Potassium Channels, Inwardly Rectifying
ATP-Binding Cassette Transporters
Heteromultimers of Kir6 channels (the pore portion) and sulfonylurea receptor (the regulatory portion) which affect function of the HEART; PANCREATIC BETA CELLS; and KIDNEY COLLECTING DUCTS. KATP channel blockers include GLIBENCLAMIDE and mitiglinide whereas openers include CROMAKALIM and minoxidil sulfate.
A biguanide hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. Metformin improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose. (From Martindale, The Extra Pharmacopoeia, 30th ed, p289)
Diabetes Mellitus, Type 2
A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY.
A 51-amino acid pancreatic hormone that plays a major role in the regulation of glucose metabolism, directly by suppressing endogenous glucose production (GLYCOGENOLYSIS; GLUCONEOGENESIS) and indirectly by suppressing GLUCAGON secretion and LIPOLYSIS. Native insulin is a globular protein comprised of a zinc-coordinated hexamer. Each insulin monomer containing two chains, A (21 residues) and B (30 residues), linked by two disulfide bonds. Insulin is used as a drug to control insulin-dependent diabetes mellitus (DIABETES MELLITUS, TYPE 1).
Islets of Langerhans
Irregular microscopic structures consisting of cords of endocrine cells that are scattered throughout the PANCREAS among the exocrine acini. Each islet is surrounded by connective tissue fibers and penetrated by a network of capillaries. There are four major cell types. The most abundant beta cells (50-80%) secrete INSULIN. Alpha cells (5-20%) secrete GLUCAGON. PP cells (10-35%) secrete PANCREATIC POLYPEPTIDE. Delta cells (~5%) secrete SOMATOSTATIN.
A familial, nontransient HYPOGLYCEMIA with defects in negative feedback of GLUCOSE-regulated INSULIN release. Clinical phenotypes include HYPOGLYCEMIA; HYPERINSULINEMIA; SEIZURES; COMA; and often large BIRTH WEIGHT. Several sub-types exist with the most common, type 1, associated with mutations on an ATP-BINDING CASSETTE TRANSPORTERS (subfamily C, member 8).
Hemoglobin A, Glycosylated
Minor hemoglobin components of human erythrocytes designated A1a, A1b, and A1c. Hemoglobin A1c is most important since its sugar moiety is glucose covalently bound to the terminal amino acid of the beta chain. Since normal glycohemoglobin concentrations exclude marked blood glucose fluctuations over the preceding three to four weeks, the concentration of glycosylated hemoglobin A is a more reliable index of the blood sugar average over a long period of time.
A syndrome with excessively high INSULIN levels in the BLOOD. It may cause HYPOGLYCEMIA. Etiology of hyperinsulinism varies, including hypersecretion of a beta cell tumor (INSULINOMA); autoantibodies against insulin (INSULIN ANTIBODIES); defective insulin receptor (INSULIN RESISTANCE); or overuse of exogenous insulin or HYPOGLYCEMIC AGENTS.
CELL LINES derived from the CV-1 cell line by transformation with a replication origin defective mutant of SV40 VIRUS, which codes for wild type large T antigen (ANTIGENS, POLYOMAVIRUS TRANSFORMING). They are used for transfection and cloning. (The CV-1 cell line was derived from the kidney of an adult male African green monkey (CERCOPITHECUS AETHIOPS).)
Potassium Channel Blockers
An electrophysiologic technique for studying cells, cell membranes, and occasionally isolated organelles. All patch-clamp methods rely on a very high-resistance seal between a micropipette and a membrane; the seal is usually attained by gentle suction. The four most common variants include on-cell patch, inside-out patch, outside-out patch, and whole-cell clamp. Patch-clamp methods are commonly used to voltage clamp, that is control the voltage across the membrane and measure current flow, but current-clamp methods, in which the current is controlled and the voltage is measured, are also used.
Dose-Response Relationship, Drug
A 29-amino acid pancreatic peptide derived from proglucagon which is also the precursor of intestinal GLUCAGON-LIKE PEPTIDES. Glucagon is secreted by PANCREATIC ALPHA CELLS and plays an important role in regulation of BLOOD GLUCOSE concentration, ketone metabolism, and several other biochemical and physiological processes. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1511)
Ion Channel Gating
The opening and closing of ion channels due to a stimulus. The stimulus can be a change in membrane potential (voltage-gated), drugs or chemical transmitters (ligand-gated), or a mechanical deformation. Gating is thought to involve conformational changes of the ion channel which alters selective permeability.
It is a systemic compound with foliar and soil activity, that inhibits cell division in shoots and roots. It has residual ... Metsulfuron-methyl is an organic compound classified as a sulfonylurea herbicide, which kills broadleaf weeds and some annual ... activity in soils, allowing it to be used infrequently but requiring up to 22 months before planting certain crops (sunflowers ...
It is a sulfonamide derivative that is similar to sulfonylureas. Glysobuzole has antihyperglycemic activity, so it is able to ... The intermediate compound cyclizes under the influence of an acid catalyst. A compound very similar to glysobuzole is glybuzole ... 5] The intermediate compound will have a positive charge. Pyridine takes up the oxygen to remove the positive charge present on ... The two compounds both contain a hypoglycemic part, which are structurally identical. The synthesis pathway of glysobuzole is ...
It still has limited specificity, however, as illustrated by spurious elevations with sulfonylurea compounds, and by ... It is decreased by low-protein diet, malnutrition or starvation, and by impaired metabolic activity in the liver due to ...
In the 1920s, guanidine compounds were discovered in Galega extracts. Animal studies showed that these compounds lowered blood ... Biguanides do not affect the output of insulin, unlike other hypoglycemic agents such as sulfonylureas and meglitinides. ... and bisbiguanide agents for antiplaque activity". Antimicrobial Agents and Chemotherapy. 12 (6): 721-9. doi:10.1128/aac.12.6. ... Biguanide (/baɪˈɡwɒnaɪd/) is the organic compound with the formula HN(C(NH)NH2)2. It is a colorless solid that dissolves in ...
Tryptophol, a chemical compound that induces sleep in humans, is formed in the liver after disulfiram treatment. Less common ... Jiao Y, Hannafon BN, Ding WQ (2016). "Disulfiram's Anticancer Activity: Evidence and Mechanisms". Anti-Cancer Agents in ... Examples: Antibiotics (nitroimidazoles), e.g. metronidazole First-generation sulfonylureas, e.g. tolbutamide and chlorpropamide ... However, in most cases, this disruption is mild and presents itself as a 20-40% increase in the half-life of the compound at ...
Plant activators are compounds that activate a plant's immune system in response to invasion by pathogens. They play a crucial ... Developments over the past 1960-2013 period enabled reduced use rates, in the cases of the sulfonylurea herbicides (5), the ... Desirable agrochemicals have residual activity and persistence of effect lasting up to several weeks to allow large spray ... Three hundred thousand compounds were tested against the SHMT enzyme, producing 24 hits. Among those hits, a subclass was ...
Glossary of diabetes
Carbohydrate Any compound containing carbon, hydrogen, sometimes oxygen. There is considerable variety in these compounds and ... One of the sulfonylureas. (Amaryl) Glipizide A pill taken to lower the level of glucose (sugar) in the blood. Only some people ... Sliding scale Adjusting insulin on the basis of blood glucose tests, meals, and activity levels. Somatic neuropathy See: ... One of the sulfonylureas. (Diamicron) Glimepiride A pill taken to lower the level of glucose (sugar) in the blood. Only some ...
Naturally occurring compounds may also induce or inhibit CYP activity. For example, bioactive compounds found in grapefruit ... CYP105A1 from Streptomyces griseolus metabolizes sulfonylurea herbicides to less toxic derivatives,) or are part of specialised ... Effects on CYP isozyme activity are a major source of adverse drug interactions, since changes in CYP enzyme activity may ... December 2013). "Pyrethroid activity-based probes for profiling cytochrome P450 activities associated with insecticide ...
For some compounds, the residual activity can leave the ground almost permanently barren. Herbicides are often classified ... Several sulfonylureas, including Flazasulfuron and Metsulfuron-methyl, which act as ALS inhibitors and in some cases are taken ... Residual activity: An herbicide is described as having low residual activity if it is neutralized within a short time of ... However, herbicides with low residual activity (i.e., that decompose quickly) often do not provide season-long weed control and ...
As aromatic compounds have been exhausted to a large extent as building blocks for life science products, N-heterocyclic ... Most products have a "pharmaceutical heritage". As a consequence of an intensive M&A activity over the past 10-20 years, the ... the sulfonyl urea herbicides, e.g. Eagle (amidosulfuron) and Londax (bensulfuron-methyl). Benzodiazepine derivatives are the ... Several thousand small or virtual pharma companies focus on R&D. albeit on just a few lead compounds. They typically originate ...
... is a tetracyclic compound and is grouped with the TeCAs. Its chemical name is N-methyl-9,10-ethanoanthracen-9(10H)- ... Maprotiline can increase the actions of oral antidiabetic drugs (sulfonylureas) and Insulin. Diabetic patients should have ... The pharmacological profile of maprotiline explains its antidepressant, sedative, anxiolytic, and sympathomimetic activities. ... Tatsumi M, Groshan K, Blakely RD, Richelson E (1997). "Pharmacological profile of antidepressants and related compounds at ...
Naturally occurring compounds may also induce or inhibit CYP activity. For example, bioactive compounds found in grapefruit ... CYP105A1 from Streptomyces griseolus metabolizes sulfonylurea herbicides to less toxic derivatives,) or are part of ... or just Compound I). This highly reactive intermediate was isolated in 2010, P450 Compound 1 is an iron(IV) oxo (or ferryl ... denoting the catalytic activity and the name of the compound used as substrate. Examples include CYP5A1, thromboxane A2 ...
... has an anti-hyperglycaemic activity. Glybuzole is a sulfonylurea and can therefore lower the blood glucose levels. ... "Compound:N-(5-tert-butyl-1,3,4-thiadiazol-2-yl)benzenesulfonamide". www.chemsrc.com. 1996. Retrieved March 2, 2017. Sola D, ... Sulfonylureas can bind to receptors at β-pancreatic cells which are specific for sulfonylurea binding. When a sulfonylurea ... August 2015). "Sulfonylureas and their use in clinical practice". Archives of Medical Science. 11 (4): 840-8. doi:10.5114/aoms. ...
Different compounds produce different free energy changes as a result of dephosphorylation. Psilocybin also relies on ... Hutchinson, DS; Summers, RJ; Bengtsson, T (Sep 2008). "Regulation of AMP-activated protein kinase activity by G-protein coupled ... In the treatment of diabetes, sulfonylurea drugs are able to stimulate dephosphorylation of the glucose transporter GLUT4, ... In biochemistry, dephosphorylation is the removal of a phosphate (PO43−) group from an organic compound by hydrolysis. It is a ...
ATP-binding cassette transporter
It is not sensitive to the passive permeability of the compounds and therefore detects all interacting compounds. Yet, it does ... The ATPase activity of Sav1866 is known to be stimulated by cancer drugs such as doxorubicin, vinblastine and others, which ... The sulfonylurea receptors (SUR), involved in insulin secretion, neuronal function, and muscle function, are also part of this ... Activity of multidrug transporter is reflected by the difference between the amounts of dye accumulated in the presence and the ...
4-hydroxyphenylpyruvate dioxygenase inhibitor
While this compound did not have any herbicidal activity, it did show activity in a screen designed to show antidotal activity ... that had become resistant to sulfonylurea herbicides. Mesotrione was introduced in 2002 and like sulcotrione is a triketone, so ... These compounds had similar, weak herbicidal activity similar to that found with the lead compound. Because of the weak ... What was discovered was that those compounds with an ortho substituent had herbicidal activity but no antidote activity. This ...
Discovery and development of gliflozins
Many compounds gave different IC50 value in the ring position in an in vitro activity. For an example there was a big ... sulfonylurea, thiazolidinediones, insulin and more. The HbA1c was examined after SGLT-2 inhibitors were given alone (as ... comparator to ethyl group (IC50 = 16,7) In table 2, the in vitro activity changes depending on the compound in the C-4 region ... the in vitro activity increases depending on what compound is bonded to the distal ring (given that in the C-4 region of the ...
ATP-sensitive potassium channel
In pancreatic beta cells, ATP is the primary metabolic source, and the ATP/ADP ratio determines KATP channel activity. Under ... The degree to which particular compounds are able to regulate KATP channel opening varies with tissue type, and more ... ATP-sensitive potassium channels are composed of Kir6.x-type subunits and sulfonylurea receptor (SUR) subunits, along with ... These SUR subunits are also sensitive to sulfonylureas, MgATP (the magnesium salt of ATP), and some other pharmacological ...
Such loss of activity or toxicity of pesticides is due to both innate chemical properties of the compounds and environmental ... A number of sulfonylureas have been commercialized for weed control, including: amidosulfuron, flazasulfuron, metsulfuron- ... Since then, pyrethrin compounds have become the dominant insecticide. Herbicides became common in the 1960s, led by "triazine ... The former involves taking direct measurement of the parent compound or its metabolites in various types of media: urine, blood ...
In trials using dogs, the compound did not cure ulcers, but proved to be a powerful vasodilator. Upjohn synthesized over 200 ... Due to anti-fibrotic activity of minoxidil inhibition of enzyme lysyl hydroxylase present in fibroblast may result in synthesis ... Possible Involvement of Sulfonylurea Receptor 2B as a Target of Minoxidil". Otomo, Susumu (March 2002). "[Hair growth effect of ... Minoxidil administration also brings an increase in plasma renin activity, largely due to the aforementioned activation of the ...
In addition, the emergence of resistance against the herbicide class of sulfonylureas has been reported recently. Due to its ... Antioxidant properties are high due to ascorbic acid and phenolic compounds. Furthermore, extracts of the flower head and ... Pirvu L., Dragomir C., Schiopu S., Mihul S. (2012). "Vegetal extracts with gastroprotective activity. Part. I. Extracts ... Centaurea cyanus contains a wide range of pharmacologically active compounds, such as flavonoids, anthocyanins and aromatic ...
However, as long as a particular compound possesses adequate chemical affinity to a channel, that compound may be able to bind ... A potential solution to this is a decrease in NMDA receptor activity, without interfering so drastically as to cause clinical ... Some of the best-known and studied substances include sulfonylureas, arylaminobenzenoates, and disulfonic stilbenes. These ... A channel block can be induced by many different types of organic compounds as long as they can bind to some portion of the ...
Activity-based proteomics - a branch of proteomics that uses covalent enzyme inhibitors as reporters to monitor enzyme activity ... This compound is a potent inhibitor of cGMP specific phosphodiesterase type 5, the enzyme that degrades the signalling molecule ... such as the sulfonylureas inhibit the enzyme acetolactate synthase. Both these enzymes are needed for plants to make branched- ... The activity will be decreased in a time-dependent manner, usually following exponential decay. Fitting these data to a rate ...
Once a compound that fulfills all of these requirements has been identified, it will begin the process of drug development ... Penicillin, introduced a few years later, provided a broader spectrum of activity compared to sulfa drugs and reduced side ... sulfonylureas, biguanides/metformin, thiazolidinediones, insulin), thyroid hormones, antithyroid drugs, calcitonin, ... Drug development is the process of bringing a new drug to the market once a lead compound has been identified through the ...
Sato K, Matsuura Y, Inoue M, Une T, Osada Y, Ogawa H, Mitsuhashi S (October 1982). "In vitro and in vivo activity of DL-8280, a ... Pyridobenzoxazine ring appears to decrease the extent of parent compound metabolism. Less than 5% is eliminated by the kidneys ... monitoring of serum glucose is advised when ofloxacin or other fluorquinolones are used by people who are taking sulfonylurea ... especially those with a broad spectrum of activity such as clindamycin, cephalosporins, and fluoroquinolones. Fluoroquinoline ...
An enzyme inhibitor is a molecule that binds to an enzyme and decreases its activity. Since blocking an enzyme's activity can ... This compound is a potent inhibitor of cGMP specific phosphodiesterase type 5, the enzyme that degrades the signalling molecule ... such as the sulfonylureas inhibit the enzyme acetolactate synthase. Both these enzymes are needed for plants to make branched- ... Activity-based proteomics - a branch of proteomics that uses covalent enzyme inhibitors as reporters to monitor enzyme activity ...
Sulfonylureas act by increasing insulin release from the beta cells in the pancreas. They often can be used as secondary ... In 1950, metformin, unlike some other similar compounds, was found not to decrease blood pressure and heart rate in animals. ... July 2002). "Metformin increases AMP-activated protein kinase activity in skeletal muscle of subjects with type 2 diabetes". ... July 2014). "Sulfonylurea versus metformin monotherapy in patients with type 2 diabetes: a Cochrane systematic review and meta- ...
The activities and clinical significance of the EETs are given on the epoxyeicosatrienoic acid page. CYP2C9 and CYP2S1 are ... Greene, J. F.; Newman, J. W.; Williamson, K. C.; Hammock, B. D. (2000). "Toxicity of epoxy fatty acids and related compounds to ... sulfonylurea-containing oral hypoglycemic agents, and the anti-(epilepsy) drug, phenytoin.[unreliable source?] 7) CYP2C19*2 ( ... The catalytic activity of endoplasmic reticulum-bound cytochrome P450 enzymes, including the epoxygenases, depends upon ...
... mutations in HNF1A cause diabetes that responds to low dose sulfonylurea agents. The identification of extreme sulfonylurea ... Real Hernandez LM, Fan J, Johnson MH, Gonzalez de Mejia E (2015-01-01). "Berry Phenolic Compounds Increase Expression of ... "The bifunctional DCOH protein binds to HNF1 independently of its 4-alpha-carbinolamine dehydratase activity". Nucleic Acids ... Accordingly, HNF-1α-induced diabetes has marked sulphonylurea sensitivity. This pharmacogenetic effect is consistent with ...
Once a compound that fulfills all of these requirements has been identified, it will begin the process of drug development ... androgens, antiandrogens, estrogens, gonadotropin, corticosteroids, human growth hormone, insulin, antidiabetics (sulfonylureas ... Penicillin, introduced a few years later, provided a broader spectrum of activity compared to sulfa drugs and reduced side ... Drug development is the process of bringing a new drug to the market once a lead compound has been identified through the ...
An herbicide described as having high residual activity will remain potent for a long term in the soil. For some compounds, the ... Several sulfonylureas, including Flazasulfuron and Metsulfuron-methyl, which act as ALS inhibitors and in some cases are taken ... Residual activity: An herbicide is described as having low residual activity if it is neutralized within a short time of ... Synergise the activity of the other component. No mixture is likely to have all these attributes, but the first two listed are ...
Items listed in bold indicate initially developed compounds of specific groups. #WHO-EM †Withdrawn drugs. ‡Veterinary use ... Decreases inflammation, pain, and fever, probably through inhibition of cyclooxygenase (COX-2 inhibitor) activity and ... Hydantoins, sulfonamides, sulfonylureas: Fenoprofen may displace these drugs from their binding site. ...
... estrogenic compounds in the diet, and endocrine-disrupting chemicals may be important also. Obesity plays an important role ... possibly due to a combination of low physical activity and high-calorie diets, and also in developing countries, where it is ... as antidiabetic drugs rather than sulfonylurea derivatives. Thiazolidinediones may cause slight weight gain but decrease " ...
Hundreds of modified compounds were synthesised in an effort to develop a model of the then-unknown H2 receptor. The first ... The use of quantitative structure-activity relationships (QSAR) led to the development of other agents - starting with ... sulfonylureas, metronidazole, and some recreational drugs such as ethanol and methylenedioxymethamphetamine (MDMA). The more ... based on the structure modification in the stomach due to the acid dissociation constant of the compound, led to the ...
These chemical compounds increase sensitivity to heat by reducing the threshold of heat receptor (TRPV1) activation from 109 °F ... Further reapplication is necessary only after activities such as swimming, sweating, and rubbing. This varies based on the ... and sulfonylureas. Unlike phototoxic reactions which resemble exaggerated sunburns, photoallergic reactions can cause intense ... sulfonylureas, tetracyclines, thiazides, and vinblastine. Photoallergic reactions: Uncommon immunological response to sunlight ...
In 2002, deCODE acquired a Chicago-based medicinal chemistry company in order to discover compounds based on its genetics ... 24 November 1996 For an overview of the company's activities and achievements in these early years, see the years 1997-2003 in ... "TCF7L2 Genetic Variation Augments Incretin Resistance and Influences Response to a Sulfonylurea and Metformin: The Study to ...
Second Generation Sulfonylurea
... , Glipizide, Glyburide, Glimepiride, Amaryl, Sulfonylurea Drug Interactions Causing Hypoglycemia. ... third-generation sulfonylurea with hypoglycemic activity. Compared to other generations of sulfonylurea compounds, glimepiride ... Second generation sulfonylurea (product), Second generation sulfonylurea, Second generation sulphonylurea. Spanish. ... Second Generation Sulfonylurea. Aka: Second Generation Sulfonylurea, Glipizide, Glyburide, Glimepiride, Amaryl, Sulfonylurea ...
Metsulfuron-methyl - Wikipedia
It is a systemic compound with foliar and soil activity, that inhibits cell division in shoots and roots. It has residual ... Metsulfuron-methyl is an organic compound classified as a sulfonylurea herbicide, which kills broadleaf weeds and some annual ... activity in soils, allowing it to be used infrequently but requiring up to 22 months before planting certain crops (sunflowers ...
ATP-Sensitive K+ Channel-Dependent Regulation of Glucagon Release and Electrical Activity by Glucose in Wild-Type and SUR1−/−...
The sulfonylurea compound tolbutamide suppresses glucagon secretion in normal and type 2 diabetic subjects (42). Furthermore, ... Glucose inhibits electrical activity in α-cells from SUR1−/− mice.. Figure 1A shows electrical activity recorded from a single ... A low activity of KATP channels is required for glucagon secretion.. Studies on isolated inside-out patches have revealed that ... Glucose reduces electrical activity in α-cells from wild-type and SUR1−/− mice. A: Current-clamp recording of membrane ...
Flow Through Components with an Antimicrobial Lining - THE BOC GROUP, INC.
A single coating of the composition can provide antimicrobial activity.. Sulfonylurea compounds that are suitable for use in ... A representative metal-containing sulfonylurea compound suitable for use in the present invention is silver tolbutamide (AgTol ... AgTol incorporates a tolbutamide ligand that is a sulfonylurea, tolbutamide.. The sulfonylureas are known for their ... as the water-soluble carboxylic acid does not affect the antimicrobial activity of the metal-containing sulfonylurea. The ...
Oral Antidiabetics | Springer for Research & Development
Sulfonylureas and Related Compounds: Chemistry and Structure-Activity Relationships H. Plümpe. Pages 65-72 ... chiefly sulfonylureas. While acknowledging the value of the ß- cytotropic sulfonylureas, we also need to recognize important ... Sulfonylureas: Physico-chemical Properties, Analytical Methods of Determination and Bioavailability S. L. Ali, H. H. Blume, B. ... Diabetes Diabetes mellitus Glucosidase inhibitors Insulin Non-Pharmacological management Pathophysiology of NIDDM Sulfonylureas ...
Benzoazine derivative or salt thereof and pharmaceutical compostion comprising the same - Patent # 5710152 - PatentGenius
The compound exhibits superior effects for reducing blood glucose value, plasma insulin value, and plasma triglyceride value, ... Although the sulfonylurea compounds exhibit a strong antidiabetic action based on pancreatic and ex-pancreatic activities, ... The compound (12) is reacted with the compound (13) in the presence of a suitable base and a solvent to obtain the compound (4 ... The acetal Compound (10) can be prepared by treating a correspondingaldehyde compound or ketone compound by a known method, ...
ISU Weed Science Online - Effect of pH on Accent Activity
The sulfonylurea herbicides (Accent, Classic, Harmony, etc.) are in a class of compounds known as weak acids. Weak acids are ... Enhancing the biological activity of nicosulfuron with pH adjusters. Weed Technol. 17:338-345.) discusses how the activity of ... Table 1. Influence of spray additives and acidifiers on water pH and Accent activity. Accent was applied at 0.25 oz/A on ... Effect of carrier pH on Accent activity. by Bob Hartzler. July 30, 2003 - While products intended to modify the pH of water ...
SULFONYL UREA DERIVATIVES AND THEIR USE IN THE CONTROL OF INTERLEUKIN-1 ACTIVITY. The present invention relates to compounds of ... HETEROCYCLIC COMPOUNDS HAVING ACTIVITY AS MODULATORS OF MUSCARINIC M1 AND/OR M4 RECEPTORS IN THE TREATMENT OF CNS DISEASES AND ... ANTIVIRAL COMPOUNDS. The present invention relates to novel compounds of general formula (I) wherein the groups X, and R1 to R4 ... COMPOUNDS THAT INHIBIT 3C AND 3CL PROTEASES AND METHODS OF USE THEREOF. Compounds, specifically protease inhibitors, more ...
Patent US6492130 - Modulation of the sulfonylurea receptor and calcium in adipocytes for ... - Google Patents
... present invention recognizes the presence of the sulfonylurea receptor in adipocytes and its utility in identifying compounds ... The invention provides methods for determining the ability of compounds to regulate lipogenesis and lipolysis by acting as a ... sulfonylurea-1 (SUR 1) potassium channel activator, an adipocyte potassium channel activator, an SUR 1 antagonist, and an ... Compounds that Modulate SUR Activity in Adipocytes Mediates Biochemical Parameters that Influence Obesity and Diabetes. Human ...
KAKEN - Research Projects | Investigation of Novel Function and Its Relation to Diseases for New Taget Proteins to Which...
Other sulfonylureas also inhibited those processes but glibenclamide was the most effective among the compounds tested. Little ... Publications] A. Kuniyasu, et al.: A new scorpion toxin which stimulates the Ca^,2+,-release channel activity of the skeletal ... We found out that glibenclamide, a typical antidiabetic sulfonylurea, bound and photolabel CD36 instead of sulfonylurea ... These results indicate that sulfonylureas act as not only inhibitor for oxidized LDL uptake via CD36 but also ACAT inhibitor, ...
gliquidone | Semantic Scholar
Like other second-generation compounds, gliquidone exerts greater binding affinity to SUR1 and increased potency compared to ... In addition, this agent exerts peroxisome proliferator-activated receptor (PPAR) gamma agonistic activity. ... A potent, second-generation sulfonylurea with antihyperglycemic activity. Like other second-generation compounds, gliquidone ... The receptor for antidiabetic sulfonylureas controls the activity of the ATP-modulated K+ channel in insulin-secreting cells. ...
COMPOSITIONS AND METHODS FOR TREATING OBESITY - Zadini, Filiberto P.
... and/or detergent compound. In some embodiments, formulations comprising liposomes include compounds which assist fat metabolism ... Overeating and reduced physical activity are considered to be the two major reasons of obesity, although several additional ... the sulfonylurea class of drugs (Tolbutamide, Glyburide), and Repaglinide (a meglitinide class drug). Thus, in a sense, while ... The compounds of the present invention (i.e., biocompatible emulsifiers) can be used alone or in combination with other ...
Protocols and Video Articles Authored by Beat Keller
Although the fungitoxic activity of these compounds is well understood, their effects on plant metabolism remain unclear. In ... Sulfonylurea compounds such as tribenuron-methyl specifically inhibit acetolactate synthase and are rapidly detoxified, but the ... Considering its transcriptional activity and the recent insertion of the element into at least two genes, Rider is a recently ... Nuclear Activity of MLA Immune Receptors Links Isolate-specific and Basal Disease-resistance Responses Science (New York, N.Y ...
OPUS at UTS: Design, synthesis and evaluation of N-aryl-glyoxamide derivatives as structurally novel bacterial quorum sensing...
Structure-Activity Relationship. en_US. dc.subject.mesh. Sulfonylurea Compounds. en_US. ... Compounds 31 and 32 exhibited the greatest QSI activity in P. aeruginosa MH602, with 48.7% and 42.7% reduction in QS activity ... Compounds 31 and 32 exhibited the greatest QSI activity in P. aeruginosa MH602, with 48.7% and 42.7% reduction in QS activity ... The QSI activity of the synthesized compounds was determined in the LasR-expressing Pseudomonas aeruginosa MH602 and LuxR- ...
First Generation Sulfonylurea
A long-acting, first-generation sulfonylurea with hypoglycemic activity. Compared to other sulfonylureas, chlorpropamide has an ... sulfonylurea compound used as a hypoglycemic in the treatment of noninsulin dependent diabetes mellitus. ... First Generation Sulfonylurea. First Generation Sulfonylurea Aka: First Generation Sulfonylurea, Tolbutamide, Tolazamide, ... First generation sulfonylurea (product), First generation sulfonylurea, First generation sulphonylurea. Spanish. sulfonilurea ...
Streptozotocin | Diabetes | Glibenclamide | Pancreas | Lipid Peroxidation | Creatinine
This sulfonylurea compound also shows extra pancreatic effect during long term administration and a greater risk of ... Schmid-Antomarchi H, De Weille J, Fosset M, Lazdunski M. The receptor for antidiabetic sulfonylureas controls the activity of ... Sulfonylurea and non-sulfonylurea hypoglycemic agents: Pharmachological properties and tissue selectivity. Diabetes Res Clin ... It is a sulfonylurea compound chemically, 5-chloro-N- [2- [4-cyclohexyl carbamoyl sulfamoyl) phenyl] ethyl]-2-methoxy benzamide ...
WO2005063226A1 - Compositions and methods for treating diabetes - Google Patents
Specifically exemplified herein is the concurrent administration of a cysteamine compound with at least one additional ... Firstly, the activity of the cysteamine compound and/or additional therapeutic agent(s) contained in the composition is ... Examples of therapeutic agents include, but are not limited to, gene-based pharmaceutical compounds; insulin; sulfonylureas (i. ... The inclusion compound host materials used in the micro-encapsulation method are preferably a cyclic polysaccharide compound ...
... invention provides for certain sulfonyl ureas and related compounds which have advantageous properties and show useful activity ... The compound is a compound of formula (I), has anti-RSV, HSV-1 and EV71 activities and has the... ... OXA-DIAZASPIRO COMPOUNDS HAVING ACTIVITY AGAINST PAIN. The present invention relates to oxa-diazaspiro compounds having ... OXA-AZASPIRO COMPOUNDS HAVING ACTIVITY AGAINST PAIN. The present invention relates to oxa-azaspiro compounds having ...
CV. Nuestros investigadores. Investigación. Universidad de Navarra
Compound 56, 1-(naphthalen-1-yl)-3-[(p-(3-pyrrolidin-1-ylpropoxy) benzene)]sulfonylurea exhibited the best H-3 antagonism ... Compounds 1a and 2a were the most active against Plasmodium falciparum strains. Structure-activity relationships demonstrated ... The new derivatives showed excellent in vitro biological activity against Trypanosoma cruzi. Compound 17, which was substituted ... and in vivo studies led to the identification of compounds 22 and 23 with significant in vitro anti-plasmodial activity against ...
... third-generation sulfonylurea with hypoglycemic activity. Compared to other generations of sulfonylurea compounds, glimepiride ... Glimepiride is a Sulfonylurea. The chemical classification of glimepiride is Sulfonylurea Compounds.. Glimepiride is a long- ... It is the first III generation sulphonyl urea it is a very potent sulphonyl urea with long duration of action.. ...
Antidiabetics and Hypoglycemics/Antiglycemics | Goldfrank's Toxicologic Emergencies, 11e | AccessEmergency Medicine | McGraw...
90 The sulfonylureas in use today are chemical modifications of that original sulfonamide compound. In the mid-1960s, the first ... 157 The hypoglycemic activity of a sulfonamide derivative used for typhoid fever was noted during World War II, and verified ... However, hypoglycemia is reported in as many as 20% of patients using sulfonylureas.73 In a study of 99,628 emergency ... 130). In an older review of 1,418 medication-related cases of hypoglycemia, sulfonylureas (especially the long-acting ...
Orally active sulfonylurea compounds (Fig. 1) have been used in the treatment of type 2 diabetes since the 1950s, following the ... and excretion of the different compounds). These differences appear as differences in intrinsic activity and potency and in ... HYPERGLYCEMIA DELAYS SULFONYLUREA ABSORPTION. *REDUCED SULFONYLUREA EFFICACY FOLLOWING CONTINUOUS EXPOSURE TO HIGH SULFONYLUREA ... REDUCED SULFONYLUREA EFFICACY FOLLOWING CONTINUOUS EXPOSURE TO HIGH SULFONYLUREA PLASMA LEVELS. The most important-but widely ...
Acetohexamide | definition of acetohexamide by Medical dictionary
sulfonylurea. [sul″fo-nil-u´re-ah] any of a class of compounds that exert hypoglycemic activity by stimulating the islet tissue ... drug class: sulfonylurea; antidiabetic; action: causes functioning β cells in the pancreas to release insulin, leading to a ... a sulfonylurea oral antidiabetic. indication It may be prescribed in the treatment of type 2 diabetes mellitus. ... a first generation sulfonylurea derivative, used as an oral hypoglycemic agent in the treatment of diabetes mellitus. ...
Characterisation of sulphonylurea and ATP-regulated K+ channels in rat pancreatic A-cells
ATP applied to the intracellular face of the membrane inhibited KATP channel activity with a Ki of 17 microM, an effect that ... Sulfonylurea Compounds / metabolism* * Sulfonylurea Receptors * Tolbutamide / pharmacology * Uridine Triphosphate / ... Characterisation of sulphonylurea and ATP-regulated K+ channels in rat pancreatic A-cells Pflugers Arch. 1999 Sep;438(4):428-36 ... The K+ channel opener diazoxide, but not cromakalim or pinacidil, inhibited electrical activity and increased the whole-cell K+ ...
The Structure and Metabolism of the Pancreatic Islets - 1st Edition
Histochemical Evidence for a Sulfonylurea Effect on the Zinc Content of the Pancreatic Islets. Role of Sulfhydryl Compounds and ... Electrical Activity in Islet Cells. Oxygen Consumption of the ß-Cells in Relation to Insulin Release. Respiration of the ß- ... The Insulin-releasing Activity of Extracts of the Porcine Intestinal Tract. The Effect of Glucose on the Insulin Secretion in ... The Activity Pattern of Enzymes Associated with Glycogen Metabolism in the Islets of Langerhans. On the Functional Significance ...
Full text] Potential role of coenzyme Q10 in health and disease conditions | NDS
... although the data are conflicting with other types of physical activity. This broad review of current CoQ10 literature, while ... an endogenously produced compound, is found in all human cells. Within the mitochondria, it plays a substantial role in energy ... There are two isomeric forms of CoQ10, which determine whether a supplement is a natural or synthetic version of the compound ( ... It is thus recommended that clinicians adjust the dosage of common diabetic medications, such as sulfonylureas and biguanides, ...
Gliclazide - DrugBank
Sulfonylureas are associated with weight gain, though less so than insulin. Due to their mechanism of action, sulfonylureas may ... Sulfonylureas increase both basal insulin secretion and meal-stimulated insulin release. Medications in this class differ in ... Sulfonylureas also increase peripheral glucose utilization, decrease hepatic gluconeogenesis and may increase the number and ... It belongs to the sulfonylurea class of insulin secretagogues, which act by stimulating β cells of the pancreas to release ...
US5929055A - Therapeutic method for management of diabetes mellitus - Google Patents
... complications characteristic of diabetic hyperglycemia are ameliorated through the activity of tetracycline compound, the ... blood glucose concentration in the mammal together with administering to the mammal an amount of a tetracycline compound ... The hypoglycemic agent can selected from among compounds such as sulfonyl ureas, thiazolidine diones, alpha-glucosidase ... Tetracycline compounds having target therapeutic activities EP2301534A1 (en) 2002-03-08. 2011-03-30. Paratek Pharmaceuticals, ...
Federal Register :: Trifloxysulfuron-sodium; Notice of Filing a Pesticide Petition to Establish a Tolerance for a...
Hydrolysis of the sulfonylurea and oxidative O-demethylation are minor pathways in the rat. Parent compound was the major ... Reduced horizontal and vertical motor activity were observed in males and females only at the time of peak effect (1-2 hours ... During the peak plasma period (1-2 hours post-dosing), motor activity parameters of the males were comparable to the control ... The multiple other metabolites formed in plants and animals are considered of equal or lesser toxicity than parent compound. ...
International Textbook of Diabetes Mellitus, 4th Ed., Excerpt #52: Incretin Physiology in Health and Disease Part 2 of 6
... increased GIP plasma concentrations have not been described in patients treated with sulfonylurea compounds, thereby ... incretin activity has been demonstrated for GIP and GLP-1 [8,17,18]. Plasma concentrations of GIP rise ∼10 - 15 min after meal ... expression of the sulfonylurea receptor subunits Kir6.2 and SUR1 as well as glucokinase have been detected . Furthermore, ... The biologic activity of these forms has been found to be rather similar . ...
TolbutamideSecretionReceptorsHypoglycemiaAntidiabeticGlyburideReceptorChlorpropamidePancreaticGlipizideGlimepirideGlucoseGeneration SulfonylureaPancreas to release insulinDerivativesBiguanidesAntihyperglycemicAbstractMetforminGlibenclamideHerbicideHerbicidesNovel sulfonylureaEffects of sulfonylureasNIDDMDerivativeMECHANISMHypoglycemic drugsOralInhibitSulfonamidePioglitazoneType II DiabePharmaceutically acceptableSynthesisMetabolismModulateDiabetesGliclazideDrugsAnticancerCompositions containing sucPotentBiologicalOxidative stressPharmacologicalDrugHyperglycemiaInhibitory ActivityMyocardialConcentrationsInvention relatesAntagonistsOrganic compoundsPharmaceuticalPresent invention
- The sulfonylureas tolbutamide (100 μmol/l) and glibenclamide (100 nmol/l) inhibited glucagon secretion to the same extent as a maximally inhibitory concentration of glucose. (diabetesjournals.org)
- Patients treated with diet plus a fixed dosage of either tolbutamide (a sulfonylurea) or phenformin (a biguanide) for 5 to 8 years had a cardiovascular mortality rate approximately 2.5 times that of patients treated with diet alone, resulting in discontinuation of both these treatments in the study. (drugs.com)
- Agents which interact with peptide terminal amine groups and epsilon amino groups of lysine [1 mM methyl acetimidate and 1 mM trinitrobenzene sulfonic acid (TNBS)] and also the guanido group of arginine (1 mM methyl glyoxal) produced a Mg(2+)-dependent irreversible inhibition of KATP channel activity which could be prevented by ATP but not tolbutamide. (dundee.ac.uk)
- Nuclear magnetic resonance (NMR) spectroscopy of inclusion compounds of tolbutamide and chlorpropamide with .BETA. (nii.ac.jp)
- Solid-state nuclear magnetic resonance spectroscopy and Raman spectroscopy of the inclusion compound of tolbutamide with .BETA. (nii.ac.jp)
- In mice lacking functional K ATP channels (SUR1 −/− ), glucagon secretion in the absence of glucose was lower than that observed in wild-type islets and both glucose (0-20 mmol/l) and the sulfonylureas failed to inhibit glucagon secretion. (diabetesjournals.org)
- However, because α-cells possess a different complement of voltage-gated ion channels involved in action potential generation than the β-cell, moderate membrane depolarization in α-cells is associated with reduced rather than increased electrical activity and secretion. (diabetesjournals.org)
- Sulfonylurea compounds and insulin which haveconventionally been used for the treatment of NIDDM mainly improve impaired insulin secretion. (patentgenius.com)
- Sulfonylureas increase both basal insulin secretion and meal-stimulated insulin release. (drugbank.ca)
- When GIP and GLP-1 were infused intravenously at their typical postprandial concentrations, glucose-stimulated insulin secretion was augmented in a similar fashion as seen after oral glucose ingestion, thereby suggesting that the insulinotropic activity of these hormones mediates the physiologic incretin effect to a near-total extent . (diabetesincontrol.com)
- Furthermore, expression of Kir6.2, Sur1, SGLT-1, GPR40, GPR119, and GPR120 was detected on rodent K cells, suggesting a potential modulation of GIP secretion through sulfonylureas and various G-protein receptor ligands . (diabetesincontrol.com)
- Enhancement of secretion by glibenclamide was reversed by pinacidil and cromakalim, indicating that the effects of glibenclamide were mediated via an action on a sulfonylurea receptor. (jneurosci.org)
- All sulfonylureas stimulate insulin secretion to reduce plasma glucose levels by inhibiting the activity of β-cell K ATP channels ( Gribble and Reimann, 2003 ). (elifesciences.org)
- These compounds stimulate secretion of insulin from pancreaticβ cells by inhibiting certain potassium channels. (sciencemag.org)
- Sulfonylureas block K+ channels in b cells, leading to depolarization, increased Ca2+ entry via voltage-dependent calcium channels, and increased secretion. (policeunitytour.com)
- Like the sulfonylureas and Prandin (repaglinide), Starlix works by stimulating insulin secretion from the beta cells of the pancreas. (mendosa.com)
- Unlike earlier drugs that stimulate insulin secretion, Starlix is fast acting and has a short duration of activity. (mendosa.com)
- This invention relates to compounds that are agonists of the muscarinic M1 receptor or M1 and M4 receptors and which are useful in the treatment of muscarinic M1 or M1/M4 receptor mediated diseases. (sumobrain.com)
- We found out that glibenclamide, a typical antidiabetic sulfonylurea, bound and photolabel CD36 instead of sulfonylurea receptors in cardiac tissues, since its affinity for the receptors was lower than the corresponding pancreatic counterparts. (nii.ac.jp)
- Each antihyperglycemic sulfonylurea appears to initiate this process via certain binding sites (sulfonylurea receptors [SURs]) at the surface of the β-cells. (diabetesjournals.org)
- Sulfonylureas also increase peripheral glucose utilization, decrease hepatic gluconeogenesis and may increase the number and sensitivity of insulin receptors. (drugbank.ca)
- However, increased GIP plasma concentrations have not been described in patients treated with sulfonylurea compounds, thereby challenging the physiologic importance of these receptors . (diabetesincontrol.com)
- Perforates the muscle fibers of the population the unpleasant after-taste of saccharin, their behavioural and cns: Compounds like amphetamine and 8- ht receptors as an adjuvant are more involved procedures (such as please write me a sonnet on the medial circumflex femoral artery. (dsaj.org)
- It also increases the activity of insulin receptors inside the cells, thereby increasing insulin sensitivity. (sepalika.com)
- It does so by specifically binding to sulfonylurea receptors of the pancreatic beta cells. (sepalika.com)
- These results demonstrate that sulfonylurea receptors can modulate Ca 2+ -dependent exocytosis via a mechanism downstream of Ca 2+ influx or mobilization. (jneurosci.org)
- Using both inhibitors and activators of K ATP channels, we report here a novel functional effect of glibenclamide to enhance catecholamine release via an action on sulfonylurea receptors that cannot be accounted for by effects on membrane potential or Ca 2+ influx. (jneurosci.org)
- Glysobuzole binds to sulfonylurea-specific receptors on pancreatic β-cells and blocks the ATP-dependent channels for potassium. (wikipedia.org)
- Although the sulfonylurea compounds exhibit a strong antidiabetic action based on pancreatic and ex-pancreatic activities, prudent care should be taken whenadministering them because these compounds may sometimes induce serious hypoglycemia. (patentgenius.com)
- Compared to other sulfonylureas, chlorpropamide has an increased risk of prolonged hypoglycemia because of its long half-life. (fpnotebook.com)
- However, hypoglycemia is reported in as many as 20% of patients using sulfonylureas. (mhmedical.com)
- However, the risk of long-lasting and hence dangerous hypoglycemia is higher with these two long-acting sulfonylureas. (diabetesjournals.org)
- Acetohexamide and tolazamide are not recommended even though they have mild diuretic activity, because their metabolic and excretion patterns may result in accumulation and hypoglycemia. (thefreedictionary.com)
- Due to their mechanism of action, sulfonylureas may cause hypoglycemia and require consistent food intake to decrease this risk. (drugbank.ca)
- Dryness or tingling of lips (This could also be caused by hypoglycemia, induced by sulfonylureas. (sepalika.com)
- In the frail elderly this hypoglycemia unawareness is compounded by mental and physical inability to respond to or treat low BG levels. (cfp.ca)
- Chapter 10 Drugs Acting on the Endocrine System 241 (c) As with all sulfonylureas, hypoglycemia is a potentially dangerous adverse effect of these short-acting agents. (policeunitytour.com)
- But at least from the studies that I saw the incidence of hypoglycemia is going to be much lower than that of the sulfonylurea drugs or Prandin. (mendosa.com)
- The receptor for antidiabetic sulfonylureas controls the activity of the ATP-modulated K+ channel in insulin-secreting cells. (semanticscholar.org)
- a sulfonylurea oral antidiabetic. (thefreedictionary.com)
- Oral antidiabetic agents sulfonylureas: These compounds have a similar rate to 50-30/minute. (dsaj.org)
- The primary objective of the present investigation is to evaluate the antidiabetic, antihyperlidemic and antioxidant activity of the methanolic extract of the Paederia foetida Linn. (biomedcentral.com)
- Glimepiride is a sulfonylurea antidiabetic medication drug, also known as a "secretagogue," that stimulates the beta cells in the pancreas to produce more insulin. (sepalika.com)
- Active compounds of plants have potency as antidiabetic that can be used in diabetes mellitus treatment. (scialert.net)
- Research of active compounds that have antidiabetic activity should be developed in order to obtain better therapeutic outcomes. (scialert.net)
- Investigational compounds in the pipeline include the potential first regenerative treatment for diabetes as well as a once-daily injectable GLP-1 agonist to be used alone, in combination with basal insulins, and/or in combination with oral antidiabetic agents. (worldpharmanews.com)
- While prominent in single-dose studies, these differences have less importance during long-term sulfonylurea treatment: at ordinary dosages, rapid- and short-acting (glipizide) and slow- and long-acting (glyburide) sulfonylureas maintained continuously effective plasma levels and similar 24-h glucose control. (diabetesjournals.org)
- Moreover, there was no difference in patient outcome between the first-generation sulfonylurea chlorpropamide and the second-generation glyburide in the U.K. Prospective Diabetes Study. (diabetesjournals.org)
- Prendergast BD "Glyburide and glipizide, second-generation oral sulfonylurea hypoglycemic agents. (drugs.com)
- Rydberg T, Jonsson A, Roder M, Melander A "Hypoglycemic activity of glyburide (glibenclamide) metabolites in humans. (drugs.com)
- Glipizide/Glimepiride/Glyburide (Sulfonylureas) stimulates the pancreas to release insulin. (sepalika.com)
- This can be compounded further by reduced renal clearance of hypoglycemic drugs such as sulfonylureas (eg, glyburide, gliclazide) and insulin. (cfp.ca)
- The present invention recognizes the presence of the sulfonylurea receptor in adipocytes and its utility in identifying compounds and in regulating lipogenesis and lipolysis. (google.com)
- The present invention relates to oxa-diazaspiro compounds having pharmacological activity towards the sigma (σ) receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in. (sumobrain.com)
- Sulfonylureas and glinides have similar mechanisms of action but differ in receptor affinity and binding sites and in absorption and elimination rates. (diabetesjournals.org)
- In these experimental models, expression of the sulfonylurea receptor subunits Kir6.2 and SUR1 as well as glucokinase have been detected . (diabetesincontrol.com)
- 1995 ) subsequently defined the mode of action and receptor target as agonist activity at the peroxisome proliferator-activated receptor-γ (PPAR-γ). (aspetjournals.org)
- A series of hydroxyfuroic acid compounds were synthesized and tested for their efficacies at activating human insulin receptor. (biomedcentral.com)
- This study reports a new non-quinone DMAQ B1 derivative, a hydroxyfuroic acid compound (D-410639), which is 128 fold less cytotoxic as DMAQ B1 and as potent as compound 2, a DMAQ B1 synthetic derivative from Merck, at activating human insulin receptor. (biomedcentral.com)
- Structure and activity relationship of the prenylindole moiety to insulin receptor activation is discussed. (biomedcentral.com)
- Therefore, a new insulin receptor activator without a quinone moiety is a logical compound to develop. (biomedcentral.com)
- Consists of 2 polypeptide chains (A and B) connected by disulfide bonds Positions B24 and B25 are important sites for receptor recognition substitution at these sites is associated with a marked change in biological activity. (powershow.com)
- Wensbo, D. "Structure-activity Relationships for the Linker in a Series of Pyridinyl-alkynes that are Antagonists of the Metabotropic Glutamate Receptor 5 (mGluR5). (gu.se)
- Zetterberg, F. Synthesis, Structure-Property Relationships and Pharmacokinetic Evaluation of Ethyl 6-Aminonicotinate Sulfonylureas as Antagonists of the P2Y12 Receptor. (gu.se)
- Pioglitazone is a thiazolidinedione compound with a mode of action as a peroxisome proliferator-activated receptor gamma agonist. (clinicaltrials.gov)
- Activation of this receptor causes increased transcriptional activity at a number of locations that are important to carbohydrate and lipid (fat) metabolism. (clinicaltrials.gov)
- A sulphonylurea hypoglycemic agent with actions and uses similar to those of CHLORPROPAMIDE. (fpnotebook.com)
- The current study reveals that glibenclamide treatment has a significant role in lowering the blood glucose but at the same time it increased the oxidative stress, which was reflected in the elevated malondialdehyde activity of both the hepatic and pancreatic tissues. (ijpsonline.com)
- We conclude that rat pancreatic A-cells express KATP channels with the nucleotide-, sulphonylurea- and K+ channel-opener sensitivities expected for a channel formed by Kir6.2 and SUR1 subunits. (nih.gov)
- showed remarkable antihyperglycemic activity due to its possible systematic effect involving in the pancreatic and extra pancreatic mechanism. (biomedcentral.com)
- Sulfonylureas, while promoting release of insulin (9-11) through blockade of metabolism regulated adenosine triphospate-sensitive potassium channel (K ATP ) channels present in pancreatic b-cell membranes (12,13) , also block K ATP channels present in cardiac cells and coronary vasculature (14-17) . (onlinejacc.org)
- Glysobuzole has antihyperglycemic activity, so it is able to lower blood glucose levels by increasing the release of insulin from the pancreatic beta cells. (wikipedia.org)
- Sulfonylureas are anti-diabetic medications that act by inhibiting pancreatic K ATP channels composed of SUR1 and Kir6.2. (elifesciences.org)
- Both compounds inhibited 86 Rb ( 42 K substitute) outflow from rat pancreatic islets perifused throughout at low (2.8 mM) d -glucose concentration. (aspetjournals.org)
- The aim of the present study was to further document the effects of BM 208 and BM 225 on the secretory activity of rat pancreatic B cells. (aspetjournals.org)
- Glucagon-like peptide-1 promotes DNA synthesis, activates phosphatidylinositol 3-kinase and increases transcription factor pancreatic and duodenal homeobox gene 1 (PDX-1) DNA binding activity in beta (INS-1)-cells. (glucagon.com)
- Glimepiride is a Sulfonylurea. (jaycochemicals.com)
- The chemical classification of glimepiride is Sulfonylurea Compounds. (jaycochemicals.com)
- Compared to other generations of sulfonylurea compounds, glimepiride is very potent and has a longer duration of action. (jaycochemicals.com)
- Compounds Ia - c , e , and IVg showed promising antihyperglycemic activity equivalent to a well-known standard antihyperglycemic drug, Glimepiride (Amaryl, 4 mg/kg). (hindawi.com)
- Glimepiride (Amaryl) is a sulfonylurea containing a pyrrole group, acting as antihyperglycemic drug [ 22 ]. (hindawi.com)
- The ability of high glucose concentrations to suppress glucagon release has been attributed to both direct actions on the α-cells ( 5 - 7 ) and paracrine effects exerted by compounds released by neighboring β- and δ-cells ( 5 , 8 - 12 ). (diabetesjournals.org)
- The compound exhibits superior effects for reducing blood glucose value, plasma insulin value, and plasma triglyceride value, and is useful as a medicament for preventing or treating diabetes, hyperlipidemia, and obesity. (patentgenius.com)
- The mechanisms involved in increased free radical production in diabetes include auto oxidation of glucose, shifts in redox balances, reduced tissue antioxidant status [ 4 ] and reduced activity of tissue antioxidant enzymes [ 5 ]. (ijpsonline.com)
- Orally active sulfonylurea compounds ( Fig. 1 ) have been used in the treatment of type 2 diabetes since the 1950s, following the serendipitous discovery a decade earlier that this kind of sulfonamides could reduce blood glucose levels ( 3 ). (diabetesjournals.org)
- A first-generation oral sulfonylurea used to reduce glucose in type 2 diabetics whose diabetes can't be controlled by diet. (thefreedictionary.com)
- A method for treating diabetes in a mammal by moderately controlling blood glucose concentration in the mammal together with administering to the mammal an amount of a tetracycline compound effective to reduce complications associated with diabetic hyperglycemia. (google.com)
- Blood glucose concentration can be controlled by moderate administration (e.g., fewer injections per day) of insulin or another glucose-modulating agent, while pathological complications characteristic of diabetic hyperglycemia are ameliorated through the activity of tetracycline compound, the latter preferably administered in an amount that is substantially non-antimicrobial. (google.com)
- Due to the hypoglycemic activity of glysobuzole it is used to treat type 2 diabetes by raising the plasma insulin levels and, effectively, lowering the blood glucose levels. (wikipedia.org)
- The current findings from both papers imply that targeting the gut with small compounds could represent the alternative strategies to lower glucose levels and reduce diabetic complications. (blogspot.com)
- Recently, dipeptidyl peptidase IV (DPP-IV) inhibitors [ 23 - 25 ] have been shown to be effective and safe compounds that control blood glucose. (hindawi.com)
- Mechanism of action (1) Sulfonylureas cause an increase in the amount of insulin secreted by the b cells in response to a glucose challenge. (policeunitytour.com)
- They were testing various compounds and stumbled on this drug as a glucose lowering agent. (mendosa.com)
- The development of new classes of blood glucose-lowering medications to supplement the older therapies, such as lifestyle-directed interventions, insulin, sulfonylureas, and metformin, has increased the treatment options for type 2 diabetes. (diabetesjournals.org)
- A potent, second-generation sulfonylurea with antihyperglycemic activity. (semanticscholar.org)
- These images are a random sampling from a Bing search on the term "First Generation Sulfonylurea. (fpnotebook.com)
- An intermediate-acting, first-generation sulfonylurea with hypoglycemic activity. (fpnotebook.com)
- a first generation sulfonylurea derivative, used as an oral hypoglycemic agent in the treatment of diabetes mellitus. (thefreedictionary.com)
- It is sometimes classified either as the first third-generation sulfonylurea or as second-generation. (hindawi.com)
Pancreas to release insulin1
- It belongs to the sulfonylurea class of insulin secretagogues, which act by stimulating β cells of the pancreas to release insulin. (drugbank.ca)
- Thiazolidine derivatives such as troglitazone and pioglitazone have been developed as compounds which possess such an action (Japanese Patent Applications Laid-open No. 22636/1980, No. 51189/1985, and No.157522/1994). (patentgenius.com)
- A solvent-free synthetic route was developed for the sulfonylurea benzothiazoline derivatives via the cyclization and carbamylation. (preprints.org)
- The third part tackles chemical structure and biological activities, such as structure-activity relationships in derivatives of anticholinesterase insecticides and the fungicidal activity of acyl anilines. (elsevier.com)
- Synthesis was developed to investigate the structure-activity relationships (SAR) of a novel series of 2-alkynylpyridine derivatives as mGluR5 antagonists. (gu.se)
- A series of pyrrole and pyrrolopyrimidine derivatives were examined for their in vivo antihyperglycemic activity. (hindawi.com)
- These huge therapeutic applications have motivated new efforts in the search for novel derivatives with improved biological activity and diverse applications in the pharmaceutical industry [ 1 - 4 , 19 , 20 ]. (hindawi.com)
- Motivated by the importance of this system and in continuation of our research efforts [ 26 - 30 ], we try to highlight aspects reported on the chemistry of some newly synthesized pyrrole and pyrrolopyrimidine derivatives and evaluate them for the antihyperglycemic activities. (hindawi.com)
- The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. (patents.com)
- Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed. (patents.com)
- The majority of NIDDM patients are treated with sulphonylurea (SU) derivatives. (nih.gov)
- Relationship between competitive adsorption by carbon black from aqueous solution and formation of molecular compounds in the solid phase for aminopyrine and barbituric acid derivatives. (nii.ac.jp)
- In this paper, we examine and discuss the structure-activity relationships and antihyperglycemic activity of these compounds. (hindawi.com)
- These findings reflect the potential antihyperglycemic and hypolipidemic effects of α, β-amyrin mixture and suggest that it could be a lead compound for drug development effective in diabetes and atherosclerosis. (biomedcentral.com)
- abstract = "The effects of several group-specific chemical reagents were examined upon the activity of the ATP-sensitive potassium (KATP) channel in the CRI-G1 insulin-secreting cell line. (dundee.ac.uk)
- There are reports in which combination treatment of sulfonylurea with metformin has been reported to achieve satisfactory glycaemic control for several years. (pdfmedfinder.com)
- Since metformin is reported to have predominant peripheral mechanism of action, therefore it lacks the anabolic effects of sulfonylureas and does not cause weight gain. (pdfmedfinder.com)
- Researchers at the Toronto General Hospital Research Institute have discovered metformin (the most widely prescribed type 2 diabetic medication) and resveratrol, a compound found in red wine, trigger novel signaling pathways in the small intestine to lower blood sugar. (blogspot.com)
- One compound studied is the commonly-used drug metformin for patients with Type 2 diabetes, and the other is resveratrol, a compound found in red wine, grapes, peanuts and blueberries. (blogspot.com)
- Treatment of diabetic patients has been focused on dietary management and oral antidiabetics, among these: sulfonylureas, metformin, acarbose, and others. (hindawi.com)
- OBJECTIVE -Therapies with metformin, sulfonylureas, or insulin improve glycemic control in the short term but do not prevent progressive islet β-cell failure or long-term deterioration in glycemia. (diabetesjournals.org)
- Furthermore, despite the initial efficacy seen with traditional agents such as sulfonylureas, metformin, or insulin, normoglycemia is frequently not obtained and progressive loss of glycemic control has been shown to correlate with declining β-cell function ( 5 ). (diabetesjournals.org)
- Metformin may be used alone or in combination with sulfonylureas and thiazolidinediones. (policeunitytour.com)
- Other sulfonylureas also inhibited those processes but glibenclamide was the most effective among the compounds tested. (nii.ac.jp)
- We discovered that glibenclamide also inhibited the activity of acyl CoA: cholesterol acyltransferase (ACAT) in macrophages. (nii.ac.jp)
- glibenclamide inhibits ACAT activity in macrophage cell lines of J774 and phorbolester-treated THP-1'J. (nii.ac.jp)
- Here, we present a cryo-EM structure of a hamster SUR1/rat Kir6.2 channel bound to a high-affinity sulfonylurea drug glibenclamide and ATP at 3.63 Å resolution, which reveals unprecedented details of the ATP and glibenclamide binding sites. (elifesciences.org)
- Metsulfuron-methyl is an organic compound classified as a sulfonylurea herbicide, which kills broadleaf weeds and some annual grasses. (wikipedia.org)
- The authors concluded that increasing the pH of the herbicide carrier could increase Accent solubility and biological activity under specific conditions. (iastate.edu)
- The molecular docking result showed that the new compound competed with chlorosulfuron to bind with the herbicide target enzyme active site to attain detoxification. (preprints.org)
- Especially advantageous compounds are those in which the salt of the herbicide of the formula (I) is formed by replacing the hydrogen of the -SO2-NH- group by a cation selected, for example, from the group consisting of the alkali metals, alkaline earth metals and ammonium ions, preferably sodium or tetrabutylammonium. (allindianpatents.com)
- Nicosulfuron is a selective herbicide belonging to the sulfonylurea family, commonly applied on maize crops. (frontiersin.org)
- Nicosulfuron (2-[(4,6-dimethoxypyrimidin-2-yl)carbamoylsulf-amoyl]- N,N -dimethylpyridine-3-carboxamide) is a sulfonylurea class herbicide used worldwide as a post-emergence herbicide to protect maize crops from weeds. (frontiersin.org)
- The sulfonylurea herbicides (Accent, Classic, Harmony, etc.) are in a class of compounds known as weak acids. (iastate.edu)
- The water solubility of sulfonylureas increases as they ionize, thus the herbicides dissolve more readily when mixed in water with a high pH. (iastate.edu)
- Screening method for nine sulfonylurea herbicides in soil and water by liquid chromatography with ultraviolet detection. (springer.com)
- In the present study, we have designed and synthesized a series of 42 novel sulfonylurea compounds with ortho-alkoxy substitutions at the phenyl ring and evaluated their herbicidal activities. (bvsalud.org)
- A series of novel sulfonylurea benzothiazoline were designed by splicing active groups and bioisosterism. (preprints.org)
Effects of sulfonylureas1
- In this project we first aim to reveal functional effects of sulfonylureas on CD36 in macrophages. (nii.ac.jp)
- Sulphonylurea treatment of NIDDM patients with cardiovascular disease: a mixed blessing? (nih.gov)
- The disclosed subject matter provides pyrazolone derivative compounds, pharmaceutical compositions comprising such compounds, kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. (sumobrain.com)
- 81 , 157 The hypoglycemic activity of a sulfonamide derivative used for typhoid fever was noted during World War II, and verified later in animals. (mhmedical.com)
- It is a sulfonamide derivative that is similar to sulfonylureas. (wikipedia.org)
- Despite numerous articles publicizing the clinical efficacy and molecular mechanism of action of thiazolidinediones, information in the peer-reviewed literature regarding the safety profile of this class of compounds in multiple animal species is incomplete. (aspetjournals.org)
- Another, beta cell-independent mechanism of the blood sugar lowering activity of sulfonylureas has also been theorized and studied. (sepalika.com)
- The mechanism of action and the controversy surrounding the clinical use of sulfonylurea drugs has recently been reviewed in detail (8) . (onlinejacc.org)
- Probenecid and colchicine contains probenecid, which is a uricosuric agent, and colchicine, which has antigout activity, the mechanism of which is unknown. (rxlist.com)
- Sulfonylureas are powerful hypoglycemic drugs that have been used for decades to treat diabetic patients. (semanticscholar.org)
- Roughly 30% -50% of the patients with diabetes in Europe and the United States are treated with oral antidiabetics, chiefly sulfonylureas. (springer.com)
- Clinical outcomes after direct balloon angioplasty for acute myocardial infarction were evaluated in 67 diabetic patients taking oral sulfonylurea drugs and 118 diabetic patients not taking these drugs. (onlinejacc.org)
- The Company currently has insulin products that are also available in injection pens for people with type 1 or type 2 diabetes, as well as an oral, once-daily sulfonylurea treatment for type 2 diabetes. (worldpharmanews.com)
- These drugs are usually combined with a sulfonylurea or another oral hypoglycemic agent. (policeunitytour.com)
- Our structure provides novel mechanistic insights of how sulfonylureas and ATP interact with the K ATP channel complex to inhibit channel activity. (elifesciences.org)
- Despite their clinical importance and decades of research, how sulfonylureas interact with and inhibit K ATP channel activity remains poorly understood. (elifesciences.org)
- The irreversible activation of the KATP channel produced by the proteolytic enzyme trypsin was prevented only when methyl glyoxal and methyl acetimidate were used in combination to inhibit channel activity. (dundee.ac.uk)
- 90 The sulfonylureas in use today are chemical modifications of that original sulfonamide compound. (mhmedical.com)
- This study described the synthesis of a number of sulofenur thiadiazole analogues with structural modification of the aryl moiety of the sulfonamide portion of the diaryl sulfonylureas. (bvsalud.org)
- Sulfonamide allergy: Chemical similarities are present among sulfonamides, sulfonylureas, carbonic anhydrase inhibitors, thiazides, and loop diuretics (except ethacrynic acid). (drugs.com)
Type II Diabe1
- Among possible contributing factors, use of sulfonylurea hypoglycemic agents has been reported to increase cardiovascular mortality in patients with non-insulin dependent (type II) diabetes mellitus (6,7) . (onlinejacc.org)
- which are endowed with antiinflammatory activity and are substantially free of antibiotic properties, to pharmaceutically acceptable salts thereof and to pharmaceutical compositions containing them as active ingredient. (patentsencyclopedia.com)
- Ye, F. Solvent-Free Synthesis and Safener Activity of Sulfonylurea Benzothiazolines. (preprints.org)
- Pesticide Chemistry: Human Welfare and the Environment, Volume I: Synthesis and Structure-Activity Relationships covers the proceedings of the Fifth International Congress of Pesticide Chemistry. (elsevier.com)
- Synthesis of compounds similar to that of the parent drug in the clinical trial will be a boon for the drug discovery programme. (omicsonline.org)
- Hence, synthesis of compounds with structure and properties similar to that of the parent compound in the clinical trial is necessary. (omicsonline.org)
- Little has been known whether sulfonylureas affect the lipid metabolism and we then investgated their effects on cholesterol metabolism. (nii.ac.jp)
- These results indicate that sulfonylureas act as not only inhibitor for oxidized LDL uptake via CD36 but also ACAT inhibitor, although chemical structures are quite different from conventional inhibitors, suggesting that they can be seeds to generate new potential inhibitors for the lipid metabolism. (nii.ac.jp)
- Additionally, type 2 diabetes is associated with increased prevalence of hypertension, disorders in lipid metabolism, fibrinolytic activity ( 2 ), and enhanced activity of markers of inflammation ( 3 ). (diabetesjournals.org)
- Synthesized compound or materials have to go through biological assays, in vitro and in vivo drug metabolism, pharmacokinetic studies, pharmacological and toxicological studies. (omicsonline.org)
- Conformationally constrained macrocyclic compounds of formula (I), including substituents E, G, and Q, as defined in the description and the claims, and salts thereof, have the property to modulate the activity of the peptidyl-prolyl cis. (sumobrain.com)
- In this review, we will summarize and discuss the major upstream signaling pathways and molecules that could modulate the NER's activity. (hindawi.com)
- Therefore, in this review, we will discuss the role of the major upstream pathways or molecules that modulate the NER activities and their potential uses as new therapeutic drugs helping to reduce NER disease symptoms. (hindawi.com)
- A sulfonylurea hypoglycemic agent used in the treatment of non-insulin-dependent diabetes mellitus not responding to dietary modification. (fpnotebook.com)
- Specifically exemplified herein is the concurrent administration of a cysteamine compound with at least one additional therapeutic agent to prevent and/or treat diabetes as well as prevent and/or treat complications associated with diabetes. (google.com)
- contraindications Its use is prohibited as sole therapy in type 1 diabetes mellitus, diabetic ketoacidosis, severe liver or kidney dysfunction, or known hypersensitivity to this drug or to other sulfonylureas. (thefreedictionary.com)
- The invention relates to a method of using tetracycline compounds in the treatment of diabetes. (google.com)
- Search for compounds that normalize hyperglycemia, hyperlipidemia and ameliorate oxidative stress is an important objective in preventing diabetes-associated complications. (biomedcentral.com)
- Some evidence shows that taking chromium picolinate (a chemical compound that contains chromium) by mouth, either alone or along with biotin, can lower fasting blood sugar, lower insulin levels, and help insulin work in people with type 2 diabetes. (webmd.com)
- Also, chromium picolinate might decrease weight gain and fat accumulation in people with type 2 diabetes who are taking a class of antidiabetes medications called sulfonylureas. (webmd.com)
- Diabetes communicates focus, and Program denotes an activity that is planned to achieve a specified end. (jameslindlibrary.org)
- However, sulfonylureas do not decrease the insulin requirements of patients with type I diabetes. (policeunitytour.com)
- This example emphasizes the relevance of information on kinetics-effect relations of therapeutic drugs, and the current overview describes some of these relations among insulin-releasing compounds, i.e., sulfonylureas and meglitinide analogs (glinides). (diabetesjournals.org)
- As the concentrations of the former two drugs were in the range of nmol/l and those of the latter two in the mumol/l range, the findings support the notion that the intrinsic activity of the two second-generation sulfonylureas is at least 1 000 times greater than that of the two first-generation drugs. (nih.gov)
- Sulfonylureas fall under the category of "Sulfa" drugs. (sepalika.com)
- Sulfonylurea drugs impair ischemic preconditioning. (onlinejacc.org)
- Whether sulfonylurea drugs affect outcome adversely in diabetic patients undergoing direct angioplasty for acute myocardial infarction is unknown. (onlinejacc.org)
- This early risk is not explained by an increase in ventricular arrhythmias, but may reflect deleterious effects of sulfonylurea drugs on myocardial tolerance for ischemia and reperfusion. (onlinejacc.org)
- Failure of drugs [ 3 ] in the clinical trials will have to be supported by group of compounds, whose structure or properties are similar to that of the drug under clinical trials. (omicsonline.org)
- Diabetics are frequently treated with a group of drugs known as sulfonylureas. (sciencemag.org)
- Bioavailability of powdered inclusion compounds of nonsteroidal antiinflammatory drugs with .BETA. (nii.ac.jp)
- We evaluated muscle tissue morphology and fibers size in the current presence of anticancer compounds, results on body structure and muscle tissue strength, combined with the modulation of chemotherapy-specific genes and protein. (gasyblog.com)
Compositions containing suc1
- The invention provides sulfoxyalkyl organonitro and related compounds, compositions containing such compounds, and methods for using such compounds and compositions to treat medical disorders, such as a neurodegenerative disorder, autoim. (sumobrain.com)
- Improvement of the inhibitory activity and chemical stability of a series of substituted piperidinyl glycine 2-cyano-4,5-methano pyrroline (DPP-IV) inhibitors was, respectively, achieved by the introduction of pyrroline moiety at the 4 position and 1 position of the piperidinyl glycine, leading to a series of potent and stable DPP-IV inhibitors [ 25 ]. (hindawi.com)
- 2003. Enhancing the biological activity of nicosulfuron with pH adjusters. (iastate.edu)
- Each of the around 40 chapters describes one or two typical syntheses of a specific compound class and provides concise information on the history of development, mode of action, biological activity and field of application, as well as structure-activity relationships. (wiley.com)
- The biological activity tests indicated the compounds could protect maize against the injury caused by chlorsulfuron to some extent. (preprints.org)
- In addition, several chemical and biological compounds have proven success in regulating NER's activity. (hindawi.com)
- among these, pyrrolo[3,2- d ]pyrimidines, a class of 7-deazapurine analogs, exhibit interesting biological activity in part due to their resemblance to pyrimidines and purines. (hindawi.com)
- While trying to maintain consistency of in vitro and in vivo biological activity, a simple scaffold replacement of thienopyrimidine with pyrrolopyrimidine lead to significantly improved metabolic stability [ 22 - 24 ], as shown in Figure 2(c) . (hindawi.com)
- Biotransformation approaches and synthetic methods in tandem provide a source for generating compounds around core structures, which can be screened for various biological activity studies. (omicsonline.org)
- After performing all the studies, compounds are to be ranked for clinical trials, and the compound that satisfies all the chemical and biological assays will be further tested. (omicsonline.org)
- The data obtained from biological activity were found highly correlated with that obtained from molecular modeling studies. (bvsalud.org)
- Supercritical fluid extraction/chromatography and immunoassay analysis are two areas of intense current activity from which substantial advances in the determination of benzidine and it's metabolites in biological samples can be anticipated. (cdc.gov)
- The purpose of the present invention is to provide a method for detecting a compound containing a formyl dehydropiperidine structure such as an acrolein-amine conjugate serving as an oxidative stress marker. (sumobrain.com)
- The present invention relates to compounds of general formula (I), wherein D 1 to D 3, -A-, n, R 1, R 2, Y 1, L and y2 are defined as in claim 1, which have valuable pharmacological properties, in particular are inhibitors of plasma kall. (sumobrain.com)
- Both compounds have an additive antihyperglycaemic effect without increasing the adverse effects of either pharmacological class. (pdfmedfinder.com)
- Patients with impaired liver and/or renal function treated with sulfonylureas may be exposed to higher serum drug concentrations, which can increase the potential for severe hypoglycemic episodes induced by these agents. (drugs.com)
- The purpose of this study was to examine the impact of sulfonylurea drug use on outcome in diabetic patients undergoing direct coronary angioplasty for acute myocardial infarction. (onlinejacc.org)
- Univariate analysis identified sulfonylurea drug, age, ventricular function, ejection fraction less than 40%, prior bypass surgery and congestive heart failure as correlates of increased in-hospital mortality. (onlinejacc.org)
- Logistic regression found sulfonylurea drug use (odds ratio 2.77, p = 0.017) to be independently associated with early mortality. (onlinejacc.org)
- Congestive heart failure, but not sulfonylurea drug use, was associated with an increased incidence of in-hospital ventricular arrhythmias. (onlinejacc.org)
- Congestive heart failure, prior bypass surgery and female gender, but not sulfonylurea drug use, were associated with late adverse events. (onlinejacc.org)
- Sulfonylurea drug use is associated with an increased risk of in-hospital mortality among diabetic patients undergoing coronary angioplasty for acute myocardial infarction. (onlinejacc.org)
- For surviving patients sulfonylurea drug use is not associated with an increased risk of serious late adverse events. (onlinejacc.org)
- Since ischemic preconditioning and coronary vasodilation act to protect the heart against ischemic insults (24) , sulfonylurea drug action within the myocardium may increase its vulnerability to ischemia (25) . (onlinejacc.org)
- Yesino if urine or syrups (see absence of drug-metabolizing enzymes fucidin can be inserted between these measurements can damage to test uid and cerebro- many patients should be the compound should be highly protein inhibitor, atazanavir. (creativephl.org)
- Empower delivers an expansive compounded drug formulary across multiple areas of treatment that address what is important to both prescribers and patients: cost, convenience, compliance, and confidence in quality. (empowerpharmacy.com)
- These studies help in screening and advancing the compounds, through various stages of drug discovery programme. (omicsonline.org)
- In the present study, a sulfonylurea urea drug was incubated with microsomal proteins to produce metabolites. (omicsonline.org)
- In silico ADMET studies suggest that most compounds possess drug-likeness properties. (bvsalud.org)
- Sanofi-aventis (EURONEXT: SAN and NYSE: SNY) and Ascendis Pharma (Ascendis) announced a global licensing and patent transfer agreement on Ascendis' proprietary TransCon Linker and Hydrogel carrier technology, which allows for a drug compound to be released in the body in a precise, time-controlled fashion, creating a long-acting effect. (worldpharmanews.com)
- The technology utilizes Ascendis Pharma's proprietary TransCon Linker families, which are a diverse group of structures with inherent chemical self-cleaving properties, making drug release independent of enzyme activity and tissue conditions. (worldpharmanews.com)
- Ascendis Pharma´s transient conjugation allows for a drug compound to be released in the body in a precise, time-controlled fashion, creating a long-acting effect for the original unmodified drug. (worldpharmanews.com)
- As PEGylation reduces the activity of the drug, higher plasma concentrations are needed to ensure efficacy, but this adds to the occurrence of peak concentration-related adverse events. (worldpharmanews.com)
- The theraTRACE® indications discovery platform allows for known drug-like compounds to be. (scienceexchange.com)
- The theraTRACE® indications discovery platform allows for known drug-like compounds to be comprehensively screened using a battery of in vivo assays spanning multiple therapeutic areas. (scienceexchange.com)
- The in vivo models utilized in the theraTRACE® platform comprise those typically used by pharmaceutical companies to determine whether a drug candidate is suitable for further clinical evaluation, however, these models are assembled in a proprietary "multiplexed" format that allows drug discoverers to evaluate a compound for potential efficacy in a broad array of therapeutic areas rapidly and cost-effectively. (scienceexchange.com)
- Accordingly, a vicious circle may be established: unrelenting hyperglycemia may promote sulfonylurea dose increase, which increases hyperglycemia, promoting further dose increase and eventually therapeutic failure. (diabetesjournals.org)
- The aim of this study was to determine in vitro inhibitory activity of α-glucosidase, α-amylase and Dipeptidyl peptidase IV from 42 ethanolic extract s of selected Indonesian plants. (scialert.net)
- Inhibitory activity was measured using spectrophotometric method. (scialert.net)
- The ethanolic extract s have DPP-IV inhibitory activity between 10-20%, lower than Diprotin as positive control, except Camelia sinensis (white) which gave the inhibition more than 30% at 62.5 μg mL 1 . (scialert.net)
- This study was conducted to find inhibitory activity of α-amylase, α-glucosidase and DPP-IV from Indonesian plants. (scialert.net)
- considerations: The larger disease cells of the compounds Pertaining from the Myocardial thinking of the sulfonylurea. (sheppardengineering.com)
- In all cases, as tribenuron methyl disappeared, two compounds were detected with increased concentrations. (bvsalud.org)
- The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their produc. (sumobrain.com)
- The present invention relates to substituted-cyanopyrrolidines of Formula (I) with activity as inhibitors of deubiquitilating enzymes, in particular, ubiquitin C-terminal hydrolase 30 or ubiquitin specific peptidase 30 (USP30), having ut. (sumobrain.com)
- The present invention relates to novel compounds and their use in the prophylactic and/or therapeutic treatment of hypertension and/or fibrosis. (sumobrain.com)
- in particular, the invention relates to herbicidal compositions comprising certain sulfonylureas and/or their salts and specific surfactants, which compositions are outstandingly suitable for controlling harmful plants in crop plants. (allindianpatents.com)
- The low aqueous solubility was addressed by variation of the linker which led to the discovery of sulfonylureas as P2Y12 antagonists. (gu.se)
- Biotransformation is a process by which organic compounds are transformed from one form to another, aided by organisms such as bacteria, fungi and enzymes. (omicsonline.org)
- Following the successful and proven concept used in "Bioactive Heterocyclic Compound Classes" by the same editors, this book is the first to present approved pharmaceutical and agrochemical compounds classified by their carboxylic acid functionality in one handy volume. (wiley.com)
- Empower is an industry leading compounding pharmacy and outsourcing facility with an 11 year history of excellence and innovation in pharmaceutical compounding. (empowerpharmacy.com)
- and a pharmaceutical composition including an effective amount of the compound. (patentgenius.com)
- It was an object of the present invention to provide herbicidal compositions having particularly high herbicidal activity. (allindianpatents.com)