Canrenoic Acid: A synthetic pregnadiene derivative with anti-aldosterone activity.Furosemide: A benzoic-sulfonamide-furan. It is a diuretic with fast onset and short duration that is used for EDEMA and chronic RENAL INSUFFICIENCY.Canrenone: A synthetic pregnadiene compound with anti-aldosterone activity.Mineralocorticoid Receptor Antagonists: Drugs that bind to and block the activation of MINERALOCORTICOID RECEPTORS by MINERALOCORTICOIDS such as ALDOSTERONE.Diuretics: Agents that promote the excretion of urine through their effects on kidney function.Spironolactone: A potassium sparing diuretic that acts by antagonism of aldosterone in the distal renal tubules. It is used mainly in the treatment of refractory edema in patients with congestive heart failure, nephrotic syndrome, or hepatic cirrhosis. Its effects on the endocrine system are utilized in the treatments of hirsutism and acne but they can lead to adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p827)Sodium Chloride Symporter Inhibitors: Agents that inhibit SODIUM CHLORIDE SYMPORTERS. They act as DIURETICS. Excess use is associated with HYPOKALEMIA.Receptors, Progesterone: Specific proteins found in or on cells of progesterone target tissues that specifically combine with progesterone. The cytosol progesterone-receptor complex then associates with the nucleic acids to initiate protein synthesis. There are two kinds of progesterone receptors, A and B. Both are induced by estrogen and have short half-lives.Mifepristone: A progestational and glucocorticoid hormone antagonist. Its inhibition of progesterone induces bleeding during the luteal phase and in early pregnancy by releasing endogenous prostaglandins from the endometrium or decidua. As a glucocorticoid receptor antagonist, the drug has been used to treat hypercortisolism in patients with nonpituitary CUSHING SYNDROME.Promegestone: A synthetic progestin which is useful for the study of progestin distribution and progestin tissue receptors, as it is not bound by transcortin and binds to progesterone receptors with a higher association constant than progesterone.Molecular Sequence Data: Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.Transcription, Genetic: The biosynthesis of RNA carried out on a template of DNA. The biosynthesis of DNA from an RNA template is called REVERSE TRANSCRIPTION.Orthohepadnavirus: A genus of HEPADNAVIRIDAE causing hepatitis in humans, woodchucks (HEPATITIS B VIRUS, WOODCHUCK) and ground squirrels. hepatitis b virus is the type species.Base Sequence: The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.Microsomes, Liver: Closed vesicles of fragmented endoplasmic reticulum created when liver cells or tissue are disrupted by homogenization. They may be smooth or rough.Glucuronides: Glycosides of GLUCURONIC ACID formed by the reaction of URIDINE DIPHOSPHATE GLUCURONIC ACID with certain endogenous and exogenous substances. Their formation is important for the detoxification of drugs, steroid excretion and BILIRUBIN metabolism to a more water-soluble compound that can be eliminated in the URINE and BILE.Glucuronosyltransferase: A family of enzymes accepting a wide range of substrates, including phenols, alcohols, amines, and fatty acids. They function as drug-metabolizing enzymes that catalyze the conjugation of UDPglucuronic acid to a variety of endogenous and exogenous compounds. EC 2.4.1.17.Morphine Derivatives: Analogs or derivatives of morphine.Dextropropoxyphene: A narcotic analgesic structurally related to METHADONE. Only the dextro-isomer has an analgesic effect; the levo-isomer appears to exert an antitussive effect.Kinetics: The rate dynamics in chemical or physical systems.Methadyl Acetate: A narcotic analgesic with a long onset and duration of action.Potassium: An element in the alkali group of metals with an atomic symbol K, atomic number 19, and atomic weight 39.10. It is the chief cation in the intracellular fluid of muscle and other cells. Potassium ion is a strong electrolyte that plays a significant role in the regulation of fluid volume and maintenance of the WATER-ELECTROLYTE BALANCE.Polypharmacy: The use of multiple drugs administered to the same patient, most commonly seen in elderly patients. It includes also the administration of excessive medication. Since in the United States most drugs are dispensed as single-agent formulations, polypharmacy, though using many drugs administered to the same patient, must be differentiated from DRUG COMBINATIONS, single preparations containing two or more drugs as a fixed dose, and from DRUG THERAPY, COMBINATION, two or more drugs administered separately for a combined effect. (From Segen, Dictionary of Modern Medicine, 1992)Drug Interactions: The action of a drug that may affect the activity, metabolism, or toxicity of another drug.Cytochrome P-450 Enzyme System: 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.Comorbidity: The presence of co-existing or additional diseases with reference to an initial diagnosis or with reference to the index condition that is the subject of study. Comorbidity may affect the ability of affected individuals to function and also their survival; it may be used as a prognostic indicator for length of hospital stay, cost factors, and outcome or survival.Receptors, Mineralocorticoid: Cytoplasmic proteins that specifically bind MINERALOCORTICOIDS and mediate their cellular effects. The receptor with its bound ligand acts in the nucleus to induce transcription of specific segments of DNA.Iodoacetates: Iodinated derivatives of acetic acid. Iodoacetates are commonly used as alkylating sulfhydryl reagents and enzyme inhibitors in biochemical research.Structure-Activity Relationship: The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.Amino Acid Sequence: The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.Steroids: A group of polycyclic compounds closely related biochemically to TERPENES. They include cholesterol, numerous hormones, precursors of certain vitamins, bile acids, alcohols (STEROLS), and certain natural drugs and poisons. Steroids have a common nucleus, a fused, reduced 17-carbon atom ring system, cyclopentanoperhydrophenanthrene. Most steroids also have two methyl groups and an aliphatic side-chain attached to the nucleus. (From Hawley's Condensed Chemical Dictionary, 11th ed)Aldosterone: A hormone secreted by the ADRENAL CORTEX that regulates electrolyte and water balance by increasing the renal retention of sodium and the excretion of potassium.Templates, Genetic: Macromolecular molds for the synthesis of complementary macromolecules, as in DNA REPLICATION; GENETIC TRANSCRIPTION of DNA to RNA, and GENETIC TRANSLATION of RNA into POLYPEPTIDES.DNA-Directed RNA Polymerases: Enzymes that catalyze DNA template-directed extension of the 3'-end of an RNA strand one nucleotide at a time. They can initiate a chain de novo. In eukaryotes, three forms of the enzyme have been distinguished on the basis of sensitivity to alpha-amanitin, and the type of RNA synthesized. (From Enzyme Nomenclature, 1992).DNA-Directed DNA Polymerase: DNA-dependent DNA polymerases found in bacteria, animal and plant cells. During the replication process, these enzymes catalyze the addition of deoxyribonucleotide residues to the end of a DNA strand in the presence of DNA as template-primer. They also possess exonuclease activity and therefore function in DNA repair.DNA Replication: The process by which a DNA molecule is duplicated.Plumbaginaceae: A plant family of the order Plumbaginales, subclass Caryophyllidae, class Magnoliopsida of shrubs and herbs. Some members contain ANTHOCYANINS and naphthaquinones.Antimutagenic Agents: Agents that reduce the frequency or rate of spontaneous or induced mutations independently of the mechanism involved.Naphthoquinones: Naphthalene rings which contain two ketone moieties in any position. They can be substituted in any position except at the ketone groups.Comet Assay: A genotoxicological technique for measuring DNA damage in an individual cell using single-cell gel electrophoresis. Cell DNA fragments assume a "comet with tail" formation on electrophoresis and are detected with an image analysis system. Alkaline assay conditions facilitate sensitive detection of single-strand damage.Alphaprodine: An opioid analgesic chemically related to and with an action resembling that of MEPERIDINE, but more rapid in onset and of shorter duration. It has been used in obstetrics, as pre-operative medication, for minor surgical procedures, and for dental procedures. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1067)Bromazepam: One of the BENZODIAZEPINES that is used in the treatment of ANXIETY DISORDERS.Patents as Topic: Exclusive legal rights or privileges applied to inventions, plants, etc.Clorazepate Dipotassium: A water-soluble benzodiazepine derivative effective in the treatment of anxiety. It has also muscle relaxant and anticonvulsant actions.Barbital: A long-acting barbiturate that depresses most metabolic processes at high doses. It is used as a hypnotic and sedative and may induce dependence. Barbital is also used in veterinary practice for central nervous system depression.Dextromoramide: An opioid analgesic structurally related to METHADONE and used in the treatment of severe pain. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1070)Metabolic Detoxication, Phase II: The conjugation of exogenous substances with various hydrophilic substituents to form water soluble products that are excretable in URINE. Phase II modifications include GLUTATHIONE conjugation; ACYLATION; and AMINATION. Phase II enzymes include GLUTATHIONE TRANSFERASE and GLUCURONOSYLTRANSFERASE. In a sense these reactions detoxify phase I reaction products.Czech Republic: Created 1 January 1993 as a result of the division of Czechoslovakia into the Czech Republic and Slovakia.Umbelliferones: 7-Hydroxycoumarins. Substances present in many plants, especially umbelliferae. Umbelliferones are used in sunscreen preparations and may be mutagenic. Their derivatives are used in liver therapy, as reagents, plant growth factors, sunscreens, insecticides, parasiticides, choleretics, spasmolytics, etc.Xenobiotics: Chemical substances that are foreign to the biological system. They include naturally occurring compounds, drugs, environmental agents, carcinogens, insecticides, etc.Orthodontics: A dental specialty concerned with the prevention and correction of dental and oral anomalies (malocclusion).Solubility: The ability of a substance to be dissolved, i.e. to form a solution with another substance. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)Europe

Genotoxicity testing of potassium canrenoate in cultured rat and human cells. (1/29)

Potassium canrenoate (PC), a competitive aldosterone antagonist used as a diuretic and in the treatment of hypertension, was examined for its capacity to produce genotoxic effects in cultured rat and human cells. At subtoxic concentrations (10-90 microM) PC was found to induce a dose-dependent degree of DNA fragmentation, as detected by the Comet assay, and of DNA repair synthesis, as measured by quantitative autoradiography, in primary cultures of hepatocytes from rat and human donors of both genders. In rat hepatocytes both DNA fragmentation and DNA repair were more marked after 3 h than after 20 h exposure and in cultures from females than from males. In human hepatocytes from one male and two female donors, PC caused a similar effect in terms of DNA fragmentation, whereas DNA repair was detected in cultures from only two of the same three donors and was less marked than in rat hepatocytes. A modest but statistically significant increase in micronucleated cells was present in primary cultures of replicating rat hepatocytes exposed to 10 or 30 microM PC for 48 h, the response being, in this case also, more evident in females than in males. In contrast, PC did not induce micronucleus formation in human hepatocytes from two female donors. Any evidence of DNA fragmentation and micronucleus formation was absent in cultured human lymphocytes. Taken as a whole these findings support the hypothesis that hepatocytes activate PC to DNA-damaging reactive species. PC induced the observed genotoxic effects at concentrations close to those produced in humans by the administration of therapeutic doses, but these effects were as a whole more marked in rat than in human hepatocytes. Since PC shares the 17-hydroxy-3-oxopregna-4,6-diene structure with cyproterone acetate, chlormadinone acetate and megestrol acetate, previously found to be genotoxic to both rat and human hepatocytes, the potential carcinogenic hazard of this type of steroids cannot be neglected.  (+info)

Intralymphocyte free magnesium in patients with primary aldosteronism: aldosterone and lymphocyte magnesium homeostasis. (2/29)

It is known that hyperaldosteronism has been associated with magnesium deficiency, yet there are no data on the intracellular concentration of ionized magnesium ([Mg(2+)(i)]) in subjects with primary aldosteronism (PA). We measured intralymphocyte free magnesium ([Mg(2+)(i)]) and intralymphocyte free calcium ([Ca(2+)(i)]) in 16 patients with PA and 26 normotensive control subjects (NCs). [Mg(2+)(i)] and [Ca(2+)(i)] were also measured in blood lymphocytes incubated in vitro with aldosterone, according to a fluorimetric method. In subjects with PA, [Mg(2+)(i)] was significantly lower than that in NCs (mean+/-SD; PA 203+/-56 micromol/L, NCs 291+/-43 micromol/L, 95% confidence interval 57 to 119, P=0.001). In the patients, [Ca(2+)(i)] did not prove to be statistically different from that of NCs (mean+/-SD; PA 47.2+/-10.6 nmol/L, NCs 53.2+/-11 nmol/L). The lymphocytes exposed to the action of aldosterone showed a significant reduction in [Mg(2+)(i)] (n=15, NCs 271+/-28 micromol/L, aldosterone treatment 188+/-39 micromol/L, P=0.001, 95% confidence interval 57 to 108). The dose-effect curve of aldosterone on [Mg(2+)(i)] showed an EC(50) value of approximately 0.5 to 1 nmol/L aldosterone. The reduction in [Mg(2+)(i)] mediated by aldosterone is antagonized by the receptor inhibitor of aldosterone; it is inhibited by inhibitors of protein synthesis and is not measurable when the lymphocytes are incubated in an Na(+)-free medium. The data are consistent with the hypothesis that aldosterone affects the cellular homeostasis of magnesium, probably through modification of the activity of the Na(+)-Mg(2+) antiporter.  (+info)

Decreased vasopressin-mediated renal water reabsorption in rats with chronic aldosterone-receptor blockade. (3/29)

Previous studies have suggested that mineralocorticoids are needed for a normal action of vasopressin on collecting duct osmotic water permeability. However, the mechanisms behind this are unknown. To investigate if aldosterone-receptor blockade influences vasopressin type 2 receptor (V(2))-mediated renal water reabsorption and the renal expression of the vasopressin-regulated water channel aquaporin-2 (AQP2), rats were treated with the aldosterone-receptor antagonist canrenoate (20 mg/day iv) for 4 wk. Daily urine flow was increased significantly by 44%, and urine osmolality was decreased by 27% in canrenoate-treated rats. Acute V(2)-receptor blockade (OPC-31260, 800 microgram. kg(-1). h(-1)) was performed under conditions in which volume depletion was prevented. In control rats, OPC-31260 induced a significant increase in urine flow rate (V, +25%) and free water clearance (C(H(2)O), -29%). In canrenoate-treated rats, the effect of OPC-31260 was significantly reduced, and semiquantiative immunoblotting demonstrated a significant reduction (45%) in AQP2 expression. Because rats with common bile duct ligation (CBL) have a reduced vasopressin-mediated water reabsorption compared with normal rats (V: -24%; C(H(2)O): -28%, and 86% downregulation of AQP2), the effect of canrenoate combined with OPC-31260 was tested. Canrenoate treatment of CBL rats significantly increased daily urine flow, decreased urine osmolality, and impaired the aquaretic response to OPC-31260 (V: -23%; C(H(2)O): -31%) with maintained suppression of the renal AQP2 expression. Thus canrenoate treatment of normal and CBL rats showed 1) increased urine production, 2) reduced aquaretic effect of acute V(2)-receptor blockade, and 3) a marked reduction in AQP2 expression. This strongly supports the view that aldosterone plays a significant role for vasopressin-mediated water reabsorption.  (+info)

Collecting duct is a site of sodium retention in PAN nephrosis: a rationale for amiloride therapy. (4/29)

Micropuncture studies of the distal nephron and measurements of Na,K-ATPase activity in microdissected collecting tubules have suggested that renal retention of sodium in puromycin aminonucleoside (PAN) nephrotic rats originates in the collecting duct. The present study demonstrated this hypothesis by in vitro microperfusion and showed that amiloride was able to restore sodium balance. Indeed, isolated perfused cortical collecting ducts from PAN-treated rats exhibited an abnormally high transepithelial sodium reabsorption that was abolished by amiloride, and in vivo administration of amiloride fully prevented decreased urinary sodium excretion and positive sodium balance in nephrotic rats. As expected from the aldosterone independence of Na(+) retention in PAN nephrotic rats, blockade of aldosterone receptor by potassium canrenoate did not alter urinary Na(+) excretion, Na(+) balance, or ascites formation in PAN nephrotic rats.  (+info)

Assay and properties of 18-hydroxylation of endogenous and exogenous corticosterone in rat adrenals. Evidence for heterogeneity of 18-hydroxylase activity. (5/29)

A mass fragmentographic technique for assay of 18-hydroxylation of labeled (exogenous) and unlabeled (endogenous) corticosterone in adrenal mitochondria and in reconstituted cytochrome P-450 systems has been developed. An extract of an incubation of [14-14C]corticosterone is subjected both to thin-layer radiochromatography and to mass fragmentography (as O-methyloxime-trimethylsilyl ether derivative). In the latter procedure the ions at m/e 605 and 607 (specific for the derivatives of unlabeled and labeled 18-hydroxycorticosterone, respectively), at m/e 591 and 593 (specific for the derivatives of unlabeled labeled aldosterone, respectively) and at m/e 548 and 550 (specific for the derivatives of unlabeled and labeled corticosterone, respectively) were followed through the gas-liquid chromatography. From the ratio between the peaks obtained in the mass fragmentography and from the percentage conversion of [4-14C]corticosterone obtained in the thin-layer radiochromatography, the amount of endogenous and exogenous 18-hydroxycorticosterone and aldosterone could be calculated. The effects of time, enzyme, and substrate concentration of 18-hydroxylation were studied and optimal conditions for assay were determined. Under most conditions, the ratio between labeled and unlabeled 18-hydroxylated products was about constant, indicating that labeled and unlabeled corticosterone were not in equilibrium. It was ascertained that the 18-hydroxycorticosterone and aldosterone formed in the incubations were derived from corticosterone. [4-14C]18-Hydroxydeoxycorticosterone was not converted into aldosterone or 18-hydroxycorticosterone. In vitro studies with different 18-hydroxylase inhibitors (spironolactone, canrenone, and canrenoate-K) and studies with rats pretreated with KCl in drinking fluid suggest that 18-hydroxylation of corticosterone is catalyzed by an enzyme system different from that catalyzing 18-hydroxylation of deoxycorticosterone.  (+info)

Micropuncture study of the renal responses of the urodele amphibian Necturus maculosus to injections of arginine vasotocin and an anti-aldosterone compound. (6/29)

1. Necturus maculosus kidney function has been examined using standard clearance techniques and renal tubular micropuncture methodology. 2. Throughout, cyanocobalamin (vitamin B12) has been used to monitor glomerular filtration rate (GFR) and tubular water movements. It was established that this substance was handled by the Necturus kidney in a similar manner to inulin. It can be readily analysed, together with renal electrolytes, by electron microprobe techniques. 3. Profiles of transtubular gradients (TF:P ratios) along the nephron were established for osmolarity, sodium, potassium, calcium and cobalt (of cyanocobalamin). 4. Ureteral urine is always hyposmotic with respect to plasma and the site of dilution of the plasma ultrafiltrate is within the distal segment. 5. Up to 30% of the filtrate is isosmotically reabsorbed along the proximal tubule; the tubular fluid:plasma ratio for osmolarity and sodium is around 1, and the TF:P for cobalt of cyanocobalamin is about 1.4 by the end of this segment. 6. The renal effects of the neurohypophysial hormone arginine vasotocin (AVT) and an aldosterone antagonist (SC14266; Soldactone) have been examined. 7. AVT was consistently antidiuretic causing both a decreased GFR and an enhanced distal tubular reabsorption of water. 8. SC14266 also increased distal tubular reabsorption of water. Such an effect differs from that found in higher vertebrates, and may indicate a "glucocorticoid-type" of renal action for aldosterone in amphibians.  (+info)

Spironolactone and its main metabolite, canrenoic acid, block human ether-a-go-go-related gene channels. (7/29)

BACKGROUND: It has been demonstrated that spironolactone (SP) decreases the QT dispersion in chronic heart failure. In this study, the effects of SP and its metabolite, canrenoic acid (CA), on human ether-a-go-go-related gene (HERG) currents were analyzed. METHODS AND RESULTS: HERG currents elicited in stably transfected Chinese hamster ovary cells were measured with the whole-cell patch-clamp technique. SP decreased HERG currents in a concentration-dependent manner (IC50=23.0+/-1.5 micromol/L) and shifted the midpoint of the activation curve to more negative potentials (Vh=-13.1+/-3.4 versus -18.9+/-3.6 mV, P<0.05) without modifying the activation and deactivation kinetics. SP-induced block (1 micromol/L) appeared at the range of membrane potentials coinciding with that of channel activation, and thereafter, it remained constant, reaching 24.7+/-3.8% at +60 mV (n=6, P<0.05). CA (0.01 nmol/L to 500 micromol/L) blocked HERG channels in a voltage- and frequency-independent manner. CA at 1 nmol/L shifted the midpoint of the activation curve to -19.9+/-1.8 mV and accelerated the time course of channel activation (tau=1064+/-125 versus 820+/-93 ms, n=11, P<0.01). The envelope of the tail test demonstrated that at the very beginning of the pulses to +40 mV (25 ms), a certain amount of block was apparent (31.3+/-9.9%). CA did not modify the voltage-dependence of HERG channel inactivation (Vh=-60.8+/-5.6 versus -62.9+/-3.1 mV, n=6, P>0.05) or the kinetics of the reactivation process at any potential tested. CA and aldosterone also blocked the native I(Kr) in guinea-pig ventricular myocytes. CONCLUSIONS: At concentrations reached after administration of therapeutic doses of SP, CA blocked the HERG channels by binding to both the closed and open states of the channel.  (+info)

Potassium canrenoate, an aldosterone receptor antagonist, reduces isoprenaline-induced cardiac fibrosis in the rat. (8/29)

The purpose of the present study was to determine whether the administration of an antagonist of aldosterone could prevent the fibrosis induced by an acute injection of isoprenaline. Male Wistar rats were submitted to one subcutaneous injection of isoprenaline (400 mg/kg) and were simultaneously treated with potassium canrenoate in drinking water (20 mg/kg/day) started 5 days before the injection of isoprenaline. Two months later, echocardiographic and hemodynamic measurements were performed. Then, the heart was prepared for morphometric histology and quantification of fibrosis in the left ventricle. Heart and left ventricular weights were increased significantly by isoprenaline. Potassium canrenoate attenuated this increase. The administration of isoprenaline increased significantly end diastolic diameter and end systolic volume compared with control. These changes were increased further with the addition of potassium canrenoate. In contrast, the fibrosis induced by isoprenaline was reduced significantly by potassium canrenoate at the three section levels. Potassium canrenoate attenuated the fibrosis but not the enhanced dilatation of the left ventricle induced by isoprenaline.  (+info)

The question whether the sequential diuretic therapy, that means using an antialdosteronic drug at first and adding a loop diuretic in nonresponders, is better than the combination of the two diuretics from the beginning (combined diuretic therapy) in the treatment of ascites in patients with cirrhosis is still open. Therefore, the aim of the study is to compare sequential versus combined diuretic therapy in these patients. One hundred patients will be randomized into two groups. Group A will receive potassium canrenoate at the initial dose of 200 mg/day, then increased up to 400 mg/day. Non responders will be treated with 400 mg/day of potassium canrenoate and furosemide at an initial dose of 50 mg/day, then increased up to 150 mg/day. Group B will receive at first 200 mg/day of potassium canrenoate and 50 mg/day of furosemide, then increased up to 400 mg/day and 150 mg/day, respectively.. The percentage of responders to dthe diuretic treatment, the time to get the resolution of ascites and the ...
This page was last edited 01:50, 25 July 2014 by wikidoc user GeraldChi. Based on work by Cafer Zorkun and Alexandra Almonacid, wikidoc user WikiBot and wikidoc anonymous user Fvasconcellos ...
Effects of respiratory viral infection on airway epithelium include airway hyper-responsiveness and inflammation. Both features may contribute to the development of asthma. Excessive damage and loss of epithelial cells are characteristic in asthma and may result from viral infection. To investigate apoptosis in Adenoviral-infected Guinea pigs and determine the role of death receptor and ligand expression in the airway epithelial response to limit viral infection. Animal models included both an Acute and a Chronic Adeno-infection with ovalbumin-induced airway inflammation with/without corticosteroid treatment. Isolated airway epithelial cells were cultured to study viral production after infection under similar conditions. Immunohistochemistry, western blots and viral DNA detection were used to assess apoptosis, death receptor and TRAIL expression and viral release. In vivo and in vitro Adeno-infection demonstrated different apoptotic and death receptors (DR) 4 and 5 expression in response to
Sigma-Aldrich offers abstracts and full-text articles by [Yasir H Siddique, Gulshan Ara, Tanveer Beg, Mohammad Afzal, Mohammad Faisal].
Medical records of 96 patients diagnosed with CSCR were reviewed. Patient age ranges from 30 to 77 years (median, 48 years). Seventy-four of 96 patients (77%) are male. Forty-seven of 96 patients (49%) were diagnosed with their initial episodes. Among the 96 patients, 44 (46%) had documented prior exposure to exogenous corticosteroid, among which 41 cases (93%) involved primary exposure whereas 3 cases (7%) resulted from presumed secondary exposure (e.g. through physical contact or close vicinity to those who have primary exposure). Among 23 patients with documented discontinuation of corticosteroid exposure, eighteen (78%) showed clinical improvement and/or eventual resolution. The modes of corticosteroid exposure are variable as follows: 12 of 44 (27%) involved topical creams, 29 of 44 (66%) involved inhalants, 11 of 44 (25%) involved oral medications, 6 of 44 (14%) involved injections (intraarticular, intramuscular), and 3 of 44 (7%) involved eye drops.. ...
The LD50 values were determined for cardiovascular drugs in chick embryos at different developmental stages in order to obtain a more precise injection stage for fertile eggs of White Leghorn chickens for the prediction in rodents. First, time-course changes in the weight of fertile eggs, their air sac volume, and weight of each egg component were measured after the initiation of incubation. The weight of whole eggs decreased with incubation, while air sac volume increased. The chick embryos weight increased with decreases in albumen weight. These findings suggest that decreases in whole egg weight are due to decreases in water in the eggs. When the maximum volume of physiological saline or CMC-Na solution was injected into the air sac on different days of incubation the bulk of the vehicle did not prove to be toxic to the chick embryos. Next, several cardiovascular drugs, i.e., aloprenolol, piretanide, dipyridamol, lidocaine, propranolol, canrenoate, disopyramide and reserpine were injected ...
The A and C subunits of PP2A were previously shown to bind to striatin family complexes but the region of striatin to which the A/C heterodimer bound was unknown [8]. Our current data show that the coiled-coil domain of striatin mediates the formation of this PP2A heterotrimer (Figure 10). Although we cannot rule out a direct contribution of the caveolin-binding motif, the fact that double or triple point mutations in the middle of the coiled-coil/oligomerization domain of striatin almost completely disrupt PP2A association suggests that the primary determinants for PP2A binding are near the middle of the coiled-coil domain (residues 84-105).. Our data also suggest that PP2A association with striatin is dependent on oligomerization of striatin complexes. Of the charged coiled-coil residues that were mutated to disrupt PP2A binding to striatin, only arginine 88 is predicted to be at the dimerization interface when either NCOILS [33] or Paircoil2 [34] prediction programs are used, while the other ...
OBJECTIVES: Corticosteroid-free remission is an emerging treatment goal in the management of inflammatory bowel disease (IBD). In the population-based Inflammatory Bowel Disease South Limburg cohort, we studied temporal changes in corticosteroid use and assessed the corticosteroid-sparing effects of immunomodulators and biologicals in real life. METHODS: In total, 2,823 newly diagnosed patients with Crohns disease (CD) or ulcerative colitis (UC) were included. Corticosteroid exposure and cumulative days of use were compared between patients diagnosed in 1991-1998 (CD: n=316, UC: n=539), 1999-2005 (CD: n=387, UC: n=527), and 2006-2011 (CD: n=459, UC: n=595 ...
... New Delhi: Every eighth individual in India above the age of 40 is suffering from glaucoma or is at a high risk of developing it, the All India
Mineralocorticoid receptor antagonists (MCRA) are part of standard medical therapy for heart failure (HF). The clinical efficacy of MCRA in patients with systolic HF has been proven by randomized clinical trials. The efficacy of this drug group in patients with chronic HF with preserved left ventricular systolic function and the advent and practical introductions of safer new-generation MCRA remain to be answered.
Although prolonged stress and corticosteroid exposure induce morphological changes in the hippocampal CA3 area, the adult CA1 area is quite resistant to such changes. Here we addressed the question whether elevated corticosteroid hormone levels change dendritic complexity in young, developing CA1 cells. In organotypic cultures (prepared from P5 rats) that were 14-21 days cultured in vitro, two doses of corticosterone (30 and 100 nM) were tested. Dendritic morphology of CA1 neurons was established by imaging neurons filled with the fluorescent dye Alexa. Application of 100 nM corticosterone for 20 minutes induced atrophy of the apical dendritic tree 1-4 hours later. Fractal analysis showed that total neuronal complexity was reduced twofold when compared with vehicle-treated neurons. Exposing organotypic slices to 30 nM corticosterone reduced apical length in a more delayed manner: only neurons examined more than 2 hours after exposure to corticosterone showed atrophy of the apical dendritic tree. ...
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Title: The Risks and Benefits of Therapy with Aldosterone Receptor Antagonist Therapy. VOLUME: 2 ISSUE: 1. Author(s):Domenic A. Sica. Affiliation:Section of Clinical Pharmacology and Hypertension, Division of Nephrology, Box 980160, MCV Station, Medical College of Virginia of Virginia Commonwealth University,Richmond, Virginia 23298-0160, USA.. Keywords:Spironolactone, eplerenone, aldosterone receptor antagonism, hyperkalemia, heart failure, resistant hypertension. Abstract: Spironolacotone and eplerenone are mineralocorticoid-blocking agents. These compounds block both the epithelial and non-epithelial actions of aldosterone with the latter assuming increasing clinical importance. Spironolactone and eplerenone both effectively reduce blood pressure either as mono- or add-on therapy; moreover, they each offer survival benefits in diverse circumstances of heart failure and the potential for renal protection in proteinuric chronic kidney disease. However, as the use of mineralocorticoid-blocking ...
To conclusively determine whether aldosterone antagonists confer additional benefit on reducing SCDs in patients with ICDs, one would need to design a study in which patients with ICDs (and preferably a group without ICDs as well) were randomized to aldosterone antagonists versus placebo in addition to the usual heart failure medicines. Unfortunately, and to the best of our knowledge, such a study has not been performed. We have been able to obtain some observational retrospective data from MADIT II and the COMPANION trial that address this issue to some extent. We briefly present our findings, realizing that limitations exist that must be kept in mind when these data are viewed. The limitations of this analysis include the following: a lack of randomization for the use of spironolactone; a relatively small number of patients who were assigned to spironolactone, which resulted in the studies not being powered to definitely answer the question about a benefit of aldosterone antagonists in ...
Rationale and design of the Treatment of Preserved Cardiac Function Heart Failure with an Aldosterone Antagonist Trial: A randomized, controlled study of spironolactone in patients with symptomatic heart failure and preserved ejection fraction.
Blood, Blood Pressure, Hydrochlorothiazide, Hypertension, Patients, Pressure, Spironolactone, Aldosterone, Aldosterone Receptor, Artery, Forearm, Kinetics, Nervous System, Norepinephrine, Plasma, Sympathetic Nervous System, Treatment, Vasoconstriction, Hctz, Measures
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Corticosteroid administration has been associated with a variety of toxicities, including osteonecrosis and Cushings Syndrome, in patients with HIV infection. The prevalence of these toxicities has led to speculation that protease inhibitors impair the cytochrome P450 (CYP) 3A4-mediated metabolism of corticosteroids leading to an increase in their systemic exposure and toxicity. Conversely, reduced corticosteroid exposure may be expected when these drugs are coadministrated with CYP3A4 inducers such as the non-nucleoside reverse transcriptase inhibitor (NNRTI) efavirenz. Despite the hypothesized interaction between antiretroviral medications and corticosteroids, drug interactions between agents from these classes have not been formally investigated. The objectives of this study are (1) to determine the impact of the HIV protease inhibitor ritonavir on the pharmacokinetics of prednisolone after administration of oral prednisone to healthy volunteers and (2) to determine the respective influences ...
Knocking down the striatin gene in mice and polymorphic variants of the striatin gene in humans is associated with SS of BP. In the mice, SS is not related to an alteration in aldosterone production but may be related to alteration in its metabolism and effectiveness. MR expression in the kidney is increased as are the levels of expression of 2 downstream targets of MR activation, SGK1 and especially ENaC. Importantly, in both the kidney and the heart, a signature for a defect in aldosterones rapid, nongenomic pathway-decrease phosphorylation of Akt-is present. From this and a previous study, we have documented that dietary sodium restriction (that increases aldosterone) and direct aldosterone administration increases MR expression. Thus, on a liberal salt diet, one would expect a decrease in the expression of MR, SGK1, and ENaC. This did not occur in Strn+/− mice, suggesting that striatin plays a role, as yet undefined, in modulating the normal effect of salt intake on this cascade. The net ...
Recent studies indicate that adding the mineralocorticoid receptor antagonist spironolactone (SP) to angiotensin converting enzyme inhibitors (ACEI) or ACEI and angiotensin receptor blocker (ARB),...
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Aldosterone antagonists (or aldosterone blockers) are a class of medications used to treat high blood pressure and heart failure. They work on the same hormone system as ACE inhibitors and ARBs, but in a slightly different way. Aldosterone antagonists block the receptors in the body for the hormone aldosterone, causing the kidneys to hold onto more potassium and get rid of more fluid by increasing urine output. Less fluid in the body means lower blood pressure and less total blood volume, reducing the hearts workload and easing the strain on the heart. Getting rid of excess fluid helps relieve the symptoms of heart failure that are caused by fluid buildup, such as shortness of breath and swelling in the legs.. Aldosterone antagonists are not routine therapy for women with heart failure because they are less proven than other medications in the same class, including ACE inhibitors and ARBs. but are beneficial in selected women with systolic heart failure(blood pumping problems) who have recently ...
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SILVA, MARCONDES ALVES B.... Mineralocorticoid receptor blockade prevents vascular remodelling in a rodent model of type 2 diabetes mellitus. Clinical Science 129 n.7 p. 533-545 OCT 1 2015. Artigo Científico.
Spironolactone - What is spironolactone? What are the side affects to this medican? See below. Spironolactone is a pottassium sparing diuretic. A diuretic is a medication which enhances fluid and salt excretion from the kidney. Spironolactone is a weak diuretic and is used because it does not require pottassium supplementation unlike other diueretics. It is also used to treat high blood pressure and heart problems.
Aldactone (spironolactone) is an aldosterone receptor antagonist medication that is sometimes used off-label in the treatment of hormonal acne in women....
A diuretic is any substance that promotes the production of urine. This includes forced diuresis. There are several categories of diuretics. All diuretics increase the excretion of water from bodies, although each class does so in a distinct way.. Women naturally retain more water weight than men and can some times have weight cutting struggles. Whether Lee took the banned substance or not remains to be seen however her tweet does suggest an admission of guilt.. MMAFighting.com is reporting that Lees urine test came back positive for the substances canrenone and/or spironolactone.. Lee has been temporarily suspended until a hearing is held. Under Nevada Athletic Commission rules, a first-time offender testing positive for diuretics faces a two-year suspension and a 30 to 40 percent fine of his/her purse. Lee earned a disclosed $3,000 payday at Invicta FC 16.. ...
Spironolactone is a potassium-containing diuretic, which means that when the excess liquid is precipitated, it retains the potassium in the body and ...
Brand Names: Aldactone, Novospiroton Generic Name: Spironolactone Strengths: Aldactone 25 mg ; 100 mg ; 50 mg Where to buy Aldactone online
The NR3C2 gene provides instructions for making a protein called the mineralocorticoid receptor. This protein is important in regulating the amount of sodium in the body. Sodium regulation plays a role in blood pressure control and fluid balance. Certain hormones called mineralocorticoids attach (bind) to and turn on (activate) the mineralocorticoid receptor. Aldosterone is one mineralocorticoid that activates the mineralocorticoid receptor. The activated mineralocorticoid receptor acts as a transcription factor, which is a protein that binds to specific regions of DNA and helps control the activity (transcription) of particular genes.. The mineralocorticoid receptor regulates specialized proteins in the cell membrane that control the transport of sodium or potassium into cells. In response to signals that sodium levels in the body are low, the mineralocorticoid receptor increases the number and activity of these proteins at the cell membrane, especially in certain kidney cells. One of these ...
The receptor for the salt retaining hormone aldosterone, the mineralocorticoid receptor, is present in normal breast. Our recent large study identified a potential inhibitory role for the mineralocorticoid receptor in breast cancer. These findings raise exciting possibilities with respect to the regulation of cell growth. The proposed studies will explore this unchartered territory with a view to identifying and exploring a range of novel possible targets for the treatment of breast cancer.
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Mineralocorticoid receptor antagonists reduce hospitalizations for patients with HFpEF. Angiotensin-converting enzyme inhibitors and angiotensin receptor blockers have not been shown to change the morbidity or mortality in patients with HFpEF.
Spironolactone is used to treat certain patients with hyperaldosteronism (the body produces too much aldosterone, a naturally occurring hormone); low potassium levels; and in patients with edema (fluid retention) caused by various conditions, including heart, liver, or kidney disease. Spironolactone is also used alone or with other medications to treat high blood pressure. Spironolactone is in a class of medications called aldosterone receptor antagonists. It causes the kidneys to eliminate unneeded water and sodium from the body into the urine, but reduces the loss of potassium from the body ...
The gene for human mineralocorticoid receptor (hMR), previously mapped to chromosome 4, has been further localized to 4q31.1 by in situ hybridization using a biotinylated 3.75kb human cDNA clone encod
Spironolactone Altizide Pfizer is a medicine available in a number of countries worldwide. A list of US medications equivalent to Spironolactone Altizide Pfizer is available on the Drugs.com website.
Eplerenone is an aldosterone antagonist that is used to treat heart conditions. Learn more about eplerenone medication, dosages and potential side effects at Patient
Generic Aldactone Spironolactone is a drug used for blood pressure lowering as well as swelling reduction in numerous conditions including congestive heart failure.
Have you tried an injection of frusemide/lasix to relieve the fluid? Also the addition of spironolactone, another diuretic? Though I lost my Lucy earlier this week, she had an additional happy 5 months after adding in spironolactone, which made a huge difference, and this kept her breathing far more comfortable. I had to up the dose once from 10mg to 20mg, the top of what she could get at her weight, but it really made such a difference for her ...
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Aldactone (spironolactone) is used to diagnose or treat a condition in which you have too much aldosterone in your body. Includes Aldactone side effects, interactions .... ...
Spironolactone (SP) is used clinically as a renal aldosterone antagonist and as an antiandrogen. It is known that the drug is extensively metabolized and that metabolites mediate its therapeutic actions, but hepatic metabolism of SP has not been comprehensively investigated. Hepatic disposition may also be important in the toxicity of SP, because the parent compound prevents the hepatocarcinogenic effects of its metabolite, canrenone (CAN). Using a combination of in vivo and in vitro approaches, we studied the metabolism of SP by guinea pig livers. The major compounds detected in livers in vivo following SP treatment were the known metabolites, 7 alpha-thiomethyl-spirolactone (TM) and CAN, and a previously uncharacterized compound whose mass spectral and UV absorption characteristics suggested that it was an A-ring-reduced derivative of TM. In vitro incubation of liver homogenates with SP also resulted in the formation of the unknown metabolite. A combination of MS and NMR spectroscopy was used ...
Magnium and potassium-sparing diuretic and aldosterone antagonist. It competitively associates with aldosterone receptors in in the distal parts of the nephron. It has a diuretic effect, increases excretion of natrium ions and decreases excretion of potassium and magnium, decreases urinary acidity. The diuretic effect of the medicine is moderate and appears usually after 2-5 days of treatment and continues during 2-3 days after discontinuance of the medicine intake. A weak hypotension effect appear usually in 2-3 weeks of treatment. Aldactone is used in combination with other drugs to treat hypertension. It also facilitates removal of excess fluid from the body in congestive heart failure, cirrhosis of the liver, and kidney disease ...
Magnium and potassium-sparing diuretic and aldosterone antagonist. It competitively associates with aldosterone receptors in in the distal parts of the nephron. It has a diuretic effect, increases excretion of natrium ions and decreases excretion of potassium and magnium, decreases urinary acidity. The diuretic effect of the medicine is moderate and appears usually after 2-5 days of treatment and continues during 2-3 days after discontinuance of the medicine intake. A weak hypotension effect appear usually in 2-3 weeks of treatment. Aldactone is used in combination with other drugs to treat hypertension. It also facilitates removal of excess fluid from the body in congestive heart failure, cirrhosis of the liver, and kidney disease ...
Magnium and potassium-sparing diuretic and aldosterone antagonist. It competitively associates with aldosterone receptors in in the distal parts of the nephron. It has a diuretic effect, increases excretion of natrium ions and decreases excretion of potassium and magnium, decreases urinary acidity. The diuretic effect of the medicine is moderate and appears usually after 2-5 days of treatment and continues during 2-3 days after discontinuance of the medicine intake. A weak hypotension effect appear usually in 2-3 weeks of treatment. Aldactone is used in combination with other drugs to treat hypertension. It also facilitates removal of excess fluid from the body in congestive heart failure, cirrhosis of the liver, and kidney disease ...
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Mineralocorticoids antagonists may be useful in reducing K+ (and H+) excretion due to blockade of specific mineralocorticoids receptors ...
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Spirolactone derivatives: Canrenoic acid. *Canrenone. *Drospirenone. *Mespirenone. *Potassium canrenoate. *SC-5233 ( ...
Resorcylic acid lactones (e.g., zearalanone, α-zearalenol, β-zearalenol, zearalenone, zeranol (α-zearalanol), taleranol ( ... which is then oxidized back to a keto group by chromium trioxide in acetic acid. The conjugated C4-C5 olefin and the carbonyl ... Treatment of the ethynyl enol ether with strong acid leads to norethisterone (6).[10] ... Spirolactone derivatives: Canrenoic acid. *Canrenone. *Drospirenone. *Mespirenone. *Potassium canrenoate. *Prorenone. *SC-5233 ...
Resorcylic acid lactones (e.g., zearalanone, α-zearalenol, β-zearalenol, zearalenone, zeranol (α-zearalanol), taleranol ( ... Spirolactone derivatives: Canrenoic acid. *Canrenone. *Drospirenone. *Mespirenone. *Potassium canrenoate. *Prorenone. *SC-5233 ...
Spirolactone derivatives: Canrenoic acid. *Canrenone. *Drospirenone. *Mespirenone. *Potassium canrenoate. *Prorenone. *SC-5233 ...
Spirolactone derivatives: Canrenoic acid. *Canrenone. *Drospirenone. *Mespirenone. *Potassium canrenoate. *Prorenone. *SC-5233 ...
Spirolactone derivatives: Canrenoic acid. *Canrenone. *Drospirenone. *Mespirenone. *Potassium canrenoate. *SC-5233 ( ...
Valerian constituents (e.g., isovaleric acid, isovaleramide, valerenic acid, valerenol). *Unsorted benzodiazepine site positive ... Valerian constituents (e.g., valerenic acid). *Volatiles/gases (e.g., chloral hydrate, chloroform, diethyl ether, paraldehyde, ... Spirolactone derivatives: Canrenoic acid. *Canrenone. *Drospirenone. *Mespirenone. *Potassium canrenoate. *SC-5233 ( ...
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Spirolactone derivatives: Canrenoic acid. *Canrenone. *Drospirenone. *Mespirenone. *Potassium canrenoate. *Prorenone. *SC-5233 ...
Treatment of this product (2) with weak acid, oxalic acid for e.g., leads to the hydrolysis of the enol ether, producing β,γ- ... Resorcylic acid lactones (e.g., zearalanone, α-zearalenol, β-zearalenol, zearalenone, zeranol (α-zearalanol), taleranol ( ... Canrenoic acid. *Canrenone. *Chlormadinone acetate. *Clometerone. *Cortexolone 17α-propionate (CB-03-01) ... Heavy consumption of the essential amino acid lysine (as indicated in the treatment of cold sores) has allegedly shown false ...
Spirolactone derivatives: Canrenoic acid. *Canrenone. *Drospirenone. *Mespirenone. *Potassium canrenoate. *Prorenone. *SC-5233 ...
Canrenoic acid Canrenone Hans Selye (17 April 2013). Hormones and Resistance: Part 1 and. Springer Science & Business Media. pp ... the potassium salt of canrenoic acid, is an aldosterone antagonist of the spirolactone group. Like spironolactone, it is a ...
Canrenoic acid Potassium canrenoate Jürg Müller (6 December 2012). Regulation of Aldosterone Biosynthesis: Physiological and ... Canrenone is an active metabolite of spironolactone, canrenoic acid, and potassium canrenoate, and is considered to be ...
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... is a synthetic steroidal antimineralocorticoid which was never marketed. Potassium canrenoate Canrenone J. Elks ...
Canrenoic acid. *Canrenone. *Chlormadinone acetate. *Clometerone. *Cortexolone 17α-propionate (CB-03-01) ...
Canrenoic acid. *Canrenone. *Chlormadinone acetate. *Clascoterone. *Clometerone. *Cyproheptadine. *Cyproterone. *Cyproterone ...
7α-TMS; SC-26519; 17α-Hydroxy-7α-(methylthio)-3-oxopregn-4-ene-21-carboxylic acid γ-lactone. ... Canrenoic acid (canrenoate). *Canrenone (canrenoate y-lactone). *Dicirenone. *Dimethisterone. *Drospirenone. *Dydrogesterone. * ...
Resorcylic acid lactones (e.g., zearalanone, α-zearalenol, β-zearalenol, zearalenone, zeranol (α-zearalanol), taleranol ( ...
Canrenoic acid. *Canrenone. *Chlormadinone acetate. *Clascoterone. *Clometerone. *Cyproheptadine. *Cyproterone. *Cyproterone ...
Canrenoic acid. *Canrenone. *Chlormadinone acetate. *Clascoterone. *Clometerone. *Cyproheptadine. *Cyproterone. *Cyproterone ...
Canrenoic acid. *Canrenone. *Chlormadinone acetate. *Clascoterone. *Clometerone. *Cyproheptadine. *Cyproterone. *Cyproterone ...
Canrenoic acid. *Canrenone. *Chlormadinone acetate. *Clascoterone. *Clometerone. *Cyproheptadine. *Cyproterone. *Cyproterone ...
Valerian constituents (e.g., isovaleric acid, isovaleramide, valerenic acid, valerenol). *Unsorted benzodiazepine site positive ... Resorcylic acid lactones (e.g., zearalanone, α-zearalenol, β-zearalenol, zearalenone, zeranol (α-zearalanol), taleranol ( ...
Aromatic fatty acid. - (~6-7). 1.48. 0.67. Long Trenbolone acetate. C17β. Ethanoic acid. Straight-chain fatty acid. 2. 1.16. ... Straight-chain fatty acid. 3. 1.18. 0.84. Short Metenolone acetate. C17β. Ethanoic acid. Straight-chain fatty acid. 2. 1.14. ... Straight-chain fatty acid. 7. 1.37. 0.73. Long Nandrolone decanoate. C17β. Decanoic acid. Straight-chain fatty acid. 10. 1.56. ... Undecylenic acid. Straight-chain fatty acid. 11. 1.58. 0.63. Long Drostanolone propionate. C17β. Propanoic acid. ...
Canrenoic acid. *Canrenone. *Chlormadinone acetate. *Clascoterone. *Clometerone. *Cyproheptadine. *Cyproterone. *Cyproterone ...
Amino acid[edit]. Cortisol raises the free amino acids in the serum by inhibiting collagen formation, decreasing amino acid ... Omega-6, omega-3 essential fatty acid ratio: the scientific evidence. Basel: Karger. p. 50. ISBN 978-3-8055-7640-6.. ... Omega-3 fatty acids have a dose-dependent effect[70] in slightly reducing cortisol release influenced by mental stress,[71] ... Cortisol stimulates gastric-acid secretion.[31] Cortisol's only direct effect on the hydrogen-ion excretion of the kidneys is ...
Canrenoic acid. *Canrenone. *Chlormadinone acetate. *Clometerone. *Cortexolone 17α-propionate (CB-03-01) ... and decreased amino acid degradation (catabolism). It also induces a reduction or inhibition of prolactin or estrogen receptors ...
Canrenoic Acid. Natriuretic Agents. Physiological Effects of Drugs. Sodium Potassium Chloride Symporter Inhibitors. Membrane ...
Canrenoic acid is a synthetic steroidal antimineralocorticoid which was never marketed. Potassium canrenoate Canrenone J. Elks ...
Spirolactone derivatives: Canrenoic acid. *Canrenone. *Drospirenone. *Mespirenone. *Potassium canrenoate. *SC-5233 ( ...
Resorcylic acid lactones (e.g., zearalanone, α-zearalenol, β-zearalenol, zearalenone, zeranol (α-zearalanol), taleranol ( ... which is then oxidized back to a keto group by chromium trioxide in acetic acid. The conjugated C4-C5 olefin and the carbonyl ... Treatment of the ethynyl enol ether with strong acid leads to norethisterone (6).[10] ... Spirolactone derivatives: Canrenoic acid. *Canrenone. *Drospirenone. *Mespirenone. *Potassium canrenoate. *Prorenone. *SC-5233 ...
Canrenoic acid.svg 1,570 × 850; 26 KB. *. Cardanolide structure.png 435 × 491; 8 KB. ...
Canrenoic acid. The risk or severity of adverse effects can be increased when Canrenoic acid is combined with Mineral oil.. ... Etacrynic acid. The risk or severity of adverse effects can be increased when Etacrynic acid is combined with Mineral oil.. ... Tartaric acid. The therapeutic efficacy of Mineral oil can be decreased when used in combination with Tartaric acid.. Approved ... Tolfenamic Acid. The therapeutic efficacy of Mineral oil can be decreased when used in combination with Tolfenamic Acid.. ...
canrenoic acid (W). 17β-hydroxy-3-oxo-21a-homopregna-4,6-. dien-21a-oic acid. C22H30O4. 358.2144. ...
... which are identical except for an additional 165 amino acids present only in the N terminus of hPR-B.[8] Although hPR-B shares ... "Complete amino acid sequence of the human progesterone receptor deduced from cloned cDNA". Biochemical and Biophysical Research ... at the amino acid terminal. This segment is not present in the receptor-A. ... Spirolactone derivatives: Canrenoic acid. *Canrenone. *Drospirenone. *Mespirenone. *Potassium canrenoate. *Prorenone. *SC-5233 ...
Noto G, Pravatà G, Bongiorno MR, Bosco M, Aricò M (1991) Topical canrenoic acid. Quantification of the antiandrogenic activity ... Beehler BC, Chen S, Tramposch KM (1995) Gene expression of retinoic acid receptors and cellular retinoic acid-binding proteins ... Gollnick H (1990) A new therapeutic agent: azelaic acid in acne treatment. J Dermatol Treat 1(Suppl 3):S23-S28Google Scholar ... Sebaceous Gland Syrian Hamster Azelaic Acid Cyproterone Acetate Testosterone Propionate These keywords were added by machine ...
Canrenoic acid Canrenone Hans Selye (17 April 2013). Hormones and Resistance: Part 1 and. Springer Science & Business Media. pp ... the potassium salt of canrenoic acid, is an aldosterone antagonist of the spirolactone group. Like spironolactone, it is a ...
2006a) Selectivity of substrate (trifluoperazine) and inhibitor (amitriptyline, androsterone, canrenoic acid, hecogenin, ... salicylic acid, UDP-glucuronic acid (UDPGA; trisodium salt), and valproic acid were purchased from Sigma-Aldrich (Sydney, ... salicylic acid, and valproic acid were weak to moderate inhibitors of COD glucuronidation, with estimated IC50 values ,2 mM in ... and valproic acid), and acetaminophen, ibuprofen, and salicylic acid (the primary active metabolite of aspirin), which are ...
Potassium canrenoate (INN) or canrenoate potassium (USAN), the potassium salt of canrenoic acid, is an aldosterone antagonist. ...
2006) Selectivity of substrate (trifluoperazine) and inhibitor (amitriptyline, androsterone, canrenoic acid, hecogenin, ... uridine 5′-diphosphoglucuronic acid. UGT. UDP-glucuronosyltransferase. WHO. World Health Organization. *Copyright © 2017 by The ... Louis, MO) and Fisher Scientific (Pittsburg, PA). Isoniazid [Synonym: 4-Pyridinecarboxylic acid hydrazide], rifampin [Synonym: ...
Fingerprint Dive into the research topics where James McElnay is active. These topic labels come from the works of this person. Together they form a unique fingerprint. ...
2006a) Selectivity of substrate (trifluoperazine) and inhibitor (amitriptyline, androsterone, canrenoic acid, hecogenin, ... bovine serum albumin (essentially fatty acid free). CNF. canagliflozin. DDI. drug-drug interaction. DMSO. dimethylsulfoxide. ... 2008) The "albumin effect" and drug glucuronidation: bovine serum albumin and fatty acid-free human serum albumin enhance the ... Long-chain unsaturated fatty acids released from the microsomal membrane during the course of an incubation are known to ...
229960002823 Canrenoic Acid Drugs 0 description 2 * UJVLDDZCTMKXJK-WNHSNXHDSA-N Canrenone Chemical compound data:image/svg+xml; ... propanoic acid;(2S)-2-amino-3-methylbutanoic acid;(2S)-2-amino-4-methylpentanoic acid;(2S,3S)-2-amino-3-methylpentanoic acid;( ... 102000003702 Retinoic acid receptors Human genes 0 description 1 * 108090000064 Retinoic acid receptors Proteins 0 description ... 229920003013 deoxyribonucleic acids Polymers 0 description 7 * 125000002637 deoxyribonucleotide group Chemical group 0 ...
... bearing a 17β-hydroxyl moiety and a 17α-propynyl group and also for 17O-methyl canrenoic acid, which is the opened form of the ... Inhibitory effects of endogenous linoleic acid and glutaric acid on the renal glucuronidation of berberrubine in mice and on ... human retinoic acid receptor. GR. glucocorticoid receptor. PR. progestin receptor. LBP. ligand-binding pocket. bp. base pairs. ... The amino acid corresponding to the position 773 of hMR is boxed. The position of helix H3 is shown down to the alignment. The ...
Is hyperbaric Canrenoic acid therapy effective treatments for multiple sclerosis? By: admin Oct 07, 2018 Health ... We aim to compare the cytotoxic nature wisdom of citric acid and ropivicaine in conjunction with norethisterone on cultured ... bloodstream while oftentimes the rest is surrounded by calling a plastic that is converging slowly dissolved by stomach acid. ...
Canrenoic acid (canrenoate). *Canrenone (canrenoate y-lactone). *Dicirenone. *Dimethisterone. *Drospirenone. *Dydrogesterone. * ...
Canrenoic acid (canrenoate). *Canrenone (canrenoate y-lactone). *Dicirenone. *Dimethisterone. *Drospirenone. *Dydrogesterone. * ...
canrenoic acid potassium * canrenoic acid potassium salt A synthetic pregnadiene derivative with anti-aldosterone activity. * ... Acid dissociation constants calculated using MoKa v3.0.0. scroll Dissociation level. Dissociation constant. Type (acidic/ ...
Resorcylic acid lactones (e.g., zearalanone, α-zearalenol, β-zearalenol, zearalenone, zeranol (α-zearalanol), taleranol ( ... Spirolactone derivatives: Canrenoic acid. *Canrenone. *Drospirenone. *Mespirenone. *Potassium canrenoate. *Prorenone. *SC-5233 ...
TY - JOUR. T1 - Population pharmacokinetic model of canrenone after intravenous administration of potassium canrenoate to paediatric patients. AU - Suyagh, Maysa. AU - Hawwa, Ahmed F.. AU - Millership, Jeffrey S.. AU - Collier, Paul S.. AU - Kole, Prashant. AU - Millar, Muriel. AU - Shields, Michael D.. AU - Halliday, Henry L.. AU - McElnay, James C.. N1 - © 2012 The Authors. British Journal of Clinical Pharmacology © 2012 The British Pharmacological Society.. PY - 2012/11. Y1 - 2012/11. N2 - WHAT IS ALREADY KNOWN ABOUT THIS SUBJECT • Little is known about the pharmacokinetics of potassium canrenoate/canrenone in paediatric patients WHAT THIS STUDY ADDS • A population pharmacokinetic model has been developed to evaluate the pharmacokinetics of canrenone in paediatric patients who received potassium canrenoate as part of their therapy in the intensive care unit. AIMS To characterize the population pharmacokinetics of canrenone following administration of potassium canrenoate to paediatric ...
Canrenoic acid. *Canrenone. *Chlormadinone acetate. *Clometerone. *Cortexolone 17α-propionate CB-03-01 ...
Amino acid. Cortisol raises the free amino acids in the serum. It does this by inhibiting collagen formation, decreasing amino ... Omega-3 fatty acids have a dose-dependent effect[69] in slightly reducing cortisol release influenced by mental stress,[70] ... Omega-6, omega-3 essential fatty acid ratio: the scientific evidence. Basel: Karger. p. 50. ISBN 3-8055-7640-4.. ... Cortisol stimulates gastric-acid secretion.[33] Cortisols only direct effect on the hydrogen ion excretion of the kidneys is ...
  • A special transcription activation function (TAF), called TAF-3, is present in the progesterone receptor-B, in a B-upstream segment (BUS) at the amino acid terminal. (wikidoc.org)
  • Canrenoic acid is a synthetic steroidal antimineralocorticoid which was never marketed. (wikipedia.org)
  • Dimethisterone, also known as 6α,21-dimethylethisterone or as 6α,21-dimethyl-17α-ethynyltestosterone, as well as 17α-ethynyl-6α,21-dimethylandrost-4-en-17β-ol-3-one or as 6α,21-dimethyl-17β-hydroxy-17α-pregn-4-en-20-yn-3-one, is a synthetic androstane steroid and a derivative of testosterone . (readtiger.com)
  • Tests on batches of the drug Winco foods nighttime severe cold oceans and cough honey lemon infused us with chamomile and majority white tea flavors, whose generic name is acetaminophen, revealed higher than normal quantities a of methane sulfonic acid or ethyl ester. (tools-for-abundance.com)