty acids.

The name "Cytochrome P-450" refers to the unique property of these enzymes to bind to carbon monoxide (CO) and form a complex that absorbs light at a wavelength of 450 nm, which can be detected spectrophotometrically.

The CYP450 enzyme system is involved in Phase I metabolism of xenobiotics, where it catalyzes oxidation reactions such as hydroxylation, dealkylation, and epoxidation. These reactions introduce functional groups into the substrate molecule, which can then undergo further modifications by other enzymes during Phase II metabolism.

There are several families and subfamilies of CYP450 enzymes, each with distinct substrate specificities and functions. Some of the most important CYP450 enzymes include:

1. CYP3A4: This is the most abundant CYP450 enzyme in the human liver and is involved in the metabolism of approximately 50% of all drugs. It also metabolizes various endogenous compounds like steroids, bile acids, and vitamin D.
2. CYP2D6: This enzyme is responsible for the metabolism of many psychotropic drugs, including antidepressants, antipsychotics, and beta-blockers. It also metabolizes some endogenous compounds like dopamine and serotonin.
3. CYP2C9: This enzyme plays a significant role in the metabolism of warfarin, phenytoin, and nonsteroidal anti-inflammatory drugs (NSAIDs).
4. CYP2C19: This enzyme is involved in the metabolism of proton pump inhibitors, antidepressants, and clopidogrel.
5. CYP2E1: This enzyme metabolizes various xenobiotics like alcohol, acetaminophen, and carbon tetrachloride, as well as some endogenous compounds like fatty acids and prostaglandins.

Genetic polymorphisms in CYP450 enzymes can significantly affect drug metabolism and response, leading to interindividual variability in drug efficacy and toxicity. Understanding the role of CYP450 enzymes in drug metabolism is crucial for optimizing pharmacotherapy and minimizing adverse effects.

Hexobarbital is a medication that belongs to the class of drugs called barbiturates. It is primarily used as a short-acting sedative and hypnotic agent, which means it can help induce sleep and reduce anxiety. Hexobarbital works by depressing the central nervous system, slowing down brain activity and causing relaxation and drowsiness.

It's important to note that hexobarbital is not commonly used in modern medical practice due to the availability of safer and more effective alternatives. Additionally, barbiturates like hexobarbital have a high potential for abuse and dependence, and their use is associated with several risks, including respiratory depression, overdose, and death, particularly when taken in combination with other central nervous system depressants such as alcohol or opioids.

Peroxides, in a medical context, most commonly refer to chemical compounds that contain the peroxide ion (O2−2). Peroxides are characterized by the presence of an oxygen-oxygen single bond and can be found in various substances.

In dentistry, hydrogen peroxide (H2O2) is a widely used agent for teeth whitening or bleaching due to its oxidizing properties. It can help remove stains and discoloration on the tooth surface by breaking down into water and oxygen-free radicals, which react with the stain molecules, ultimately leading to their oxidation and elimination.

However, it is essential to note that high concentrations of hydrogen peroxide or prolonged exposure can cause tooth sensitivity, irritation to the oral soft tissues, and potential damage to the dental pulp. Therefore, professional supervision and appropriate concentration control are crucial when using peroxides for dental treatments.

Pyrazolones are a group of non-steroidal anti-inflammatory drugs (NSAIDs) that contain a pyrazole ring in their chemical structure. They have analgesic, antipyretic, and anti-inflammatory properties. Pyrazolones include drugs such as phenylbutazone, oxyphenbutazone, and aminopyrine. However, due to their potential for serious side effects, including agranulocytosis (a severe decrease in white blood cells), pyrazolones are rarely used in modern clinical practice.

Secobarbital is a barbiturate medication that is primarily used for the treatment of short-term insomnia and as a preoperative sedative. It works by depressing the central nervous system, producing a calming effect and helping to induce sleep. Secobarbital has a rapid onset of action and a relatively short duration of effect.

It is available in various forms, including capsules and injectable solutions, and is typically prescribed for use on an as-needed basis rather than as a regular medication. Secobarbital can be habit-forming and carries a risk of dependence and withdrawal, so it should only be used under the close supervision of a healthcare provider.

It's important to note that Secobarbital is not commonly prescribed in modern medical practice due to its high potential for abuse and the availability of safer and more effective sleep aids.

Glutethimide is a sedative-hypnotic drug that was previously used for the treatment of insomnia and anxiety disorders. It belongs to the class of drugs known as non-barbiturate hypnotics. Glutethimide works by depressing the central nervous system (CNS), producing a calming effect on the brain.

Due to its potential for abuse, addiction, and its narrow therapeutic index, glutethimide is no longer commonly used in clinical practice. It has been replaced by safer and more effective sleep aids with fewer side effects and lower potential for misuse.

It's important to note that the use of glutethimide should be under the strict supervision of a healthcare professional, and it should only be taken as prescribed. Misuse or overuse of this medication can lead to serious health consequences, including respiratory depression, coma, and even death.

The seminal vesicles are a pair of glands located in the male reproductive system, posterior to the urinary bladder and superior to the prostate gland. They are approximately 5 cm long and have a convoluted structure with many finger-like projections called infoldings. The primary function of seminal vesicles is to produce and secrete a significant portion of the seminal fluid, which makes up the bulk of semen along with spermatozoa from the testes and fluids from the prostate gland and bulbourethral glands.

The secretion of the seminal vesicles is rich in fructose, which serves as an energy source for sperm, as well as various proteins, enzymes, vitamins, and minerals that contribute to maintaining the optimal environment for sperm survival, nourishment, and transport. During sexual arousal and ejaculation, the smooth muscles in the walls of the seminal vesicles contract, forcing the stored secretion into the urethra, where it mixes with other fluids before being expelled from the body as semen.

Phenobarbital is a barbiturate medication that is primarily used for the treatment of seizures and convulsions. It works by suppressing the abnormal electrical activity in the brain that leads to seizures. In addition to its anticonvulsant properties, phenobarbital also has sedative and hypnotic effects, which can be useful for treating anxiety, insomnia, and agitation.

Phenobarbital is available in various forms, including tablets, capsules, and elixirs, and it is typically taken orally. The medication works by binding to specific receptors in the brain called gamma-aminobutyric acid (GABA) receptors, which help to regulate nerve impulses in the brain. By increasing the activity of GABA, phenobarbital can help to reduce excessive neural activity and prevent seizures.

While phenobarbital is an effective medication for treating seizures and other conditions, it can also be habit-forming and carries a risk of dependence and addiction. Long-term use of the medication can lead to tolerance, meaning that higher doses may be needed to achieve the same effects. Abruptly stopping the medication can also lead to withdrawal symptoms, such as anxiety, restlessness, and seizures.

Like all medications, phenobarbital can have side effects, including dizziness, drowsiness, and impaired coordination. It can also interact with other medications, such as certain antidepressants and sedatives, so it is important to inform your healthcare provider of all medications you are taking before starting phenobarbital.

In summary, phenobarbital is a barbiturate medication used primarily for the treatment of seizures and convulsions. It works by binding to GABA receptors in the brain and increasing their activity, which helps to reduce excessive neural activity and prevent seizures. While phenobarbital can be effective, it carries a risk of dependence and addiction and can have side effects and drug interactions.

Dealkylation is a chemical process that involves the removal of an alkyl group from a molecule. In the context of medical and biological sciences, dealkylation often refers to the breakdown of drugs or other xenobiotics (foreign substances) in the body by enzymes.

Dealkylation is one of the major metabolic pathways for the biotransformation of many drugs, including chemotherapeutic agents, opioids, and benzodiazepines. This process can result in the formation of more polar and water-soluble metabolites, which can then be excreted from the body through the urine or bile.

Dealkylation can occur via several mechanisms, including oxidative dealkylation catalyzed by cytochrome P450 enzymes, as well as non-oxidative dealkylation mediated by other enzymes. The specific dealkylation pathway depends on the structure of the substrate and the type of enzyme involved.

Nitroanisole O-Demethylase is not a commonly used medical term, but it is related to the field of biochemistry and toxicology. It refers to an enzyme that catalyzes the removal of a methyl group (CH3) from a specific chemical compound called nitroanisole.

Nitroanisole is an organic compound consisting of a methoxy (O-CH3) group attached to the phenyl ring of a nitrobenzene molecule. The enzyme Nitroanisole O-Demethylase facilitates the biotransformation process by breaking down nitroanisole into other compounds, specifically into nitrophenol and formaldehyde.

This reaction is important in understanding how the body metabolizes and eliminates foreign substances like drugs or toxins. However, it is not a term typically used in clinical medicine for diagnosing or treating medical conditions.

Gastric mucosa refers to the innermost lining of the stomach, which is in contact with the gastric lumen. It is a specialized mucous membrane that consists of epithelial cells, lamina propria, and a thin layer of smooth muscle. The surface epithelium is primarily made up of mucus-secreting cells (goblet cells) and parietal cells, which secrete hydrochloric acid and intrinsic factor, and chief cells, which produce pepsinogen.

The gastric mucosa has several important functions, including protection against self-digestion by the stomach's own digestive enzymes and hydrochloric acid. The mucus layer secreted by the epithelial cells forms a physical barrier that prevents the acidic contents of the stomach from damaging the underlying tissues. Additionally, the bicarbonate ions secreted by the surface epithelial cells help neutralize the acidity in the immediate vicinity of the mucosa.

The gastric mucosa is also responsible for the initial digestion of food through the action of hydrochloric acid and pepsin, an enzyme that breaks down proteins into smaller peptides. The intrinsic factor secreted by parietal cells plays a crucial role in the absorption of vitamin B12 in the small intestine.

The gastric mucosa is constantly exposed to potential damage from various factors, including acid, pepsin, and other digestive enzymes, as well as mechanical stress due to muscle contractions during digestion. To maintain its integrity, the gastric mucosa has a remarkable capacity for self-repair and regeneration. However, chronic exposure to noxious stimuli or certain medical conditions can lead to inflammation, erosions, ulcers, or even cancer of the gastric mucosa.

NADPH-ferrihemoprotein reductase, also known as diaphorase or NO synthase reductase, is an enzyme that catalyzes the reduction of ferrihemoproteins using NADPH as a reducing cofactor. This reaction plays a crucial role in various biological processes such as the detoxification of certain compounds and the regulation of cellular signaling pathways.

The systematic name for this enzyme is NADPH:ferrihemoprotein oxidoreductase, and it belongs to the family of oxidoreductases that use NADH or NADPH as electron donors. The reaction catalyzed by this enzyme can be represented as follows:

NADPH + H+ + ferrihemoprotein ↔ NADP+ + ferrohemoprotein

In this reaction, the ferric (FeIII) form of hemoproteins is reduced to its ferrous (FeII) form by accepting electrons from NADPH. This enzyme is widely distributed in various tissues and organisms, including bacteria, fungi, plants, and animals. It has been identified as a component of several multi-enzyme complexes involved in different metabolic pathways, such as nitric oxide synthase (NOS) and cytochrome P450 reductase.

In summary, NADPH-ferrihemoprotein reductase is an essential enzyme that catalyzes the reduction of ferrihemoproteins using NADPH as a reducing agent, playing a critical role in various biological processes and metabolic pathways.

A breath test is a medical or forensic procedure used to analyze a sample of exhaled breath in order to detect and measure the presence of various substances, most commonly alcohol. The test is typically conducted using a device called a breathalyzer, which measures the amount of alcohol in the breath and converts it into a reading of blood alcohol concentration (BAC).

In addition to alcohol, breath tests can also be used to detect other substances such as drugs or volatile organic compounds (VOCs) that may indicate certain medical conditions. However, these types of breath tests are less common and may not be as reliable or accurate as other diagnostic tests.

Breath testing is commonly used by law enforcement officers to determine whether a driver is impaired by alcohol and to establish probable cause for arrest. It is also used in some healthcare settings to monitor patients who are being treated for alcohol abuse or dependence.

Histamine is defined as a biogenic amine that is widely distributed throughout the body and is involved in various physiological functions. It is derived primarily from the amino acid histidine by the action of histidine decarboxylase. Histamine is stored in granules (along with heparin and proteases) within mast cells and basophils, and is released upon stimulation or degranulation of these cells.

Once released into the tissues and circulation, histamine exerts a wide range of pharmacological actions through its interaction with four types of G protein-coupled receptors (H1, H2, H3, and H4 receptors). Histamine's effects are diverse and include modulation of immune responses, contraction and relaxation of smooth muscle, increased vascular permeability, stimulation of gastric acid secretion, and regulation of neurotransmission.

Histamine is also a potent mediator of allergic reactions and inflammation, causing symptoms such as itching, sneezing, runny nose, and wheezing. Antihistamines are commonly used to block the actions of histamine at H1 receptors, providing relief from these symptoms.

Aniline compounds, also known as aromatic amines, are organic compounds that contain a benzene ring substituted with an amino group (-NH2). Aniline itself is the simplest and most common aniline compound, with the formula C6H5NH2.

Aniline compounds are important in the chemical industry and are used in the synthesis of a wide range of products, including dyes, pharmaceuticals, and rubber chemicals. They can be produced by reducing nitrobenzene or by directly substituting ammonia onto benzene in a process called amination.

It is important to note that aniline compounds are toxic and can cause serious health effects, including damage to the liver, kidneys, and central nervous system. They can also be absorbed through the skin and are known to have carcinogenic properties. Therefore, appropriate safety measures must be taken when handling aniline compounds.

Microsomes are subcellular membranous vesicles that are obtained as a byproduct during the preparation of cellular homogenates. They are not naturally occurring structures within the cell, but rather formed due to fragmentation of the endoplasmic reticulum (ER) during laboratory procedures. Microsomes are widely used in various research and scientific studies, particularly in the fields of biochemistry and pharmacology.

Microsomes are rich in enzymes, including the cytochrome P450 system, which is involved in the metabolism of drugs, toxins, and other xenobiotics. These enzymes play a crucial role in detoxifying foreign substances and eliminating them from the body. As such, microsomes serve as an essential tool for studying drug metabolism, toxicity, and interactions, allowing researchers to better understand and predict the effects of various compounds on living organisms.

Mixed Function Oxygenases (MFOs) are a type of enzyme that catalyze the addition of one atom each from molecular oxygen (O2) to a substrate, while reducing the other oxygen atom to water. These enzymes play a crucial role in the metabolism of various endogenous and exogenous compounds, including drugs, carcinogens, and environmental pollutants.

MFOs are primarily located in the endoplasmic reticulum of cells and consist of two subunits: a flavoprotein component that contains FAD or FMN as a cofactor, and an iron-containing heme protein. The most well-known example of MFO is cytochrome P450, which is involved in the oxidation of xenobiotics and endogenous compounds such as steroids, fatty acids, and vitamins.

MFOs can catalyze a variety of reactions, including hydroxylation, epoxidation, dealkylation, and deamination, among others. These reactions often lead to the activation or detoxification of xenobiotics, making MFOs an important component of the body's defense system against foreign substances. However, in some cases, these reactions can also produce reactive intermediates that may cause toxicity or contribute to the development of diseases such as cancer.

Semicarbazides are organic compounds that contain the functional group -NH-CO-NH-NH2. They are derivatives of hydrazine and carbamic acid, with the general structure (CH3)NHCSNH2. Semicarbazides are widely used in the synthesis of various chemical compounds, including heterocyclic compounds, pharmaceuticals, and agrochemicals.

In a medical context, semicarbazides themselves do not have any therapeutic use. However, they can be used in the preparation of certain drugs or drug intermediates. For example, semicarbazones, which are derivatives of semicarbazides, can be used to synthesize some antituberculosis drugs.

It is worth noting that semicarbazides and their derivatives have been found to have mutagenic and carcinogenic properties in some studies. Therefore, they should be handled with care in laboratory settings, and exposure should be minimized to reduce potential health risks.

"Inbred strains of rats" are genetically identical rodents that have been produced through many generations of brother-sister mating. This results in a high degree of homozygosity, where the genes at any particular locus in the genome are identical in all members of the strain.

Inbred strains of rats are widely used in biomedical research because they provide a consistent and reproducible genetic background for studying various biological phenomena, including the effects of drugs, environmental factors, and genetic mutations on health and disease. Additionally, inbred strains can be used to create genetically modified models of human diseases by introducing specific mutations into their genomes.

Some commonly used inbred strains of rats include the Wistar Kyoto (WKY), Sprague-Dawley (SD), and Fischer 344 (F344) rat strains. Each strain has its own unique genetic characteristics, making them suitable for different types of research.

Benzphetamine is a sympathomimetic amine, which is a type of drug that stimulates the sympathetic nervous system. It is a central nervous system stimulant and an appetite suppressant. Benzphetamine is used as a short-term supplement to diet and exercise in the treatment of obesity.

The medical definition of benzphetamine is:

A CNS stimulant and anorectic, structurally related to amphetamines, but pharmacologically related to the phenylethylamines. It has a longer duration of action than other amphetamines because it is absorbed more slowly and is excreted more slowly. Benzphetamine is used as an appetite suppressant in the treatment of obesity.

It's important to note that benzphetamine, like other weight-loss medications, should be used in conjunction with a reduced-calorie diet and exercise. It also has a risk for abuse and dependence, so it is usually prescribed for short-term use only.

Cytochrome reductases are a group of enzymes that play a crucial role in the electron transport chain, a process that occurs in the mitochondria of cells and is responsible for generating energy in the form of ATP (adenosine triphosphate). Specifically, cytochrome reductases are responsible for transferring electrons from one component of the electron transport chain to another, specifically to cytochromes.

There are several types of cytochrome reductases, including NADH dehydrogenase (also known as Complex I), succinate dehydrogenase (also known as Complex II), and ubiquinone-cytochrome c reductase (also known as Complex III). These enzymes help to facilitate the flow of electrons through the electron transport chain, which is essential for the production of ATP and the maintenance of cellular homeostasis.

Defects in cytochrome reductases can lead to a variety of mitochondrial diseases, which can affect multiple organ systems and may be associated with symptoms such as muscle weakness, developmental delays, and cardiac dysfunction.

The liver is a large, solid organ located in the upper right portion of the abdomen, beneath the diaphragm and above the stomach. It plays a vital role in several bodily functions, including:

1. Metabolism: The liver helps to metabolize carbohydrates, fats, and proteins from the food we eat into energy and nutrients that our bodies can use.
2. Detoxification: The liver detoxifies harmful substances in the body by breaking them down into less toxic forms or excreting them through bile.
3. Synthesis: The liver synthesizes important proteins, such as albumin and clotting factors, that are necessary for proper bodily function.
4. Storage: The liver stores glucose, vitamins, and minerals that can be released when the body needs them.
5. Bile production: The liver produces bile, a digestive juice that helps to break down fats in the small intestine.
6. Immune function: The liver plays a role in the immune system by filtering out bacteria and other harmful substances from the blood.

Overall, the liver is an essential organ that plays a critical role in maintaining overall health and well-being.

Pernicious anemia is a specific type of vitamin B12 deficiency anemia that is caused by a lack of intrinsic factor, a protein made in the stomach that is needed to absorb vitamin B12. The absence of intrinsic factor leads to poor absorption of vitamin B12 from food and results in its deficiency.

Vitamin B12 is essential for the production of healthy red blood cells, which carry oxygen throughout the body. Without enough vitamin B12, the body cannot produce enough red blood cells, leading to anemia. Pernicious anemia typically develops slowly over several years and can cause symptoms such as fatigue, weakness, pale skin, shortness of breath, and a decreased appetite.

Pernicious anemia is an autoimmune disorder, which means that the body's immune system mistakenly attacks healthy cells in the stomach lining, leading to a loss of intrinsic factor production. It is more common in older adults, particularly those over 60 years old, and can also be associated with other autoimmune disorders such as type 1 diabetes, Hashimoto's thyroiditis, and Addison's disease.

Treatment for pernicious anemia typically involves vitamin B12 replacement therapy, either through oral supplements or injections of the vitamin. In some cases, dietary changes may also be recommended to ensure adequate intake of vitamin B12-rich foods such as meat, fish, poultry, and dairy products.

Lipid peroxides are chemical compounds that form when lipids (fats or fat-like substances) oxidize. This process, known as lipid peroxidation, involves the reaction of lipids with oxygen in a way that leads to the formation of hydroperoxides and various aldehydes, such as malondialdehyde.

Lipid peroxidation is a naturally occurring process that can also be accelerated by factors such as exposure to radiation, certain chemicals, or enzymatic reactions. It plays a role in many biological processes, including cell signaling and regulation of gene expression, but it can also contribute to the development of various diseases when it becomes excessive.

Examples of lipid peroxides include phospholipid hydroperoxides, cholesteryl ester hydroperoxides, and triglyceride hydroperoxides. These compounds are often used as markers of oxidative stress in biological systems and have been implicated in the pathogenesis of atherosclerosis, cancer, neurodegenerative diseases, and other conditions associated with oxidative damage.

Tsyrlov, I. B.; Gerasimov, K. E. (1991). "Aminopyrine-N-demethylase. I. Directed modification of substrates' structure as a way ...
Aminopyrine Hart FD, Boardman PL (June 1964). "Trial of Nifenazone ("Thylin")". British Medical Journal. 1 (5397): 1553-4. doi: ...
In 1897 he invented "Pyramidon", the trade name for aminopyrine. With Arthur Stoll, he is credited with the isolation of ...
... (or aminopyrine, amidopyrine, Pyramidon) is a non-narcotic analgesic substance. It is a pyrazolone and a ... Caubet MS, Laplante A, Caillé J, Brazier JL (June 2002). "[13C]aminopyrine and [13C]caffeine breath test: influence of gender, ... A breath test with 13C-labeled aminopyrine has been used as a non-invasive measure of cytochrome P-450 metabolic activity in ...
... is a metabolite of aminopyrine with analgesic, anti-inflammatory, and antipyretic properties. Its use as a drug is ...
In 1893, a derivative of antipyrine, aminopyrine, was made by Friedrich Stolz at Hoechst.: 26-27 Yet later, chemists at Hoechst ...
Imaoka S, Inoue K, Funae Y (1988). "Aminopyrine metabolism by multiple forms of cytochrome P-450 from rat liver microsomes: ... simultaneous quantitation of four aminopyrine metabolites by high-performance liquid chromatography". Arch. Biochem. Biophys. ...
... hexachlorobiphenyl found increased activation of ethoxyresorufin deethylase and aminopyrine demethylase. However, while also ...
... aminopyrine MeSH D03.383.129.539.850.077.025 - ampyrone MeSH D03.383.129.539.850.077.150 - dipyrone (metamizole) MeSH D03.383. ...
... or aminopyrine PNU-91356A (U-91356) This set index page lists chemical structure articles associated with the same molecular ...
... aminopyrine n-demethylase MeSH D08.811.682.662.582.338 - cytochrome p-450 cyp2e1 MeSH D08.811.682.662.582.353 - cytochrome p- ...
Characterization of cytochrome P-450-dependent aminopyrine N-demethylase in rat brain: comparison with hepatic aminopyrine N- ... Characterization of cytochrome P-450-dependent aminopyrine N-demethylase in rat brain: comparison with hepatic aminopyrine N- ... Characterization of cytochrome P-450-dependent aminopyrine N-demethylase in rat brain: comparison with hepatic aminopyrine N- ... Characterization of cytochrome P-450-dependent aminopyrine N-demethylase in rat brain: comparison with hepatic aminopyrine N- ...
Involvement of Radical Species in the Oxidation of Aminopyrine and 4-Aminoantipyrine by Cumene Hydroperoxide in Rat Liver ... Involvement of Radical Species in the Oxidation of Aminopyrine and 4-Aminoantipyrine by Cumene Hydroperoxide in Rat Liver ... Involvement of Radical Species in the Oxidation of Aminopyrine and 4-Aminoantipyrine by Cumene Hydroperoxide in Rat Liver ... Involvement of Radical Species in the Oxidation of Aminopyrine and 4-Aminoantipyrine by Cumene Hydroperoxide in Rat Liver ...
Aminopyrine interacts with CELERY Celery juice might decrease how quickly the liver breaks down and removes aminopyrine. Taking ... celery juice with aminopyrine might increase the effects and side effects of aminopyrine. ...
Tsyrlov, I. B.; Gerasimov, K. E. (1991). "Aminopyrine-N-demethylase. I. Directed modification of substrates structure as a way ...
aminopyrine. *heavy metals. *phenothiazine. *sulfonamides. *penicillins. Other medications that can lead to leukopenia include: ...
Aminopyrine and dipyrone have been withdrawn from the market in many countries due to risk of agranulocytosis. ... This mechanism operates in cases due to gold, aminopyrine, and antithyroid drugs. The antibodies destroy the granulocytes and ...
... the extract showed inhibitory actions on aminopyrine N-demethylase and xanthine oxidase activities as well as an pro-oxidant ...
Using aminopyrine as a nitrogen-enriched small molecule precursor to synthesize high-performing nitrogen doped mesoporous ... With aminopyrine as a nitrogen-enriched small molecule precursor, a series of nitrogen doped carbon materials have been ... Using aminopyrine as a nitrogen-enriched small molecule precursor to synthesize high-performing nitrogen doped mesoporous ... Using aminopyrine as a nitrogen-enriched small molecule precursor to synthesize high-performing nitrogen doped mesoporous ...
C.01.131 - Aminopyrine and Dipyrone *C.01.134 - Coated Potassium Salts *C.01.401 - Antibiotics ...
C.01.131 - Aminopyrine and Dipyrone *C.01.134 - Coated Potassium Salts *C.01.401 - Antibiotics ...
C.01.131 - Aminopyrine and Dipyrone *C.01.134 - Coated Potassium Salts *C.01.401 - Antibiotics ...
C.01.131 - Aminopyrine and Dipyrone *C.01.134 - Coated Potassium Salts *C.01.401 - Antibiotics ...
Aminopyrine breath test predicts surgical risk for patients with liver disease. Ann Surg. 1983 Dec. 198(6):701-4. [QxMD MEDLINE ...
... aminopyrine and chlorpromazine). The increases for hexobarbital and aminopyrine were dose-related. In vivo hexobarbital ... aminopyrine, and chlorpromazine (Hart et al., 1963). Treatment of newborn rabbits with 50 mg/kg of gamma-chlordane daily for 3 ... aminopyrine, zoxazolamine and p-nitrobenzoic acid (Fouts and Rogers, 1965). Pretreatment of rats for several days with ... days increased the activity of liver enzymes that metabolize hexobarbital, aminopyrine and p-nitrobenzoic acid. Treatment of ...
Afolabi, P., Wright, M., Wootton, S. A., & Jackson, A. A. (2013). 13C-aminopyrine demethylation is decreased in cirrhotic ... A comparison of the reproducibility of the parameters of the ¹³C-aminopyrine breath test for the assessment of hepatic function ...
1886, fluorine; aminopyrine; steam sterilisation; aluminium by hydrolysis; hydroelectric installations at Niagara Falls; Coca- ...
C.01.131 - Aminopyrine and Dipyrone *C.01.134 - Coated Potassium Salts *C.01.401 - Antibiotics ...
Rats administered aminopyrine (0.01%) and sodium nitrite (0.1%) and contemporary drinking coffee solution for 630 days. ↓ ... extended these results by showing decreased incidences of liver tumors in rats given a concurrent administration of aminopyrine ...
Rubin, B. & Waugh, M. H. Antiphlogistic effects of antiserotonin (SQ 10,643) and aminopyrine in rats versus endotoxin and other ...
The effects on aminopyrine-demethylase and acetanilide-hydroxylase activity were evaluated. The extracts were examined by thin ... Isooctane did not inhibit aminopyrine-demethylase or acetanilide-hydroxylase activity. TLC spots corresponding to ...
13C-aminopyrine, 13C-methacetin, 13C-erythromycin, or 13C-caffeine, for monitoring microsomal functions; 13C-alpha- ...
13C-aminopyrine demethylation blood test for hepatic function testing12 Currently there is no hepatic function test available ... 13C-aminopyrine breath tests have been used to evaluate hepatic function in both human beings and laboratory animals. These ... 13C-aminopyrine is administered intravenously and reaches the liver where it is demethylated by microsomal enzymes. 13C is ... Preliminary studies of a canine 13C-aminopyrine demethylation blood test. Can J Vet Res 2001; 65:45-49. ...
Aktuelle API Auditberichte • GMP-Audits der Herstelung pharmazeutischer Ausgangs- und Wirkstoffe nach ICH Q7 / EU GMP Guide Part II • Diapharm
Acid secretion was assessed by measuring [14C]aminopyrine accumulation, and the concentration of cGMP was determined by ...
It was shown that THC (10-4 M) inhibits in the liver microsomal oxidation of aminopyrine by 50%, of hexobarbital by 58%, ...
... and to a lesser extent by aminopyrine and Tofranil (50 mg/kg), and was moderately inhibited by aspirin, antipyrine, LSD (100 ...
... aminopyrine accumulation), whereas the tetrapeptide of gastrin (14-17) had a much lower potency. Proglumide inhibited gastrin ...
  • The spin-trap nitrosobenzene strongly inhibited not only the cumene hydroperoxide-supported oxidation of aminopyrine and its metabolite, but also the oxygen utilization of microsomes stimulated by this hydroperoxide. (aspetjournals.org)
  • Spectral changes observed during the microsomal oxidation of aminopyrine by cumene hydroperoxide have demonstrated the formation of the aminopyrine radical prior to, and concomitant with, the formation of antipyrine red. (aspetjournals.org)
  • The 5-HT-induced increase in permeability was very markedly inhibited by chlorpromazine (1-25 mg/kg) and to a lesser extent by aminopyrine and Tofranil (50 mg/kg), and was moderately inhibited by aspirin, antipyrine, LSD (100 mcg/kg) and Tofranil (5 mg/kg). (erowid.org)
  • Antiinflammatory action could also be Antipyrine (phenazone) and amidopyrine (aminopyrine) exerted by other mechanisms as nicely [url=https://aghgol.com/docs/order-cheap-prednisone/] allergy medicine 4 year old buy discount prednisone 20mg[/url]. (tmshelp.com)
  • no significant changes were noted in liver aminopyrine - N - demethylase or aniline hydrolase activities. (cdc.gov)
  • 1964). In vitro metabolism by hepatic microsomal enzymes from rats treated 8 days previously with single i.p. doses of 10 or 100 mg/kg of chlordane in corn oil was increased for the 3 drugs reported (hexobarbital, aminopyrine and chlorpromazine). (inchem.org)
  • The phenobarbital-induced increase in the microsomal content of CO-binding pigment and in the activities of TPNH-cytochrome c reductase and the oxidative demethylation of aminopyrine is proportional, within certain limits, to the amount of phenobarbital injected. (rupress.org)
  • In the pharmaceutical industry, it is applied to produce intermediates of metamizole and aminopyrine. (choice-chem.com)
  • The effects on aminopyrine-demethylase and acetanilide-hydroxylase activity were evaluated. (cdc.gov)
  • Isooctane did not inhibit aminopyrine-demethylase or acetanilide-hydroxylase activity. (cdc.gov)
  • Although S. baicalensis inhibited the lipid peroxidation in rat liver microsomes and red blood cells, the extract showed inhibitory actions on aminopyrine N-demethylase and xanthine oxidase activities as well as an pro-oxidant effect observed in the Fe3+-EDTA-H2O2 system. (nih.gov)
  • However, there was no change in activities of either hepatic microsomal aminopyrine demethylase or glucose-6-phosphatase. (nih.gov)
  • no significant changes were noted in liver aminopyrine - N - demethylase or aniline hydrolase activities. (cdc.gov)
  • total cytochrome P450 (CYP) contents, aminopyrine N-demethylase activity and delta-aminolevulinic acid synthetase activity also decreased significantly in the CRF rats. (nih.gov)
  • Aminopyrine demethylase activity in normal and vitamin E-deficient male rats. (illinois.edu)
  • The rates of oxidative metabolism of antipyrine, aminopyrine, ethylmorphine, aniline, and benzo(a)pyrene were all increased by more than 45% in the petrol-exposed rats. (bmj.com)
  • Brodie and Axelrod continued to collaborate on a number of projects related to the metabolism of analgesic drugs including phenacetin, antipyrine, aminopyrine, and dicoumerol. (nih.gov)
  • 1. It is mainly used in the production of antipyrine, aminopyrine and analgin. (huatengsci.com)
  • G17 and carboxyl terminal octapeptide of cholecystokinin (26-33) were equipotent in displacing tracer binding and in stimulating parietal cell function ( [14C]aminopyrine accumulation), whereas the tetrapeptide of gastrin (14-17) had a much lower potency. (jci.org)
  • Accumulation of the weak base aminopyrine was used as an index of acid secretory activity in rat isolated parietal cells. (port.ac.uk)
  • The nitric oxide (NO) donor, S-nitroso-N-acetyl-penicillamine (SNAP) caused a dose-dependent inhibition of aminopyrine accumulation (half-maximally effective concentration 247 μM) which was accompanied by an increase in guanosine 3',5'-cyclic monophosphate (cGMP) but no decrease in cell viability (trypan blue), glucose oxidation or adenosine 3',5'-cyclic monophosphate (cAMP) content. (port.ac.uk)
  • Prior exposure of intact cells to SNAP also reduced aminopyrine accumulation in response to ATP in permeabilised cells, an effect prevented by Rp-8-bromoguanosine 3',5'-monophosphorothioate, which inhibits activation of cGMP-dependent protein kinase, but not by the Sp-isomer. (port.ac.uk)
  • METHODS: We adopted and extensively characterised the mouse gastric gland preparation and its secretory capacity, which was measured using (14)C-aminopyrine accumulation. (mcmaster.ca)
  • RESULTS: (14)C-aminopyrine accumulation in mouse gastric glands was shown to be a very sensitive "in vitro" method of testing classical secretagogues and antisecretory compounds, and provided pharmacological data on acid secretion in the mouse. (mcmaster.ca)
  • The aminopyrine breath test has been shown to be a sensitive noninvasive indicator of liver cell dysfunction. (nih.gov)
  • In a search for a noninvasive method of monitoring the effects of methotrexate therapy, we have investigated the use of the aminopyrine breath test in patients receiving methotrexate for the treatment of severe psoriasis. (nih.gov)
  • The [14C]-aminopyrine breath test was performed in 20 normal control subjects, 32 patients with psoriasis receiving methotrexate therapy, and 8 patients with histologically confirmed cirrhosis of differing etiology. (nih.gov)
  • The aminopyrine breath test was only able to detect the later severe stages of methotrexate hepatotoxicity, grade III, when fibrosis occurs, before established cirrhosis was present. (nih.gov)
  • Our data suggests that the aminopyrine breath test is not a sensitive indicator for the detection of early methotrexate-induced hepatotoxicity, (stages I and II), but will detect the precirrhotic stage III change. (nih.gov)
  • Consequently, we recommend that a liver biopsy should be performed annually in all psoriatic patients receiving methotrexate, to detect histological damage, especially when the aminopyrine breath test score falls below the 95% confidence limits of normal. (nih.gov)
  • Aminopyrine breath test in the prognostic evaluation of patients with cirrhosis. (bmj.com)
  • 22. Aminopyrine breath test predicts liver-related events and death in HCV-related cirrhosis on SVR after DAA therapy. (nih.gov)
  • A breath test with 13C-labeled aminopyrine has been used as a non-invasive measure of CYTOCHROME P-450 metabolic activity in LIVER FUNCTION TESTS . (nih.gov)