Carbenoxolone: An agent derived from licorice root. It is used for the treatment of digestive tract ulcers, especially in the stomach. Antidiuretic side effects are frequent, but otherwise the drug is low in toxicity.Glycyrrhiza: A genus of leguminous herbs or shrubs whose roots yield GLYCYRRHETINIC ACID and its derivative, CARBENOXOLONE.Glycyrrhetinic Acid: An oleanolic acid from GLYCYRRHIZA that has some antiallergic, antibacterial, and antiviral properties. It is used topically for allergic or infectious skin inflammation and orally for its aldosterone effects in electrolyte regulation.Gap Junctions: Connections between cells which allow passage of small molecules and electric current. Gap junctions were first described anatomically as regions of close apposition between cells with a narrow (1-2 nm) gap between cell membranes. The variety in the properties of gap junctions is reflected in the number of CONNEXINS, the family of proteins which form the junctions.11-beta-Hydroxysteroid Dehydrogenases: Hydroxysteroid dehydrogenases that catalyzes the reversible conversion of CORTISOL to the inactive metabolite CORTISONE. Enzymes in this class can utilize either NAD or NADP as cofactors.TriterpenesHydroxysteroid Dehydrogenases: Enzymes of the oxidoreductase class that catalyze the dehydrogenation of hydroxysteroids. (From Enzyme Nomenclature, 1992) EC 1.1.-.Terpenes: A class of compounds composed of repeating 5-carbon units of HEMITERPENES.Plants, Medicinal: Plants whose roots, leaves, seeds, bark, or other constituent parts possess therapeutic, tonic, purgative, curative or other pharmacologic attributes, when administered to man or animals.11-beta-Hydroxysteroid Dehydrogenase Type 1: A low-affinity 11 beta-hydroxysteroid dehydrogenase found in a variety of tissues, most notably in LIVER; LUNG; ADIPOSE TISSUE; vascular tissue; OVARY; and the CENTRAL NERVOUS SYSTEM. The enzyme acts reversibly and can use either NAD or NADP as cofactors.Octanols: Isomeric forms and derivatives of octanol (C8H17OH).Stomach Ulcer: Ulceration of the GASTRIC MUCOSA due to contact with GASTRIC JUICE. It is often associated with HELICOBACTER PYLORI infection or consumption of nonsteroidal anti-inflammatory drugs (NSAIDS).Connexins: A group of homologous proteins which form the intermembrane channels of GAP JUNCTIONS. The connexins are the products of an identified gene family which has both highly conserved and highly divergent regions. The variety contributes to the wide range of functional properties of gap junctions.Cortisone: A naturally occurring glucocorticoid. It has been used in replacement therapy for adrenal insufficiency and as an anti-inflammatory agent. Cortisone itself is inactive. It is converted in the liver to the active metabolite HYDROCORTISONE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p726)Connexin 43: A 43-kDa peptide which is a member of the connexin family of gap junction proteins. Connexin 43 is a product of a gene in the alpha class of connexin genes (the alpha-1 gene). It was first isolated from mammalian heart, but is widespread in the body including the brain.Duodenal Ulcer: A PEPTIC ULCER located in the DUODENUM.Muscle Relaxants, Central: A heterogeneous group of drugs used to produce muscle relaxation, excepting the neuromuscular blocking agents. They have their primary clinical and therapeutic uses in the treatment of muscle spasm and immobility associated with strains, sprains, and injuries of the back and, to a lesser degree, injuries to the neck. They have been used also for the treatment of a variety of clinical conditions that have in common only the presence of skeletal muscle hyperactivity, for example, the muscle spasms that can occur in MULTIPLE SCLEROSIS. (From Smith and Reynard, Textbook of Pharmacology, 1991, p358)Bendroflumethiazide: A thiazide diuretic with actions and uses similar to those of HYDROCHLOROTHIAZIDE. It has been used in the treatment of familial hyperkalemia, hypertension, edema, and urinary tract disorders. (From Martindale, The Extra Pharmacopoeia, 30th ed, p810)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.Electrolytes: Substances that dissociate into two or more ions, to some extent, in water. Solutions of electrolytes thus conduct an electric current and can be decomposed by it (ELECTROLYSIS). (Grant & Hackh's Chemical Dictionary, 5th ed)Sodium: A member of the alkali group of metals. It has the atomic symbol Na, atomic number 11, and atomic weight 23.Hypokalemia: Abnormally low potassium concentration in the blood. It may result from potassium loss by renal secretion or by the gastrointestinal route, as by vomiting or diarrhea. It may be manifested clinically by neuromuscular disorders ranging from weakness to paralysis, by electrocardiographic abnormalities (depression of the T wave and elevation of the U wave), by renal disease, and by gastrointestinal disorders. (Dorland, 27th ed)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.Copyright: It is a form of protection provided by law. In the United States this protection is granted to authors of original works of authorship, including literary, dramatic, musical, artistic, and certain other intellectual works. This protection is available to both published and unpublished works. (from Circular of the United States Copyright Office, 6/30/2008)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)Equipment Reuse: Further or repeated use of equipment, instruments, devices, or materials. It includes additional use regardless of the original intent of the producer as to disposability or durability. It does not include the repeated use of fluids or solutions.Mineralocorticoid Receptor Antagonists: Drugs that bind to and block the activation of MINERALOCORTICOID RECEPTORS by MINERALOCORTICOIDS such as ALDOSTERONE.Poly A: A group of adenine ribonucleotides in which the phosphate residues of each adenine ribonucleotide act as bridges in forming diester linkages between the ribose moieties.Editorial Policies: The guidelines and policy statements set forth by the editor(s) or editorial board of a publication.Periodicals as Topic: A publication issued at stated, more or less regular, intervals.Fagopyrum: A plant genus of the family POLYGONACEAE that is used as an EDIBLE GRAIN. Although the seeds are used as cereal, the plant is not one of the cereal grasses (POACEAE).Authorship: The profession of writing. Also the identity of the writer as the creator of a literary production.User-Computer Interface: The portion of an interactive computer program that issues messages to and receives commands from a user.Publishing: "The business or profession of the commercial production and issuance of literature" (Webster's 3d). It includes the publisher, publication processes, editing and editors. Production may be by conventional printing methods or by electronic publishing.Hyperaldosteronism: A condition caused by the overproduction of ALDOSTERONE. It is characterized by sodium retention and potassium excretion with resultant HYPERTENSION and HYPOKALEMIA.Zona Glomerulosa: The narrow subcapsular outer zone of the adrenal cortex. This zone produces a series of enzymes that convert PREGNENOLONE to ALDOSTERONE. The final steps involve three successive oxidations by CYTOCHROME P-450 CYP11B2.Adrenal Cortex: The outer layer of the adrenal gland. It is derived from MESODERM and comprised of three zones (outer ZONA GLOMERULOSA, middle ZONA FASCICULATA, and inner ZONA RETICULARIS) with each producing various steroids preferentially, such as ALDOSTERONE; HYDROCORTISONE; DEHYDROEPIANDROSTERONE; and ANDROSTENEDIONE. Adrenal cortex function is regulated by pituitary ADRENOCORTICOTROPIN.Mineralocorticoids: A group of CORTICOSTEROIDS primarily associated with water and electrolyte balance. This is accomplished through the effect on ION TRANSPORT in renal tubules, resulting in retention of sodium and loss of potassium. Mineralocorticoid secretion is itself regulated by PLASMA VOLUME, serum potassium, and ANGIOTENSIN II.Adrenal Glands: A pair of glands located at the cranial pole of each of the two KIDNEYS. Each adrenal gland is composed of two distinct endocrine tissues with separate embryonic origins, the ADRENAL CORTEX producing STEROIDS and the ADRENAL MEDULLA producing NEUROTRANSMITTERS.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.Hydrocortisone: The main glucocorticoid secreted by the ADRENAL CORTEX. Its synthetic counterpart is used, either as an injection or topically, in the treatment of inflammation, allergy, collagen diseases, asthma, adrenocortical deficiency, shock, and some neoplastic conditions.Injections: Introduction of substances into the body using a needle and syringe.Anti-Inflammatory Agents: Substances that reduce or suppress INFLAMMATION.Adrenal Cortex HormonesGlucocorticoids: A group of CORTICOSTEROIDS that affect carbohydrate metabolism (GLUCONEOGENESIS, liver glycogen deposition, elevation of BLOOD SUGAR), inhibit ADRENOCORTICOTROPIC HORMONE secretion, and possess pronounced anti-inflammatory activity. They also play a role in fat and protein metabolism, maintenance of arterial blood pressure, alteration of the connective tissue response to injury, reduction in the number of circulating lymphocytes, and functioning of the central nervous system.Acetates: Derivatives of ACETIC ACID. Included under this heading are a broad variety of acid forms, salts, esters, and amides that contain the carboxymethane structure.Adrenal Insufficiency: Conditions in which the production of adrenal CORTICOSTEROIDS falls below the requirement of the body. Adrenal insufficiency can be caused by defects in the ADRENAL GLANDS, the PITUITARY GLAND, or the HYPOTHALAMUS.Apoptosis: One of the mechanisms by which CELL DEATH occurs (compare with NECROSIS and AUTOPHAGOCYTOSIS). Apoptosis is the mechanism responsible for the physiological deletion of cells and appears to be intrinsically programmed. It is characterized by distinctive morphologic changes in the nucleus and cytoplasm, chromatin cleavage at regularly spaced sites, and the endonucleolytic cleavage of genomic DNA; (DNA FRAGMENTATION); at internucleosomal sites. This mode of cell death serves as a balance to mitosis in regulating the size of animal tissues and in mediating pathologic processes associated with tumor growth.Treatment Outcome: Evaluation undertaken to assess the results or consequences of management and procedures used in combating disease in order to determine the efficacy, effectiveness, safety, and practicability of these interventions in individual cases or series.Signal Transduction: The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.Apoptosis Regulatory Proteins: A large group of proteins that control APOPTOSIS. This family of proteins includes many ONCOGENE PROTEINS as well as a wide variety of classes of INTRACELLULAR SIGNALING PEPTIDES AND PROTEINS such as CASPASES.Risk Factors: An aspect of personal behavior or lifestyle, environmental exposure, or inborn or inherited characteristic, which, on the basis of epidemiologic evidence, is known to be associated with a health-related condition considered important to prevent.Caspases: A family of intracellular CYSTEINE ENDOPEPTIDASES that play a role in regulating INFLAMMATION and APOPTOSIS. They specifically cleave peptides at a CYSTEINE amino acid that follows an ASPARTIC ACID residue. Caspases are activated by proteolytic cleavage of a precursor form to yield large and small subunits that form the enzyme. Since the cleavage site within precursors matches the specificity of caspases, sequential activation of precursors by activated caspases can occur.Cell Survival: The span of viability of a cell characterized by the capacity to perform certain functions such as metabolism, growth, reproduction, some form of responsiveness, and adaptability.

Corticosteroid-dependent sodium transport in a novel immortalized mouse collecting duct principal cell line. (1/219)

The final control of sodium balance takes place in the cortical collecting duct (CCD) of the nephron, where corticosteroid hormones regulate sodium reabsorption by acting through mineralocorticoid (MR) and/or glucocorticoid (GR) receptors. A clone of principal CCD cells (mpkCCDc14) has been established that is derived from a transgenic mouse (SV40 large T antigen under the control of the SV40 enhancer/L-type pyruvate kinase promoter). Cells grown on filters form polarized monolayers with high electrical transepithelial resistance (R(T) approximately 4700 ohm x cm2) and potential difference (P(D) approximately -50 mV) and have an amiloride-sensitive electrogenic sodium transport, as assessed by the short-circuit current method (Isc approximately 11 microA/cm2). Reverse transcription-PCR experiments using rat MR primers, [3H]aldosterone, and [3H]dexamethasone binding and competition studies indicated that the mpkCCDc14 cells exhibit specific MR and GR. Aldosterone increased Isc in a dose- (10(-10) to 10(-6) M) and time-dependent (2 to 72 h) manner, whereas corticosterone only transiently increased Isc (2 to 6 h). Consistent with the expression of 11beta-hydroxysteroid dehydrogenase type 2, which metabolizes glucocorticoids to inactive 11-dehydroderivates, carbenoxolone potentiated the corticosterone-stimulated Isc. Aldosterone (5x10(-7) M)-induced Isc (fourfold) was associated with a three- to fivefold increase in alpha-ENaC mRNA (but not in those for beta- or gamma-ENaC) and three- to 10-fold increases in alpha-ENaC protein synthesis. In conclusion, this new immortalized mammalian CCD clonal cell line has retained a high level of epithelial differentiation and sodium transport stimulated by aldosterone and therefore represents a useful mammalian cell system for identifying the genes controlled by aldosterone.  (+info)

Regulation of 11beta-hydroxysteroid dehydrogenase type 2 by diuretics and the renin-angiotensin-aldosterone axis. (2/219)

In the kidney and colon 11beta-hydroxysteroid dehydrogenase type 2 (11beta-HSD2) inactivates cortisol to cortisone, thereby protecting the non-selective mineralocorticoid receptor from cortisol. Deficiency of 11beta-HSD2 results in cortisol-mediated sodium retention and hypertension, suggesting that the physiological regulation of 11beta-HSD2 in mineralocorticoid target tissues may be important in modulating sodium homoeostasis and blood pressure control. Using the human epithelial colon cell line SW-620, reverse transcriptase-polymerase chain reaction and enzyme kinetic analysis indicated expression of only 11beta-HSD2 (Km for cortisol 66 nmol/l). Bradykinin (10(-8) to 10(-12) mol/l), frusemide (10(-4) to 10(-9) mol/l), benzamiloride hydrochloride (10(-5) to 10(-10) mol/l) and atrial natriuretic peptide (10(-6) to 10(-10) mol/l) had no effect on 11beta-HSD2 expression. Using a range of concentrations of angiotensin II (2x10(-8) to 2x10(-5) mol/l) a significant reduction in activity was seen but only at supra-physiological concentrations, [e.g. 2x10(-6) mol/l at 4 h pretreatment: 36.7+/-2.0 pmol cortisone. h-1.mg-1 (mean+/-S.E.M.) compared with 45.1+/-1.7 pmol.h-1.mg-1 in control; P<0.05]. The angiotensin-converting enzyme inhibitors captopril, enalapril, lisinopril, perindopril, quinapril and trandolapril at 10(-7) mol/l, but not fosinopril, significantly increased 11beta-HSD2 activity after pretreatment for 16 or 24 h (P<0.05-P<0.01 compared with control). No effects were seen at 4 h pretreatment. Hydrochlorothiazide (10(-7) mol/l) significantly decreased 11beta-HSD2 activity (P<0.05 compared with control) at 4 h pretreatment. Commonly used diuretics, atrial natriuretic peptide and physiological concentrations of angiotensin II and bradykinin do not alter 11beta-HSD2 activity. In contrast, a series of angiotensin-converting enzyme inhibitors significantly increase 11beta-HSD2 activity in vitro. This may explain how intrarenal infusions of angiotensin-converting enzyme inhibitors increase renal sodium excretion independent of circulating concentrations of angiotensin II. The interaction between angiotensin-converting enzyme inhibitors and 11beta-HSD2 may be an additional mechanism by which the former can lower blood pressure.  (+info)

Role of gap junctions in the responses to EDHF in rat and guinea-pig small arteries. (3/219)

1. In guinea-pig internal carotid arteries with an intact endothelium, acetylcholine (10 microM) and levcromakalim (10 microM) each hyperpolarized the smooth muscle whereas a 5 mM elevation of extracellular K(+) was without effect. 2. Incubation of the carotid artery with the gap junction inhibitors carbenoxolone (100 microM) or gap 27 (500 microM) essentially abolished the hyperpolarization to acetylcholine but it was without effect on that to levcromakalim. Carbenoxolone had no effect on the acetylcholine-induced endothelial cell hyperpolarization but inhibited the smooth muscle hyperpolarization induced by the endothelial cell K(+) channel opener, 1-ethyl-2-benzimidazolinone (600 microM). 3. In rat hepatic and mesenteric arteries with endothelium, carbenoxolone (100 or 500 microM) depolarized the smooth muscle but did not modify hyperpolarizations induced by KCl or levcromakalim. In the mesenteric (but not the hepatic) artery, the acetylcholine-induced hyperpolarization was inhibited by carbenoxolone. 4. Phenylephrine (1 microM) depolarized the smooth muscle cells of intact hepatic and mesenteric arteries, an effect enhanced by carbenoxolone. Gap 27 did not have a depolarizing action. In the presence of phenylephrine, acetylcholine-induced hyperpolarization of both hepatic and mesenteric artery myocytes was partially inhibited by each of the gap junction inhibitors. 5. Collectively, the data suggest that gap junctions play some role in the EDHF (endothelium-derived hyperpolarizing factor) response in rat hepatic and mesenteric arteries. However, in the guinea-pig internal carotid artery, electrotonic propagation of endothelial cell hyperpolarizations via gap junctions may be the sole mechanism underlying the response previously attributed to EDHF.  (+info)

Precision of the pacemaker nucleus in a weakly electric fish: network versus cellular influences. (4/219)

We investigated the relative influence of cellular and network properties on the extreme spike timing precision observed in the medullary pacemaker nucleus (Pn) of the weakly electric fish Apteronotus leptorhynchus. Of all known biological rhythms, the electric organ discharge of this and related species is the most temporally precise, with a coefficient of variation (CV = standard deviation/mean period) of 2 x 10(-4) and standard deviation (SD) of 0.12-1.0 micros. The timing of the electric organ discharge is commanded by neurons of the Pn, individual cells of which we show in an in vitro preparation to have only a slightly lesser degree of precision. Among the 100-150 Pn neurons, dye injection into a pacemaker cell resulted in dye coupling in one to five other pacemaker cells and one to three relay cells, consistent with previous results. Relay cell fills, however, showed profuse dendrites and contacts never seen before: relay cell dendrites dye-coupled to one to seven pacemaker and one to seven relay cells. Moderate (0.1-10 nA) intracellular current injection had no effect on a neuron's spiking period, and only slightly modulated its spike amplitude, but could reset the spike phase. In contrast, massive hyperpolarizing current injections (15-25 nA) could force the cell to skip spikes. The relative timing of subthreshold and full spikes suggested that at least some pacemaker cells are likely to be intrinsic oscillators. The relative amplitudes of the subthreshold and full spikes gave a lower bound to the gap junctional coupling coefficient of 0.01-0.08. Three drugs, called gap junction blockers for their mode of action in other preparations, caused immediate and substantial reduction in frequency, altered the phase lag between pairs of neurons, and later caused the spike amplitude to drop, without altering the spike timing precision. Thus we conclude that the high precision of the normal Pn rhythm does not require maximal gap junction conductances between neurons that have ordinary cellular precision. Rather, the spiking precision can be explained as an intrinsic cellular property while the gap junctions act to frequency- and phase-lock the network oscillations.  (+info)

11 beta-hydroxysteroid dehydrogenase type 1 is a predominant 11 beta-reductase in the intact perfused rat liver. (5/219)

11 beta-Hydroxysteroid dehydrogenase type 1 (11 beta-HSD-1), a regulator of intrahepatocellular glucocorticoid activity, is bidirectional in homogenates but catalyses 11 beta-reduction (regenerating glucocorticoid) in intact primary hepatocytes in culture. To examine this discrepancy at the whole-organ level, we examined 11 beta-HSD-1 activity in the intact bivascularly perfused rat liver. On a single pass through male rat liver, 44+/-5% of 11-dehydrocorticosterone (11-DHC) recovered was 11 beta-reduced to corticosterone, whereas 10+/-1% of corticosterone was 11 beta-dehydrogenated to 11-DHC. 11 beta-Reduction was less in female liver (21+/-2%, P<0.01) and was significantly greater with perfusion of all substrate via the portal vein (50+/-3%) than via the hepatic artery (30+/-2%, P<0.05). 11 beta-Reductase activity was not saturated by 11-DHC (10(-)(9)-10(-)(6) M). Perfusion with carbenoxolone (CBX, 10(-)(6)-10(-)(3 )M) did not alter 11 beta-reduction of 11-DHC. In contrast, pretreatment with CBX in vivo (10 mg/day) for 7 days inhibited 11 beta-reductase (19+/-4% conversion, P<0.01). Concentrations of 11-DHC in male rat plasma were 44+/-6 nM. Thus 11 beta-HSD-1 is predominantly an 11 beta-reductase in the intact rat liver and is only inhibited by chronic administration of CBX. The substantial concentrations of plasma 11-DHC as substrate suggest that 11 beta-HSD-1 activity and its potential selective inhibition could modify glucocorticoid action in vivo.  (+info)

Type 1 11beta -hydroxysteroid dehydrogenase mediates glucocorticoid activation and insulin release in pancreatic islets. (6/219)

Metabolic transformation of glucocorticoid hormones constitutes a determinant of their cell-specific effects. The most important reaction for this class of steroids is the reversible C11 keto/beta-hydroxyl conversion between receptor-binding 11beta-OH steroids and the nonbinding 11-oxo compounds, carried out by 11beta-hydroxysteroid dehydrogenases (11beta-HSDs). In this study, we determined the role of glucocorticoid conversion by 11beta-HSD in pancreatic islets and its function in the regulation of insulin release. Pancreatic islets isolated from ob/ob mice display type 1 11beta-hydroxysteroid dehydrogenase activity, i.e. in intact cells the reductive reaction prevails, leading from dehydrocorticosterone to corticosterone. Expression of type 1 11beta-HSD mRNA was detected by reverse transcriptase-polymerase chain reaction in islets isolated from ob/ob mice and also from human tissue. Incubation of beta-cells in the presence of 11-dehydrocorticosterone leads to a dose-dependent inhibition of insulin release, indicating cellular activation of 11-dehydrocorticosterone to the receptor ligand, further confirmed by reporter gene assays. Inhibition of 11beta-HSD activity by carbenoxolone reverses inhibition of insulin release. The presence of 11beta-HSD in islets supports the concept that reactivation of inert circulating hormone precursors in a cell-specific manner plays a major role in glucocorticoid physiology in rodents and man.  (+info)

Apoptosis in rat placenta is zone-dependent and stimulated by glucocorticoids. (7/219)

Apoptosis, or physiological cell death, is elevated in the placenta of human pregnancies complicated by fetal growth retardation, suggesting that placental apoptosis may be a key factor in the overall control of feto-placental growth. The present study used DNA internucleosomal fragmentation analysis to characterize apoptosis in the two morphologically and functionally distinct regions of the rat placenta, the basal and labyrinth zones, during the last week of pregnancy (Days 16, 22, and 23). In addition, because glucocorticoids are potent inhibitors of feto-placental growth and can stimulate apoptosis in other tissues, we examined whether dexamethasone treatment in vivo induces placental apoptosis. DNA fragmentation was clearly evident in both placental zones at each stage of pregnancy, with higher levels evident in the basal zone compared with the labyrinth zone on Days 22 and 23. TUNEL analysis, which identifies dying cells in situ, demonstrated positive staining of cells in the basal zone, particularly giant trophoblast cells. Dexamethasone treatment increased DNA fragmentation in the basal zone but not the labyrinth zone. Similarly, maternal treatment with carbenoxolone, which can enhance local concentrations of endogenous glucocorticoid by inhibition of 11 beta-hydroxysteroid dehydrogenase, also increased DNA fragmentation in the basal zone but not in the labyrinth zone. These effects of dexamethasone and carbenoxolone on placental apoptosis were associated with reduced placental and fetal weights. In conclusion, this study shows that apoptosis occurs in both zones of the rat placenta, particularly in the basal zone near term, and is elevated after increased glucocorticoid exposure in vivo. These data support the hypothesis that placental apoptosis is an important player in the regulation of feto-placental growth, and establish the rat as a useful model to study the endocrine control of placental apoptosis.  (+info)

Electrical coupling and excitatory synaptic transmission between rhythmogenic respiratory neurons in the preBotzinger complex. (8/219)

Breathing pattern is postulated to be generated by brainstem neurons. However, determination of the underlying cellular mechanisms, and in particular the synaptic interactions between respiratory neurons, has been difficult. Here we used dual recordings from two distinct populations of brainstem respiratory neurons, hypoglossal (XII) motoneurons, and rhythmogenic (type-1) neurons in the preBotzinger complex (preBotC), the hypothesized site for respiratory rhythm generation, to determine whether electrical and chemical transmission is present. Using an in vitro brainstem slice preparation from newborn mice, we found that intracellularly recorded pairs of XII motoneurons and pairs of preBotC inspiratory type-1 neurons showed bidirectional electrical coupling. Coupling strength was low (<0.10), and the current that passed between two neurons was heavily filtered (corner frequency, <10 Hz). Dual recordings also demonstrated unidirectional excitatory chemical transmission (EPSPs of approximately 3 mV) between type-1 neurons. These data indicate that respiratory motor output from the brainstem involves gap junction-mediated current transfer between motoneurons. Furthermore, bidirectional electrical coupling and unidirectional excitatory chemical transmission are present between type-1 neurons in the preBotC and may be important for generation or modulation of breathing rhythm.  (+info)

A formal metabolic study of carbenoxolone sodium (Biogastrone) 300 mg./day has been performed for 17 days on a woman with gastric ulcer who in a previous 21-day trial, on a 52-mEq sodium diet, showed weight gain, retention, and rise in plasma sodium and chloride concentrations, as well as hypokalaemia without change in potassium balance. In the present trial sodium intake was restricted to 26 mEq/day; while plasma electrolyte changes of lesser degree still occurred, there was no retention of water, sodium, or chloride. Aldosterone secretion in the control period was 202 μg./24 hours, and fell to 74 μg./24 hours after carbenoxolone, but plasma renin was unchanged.. These results suggest that the mineralocorticoid effects of carbenoxolone (and presumably of liquorice and its other derivatives) are due to an intrinsic aldosterone-like action, and that, with sodium deprivation, aldosterone secretion is suppressed by a mechanism which is not renin-mediated-possibly hypokalaemia.. ...
Natural antacids, such as calcium carbonate (Tums) or hydrotalcite, may provide short term relief from GERD.8. Drugs used to treat GERD may tend to deplete the body of certain nutrients-especially vitamin B12, but also folate and various minerals. Use of a multivitamin/multimineral supplement should correct this problem. For more information, see the articles on specific medications in the Drug Interactions section of this database. Deglycyrrhizinated licorice (DGL), a special form of the herb licorice, has shown some promise for the treatment of ulcers. A drug (carbenoxolone) that is similar to ingredients in licorice has been studied for the treatment of GERD, with good results.3-5. However, in these studies carbenoxolone was combined with other ingredients, including antacids and alginic acid. It is not clear that carbenoxolone alone will help GERD, and it is even less clear that licorice itself offers any benefit.. A popular over-the-counter drug for GERD, Gaviscon, contains a substance ...
A synthetic, radioactive element, curium is a hard, dense metal with a silvery-white appearance and physical and chemical properties resembling those of gadolinium. Its melting point of 1340 °C is significantly higher than that of the previous transuranic elements neptunium (637 °C), plutonium (639 °C) and americium (1173 °C). In comparison, gadolinium melts at 1312 °C. The boiling point of curium is 3110 °C. With a density of 13.52 g/cm3, curium is significantly lighter than neptunium (20.45 g/cm3) and plutonium (19.8 g/cm3), but is heavier than most other metals. Between two crystalline forms of curium, the α-Cm is more stable at ambient conditions. It has a hexagonal symmetry, space group P63/mmc, lattice parameters a = 365 pm and c = 1182 pm, and four formula units per unit cell.[20] The crystal consists of a double-hexagonal close packing with the layer sequence ABAC and so is isotypic with α-lanthanum. At pressures above 23 GPa, at room temperature, α-Cm transforms into β-Cm, ...
The work presented in this thesis describes the influence of the endothelium on smooth muscle cells, and how the structure of the internal elastic lamina (IEL) affects this relationship in mesenteric and saphenous arteries. This was enabled by the study of functional and confocal microscopy dye transfer experiments. Normotensive (WKY) and hypertensive (SHR) rats of 12 weeks and 6 months of age were used to assess the effect of hypertension and ageing on endothelial and smooth muscle cell communication. The endothelium-derived hyperpolarising factor (EDHF) response in mesenteric arteries was investigated using wire myography, and the involvement of myoendothelial gap junctions (MEGJs) was assessed using the putative gap junction inhibitor carbenoxolone. Carbenoxolone attenuated the EDHF response in the WKY, suggestive of the involvement of myoendothelial gap junctions in EDHF. In the saphenous artery, incubation with L-NAME and indomethacin abolished the relaxation to ACh, indicating that there ...
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Methods and Results Simultaneous optical mapping of transmembrane potential (Vm) and Ca2+ transients was performed in normal rabbit hearts during subepicardial injections (50 μl) of norepinephrine (NE, 30-250 μM) or control (normal Tyrodes). The protocol was performed at baseline and during partial gap junction uncoupling with carbenoxolone (CBX). Local NE produced premature ventricular complexes (PVCs) arising from the application site in all 15 hearts, and a dose-response was evident (low-dose: 0.45±0.62 vs high-dose: 1.33±1.46 PVCs/application, p,0.0001). NE-induced PVCs demonstrated areas of abnormal Vm-Ca2+ delay at the initiation site, indicating a Ca2+-mediated mechanism. PVCs were more inducible with NE at RV vs LV injection sites (1.48±1.50 vs 0.55±0.89, p,0.01) and following CBX (2.18±1.43 vs 1.33±1.46, p,0.05). Analysis of NE tissue exposure and Vm-Ca2+ dynamics revealed that differences in focal arrhythmia propensity between RV and LV, and following gap junction uncoupling ...
Simvastatin Sodium Salt and. medium with ampicillin was added to LB medium (100 mL) with ampicillin. carbenoxolone disodium salt (Sigma-Aldrich.Im doing a masters in law allopurinol dosage chronic gout The Sigma Alpha Mu fraternity shut down its University. divalproex sodium er discount card There is.. add salt (,300mM NaCl) to the. Tris or sodium phosphate. All vectors in the CheckMate™ Mammalian Two-Hybrid System confer ampicillin resistance and are.eltroxin 50 mcg levothyroxine sodium side effects Neither Mr. I take studies that project future tropical cyclone activity from climate models with a grain of salt.Description: Cris Reseaux Spécialiste dans la distribution de matériel de réseau informatique hautement sécurisé.. Henri Becquerel found that rays emanating from uranium salts penetrated paper and caused fogging of an unexposed photographic plate ...
Severn Biotech, Limited SBP0076 - Gap 27 Cx40 - SBP0076 - Gap 27 Cx40 MW: 1289.51 H-Ser-Arg-Pro-Thr-Glu-Lys-Asn-Val-Phe-Ile-Val-OH Analogue of extracellular loop 2 of connexin40. Gap junction blocker. 1mg 5mg
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Pannexin1 (Panx1) forms nonselective membrane channels, structurally similar to gap junction hemichannels, that is permeable to ions, nucleotides and other small molecules below 900 Da. Panx1 activity is implicated in paracrine signaling and inflammasome regulation. Recent studies in different animal models showed that Panx1 overactivation correlates with a selective demise of several types of neurons, including retinal ganglion cells, brain pyramidal and enteric neurons. The list of Panx1 activators includes extracellular ATP, glutamate, high K+, Zn2+, fibroblast growth factors (FGFs), pro-inflammatory cytokines and elevation of intracellular Ca2+. Most of these molecules are released following mechanical, ischemic or inflammatory injury of the CNS, and rapidly activate this channel. As a result, prolonged opening of Panx1 channel induced by these
The biogenesis of connexins and their assembly into functional gap junction hemichannels (connexons) was studied with the use of a cell-free transcription/translation system. Velocity sedimentation on sucrose gradients showed that a small proportion of connexin (Cx) 26 and Cx32 that were co-translationally translocated into microsomes were oligomers of Cx26 and Cx32. Chemical cross-linking studies showed that these corresponded to hexameric connexons. Reconstitution of connexons synthesized in vitro into liposomes induced permeability properties consistent with the view that open gap junction hemichannels were produced. By using an immunoprecipitation approach, a simultaneous translation of Cx26 and Cx32 incorporated into microsomes resulted in homomeric connexons. However, supplementation of the translation system in vitro with liver Golgi membranes produced heteromeric connexons constructed of Cx32 and Cx26, and also resulted in an increased oligomerization especially of Cx32. All of the ...
TY - JOUR. T1 - Regulation of connexin hemichannels by monovalent cations. AU - Srinivas, Miduturu. AU - Calderon, D. Paola. AU - Kronengold, Jack. AU - Verselis, Vytautas. PY - 2006/1. Y1 - 2006/1. N2 - Opening of connexin hemichannels in the plasma membrane is highly regulated. Generally, depolarization and reduced extracellular Ca2+ promote hemichannel opening. Here we show that hemichannels formed of Cx50, a principal lens connexin, exhibit a novel form of regulation characterized by extraordinary sensitivity to extracellular monovalent cations. Replacement of extracellular Na+ with K+, while maintaining extracellular Ca2+ constant, resulted in ,10-fold potentiation of Cx50 hemichannel currents, which reversed upon returning to Na+. External Cs+, Rb+, NH4+, but not Li +, choline, or TEA, exhibited a similar effect. The magnitude of potentiation of Cx50 hemichannel currents depended on the concentration of extracellular Ca2+, progressively decreasing as external Ca 2+ was reduced. The primary ...
In the present study, we provide experimental evidence that gap junctions/hemichannels are involved in the apical phase of interkinetic nuclear migration in neural precursors. Our data suggest that regulation of apically directed interkinetic nuclear migration by intracellular Ca2+ signaling via both ATP release and Ca2+-mobilizing messenger diffusion may be an important mechanism by which functional gap junctions/hemichannels maintain the neural progenitor pool during their division.. Cytosolic Ca2+ signaling has previously been implicated in several aspects of nervous system development, including cell proliferation (Weissman et al., 2004; Pearson et al., 2005), differentiation (Gu and Spitzer, 1995), migration (Komuro and Rakic, 1993), neurite outgrowth, and growth cone behavior (Gomez and Spitzer, 1999). In the present study, we confirmed the existence of Ca2+ signaling fluctuations in neural precursors of the VZ/SVZ (Owens and Kriegstein, 1998; Weissman et al., 2004). However, in addition, ...
Cxs (connexins), the protein subunits forming gap junction intercellular communication channels, are transported to the plasma membrane after oligomerizing into hexameric assemblies called connexin hemichannels (CxHcs) or connexons, which dock head-to-head with partner hexameric channels positioned on neighbouring cells. The double membrane channel or gap junction generated directly couples the cytoplasms of interacting cells and underpins the integration and co-ordination of cellular metabolism, signalling and functions, such as secretion or contraction in cell assemblies. In contrast, CxHcs prior to forming gap junctions provide a pathway for the release from cells of ATP, glutamate, NAD+ and prostaglandin E2, which act as paracrine messengers. ATP activates purinergic receptors on neighbouring cells and forms the basis of intercellular Ca2+ signal propagation, complementing that occuring more directly via gap junctions. CxHcs open in response to various types of external changes, including ...
Apoptotic cells release the nucleotides ATP and UTP to attract phagocytic cells, which in turn clear the apoptotic cells. Chekeni et al. found that carbenoxolone (CBX), which inhibits connexins (which form gap junctions) and pannexins (which form plasma membrane channels), and probenicid, which is thought to be more specific for pannexins, reduced ATP release from apoptotic Jurkat cells to a similar extent as the caspase inhibitor zVAD (which blocks the release of ATP from apoptotic cells). Small interfering RNAs (siRNAs) directed against pannexin 1 (PANX1) decreased the release of ATP and UTP from apoptotic Jurkat cells but did not prevent apoptosis. Supernatant from PANX1 siRNA-transfected apoptotic cells recruited fewer monocytes in an in vitro assay of cell migration and when placed in a subcutaneous air pouch in mice. In contrast, Jurkat cells stably overexpressing PANX1 released more ATP and UTP, and supernatants from these cells (after apoptosis had been induced) recruited more monocytes ...
Sigma-Aldrich offers abstracts and full-text articles by [Anna R Moore, Wen-Liang Zhou, Carissa L Sirois, Glenn S Belinsky, Nada Zecevic, Srdjan D Antic].
Intracellular calcium (Ca2+) concentration exhibits periodic oscillations in vascular smooth muscle cells. This is thought to result from Ca2+ release from intracellular stores, due to inositol triphosphate and ryanodine-sensitive channel activation. This activation has been shown to result in either Ca2+ "sparks", highly localized calcium increases, or "waves", global Ca2+ increase that propagates the length of the cell.[3] To allow vasomotion to occur, synchronization must occur between the individual oscillations, resulting in global calcium synchronization and vessel tone oscillation.[4] Gap junctions are thought to play a large role in this synchronization, as application of gap junction blockers has been shown to abolish vasomotion, indicating a critical role.[5] Due to regional variations in gap junction distribution and coupling (homocellular vs. heterocellular) several hypotheses have been suggested to account for vasomotion occurrence. The "classic" mechanism of vasomotion generation ...
In the present study we demonstrated, by various experimental approaches, that cAMP and PKC are involved in the modulation of inter-TEC GJIC: the cAMP agonist 8-Br-cAMP enhanced inter-TEC coupling whereas PMA-induced PKC activation triggered an opposite effect.. Using flow cytometry we first detected in a mouse TEC line, that up to 90% of DiIc18(3)+ cells co-cultured in 1:1 ratio with calcein+ cells became double positive, a phenomenon which was readily inhibited by the gap junction inhibitors 18-β-glycyrrhetinic acid and carbenoxolone. This result clearly demonstrates that the thymic epithelium spontaneously forms a GJIC-dependent functional syncytium in vitro. Under these conditions, 8-Br-cAMP and forskolin did not significantly modify this spontaneous percentage of coupled cells. However, both compounds enhanced up to 3 fold the calcein fluorescence intensity of the double positive cells, indicating an increase in the rate of dye transfer among coupled cells. Importantly, 8-Br-cAMP also ...
Carbenoxolone (CBX) has been discovered to inhibit cortisol and prednisolone production via 11ß-hydroxysteroid dehydrogenase (11ß-HSD)1 inhibition. Decreasing glucocorticoid (GC) levels has been determined to be a requirement for GC-induced lipolysis.. Previous studies have concluded that CBX increases levels of urinary free cortisol (UFF) and decreases levels of urinary free cortisone (UFE). This is reflects upon the inhibition of renal 11ß-HSD2. A decrease in tetrahydrometabolites of cortisol (THF + 5 THF) and an increase in tetrahydrocortisone (THE) levels were also discovered to occur.. 11ß-HSD1 and -2 are capable of interconverting cortisol and cortisone, as well as prednisone and prednisolone. The activities of these enzymes were also able to be inhibited by glycyrrhetinic acid (GE), because of their similar enzyme kinetics. Dexamethasone has been established as an 11ß-HSD1 substrate, and could act as a competitive inhibitor with cortisone.. Experimental GC induction might be ...
OBJECTIVE: To assess the influence of blocking smooth muscle large conductance Ca(2+) -activated K+ channels and voltage-gated K+ channels on the conducted dilation to ACh and isoproterenol. MATERIALS AND METHODS: Rat mesenteric arteries were isolated with a bifurcation, triple-cannulated, pressurized and imaged using confocal microscopy. Phenylephrine was added to the superfusate to generate tone, and agonists perfused into a sidebranch to evoke local dilation and subsequent conducted dilation into the feed artery. RESULTS: Both ACh- and isoproterenol-stimulated local and conducted dilation with similar magnitudes of decay with distance along the feed artery (2000μm: ∼15% maximum dilation). The gap junction uncoupler carbenoxolone prevented both conducted dilation and intercellular spread of dye through gap junctions. IbTx, TEA or 4-AP, blockers of large conductance Ca(2+) -activated K+ channels and voltage-gated K+ channels, did not affect conducted dilation to either agonist. A combination
Communication among cells via direct cell-cell contact by connexin gap junctions, or between cell and extracellular environment via pannexin channels or connexin hemichannels, is a key factor in cell...
In humans, connexins (Cxs) and pannexins (Panxs) are the building blocks of hemichannels. These proteins are frequently altered in neoplastic cells and have traditionally been considered as tumor suppressors. Alteration of Cxs and Panxs in cancer cells can be due to genetic, epigenetic and post-transcriptional/post-translational events. Activated hemichannels mediate the diffusional membrane transport of ions and small signaling molecules. In the last decade hemichannels have been shown to participate in diverse cell processes including the modulation of cell proliferation and survival. However, their possible role in tumor growth and expansion remains largely unexplored. Herein, we hypothesize about the possible role of hemichannels in carcinogenesis and tumor progression. To support this theory, we summarize the evidence regarding the involvement of hemichannels in cell proliferation and migration, as well as their possible role in the anti-tumor immune responses. In addition, we discuss the evidence
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1-methoxyphaseollin, 17?-hydroxysteroid dehydrogenase, 18(beta)-glycyrrhetinic acid, 22?-acetoxylglycyrrhizic acid, Alcacuz (Portuguese, Spanish), alcazuz, asam boi, biogastrone, bois doux (French), CankerMelts GX, carbenoxolone, carbenoxolone sodium, chalcones, Chinese licorice, deglycyrrhizinised liquorice, deglycyrrhizinized succus Liquiritiae, DGL, duogastrone, Fabaceae (family), flavonoid, flavonoid glycosides, gan cao, gan zao, glabrene, glabridin, glabrol, GlavonoidT, glucoliquiritin apioside, glycyrrhetenic acid, glycyrrhetic acid, glycyrrhiza, Glycyrrhiza glabra, Glycyrrhiza glabra glandulifera, Glycyrrhiza glabra Linne, Glycyrrhiza glabra typica, Glycyrrhiza glabra violacea, Glycyrrhiza palidiflora, glycyrrhiza root, Glycyrrhiza uralensis, glycyrrhizic acid, glycyrrhizin, glycyrrhizinic acid, glycyrrhizol-A, hochu-ekki-to, isoflavone, isoflavonoids, isoliquiritigenin, isoliquiritin, kanzo (Japanese), lakrids (Danish), lakritze, Lakritzenwurzel (German), Leguminoseae (family), ...
Receptor activator of NF-kappaB ligand (RANKL) is crucial in osteoclastogenesis but signaling events involved in osteoclast differentiation are far from complete and other signals may play a role in osteoclastogenesis. A more direct pathway for cellular crosstalk is provided by gap junction intercellular channel, which allows adjacent cells to exchange second messengers, ions, and cellular metabolites. Here we have investigated the role of gap junction communication in osteoclastogenesis in mouse bone marrow cultures. Immunoreactive sites for the gap junction protein connexin 43 (Cx43) were detected in the marrow stromal cells and in mature osteoclasts. Carbenoxolone (CBX) functionally blocked gap junction communication as demonstrated by a scrape loading Lucifer Yellow dye transfer technique. CBX caused a dose-dependent inhibition (significant , or = 90 microM) of the number of tartrate-resistant acid phosphatase (TRAP)-positive multinucleated cells formed in 7- to 8-day marrow cultures ...
Ng, FS, Lyon, AR, Shadi, IT, Chang, ETY, Chowdhury, RA, Dupont, E and Peters, NS (2010) GAP JUNCTIONAL UNCOUPLING WITH CARBENOXOLONE SLOWS CONDUCTION AND INCREASES VULNERABILITY TO VENTRICULAR ARRHYTHMIAS IN STRUCTURALLY NORMAL HEARTS: AN OPTICAL MAPPING STUDY In: Annual Conference and Exhibition of the British-Cardiovascular-Society, 2010-06-07 - 2010-06-09, Manchester, ENGLAND. Ng, FS, Lyon, AR, Shadi, IT, Chang, ETY, Chowdhury, RA, Dupont, E and Peters, NS (2010) MODULATION OF GAP JUNCTIONAL COUPLING AS AN ANTI-ARRHYTHMIC STRATEGY TO PREVENT REPERFUSION VENTRICULAR ARRHYTHMIAS In: Annual Conference and Exhibition of the British-Cardiovascular-Society, 2010-06-07 - 2010-06-09, Manchester, ENGLAND. Dhillon, PS, Gray, R, Kojodjojo, P, Jabr, R, Chowdhury, RA, Fry, CH and Peters, NS (2009) The Relationship Between Gap Junction Conductance and Conduction Velocity in Intact Myocardium In: 82nd Scientific Session of the American-Heart-Association, 2009-11-14 - 2009-11-18, Orlando, FL. Dhillon, P, ...
0016]Tetrahydrocortisol, especially the 3-alpha-5-beta isomer, has been shown to lower intraocular pressure (IOP) in rabbits made ocularly hypertensive with dexamethasone (Southren Weinstein el al., Invest. Ophthalmol. Vis. Sci. 28, 901 (1987) and to be useful in the prevention of the elevation in intraocular pressure resulting from treatment with glucocorticoids (U.S. Pat. No. 5,358,943, Clark et al.). 3-α-5-β-Tetrahydrocortisol has been shown to lower intraocular pressure in patients when applied topically as a 1% suspension. (J. Ocul. Pharmacol. 10,385 (1994) and in U.S. Pat. No. 4,997,826 (Southren et al.)). THC may affect intraocular pressure by preventing changes in the trabecular meshwork cytoskeleton caused by glucocorticoids, such as cortisol (Invest. Opthalmol. Vis. Sci. 37, 805-13(1996)). In line with this proposal is the observation that decreasing cortisol formation in the eye by inhibition of its synthesis reduces IOP. Carbenoxolone treatment resulted in a 20% decrease in ...
The KOMP Repository is located at the University of California Davis and Childrens Hospital Oakland Research Institute. Question? Comments? For Mice, Cells, and germplasm please contact us at [email protected], US 1-888-KOMP-MICE or International +1-530-752-KOMP, or for vectors [email protected] or +1-510-450-7917 ...
Gap junctions - the channels that allow adjacent cells to exchange molecules - are made of two hemichannels that dock with one another through their extracellular domains. Undocked hemichannels are also thought to have roles in intercellular communication, but until now these had not been investigated in vivo. Gerald Kidder and colleagues (p. 4016) have been probing possible roles for undocked hemichannels, using mouse folliculogenesis as a model. During folliculogenesis, developing oocytes are surrounded and nurtured by granulosa cells that are connected to one another by gap junctions containing the protein connexin 43 (Cx43). To find out whether undocked hemichannels have a role in this process, the researchers produced constructs encoding wild-type Cx43 or a Cx43 mutant that can form hemichannels but not intercellular gap junctions. They then expressed these in Cx43-deficient granulosa cells and combined them with wild-type oocytes to make reaggregated ovaries. Whereas wild-type Cx43 ...
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Avicin Therapeutics Ltd. is developing avicin d for the treatment of multiple myeloma. Avicins are triterpenoid compounds that occur naturally in Acacia
Communication between AEC I and AEC II can be accomplished by means of two major routes: gap junction and paracrine communication (Koval, 2002). What are the mechanisms for P2X7R-mediated AEC I and AEC II communication? Cell-to-cell contact and/or gap junction communication as a major mechanism is unlikely given that the gap junction blocker β-glycyrrhetinic acid did not block BzATP-stimulated surfactant secretion. Furthermore, the conditioned medium from BzATP-stimulated E10 or HEK-P2X7R cells showed that there was a stimulation of surfactant secretion comparable with that seen during the co-culture of these cells with AEC II. Thus, the release of soluble factors from AEC I upon the activation of P2X7R is probably responsible for AEC I and AEC II communication. One such factor is ATP. Indeed, P2X7R activation in the heterocellular culture of AEC I and AEC II caused release of ATP into the bulk milieu, which was blocked by BBG. This effect was completely absent in the AEC II monoculture. The ...
The nano-sized triterpenoid 18β-glycyrrhetinic acid extractable from Glycyrrhiza glabra self assembled in different liquids affording mostly nano to microsized spherical and flower like objects consisting of fibrillar networks yielding thermoreversible gels. The self-assemblies have been utilized for the tem
Gap junctions contain intercellular channels that allow direct communication between the cytosolic compartments of adjacent cells. Each gap junction channel is formed by docking of two hemichannels, each containing six connexins, contributed by each neighboring cell. These channels permit the direct transfer of small molecules including ions, amino acids, nucleotides, second messengers and other metabolites between adjacent cells. Gap junctional communication is essential for many physiological events, including embryonic development, electrical coupling, metabolic transport, apoptosis, and tissue homeostasis. Communication through Gap Junction is sensitive to a variety of stimuli, including changes in the level of intracellular Ca2+, pH, transjunctional applied voltage and phosphorylation/dephosphorylation processes. This figure represents the possible activation routes of different protein kinases involved in Cx43 and Cx36 phosphorylation ...
Gap junctions contain intercellular channels that allow direct communication between the cytosolic compartments of adjacent cells. Each gap junction channel is formed by docking of two hemichannels, each containing six connexins, contributed by each neighboring cell. These channels permit the direct transfer of small molecules including ions, amino acids, nucleotides, second messengers and other metabolites between adjacent cells. Gap junctional communication is essential for many physiological events, including embryonic development, electrical coupling, metabolic transport, apoptosis, and tissue homeostasis. Communication through Gap Junction is sensitive to a variety of stimuli, including changes in the level of intracellular Ca2+, pH, transjunctional applied voltage and phosphorylation/dephosphorylation processes. This figure represents the possible activation routes of different protein kinases involved in Cx43 and Cx36 phosphorylation ...
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Mutations in the GJB2 gene that encodes the Cx26 gap junction (GJ) protein are one of the most common causes of inherited deafness in the human population. A su...
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Mutations in connexin26 (Cx26) underlie a range of serious human pathologies. Previously we have shown that Cx26 hemichannels are directly opened by CO2 (Meigh et al., 2013). However the effects of human disease-causing mutations on the CO2 sensitivity of Cx26 are entirely unknown. Here, we report the first connection between the CO2 sensitivity of Cx26 and human pathology, by demonstrating that Cx26 hemichannels with the mutation A88V, linked to Keratitis-Ichthyosis-Deafness syndrome, are both CO2 insensitive and associated with disordered breathing in humans.. ...
The protein encoded by this gene belongs to the innexin family. Innexin family members are the structural components of gap junctions. This protein and pannexin 2 are abundantly expressed in central nerve system (CNS) and are coexpressed in various neuronal populations. Studies in Xenopus oocytes suggest that this protein alone and in combination with pannexin 2 may form cell type-specific gap junctions with distinct properties. [provided by RefSeq, Jul 2008 ...
Human CBX1 partial ORF ( NP_006798.1, 2 a.a. - 99 a.a.) recombinant protein with GST-tag at N-terminal. (H00010951-Q01) - Products - Abnova
During the assembly of gap junctions, a hemichannel in the plasma membrane of one cell is thought to align and dock with another in an apposed membrane to form a cell-to-cell channel. We report here on the existence and properties of nonjunctional, plasma membrane connexin43 (Cx43) hemichannels. The opening of the hemichannels was demonstrated by the cellular uptake of 5(6)-carboxyfluorescein from the culture medium when extracellular calcium levels were reduced. Dye uptake exhibited properties similar to those of gap junction channels. For example, using different dyes, the levels of uptake were correlated with molecular size: 5(6)-carboxyfluorescein (approximately 32%), 7-hydroxycoumarin-3-carboxylic acid (approximately 24%), fura-2 (approximately 11%), and fluorescein-dextran (approximately 0.4%). Octanol and heptanol also reduced dye uptake by approximately 50%. Detailed analysis of one clone of Novikoff cells transfected with a Cx43 antisense expression vector revealed a reduction in dye ...
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Activation of the inflammasome, a complex that processes interleukin-1β (IL-1β), occurs in response to activation of the adenosine triphosphate receptor P2X7 on macrophages. Activation of P2X7 also triggers the opening of a nonselective, large pore in the plasma membrane. Pelegrin and Surprenant found that pannexin-1 (panx1), a protein that produces hemichannel currents when ectopically expressed in oocytes, was present in monocytes, macrophages, astrocytes, and various cell lines. Panx1, when expressed in transfected HEK cells, coimmunoprecipitated with the P2X7 receptor and colocalized with the P2X7 receptors in ATP-stimulated cells. Using either an siRNA to knock down panx1 or a peptide inhibitor to block the pore function of panx1, the authors showed that dye uptake (a measure of pore opening) in response to P2X7 required panx1. When overexpressed in cells that lack P2X7 receptors, panx1 caused constitutive dye uptake, and when overexpressed in cells that contain P2X7 receptors, panx1 ...
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Nel corso di questo lavoro, abbiamo osservato che le cellule cocleari non-sensoriali che compongono il greater and lesser epithelial ridge (GER e LER, rispettivamente) condividono la stessa cascata di trasduzione del segnale attivato da ATP dipendente da PLC e IP3R. Inoltre, abbiamo dimostrato che lattività dei segnali Ca2+ ATP-dipendente nelle cellule cocleari non-sensoriale è spazialmente ordinata dallapice alla base della coclea durante la prima settimana postnatale. Il segnale di Ca2+ in queste condizioni dipende della generazione delinositolo-1,4,5-trifosfato a partire dellidrolisi di PI(4,5)P(2) dipendente da PLC. Abbiamo quindi analizzato dei topi con espressione difettosa di PIPKIγ e abbiamo mostrato che (i) tale enzima è essenziale per lacquisizione delludito, (ii) è responsabile principalmente della sintesi di pool di PI(4,5)P(2) regolati da recettore e sensibili a PLC nei sincizi cellulari che fanno da supporto alle cellule ciliate uditive, e che (iii) la diminuzione ...
Sigma-Aldrich offers abstracts and full-text articles by [Peter J Minogue, Jun-Jie Tong, Anita Arora, Isabelle Russell-Eggitt, David M Hunt, Anthony T Moore, Lisa Ebihara, Eric C Beyer, Viviana M Berthoud].
Carbenoxolone Enoxolone. ...
... and carbenoxolone". Gastroenterology. 80 (4): 770-5. PMID 6162705. Hwang, S. H.; Litt, M.; Forsman, W. C. (1969). "Rheological ...
Anti-aggregation agents such as apomorphine, or carbenoxolone. The latter has commonly been used as a treatment for peptic ... By binding with high affinity to Aβ42 fragments, primarily via hydrogen bonding, carbenoxolone captures the peptides before ... "Inhibition of Alzheimer's amyloid-beta aggregation in-vitro by carbenoxolone: Insight into mechanism of action". Neurochemistry ...
A synthetic analog, carbenoxolone, was developed in Britain.[citation needed] Both glycyrrhetinic acid and carbenoxolone have a ...
Steer, H.W.; D.G. Colin-Jones (1975). "Mucosal changes in gastric ulceration and their response to carbenoxolone sodium". Gut. ...
"Mucosal changes in gastric ulceration and their response to carbenoxolone sodium". Gut. 16 (8): 590-7. doi:10.1136/gut.16.8.590 ...
Berg M, Geisel A, Necheles H (1975). "The influence of carbenoxolone on steroid-induced ulcer and mucus secretion in the rat". ...
11α-OHP is a more potent inhibitor of 11β-HSD than enoxolone (glycyrrhetinic acid) or carbenoxolone in vitro (IC50 = 0.9 nM; ...
11β-HSD1 is inhibited by carbenoxolone, a drug typically used in the treatment of peptic ulcers. Moreover, 18alpha-glycyrrhizic ...
Gastric cytoprotective drugs include carbenoxolone, deglycyrrhizinised liquorice, sucralfate (aluminium hydroxide and sulphated ...
... carbenoxolone (INN) carbenzide (INN) carbetapentane carbetapentane tannate carbetimer (INN) carbetocin (INN) carbidopa (INN) ...
... carbenoxolone MeSH D02.455.849.919.305 --- glycyrrhizic acid MeSH D02.455.849.919.490 --- limonins MeSH D02.455.849.919.570 ...
... clarithromycin and metronidazole A02BX01 Carbenoxolone A02BX02 Sucralfate A02BX03 Pirenzepine A02BX04 Methiosulfonium chloride ... combinations excluding psycholeptics A02BX71 Carbenoxolone, combinations with psycholeptics A02BX77 Gefarnate, combinations ... A02BX10 Zolimidine A02BX11 Troxipide A02BX12 Bismuth subnitrate A02BX13 Alginic acid A02BX14 Rebamipide A02BX51 Carbenoxolone, ...
... is a modestly potent, reasonably effective, water-soluble blocker of gap junctions. Carbenoxolone has also been ... Electrolyte imbalance is a serious side effect of carbenoxolone when used systemically. Carbenoxolone reversibly inhibits the ... However, potassium-sparing diuretic amiloride was co-administered with carbenoxolone, since carbenoxolone used by itself may ... Carbenoxolone may decrease the amount of active glucocortocoid in the brain, because the drug inhibits 11β-HSD, an enzyme which ...
Long-term use of methylprednisolone, as with all corticosteroids, can be associated with hyperglycemia, decreased resistance to infection, swelling of face, weight gain, congestive cardiac insufficiency, fluid and sodium retention, edema, hypertension, increased eye pressure, glaucoma, osteoporosis, and psychosis, especially when used at high doses.[11][12] The most serious side effect occurs after the adrenal glands cease natural production of cortisol, which methylprednisolone will replace. Abrupt cessation of the drug after this occurs can result in a condition known as Addisonian crisis, which can be fatal. To prevent this, the drug is usually prescribed with a tapering dose, including a predosed "dose pack" detailing a specific number of tablets to take at designated times over a several-day period. Pharmacists sometimes advise that this drug may cause sleeplessness and "down" moods. Measles and chicken pox are very dangerous and potentially fatal for people on methylprednisolone therapy. ...
Important drug interactions are rare.[27][28] However, the most significant major drug interaction concern is the decreased activation of clopidogrel when taken together with omeprazole.[29] Although still controversial,[30] this may increase the risk of stroke or heart attack in people taking clopidogrel to prevent these events. This interaction is possible because omeprazole is an inhibitor of the enzymes CYP2C19 and CYP3A4.[31] Clopidogrel is an inactive prodrug that partially depends on CYP2C19 for conversion to its active form. Inhibition of CYP2C19 may block the activation of clopidogrel, which could reduce its effects.[32][33] Almost all benzodiazepines are metabolised by the CYP3A4 and CYP2D6 pathways, and inhibition of these enzymes results in a higher AUC (i.e., the total effect over time of a given dose). Other examples of drugs dependent on CYP3A4 for their metabolism are escitalopram,[34] warfarin,[35] oxycodone, tramadol, and oxymorphone. The concentrations of these drugs may ...
... was first prepared as AH19065 by John Bradshaw in the summer of 1977 in the Ware research laboratories of Allen & Hanburys, part of the Glaxo organization.[36][37] Its development was a response to the first in class histamine H2 receptor antagonist, cimetidine, developed by Sir James Black at Smith, Kline and French, and launched in the United Kingdom as Tagamet in November 1976. Both companies would eventually become merged as GlaxoSmithKline following a sequence of mergers and acquisitions starting with the integration of Allen & Hanbury's Ltd and Glaxo to form Glaxo Group Research in 1979, and ultimately with the merger of Glaxo Wellcome and SmithKline Beecham in 2000. Ranitidine was the result of a rational drug-design process using what was by then a fairly refined model of the histamine H2 receptor and quantitative structure-activity relationships. Glaxo refined the model further by replacing the imidazole ring of cimetidine with a furan ring with a nitrogen-containing ...
Some studies have shown a correlation between use of PPIs and Clostridium difficile infections. While the data are contradictory and controversial, the FDA had sufficient concern to include a warning about this adverse effect on the label of PPI drugs.[25] Concerns have also been raised about spontaneous bacterial peritonitis in older people taking PPIs and in people with irritable bowel syndrome taking PPIs; both types of infections arise in these populations due to underlying conditions and it is not clear if this is a class effect of PPIs.[25] PPIs may predispose an individual to developing small intestinal bacterial overgrowth or fungal overgrowth.[30][31] Long-term use of PPIs is associated with the development of benign polyps from fundic glands (which is distinct from fundic gland polyposis); these polyps do not cause cancer and resolve when PPIs are discontinued. There is no association between PPI use and cancer[25] or pre-cancer.[32] There is concern that use of PPIs may mask gastric ...
... is a glucocorticoid used to treat asthma and allergic rhinitis. It is marketed under the brand names Alvesco for asthma and Omnaris, Omniair, and Zetonna for hay fever in the US and Canada. Phase 3 trials for the hay fever indication outside the US are ongoing.[1] The drug was approved for adults and children 12 and over by the US Food and Drug Administration in October 2006.[2] Side effects of the medication include headache, nosebleeds, and inflammation of the nose and throat linings.[3] ...
... , sold under the brand name Prevacid among others, is a medication which reduces stomach acid.[1] It is used to treat peptic ulcer disease, gastroesophageal reflux disease, and Zollinger-Ellison syndrome.[2] Effectiveness is similar to other proton pump inhibitors (PPIs).[3] It is taken by mouth.[1] Onset is over a few hours and effects last up to a couple of days.[1] Common side effects include constipation, abdominal pain, and nausea.[1][4] Serious side effects may include osteoporosis, low blood magnesium, Clostridium difficile infection, and pneumonia.[1][4] Use in pregnancy and breastfeeding is of unclear safety.[5] It works by blocking H+/K+-ATPase in the parietal cells of the stomach.[1] Lansoprazole was patented in 1984 and came into medical use in 1992.[6] It is available as a generic medication.[2] A one month supply, in the United Kingdom, costs the NHS less than £5, as of 2019[update].[2] In the United States, the wholesale cost of this amount is about $5.40, as of ...
... (INN,[1] USAN, codenamed AH25352) is a long-acting competitive H2 receptor antagonist which was under development as an antiulcerant by Glaxo (now GlaxoSmithKline).[2] It was planned to be a follow-up compound to ranitidine (Zantac).[3] When taken in doses of 600 mg twice daily it induced virtually 24-hour gastric anacidity[4] thus closely resembling the antisecretory effect of the proton pump inhibitor omeprazole.[5] Its development was terminated in 1989[6] from phase III clinical trials based on the appearance of carcinoid tumors in long-term toxicity testing in rodents.[7] ...
InChI=1S/C22H28O5/c1-12-8-16-15-5-4-13-9-14(24)6-7-20(13,2)19(15)17(25)10-21(16,3)22(12,27)18(26)11-23/h6-7,9,12,15-16,19,23,27H,4-5,8,10-11H2,1-3H3/t12-,15-,16-,19+,20-,21-,22-/m0/s1 ...
InChI=1S/C24H33FO6/c1-21(2)30-19-9-14-13-8-16(25)15-7-12(27)5-6-22(15,3)20(13)17(28)10-23(14,4)24(19,31-21)18(29)11-26/h7,13-14,16-17,19-20,26,28H,5-6,8-11H2,1-4H3/t13-,14-,16-,17-,19+,20+,22-,23-,24+/m0/s1 ...
InChI=1S/C22H23FN4/c1-14-15(2)24-22(25-19-10-8-18(23)9-11-19)26-21(14)27-13-12-17-6-4-5-7-20(17)16(27)3/h4-11,16H,12-13H2,1-3H3,(H,24,25,26 ...
In January 2015, the FDA granted fast track status to Marathon Pharmaceuticals to pursue approval of deflazacort as a potential treatment for Duchenne muscular dystrophy, a rare, "progressive and fatal disease" that affects boys.[7] Although deflazacort was approved by the FDA for use in treatment of Duchenne muscular dystrophy on February 9, 2017,[8][9] Marathon CEO announced on February 13, 2017 that the launch of deflazacort (Emflaza) would be delayed amidst controversy over the steep price Marathon was asking for the drug in the United States - $89,000 per year, which is "roughly 70 times" more than it would cost overseas.[10] Because deflazacort is an older drug which has been long-approved in some other countries, it is now available in many places as an inexpensive generic. For example, in Canada deflazacort can be purchased for around $1 per tablet.[11] Deflazacort is sold in the United States under the trade name Emflaza after a company called PTC Therapeutics, Inc. acquired all rights ...
CHEBI:31351 - Carbenoxolone sodium. Main. ChEBI Ontology. Automatic Xrefs. Reactions. Pathways. Models. ...
Carbenoxolone is a modestly potent, reasonably effective, water-soluble blocker of gap junctions. Carbenoxolone has also been ... Electrolyte imbalance is a serious side effect of carbenoxolone when used systemically. Carbenoxolone reversibly inhibits the ... However, potassium-sparing diuretic amiloride was co-administered with carbenoxolone, since carbenoxolone used by itself may ... Carbenoxolone may decrease the amount of active glucocortocoid in the brain, because the drug inhibits 11β-HSD, an enzyme which ...
Metabolic Studies, Aldosterone Secretion Rate, and Plasma Renin after Carbenoxolone Sodium Br Med J 1969; 2 :793 ... A formal metabolic study of carbenoxolone sodium (Biogastrone) 300 mg./day has been performed for 17 days on a woman with ... Aldosterone secretion in the control period was 202 μg./24 hours, and fell to 74 μg./24 hours after carbenoxolone, but plasma ... These results suggest that the mineralocorticoid effects of carbenoxolone (and presumably of liquorice and its other ...
However, potassium-sparing diuretic amiloride was co-administered with carbenoxolone, since carbenoxolone used by itself may ... "Tales of a Dirty Drug: Carbenoxolone, Gap Junctions, and Seizures".. *↑ Sandeep TC, Yau JL, MacLullich AM; et al. (2004). " ... Carbenoxolone (CBX) is a glycyrrhetinic acid derivative with a steroid-like structure, similar to substances found in the root ... Carbenoxolone has also been investigated for nootropic effects.[5] This research started from an observation that long-term ...
If you wish to reuse any or all of this article please use the link below which will take you to the Copyright Clearance Centers RightsLink service. You will be able to get a quick price and instant permission to reuse the content in many different ways.. ...
These effects of BAC were reversed by topical carbenoxolone treatment. These results demonstrate that carbenoxolone can prevent ... slowed down by carbenoxolone. Finally, octanol or carbenoxolone blocked 4AP-induced ictal-like discharges (duration = up to 35 ... Although carbenoxolone is able to decrease the SR101-labeling of astrocytes in the hippocampus, it is unlikely that SR101 is ... For the in vivo study, carbenoxolone or a solvent was administered to the BAC-induced DES model twice daily. BAC-treated rat ...
Pyrogastrone information about active ingredients, pharmaceutical forms and doses by Sanofi-Aventis, Pyrogastrone indications, usages and related health products lists
View and buy high purity Carbenoxolone disodium from Tocris Bioscience. Gap junction blocker. Also inhibitor of 11 β- ... Reviews for Carbenoxolone disodium. There are currently no reviews for this product. Be the first to review Carbenoxolone ... Keywords: Carbenoxolone disodium, Carbenoxolone disodium supplier, Gap, junction, blockers, inhibitors, inhibits, 11, β- ... Have you used Carbenoxolone disodium?. Submit a review and receive an Amazon gift card.. $50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen ...
Carbenoxolone appeared to increase the amount of mucus but had little effect upon the number of bacteria found. The possible ... the effect of treatment with carbenoxolone sodium was studied. There is a statistically significant reduction in the total ... of intraepithelial lymphocytes in those patients with lesser curve gastric ulcers successfully treated with carbenoxolone ... number of intraepithelial polymorphonuclear leucocytes before and after successful treatment with carbenoxolone sodium. There ...
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The carbenoxolone group was given capsules containing 50 mg carbenoxolone four times a day for 12 weeks while the controls ... Review at three months and at six months revealed a slight but clinically insignificant trend in favour of the carbenoxolone ... A controlled trial of carbenoxolone sodium positioned-release capsules (Duogastrone) was carried out on a randomized series of ... Fifty-seven patients completed the trial, 29 in the carbenoxolone group and 28 in the control group. ...
Anticonvulsive effects of carbenoxolone on penicillin-induced epileptiform activity:: An in vivo study. ... Carbenoxolone suppressed epileptiform activity by decreasing the amplitude and frequency of epileptiform spikes and by ... Effects of carbenoxolone on epileptiform activity were assessed by both electrophysiological and behavioral analysis. ... The aim of present study is to investigate the effects of gap junction blocker carbenoxolone on penicillin-induced experimental ...
Carbenoxolone has been labelled with [14]C and [3]H. [[14]C]Carbenoxolone administered as a positioned-release capsule to ... Carbenoxolone was excreted in the bile mainly as carbenoxolone-30-glucuronid Conjugation appeared to be a pre-requisite for ... Most of the dose was recovered as carbenoxolone in the faeces, although a portion (, 15%) was present as carbenoxolone-30- ... carbenoxolone also induced a conformational change in the albumin. The distribution of [[14]C]carbenoxolone in the rat showed ...
Yulyana, Y., Endaya, B.B., Ng, W.H., Guo, C.M., Hui, K.M., Lam, P.Y.P., Ho, I.A.W. (2013-07-01). Carbenoxolone enhances TRAIL- ... Carbenoxolone enhances TRAIL-induced apoptosis through the upregulation of death receptor 5 and inhibition of gap junction ... inhibitory effect of carbenoxolone (CBX) to target orthotopic glioma. MSC were engineered to express TRAIL (MSC-TRAIL) by ...
carbenoxolone ligand page. Quantitative data and detailed annnotation of the targets of licensed and experimental drugs. ... Carbenoxolone is derived from licorice root, and has a steroid-like chemical structure. Formulations used clinically typically ...
Carbenoxolone chemical safety search, Chemical Carbenoxolone safety technical specifications ect. ...
Carbenoxolone Application. In vitro, 75 μmol/L carbenoxolone (CBX; disodium salt; Sigma) was added to slice culture medium.12 ... Vessey JP, Lalonde MR, Mizan HA, Welch NC, Kelly ME, Barnes S. Carbenoxolone inhibition of voltage-gated Ca channels and ... Administration of carbenoxolone to ischemic pups immediately after intrauterine HI prevented caspase-3 activation and ... The gap junction blocker carbenoxolone applied to hippocampal slice cultures before, during, or 60 minutes after OGD markedly ...
BIOPLEX , BIOGASTRONE , Carbenoxolone Disodium , BIORAL , Carbenoxolone , DUOGASTRONE , CARBENOXOLONE SODIUM. Max Phase. 4 ( ... A02BX71 - carbenoxolone, combinations with psycholeptics. A - ALIMENTARY TRACT AND METABOLISM. A02 - DRUGS FOR ACID RELATED ... A02BX51 - carbenoxolone, combinations excl. psycholeptics. A - ALIMENTARY TRACT AND METABOLISM. A02 - DRUGS FOR ACID RELATED ... Carbenoxolone Disodium , BIORAL , Carbenoxolone , DUOGASTRONE , CARBENOXOLONE SODIUM ...
Carbenoxolone Sodium Br Med J 1967; 3 :177 (Published 15 July 1967) ...
Detailed drug Information for Moduretic 5-50. Includes common brand names, drug descriptions, warnings, side effects and dosing information.
carbenoxolone. *potassium-losing diuretics, eg furosemide, bendroflumethiazide. * theophylline. If the amount of potassium in ...
carbenoxolone *potassium-losing diuretics, eg furosemide, bendroflumethiazide. * theophylline.. Methylprednisolone may enhance ...
carbenoxolone *beta-agonist bronchodilators such as salbutamol *stimulant laxatives, eg bisacodyl. This medicine may increase ...
carbenoxolone. * beta-agonist bronchodilators such as salbutamol. *stimulant laxatives, eg bisacodyl.. If the amount of ...
carbenoxolone. * beta agonist bronchodilators such as salbutamol.. If you are taking any of these medicines that could affect ...
  • The carbenoxolone group was given capsules containing 50 mg carbenoxolone four times a day for 12 weeks while the controls received a capsule identical in every respect except that it did not contain carbenoxolone. (bmj.com)
  • As a corollary to this controlled trial, those patients (38 in all) who did not have an early remission of symptoms were removed from the trial and placed on capsules known to contain carbenoxolone. (bmj.com)
  • Treatment of gastric ulcer with carbenoxolone: antagonistic effect of spironolactone. (bmj.com)
  • Gastric cytoprotective drugs include carbenoxolone, deglycyrrhizinised liquorice, sucralfate (aluminium hydroxide and sulphated sucrose), misoprostol (a prostaglandin analogue) and bismuth chelate (tri-potassium di-citrato bismuthate). (wikipedia.org)
  • Administration of carbenoxolone to ischemic pups immediately after intrauterine HI prevented caspase-3 activation and dramatically reduced long-term neuronal damage. (ahajournals.org)
  • When further examined, Carbenoxolone also led to a significant reduction in infarction size and neuronal damage in the ischemic penumbra when administered six hours post middle cerebral artery occlusion in rats. (jove.com)
  • Redox-Active Mn Porphyrin-based Potent SOD Mimic, MnTnBuOE-2-PyP(5+), Enhances Carbenoxolone-Mediated TRAIL-Induced Apoptosis in Glioblastoma Multiforme. (duke.edu)
  • We investigated whether pannexin-1, a carbenoxolone-sensitive hemichannel activated in erythrocytes by swelling, could contribute to swelling-activated chloride currents (ICl,swell) in HEK-293 cells. (bioentryplus.com)
  • Carbenoxolone has also been used in topical creams such as Carbosan gel, marketed for treatment of lip sores and mouth ulcers. (wikipedia.org)
  • 11β-HSD1 is inhibited by carbenoxolone, a drug typically used in the treatment of peptic ulcers. (wikipedia.org)
  • Review at three months and at six months revealed a slight but clinically insignificant trend in favour of the carbenoxolone group. (bmj.com)
  • Compared with vehicle treatment, chronic systemic administration of 20 mg/kg or 40 mg/kg carbenoxolone caused a significantly later onset and attenuation of movement-evoked and on-going pain, assessed with limb use. (worldwidescience.org)
  • Carbenoxolone appeared to increase the amount of mucus but had little effect upon the number of bacteria found. (bmj.com)
  • Carbenoxolone is used for the treatment of peptic, esophageal and oral ulceration and inflammation. (wikipedia.org)
  • In our screen about 50% of the compounds in a library of pharmacologically active compounds displayed some degree of neuroprotective activity if tested in a pre-treatment toxicity assay but just a few of these compounds, including Carbenoxolone, remained active when tested in a post-treatment protocol. (jove.com)
  • In addition, the carbenoxolone -treated groups demonstrated a significant delay in time to reach the humane endpoint. (worldwidescience.org)
  • No significant hydrolysis of [C]carbenoxolone occurred after administration to intact or biliary-cannulated squirrel monkeys. (surrey.ac.uk)
  • Fifty-seven patients completed the trial, 29 in the carbenoxolone group and 28 in the control group. (bmj.com)
  • Subsequently these patients did not show an advantage for carbenoxolone. (bmj.com)
  • 24 hours after carbenoxolone, but plasma renin was unchanged. (bmj.com)
  • Carbenoxolone has been found to be highly bound to the plasma proteins of man and common laboratory species. (surrey.ac.uk)
  • The distribution of [C]carbenoxolone in the rat showed that it was confined largely to the gastrointestinal tract, liver and plasma. (surrey.ac.uk)
  • Epileptiform activity monitored from a digital recording system, when it reached its maximum intensity, carbenoxolone (100, 200, 500 nmol) was applied in the same way with penicillin. (ovid.com)
  • Carbenoxolone suppressed epileptiform activity by decreasing the amplitude and frequency of epileptiform spikes and by attenuating the epileptiform behavior. (ovid.com)
  • Electrolyte imbalance is a serious side effect of carbenoxolone when used systemically. (wikipedia.org)