4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone: Inhibitor of phosphodiesterases.Imidazolidines: Compounds based on reduced IMIDAZOLINES which contain no double bonds in the ring.Receptors, Epoprostenol: Cell surface receptors for EPOPROSTENOL. They are coupled to HETEROTRIMERIC G-PROTEINS.Mannosides: Glycosides formed by the reaction of the hydroxyl group on the anomeric carbon atom of mannose with an alcohol to form an acetal. They include both alpha- and beta-mannosides.Imidazoles: Compounds containing 1,3-diazole, a five membered aromatic ring containing two nitrogen atoms separated by one of the carbons. Chemically reduced ones include IMIDAZOLINES and IMIDAZOLIDINES. Distinguish from 1,2-diazole (PYRAZOLES).Receptors, Serotonin, 5-HT1: A subclass of G-protein coupled SEROTONIN receptors that couple preferentially to GI-GO G-PROTEINS resulting in decreased intracellular CYCLIC AMP levels.GTP-Binding Proteins: Regulatory proteins that act as molecular switches. They control a wide range of biological processes including: receptor signaling, intracellular signal transduction pathways, and protein synthesis. Their activity is regulated by factors that control their ability to bind to and hydrolyze GTP to GDP. EC 3.6.1.-.Radioligand Assay: Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).Binding, Competitive: The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements.Binding Sites: The parts of a macromolecule that directly participate in its specific combination with another molecule.Guanosine 5'-O-(3-Thiotriphosphate): Guanosine 5'-(trihydrogen diphosphate), monoanhydride with phosphorothioic acid. A stable GTP analog which enjoys a variety of physiological actions such as stimulation of guanine nucleotide-binding proteins, phosphoinositide hydrolysis, cyclic AMP accumulation, and activation of specific proto-oncogenes.Molecular Sequence Data: Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.Receptors, N-Methyl-D-Aspartate: A class of ionotropic glutamate receptors characterized by affinity for N-methyl-D-aspartate. NMDA receptors have an allosteric binding site for glycine which must be occupied for the channel to open efficiently and a site within the channel itself to which magnesium ions bind in a voltage-dependent manner. The positive voltage dependence of channel conductance and the high permeability of the conducting channel to calcium ions (as well as to monovalent cations) are important in excitotoxicity and neuronal plasticity.Schizophrenia: A severe emotional disorder of psychotic depth characteristically marked by a retreat from reality with delusion formation, HALLUCINATIONS, emotional disharmony, and regressive behavior.Endophenotypes: Measurable biological (physiological, biochemical, and anatomical features), behavioral (psychometric pattern) or cognitive markers that are found more often in individuals with a disease than in the general population. Because many endophenotypes are present before the disease onset and in individuals with heritable risk for disease such as unaffected family members, they can be used to help diagnose and search for causative genes.Evoked Potentials: Electrical responses recorded from nerve, muscle, SENSORY RECEPTOR, or area of the CENTRAL NERVOUS SYSTEM following stimulation. They range from less than a microvolt to several microvolts. The evoked potential can be auditory (EVOKED POTENTIALS, AUDITORY), somatosensory (EVOKED POTENTIALS, SOMATOSENSORY), visual (EVOKED POTENTIALS, VISUAL), or motor (EVOKED POTENTIALS, MOTOR), or other modalities that have been reported.Electroencephalography: Recording of electric currents developed in the brain by means of electrodes applied to the scalp, to the surface of the brain, or placed within the substance of the brain.Photic Stimulation: Investigative technique commonly used during ELECTROENCEPHALOGRAPHY in which a series of bright light flashes or visual patterns are used to elicit brain activity.Baclofen: A GAMMA-AMINOBUTYRIC ACID derivative that is a specific agonist of GABA-B RECEPTORS. It is used in the treatment of MUSCLE SPASTICITY, especially that due to SPINAL CORD INJURIES. Its therapeutic effects result from actions at spinal and supraspinal sites, generally the reduction of excitatory transmission.Dermatitis, Atopic: A chronic inflammatory genetically determined disease of the skin marked by increased ability to form reagin (IgE), with increased susceptibility to allergic rhinitis and asthma, and hereditary disposition to a lowered threshold for pruritus. It is manifested by lichenification, excoriation, and crusting, mainly on the flexural surfaces of the elbow and knee. In infants it is known as infantile eczema.Psoriasis: A common genetically determined, chronic, inflammatory skin disease characterized by rounded erythematous, dry, scaling patches. The lesions have a predilection for nails, scalp, genitalia, extensor surfaces, and the lumbosacral region. Accelerated epidermopoiesis is considered to be the fundamental pathologic feature in psoriasis.Xanthines: Purine bases found in body tissues and fluids and in some plants.Pentoxifylline: A METHYLXANTHINE derivative that inhibits phosphodiesterase and affects blood rheology. It improves blood flow by increasing erythrocyte and leukocyte flexibility. It also inhibits platelet aggregation. Pentoxifylline modulates immunologic activity by stimulating cytokine production.Administration, Topical: The application of drug preparations to the surfaces of the body, especially the skin (ADMINISTRATION, CUTANEOUS) or mucous membranes. This method of treatment is used to avoid systemic side effects when high doses are required at a localized area or as an alternative systemic administration route, to avoid hepatic processing for example.Dermatitis: Any inflammation of the skin.Dyphylline: A THEOPHYLLINE derivative with broncho- and vasodilator properties. It is used in the treatment of asthma, cardiac dyspnea, and bronchitis.Fluspirilene: A long-acting injectable antipsychotic agent used for chronic schizophrenia.Penfluridol: One of the long-acting ANTIPSYCHOTIC AGENTS used for maintenance or long-term therapy of SCHIZOPHRENIA and other PSYCHOTIC DISORDERS.Spiro Compounds: A group of compounds consisting in part of two rings sharing one atom (usually a carbon) in common.Spectrophotometry, Ultraviolet: Determination of the spectra of ultraviolet absorption by specific molecules in gases or liquids, for example Cl2, SO2, NO2, CS2, ozone, mercury vapor, and various unsaturated compounds. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)Volatile Organic Compounds: Organic compounds that have a relatively high VAPOR PRESSURE at room temperature.Hazardous Substances: Elements, compounds, mixtures, or solutions that are considered severely harmful to human health and the environment. They include substances that are toxic, corrosive, flammable, or explosive.Environmental Pollutants: Substances or energies, for example heat or light, which when introduced into the air, water, or land threaten life or health of individuals or ECOSYSTEMS.Epoxy Compounds: Organic compounds that include a cyclic ether with three ring atoms in their structure. They are commonly used as precursors for POLYMERS such as EPOXY RESINS.Xenobiotics: Chemical substances that are foreign to the biological system. They include naturally occurring compounds, drugs, environmental agents, carcinogens, insecticides, etc.Butadienes: Four carbon unsaturated hydrocarbons containing two double bonds.Lymphoma, Large-Cell, Immunoblastic: Malignant lymphoma characterized by the presence of immunoblasts with uniformly round-to-oval nuclei, one or more prominent nucleoli, and abundant cytoplasm. This class may be subdivided into plasmacytoid and clear-cell types based on cytoplasmic characteristics. A third category, pleomorphous, may be analogous to some of the peripheral T-cell lymphomas (LYMPHOMA, T-CELL, PERIPHERAL) recorded in both the United States and Japan.Therapies, Investigational: Treatments which are undergoing clinical trials or for which there is insufficient evidence to determine their effects on health outcomes; coverage for such treatments is often denied by health insurers.Lymphoma, Mantle-Cell: A form of non-Hodgkin lymphoma having a usually diffuse pattern with both small and medium lymphocytes and small cleaved cells. It accounts for about 5% of adult non-Hodgkin lymphomas in the United States and Europe. The majority of mantle-cell lymphomas are associated with a t(11;14) translocation resulting in overexpression of the CYCLIN D1 gene (GENES, BCL-1).Cyclin D1: Protein encoded by the bcl-1 gene which plays a critical role in regulating the cell cycle. Overexpression of cyclin D1 is the result of bcl-1 rearrangement, a t(11;14) translocation, and is implicated in various neoplasms.Pectinidae: A large family of mollusks in the class BIVALVIA, known commonly as scallops. They possess flat, almost circular shells and are found in all seas from shallow water to great depths.Lymphoma, Large B-Cell, Diffuse: Malignant lymphoma composed of large B lymphoid cells whose nuclear size can exceed normal macrophage nuclei, or more than twice the size of a normal lymphocyte. The pattern is predominantly diffuse. Most of these lymphomas represent the malignant counterpart of B-lymphocytes at midstage in the process of differentiation.Cyclin-Dependent Kinases: Protein kinases that control cell cycle progression in all eukaryotes and require physical association with CYCLINS to achieve full enzymatic activity. Cyclin-dependent kinases are regulated by phosphorylation and dephosphorylation events.Patents as Topic: Exclusive legal rights or privileges applied to inventions, plants, etc.Inventions: A novel composition, device, or process, independently conceived de novo or derived from a pre-existing model.Biotechnology: Body of knowledge related to the use of organisms, cells or cell-derived constituents for the purpose of developing products which are technically, scientifically and clinically useful. Alteration of biologic function at the molecular level (i.e., GENETIC ENGINEERING) is a central focus; laboratory methods used include TRANSFECTION and CLONING technologies, sequence and structure analysis algorithms, computer databases, and gene and protein structure function analysis and prediction.Rats, Inbred F344Apolipoprotein B-100: A 513-kDa protein synthesized in the LIVER. It serves as the major structural protein of low-density lipoproteins (LIPOPROTEINS, LDL; LIPOPROTEINS, VLDL). It is the ligand for the LDL receptor (RECEPTORS, LDL) that promotes cellular binding and internalization of LDL particles.F Factor: A plasmid whose presence in the cell, either extrachromosomal or integrated into the BACTERIAL CHROMOSOME, determines the "sex" of the bacterium, host chromosome mobilization, transfer via conjugation (CONJUGATION, GENETIC) of genetic material, and the formation of SEX PILI.F2-Isoprostanes: Isoprostanes derived from the free radical oxidation of ARACHIDONIC ACID. Although similar in structure to enzymatically synthesized prostaglandin F2alpha (DINOPROST), they occur through non-enzymatic oxidation of cell membrane lipids.
2,3,4,5-tetrahydro-8-chloro-3-methyl-5-phenyl-1h-3-benzazepin-7-ol MeSH D03.438.079.800 --- 2,3,4,5-tetrahydro-7,8-dihydroxy-1- ... quinolizin-2-ol, 2-ethyl-1,3,4,6,7,11b-hexahydro-3-isobutyl-9,10-dimethoxy- MeSH D03.438.834.775 --- sparteine MeSH D03.438. ... 5-amino-3-((5-nitro-2-furyl)vinyl)-1,2,4-oxadiazole MeSH D03.383.129.462.580.400 --- 4-chloro-7-nitrobenzofurazan MeSH D03.383. ... 5-amino-3-((5-nitro-2-furyl)vinyl)-1,2,4-oxadiazole MeSH D03.383.312.649.290 --- fanft MeSH D03.383.312.649.308 --- furagin ...
The action of azimilide is directed to the different currents present in atrial and ventricular cardiac myocytes. It principally blocks IKr, and IKs, with much weaker effects on INa, ICa, INCX and IK.Ach. The IKr(rapid)and IKs (slow) are inward rectifier potassium currents, responsible for repolarizing cardiac myocytes towards the end of the cardiac action potential. A somewhat higher concentration of azimilide is needed to block the IKs current. Both blockages result in an increase of the QT interval and a prolongation of atrial and ventricular refractory periods. Azimilide blocks hERG channels (which encode the IKr current) with an affinity comparable to that with which KvLQT1 / minK channels (which encode the IKs current) are blocked. This block exhibits reverse use-dependence, i.e. the channel blocking effect wanes at faster pulsing rates of the cell. A possible explanation is an interaction of azimilide with K+ close to its binding site in the ion channel. However, there is an agonist ...
... is due to a genetic polymorphism of the enzyme alcohol dehydrogenase, the enzyme that metabolises ingested alcohol. This polymorphism is most often reported in Asian patients.[1] It can also be an effect or side effect associated with certain drugs such as disulfiram, metronidazole, or nilutamide. Stuffy nose and skin flushing are the most common symptoms when ingesting alcohol.[2] It may also be characterized as intolerance causing hangover symptoms similar to the "disulfiram-like reaction" of aldehyde dehydrogenase deficiency or chronic fatigue syndrome. Severe pain after drinking alcohol may indicate a more serious condition.[3] If people are intolerant, some nearly non-alcoholic beverages may be a problem, similar to alcohol-containing medications, vinegar, inhalation of alcohol or the vapour of alcohol-containing cleaning agents. Drinking alcohol first or afterwards together with Calcium cyanamide, an inorganic compound used as a fertilizer, can cause permanent or long ...
... (also known as AS-3201) is an aldose reductase inhibitor being developed for the treatment of diabetic neuropathy by Dainippon Sumitomo Pharma and PharmaKyorin. It has been granted orphan drug status. The drug is to be used orally. A Canadian Phase III clinical trial has been completed. Phase III trials in Europe and the US started in June 2009 and are expected to complete in April 2013. Ranirestat is aldose reductase inhibitor that acts by reducing sorbitol accumulation in cells. Aldose reductase is an enzyme that catalyzes one of the steps in sorbitol (polyol) pathway which is responsible for formation of fructose from glucose. Aldose reductase activity is increased, parallel to glucose blood levels, in tissues that are not insulin sensitive, including lenses, peripheral nerves and renal glomeruli. Sorbitol does not diffuse through cell membranes easily and therefore accumulates in these tissues, causing osmotic damage, leading to retinopathy and neuropathy. Results from a Canadian ...
In enzymology, aldose reductase (or aldehyde reductase) (EC 1.1.1.21) is a cytosolic NADPH-dependent oxidoreductase that catalyzes the reduction of a variety of aldehydes and carbonyls, including monosaccharides. It is primarily known for catalyzing the reduction of glucose to sorbitol, the first step in polyol pathway of glucose metabolism. Aldose reductase catalyzes the NADPH-dependent conversion of glucose to sorbitol, the first step in polyol pathway of glucose metabolism. The second and last step in the pathway is catalyzed by sorbitol dehydrogenase, which catalyzes the NAD-linked oxidation of sorbitol to fructose. Thus, the polyol pathway results in conversion of glucose to fructose with stoichiometric utilization of NADPH and production of NADH. glucose + NADPH + H+ ⇌ {\displaystyle \rightleftharpoons } sorbitol + NADP+ Galactose is also a substrate for the polyol pathway, but the corresponding keto sugar is not produced because sorbitol dehydrogenase is incapable of oxidizing ...
Also called the sorbitol-aldose reductase pathway, the polyol pathway is a two-step process that converts glucose to fructose. In this pathway glucose is reduced to sorbitol, which is subsequently oxidized to fructose. The pathway is implicated in diabetic complications, especially in microvascular damage to the retina, kidney, and nerves. Sorbitol cannot cross cell membranes, and, when it accumulates, it produces osmotic stresses on cells by drawing water into the insulin-independent tissues. Cells use glucose for energy. This normally occurs by phosphorylation via the enzyme hexokinase. However, if large amounts of glucose are present (as in diabetes mellitus), hexokinase becomes saturated and the excess glucose enters the polyol pathway when aldose reductase reduces it to sorbitol. This reaction oxidizes NADPH to NADP+. Sorbitol dehydrogenase can then oxidize sorbitol to fructose, which produces NADH from NAD+. Hexokinase can return the molecule to the glycolysis pathway by phosphorylating ...
An aldose is a monosaccharide (a simple sugar) with a carbon backbone chain with a carbonyl group on the endmost carbon atom, making it an aldehyde, and hydroxyl groups connected to all the other carbon atoms. Aldoses can be distinguished from ketoses, which have the carbonyl group away from the end of the molecule, and are therefore ketones. Like most carbohydrates, simple aldoses have the general chemical formula Cn(H2O)n. Because formaldehyde (n=1) and glycolaldehyde (n=2) are not generally considered to be carbohydrates, the simplest possible aldose is the triose glyceraldehyde, which only contains three carbon atoms. Because they have at least one asymmetric carbon center, all aldoses exhibit stereoisomerism. Aldoses can exist in either a D- form or L- form. The determination is made based on the chirality of the asymmetric carbon furthest from the aldehyde end, namely the second-last carbon in the chain. Aldoses with alcohol groups on the right of the Fischer projection are D-aldoses, and ...
The Prostacyclin receptor , also termed the prostaglandin I2 receptor or just IP, is a receptor belonging to the prostaglandin (PG) group of receptors. IP binds to and mediates the biological actions of prostacyclin (also termed Prostaglandin I2, PGI2, or when used as a drug, epoprostenol). IP is encoded in humans by the PTGIR gene. While possessing many functions as defined in animal model studies, the major clinical relevancy of IP is as a powerful vasodilator: stimulators of IP are used to treat severe and even life-threatening diseases involving pathological vasoconstriction. The PTGIR gene is located on human chromosome 19 at position q13.32 (i.e. 19q13.32), contains 6 exons, and codes for a G protein coupled receptor (GPCR) of the rhodopsin-like receptor family, Subfamily A14 (see rhodopsin-like receptors#Subfamily A14). IP is most highly expressed in brain and thymus and is readily detected in most other tissues. It is found throughout the vascular network on endothelium and smooth muscle ...
Lawler OA, Miggin SM, Kinsella BT (2001). "Protein kinase A-mediated phosphorylation of serine 357 of the mouse prostacyclin receptor regulates its coupling to G(s)-, to G(i)-, and to G(q)-coupled effector signaling.". J. Biol. Chem. 276 (36): 33596-607. PMID 11443126. doi:10.1074/jbc.M104434200. ...
Mouse studies indicate that the PGI2-IP axis activates cellular signaling pathways that tend to suppress allergic inflammation. The axis inhibits bone marrow-derived dendritic cells (i.e. antigen-presenting cells that process antigen material, present it on their surfaces for delivery to T cells, and otherwise regulate innate and adaptive immune system responses) from producing pro-inflammatory cytokines (e.g. IL-12, TNF-alpha, IL-1-alpha, and IL-6) while stimulating them to increase production of the anti-inflammatory cytokine, IL-10. IP receptor activation of these cells also blocks their lipopolysaccharide-stimulated expression of pro-inflammatory cell surface proteins (i.e. CD86, CD40, and MHC class II molecules) that are critical for developing adaptive immune responses. IL receptor-activated bone marrow-derived dendritic cells showed a greatly reduced ability to stimulate the proliferation of T helper cell as well as the ability of these cells to produce pro-allergic cytokines (i.e. IL-5 ...
... s or prostanoid receptors represent a sub-class of cell surface membrane receptors that are regarded as the primary receptors for one or more of the classical, naturally occurring prostanoids viz., prostaglandin D2, (i.e. PGD2), PGE2, PGF2alpha, prostacyclin (PGI2), thromboxane A2 (TXA2), and PGH2.[1] They are named based on the prostanoid to which they preferentially bind and respond, e.g. the receptor responsive to PGI2 at lower concentrations than any other prostanoid is named the Prostacyclin receptor (IP). One exception to this rule is the receptor for thromboxane A2 (TP) which binds and responds to PGH2 and TXA2 equally well. All of the prostanoid receptors are G protein-coupled receptors belonging to the Subfamily A14 of the rhodopsin-like receptor family except for the Prostaglandin DP2 receptor which is more closely related in amino acid sequence and functionality to chemotactic factor receptors such as the receptors for C5a and leukotriene B4.[2] Prostanoid ...
The drug is clear with a pH of 10.[7] Its production is inhibited indirectly by NSAIDs, which inhibit the cyclooxygenase enzymes COX1 and COX2. These convert arachidonic acid to prostaglandin H2 (PGH2), the immediate precursor of prostacyclin. Since thromboxane (an eicosanoid stimulator of platelet aggregation) is also downstream of COX enzymes, one might think that the effect of NSAIDs would act to balance. However, prostacyclin concentrations recover much faster than thromboxane levels, so aspirin administration initially has little to no effect but eventually prevents platelet aggregation (the effect of prostaglandins predominates as they are regenerated). This is explained by understanding the cells that produce each molecule, TXA2 and PGI2. Since PGI2 is primarily produced in a nucleated endothelial cell, the COX inhibition by NSAID can be overcome with time by increased COX gene activation and subsequent production of more COX enzymes to catalyze the formation of PGI2. In contrast, TXA2 is ...
Fosforibozilaminoimidazolna karboksilaza (EC 4.1.1.21, 5-fosforibozil-5-aminoimidazolna karboksilaza, 5-amino-1-ribozilimidazol 5-fosfatna karboksilaza, AIR karboksilaza, 1-(5-fosforibozil)-5-amino-4-imidazolkarboksilatna karboksi-lijaza, ADE2, klasa II PurE, 5-amino-1-(5-fosfo-D-ribozil)imidazol-4-karboksilatna karboksi-lijaza) je enzim sa sistematskim imenom 5-amino-1-(5-fosfo-D-ribozil)imidazol-4-karboksilat karboksi-lijaza (formira 5-amino-1-(5-fosfo-D-ribozil)imidazol).[1][2][3] Ovaj enzim katalizuje sledeću hemijsku reakciju ...
میدازولام (آیوپاک آدی: 8-chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a][1,4]benzodiazepine, اینگیلیسجه: Midazolam, (چینجه:咪達唑侖‎)، عربجه: ميدازولام‎، روسجا: Мидазолам) بیر شیمیایی بیلشیک دواء. بۇ دواءنین مول جرمیسی مول/قرم ۳۲۵٫۷۸ دیر. نیمه عمر یا یاریلانما سۆرعتی ۱٫۵-۲٫۵ ساعات زامان آپاریر. متابولیسمی قاراجییرده باش وئریر. ...
N6-(4-aminobenzyl)-5′-N-methylcarboxamidoadenosine. IB-MECA. N6-(3-iodobenzyl)-5′-N-methylcarboxamidoadenosine. HEPES. 4-(2- ... Figure 4 Time course of agonist-induced AC sensitization. A, Transfected CHO cells were treated with 10 μm NECA at 37° for the ... 3). Therefore, the ability of chronic A3AR activation to sensitize AC stimulation is not a result of Gidown-regulation and ... The cell line used for these experiments bound the A3AR agonist radioligand125I-AB-MECA with high affinity (Kd = 1.24 ± 0.41 nm ...
2,3,4,5-tetrahydro-8-chloro-3-methyl-5-phenyl-1h-3-benzazepin-7-ol MeSH D03.438.079.800 --- 2,3,4,5-tetrahydro-7,8-dihydroxy-1- ... quinolizin-2-ol, 2-ethyl-1,3,4,6,7,11b-hexahydro-3-isobutyl-9,10-dimethoxy- MeSH D03.438.834.775 --- sparteine MeSH D03.438. ... 5-amino-3-((5-nitro-2-furyl)vinyl)-1,2,4-oxadiazole MeSH D03.383.129.462.580.400 --- 4-chloro-7-nitrobenzofurazan MeSH D03.383. ... 5-amino-3-((5-nitro-2-furyl)vinyl)-1,2,4-oxadiazole MeSH D03.383.312.649.290 --- fanft MeSH D03.383.312.649.308 --- furagin ...
d-Pen2,d-Pen5]-enkephalin. ICI-174864. N,N-diallyl-Tyr-Aib-Aib-Phe-Leu-OH. TIPP. H-Tyr-Tic-Phe-Phe-OH. DOR. δ-opioid receptor. ... 4-[(αR)-α-((2S,5R)-4-ally1-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]-N,N-diethylbenzamide. BW373U86. (±)-4-((α-R*)-α-((2S*,5 ... 4; Table 2). Importantly, the EC50 for G-protein activation by TIPP in this assay was similar to its affinity (Ki) for δ-opioid ... guanosine 5′-O-(3-[35S]thio)triphosphate. KRHB. Krebs-Ringer-HEPES buffer. GppNHp. 5′-guanylylimidodiphosphate. SNC80. (+)- ...
2. The P20 responses to S1 and S2 for E1 and E5 are displayed for each of the habituation and stress days. Both genotypes are ... 4. For the N40 component of the habituation trials, S1 during E1 on the stress day reduced to the level of S2. There was no ... 3. For the P20 component of habituation trials, only the NR1neo(−/−) mice showed a reduction in amplitude during E1 on the ... 3). However, there were no significant three-way interactions among other sets of variables (Table 1). The NR1neo(−/−) mice ...
Habre, W., Peták, F., Sly, P. D., Hantos, Z. & Morel, D. R., Jan 1 2001, In : Anesthesiology. 94, 2, p. 348-353 6 p.. Research ... Tulić, M. K., Wale, J. L., Peták, F. & Sly, P. D., Jun 3 1999, In : Thorax. 54, 6, p. 531-537 7 p.. Research output: ... Adamicza, Á., Peták, F., Asztalos, T. & Hantos, Z., May 29 1999, In : European Respiratory Journal. 13, 4, p. 767-774 8 p.. ... Suki, B., Petak, F., Adamicza, A., Hantos, Z. & Lutchen, K. R., Jan 1 1995, In : Journal of Applied Physiology. 79, 3, p. 861- ...
2-Polycyclic propynyl adenosine analogs having A2A agonist activity FR2884419A1 (en) * 2005-04-19. 2006-10-20. Galderma Sa. ... 2-Polycyclic propynyl adenosine analogs having A2A agonist activity US20090042901A1 (en) * 2005-02-02. 2009-02-12. Kowa Co., ... Substituted 4--piperidine-1-carboxylic acid esters as a2ar agonists US20110129546A1 (en) * 2008-06-20. 2011-06-02. Ignacio ... Substituted 4--piperidine-1-carboxylic acid esters as a2ar agonists US20110129546A1 (en) * 2008-06-20. 2011-06-02. Ignacio ...
Y1 - 2010/2/10. N2 - The aim of the present study was to investigate the mode of action of luteolin on phisphodiesterase (PDE) ... 於: European Journal of Pharmacology, 卷 627, 編號 1-3, 10.02.2010, p. 269-275.. 研究成果: 雜誌貢獻 › 文章 ... Yu MC, Chen JH, Lai CY, Han CY, Ko W-C. Luteolin, a non-selective competitive inhibitor of phosphodiesterases 1-5, displaced [3 ... The EC50 (PDE4H) values of luteolin and Ro 20-1724, a selective PDE4 inhibitor, for displacing 2 nM [3H]-rolipram binding were ...
KW - 3,5-Cyclic-AMP Phosphodiesterases/antagonists & inhibitors. KW - 4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone/ ... keywords = "3,5-Cyclic-AMP Phosphodiesterases/antagonists & inhibitors, 4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone/ ... The suppression in cAMP accumulation caused by ethanol feeding was associated with increased activity of phosphodiesterase 4. ... The suppression in cAMP accumulation caused by ethanol feeding was associated with increased activity of phosphodiesterase 4. ...
The imidazolidinone derivative, Ro 20-1724, significantly and consistently inhibited both the elevated cAMP phosphodiesterase ... The imidazolidinone derivative, Ro 20-1724, significantly and consistently inhibited both the elevated cAMP phosphodiesterase ... The imidazolidinone derivative, Ro 20-1724, significantly and consistently inhibited both the elevated cAMP phosphodiesterase ... The imidazolidinone derivative, Ro 20-1724, significantly and consistently inhibited both the elevated cAMP phosphodiesterase ...
4-(3-Butoxy-4-methoxybenzyl)-2-imidazolidinone. Ro 4-1284. 2H-Benzo(a)quinolizin-2-ol 2-Ethyl-1,3,4,6,7,11b-hexahydro-3- ... trans-1,4-Bis(2-chlorobenzaminomethyl)cyclohexane Dihydrochloride. BW 284 C 51. Benzenaminium, 4,4-(3-oxo-1,5-pentanediyl)bis( ... 4-(m-Chlorophenylcarbamoyloxy)-2-butynyl)trimethylammonium Chloride. SQ-18506. 5-Amino-3-((5-nitro-2-furyl)vinyl)-1,2,4- ... Insulin-Like Growth Factor Binding Protein 4. Insulin-Like Growth Factor-Binding Protein 2. Insulin-Like Growth Factor Binding ...
This graph shows the total number of publications written about "Fluspirilene" by people in this website by year, and whether "Fluspirilene" was a major or minor topic of these publications ...
Bai A, Yong M, Ma AG, Ma Y, Weiss CR, Guan Q, Bernstein CN, Peng Z. Novel anti-inflammatory action of 5-aminoimidazole-4- ... The suppressor of cytokine signaling 3 inhibits leptin activation of AMP-kinase in cultured skeletal muscle of obese humans. J ... Nath N, Giri S, Prasad R, Salem ML, Singh AK, Singh I. 5-aminoimidazole-4-carboxamide ribonucleoside: a novel immunomodulator ... Rattan R, Giri S, Singh AK, Singh I. 5-Aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside inhibits cancer cell proliferation ...
The dunce locus of Drosophila melanogaster codes for a low Km, cAMP phosphodiesterase. The correct function of this gene is required for normal learning and memory activity in flies, because dunce mutants fail in tests of behavioral conditioning. These observations have indicated that cAMP regulation is an important aspect of the biochemistry underlying learning and memory processes in insects. To determine whether the locus is functionally conserved in mammals, we have expressed dunce gene homologs from the rat in a yeast expression system. We find that the rat homologs encode low Km, cAMP phosphodiesterases similar to that coded for by the Drosophila dunce+ gene and, more importantly, that the mammalian enzymes are inhibited by rolipram and RO 20-1724, drugs with antidepressant properties. Surprisingly, the dunce-encoded phosphodiesterase was not inhibited by rolipram or RO 20-1724. These findings suggest that the phosphodiesterases, through their regulation of cAMP levels, influence learning ...
1-tert-butoxy-2-methyl-1-oxopropan-2-yl)ox, (2Z,4Z)-2,4-hexadienedinitrile, (2a,6a,8a,9ab)-hexahydro-8-hydroxy-2,6-methano-2h ... p-methoxybenzyl)-3-isopropyl-piperazi, (R)-N-(tert-Butoxycarbonyl)-tert-leucine, (R)-N-4-Benzyl-2-phenylpiperazine, (R)-N-Boc-2 ... imidazolidinone, 1-(1,2-Benzisothiazol-3-yl) Piperazine, 1-(1-ethoxyethyl)-4-(4,4,5,5-tetramethyl-1,3,2-dio, 1-(2,3-Dichloro ... p-methoxybenzyl)-3-isopropyl-piperazi, (S)-N,N-dimethylpiperidine-3-carboxamide, (S)-N-(2,6-dimethylphenyl)-1-propylpiperidine- ...
4-oxa-heptane-2,6-diol, (2S,6S)-. 4-tert-Butylaniline; 4-tert-Butylaniline; Aniline, p-tert-butyl-; Benzenamine, 4-(1,1- ... trans-1,2-Dichloroethylene; Ethene, 1,2-dichloro-, (trans)-. Please note that this spectral library may contain trade names ... 1,3,5,7-Tetraazatricyclo[3.3.1.13,7]decane; Urotropine. 1,3,5-Triazine-2,4,6-triamine; 2,4,6-Triamino-1,3,5-triazine; Melamine ... 2,6-Dimethyl-N,N-dimethylaniline; Aniline, N,N,2,6-tetramethyl-; Benzenamine, N,N,2,6-tetramethyl-; N,N-Dimethyl-2,6-xylidene. ...
2-Amino-5-phosphonovaleric Acid use 2-Amino-5-phosphonovalerate 2-Amino-6-(1,2,3-trihydroxypropyl)-4(3H)-pteridinone use ... 2-Dehydro-3-Deoxyphosphoheptonate Aldolase use 3-Deoxy-7-Phosphoheptulonate Synthase 2-Fluoro-2-deoxy-D-glucose use ... 2,6-Dichlorophenolindophenol use 2,6-Dichloroindophenol 3 beta-Hydroxy-delta-5-Steroid Dehydrogenase use Progesterone Reductase ... 2-Oxoisovalerate Dehydrogenase (Lipoamide) use 3-Methyl-2-Oxobutanoate Dehydrogenase (Lipoamide) 2-PAM Compounds use ...
benzyl groups such as a/?flra-methoxybenzyl (PMB) group and tetrahydropyranyl (THP) groups.. A carboxylic acid group may be ... as a t-butoxy amide (-NHCO-OC(CH3)3, -NH-Boc); a 2-biphenyl-2-propoxy amide (-NHCO-OC(CH3)2C6H4C6H5, -NH-Bpoc), as a 9- ... imidazolidinone, oxazoline, thiazoline, 2-pyrazoline, pyrazolidine, piperazine, and N-ali. One preferred sub-set of non- ... Table 4. Example No. Method of Preparation LCMS. 44©-/1y. lengths), 70% ethyl acetate: hexane (10 column lengths) to give 1.25 ...
... n-butoxy group or tert-butoxy group, and most preferably a methoxy group or an ethoxy group. [0309]The halogen atom, with which ... 0340]n4 is preferably 0 to 2, and more preferably 0 or 1. [0341]n5 is preferably 0 or 1, and more preferably 0. [0342]n6 is ... 0018][Non-Patent Document 2] [0019]Proceedings of SPIE (U.S.), vol. 4690, pp. 76-83 (2002) [0020][Patent Document 1] [0021] ... R3 and R4 may be either the same or different, and are preferably the same. [0384]v is either 0 or an integer from 0 to 2, ...
... supplier and exporter of 1-tert-BUTOXY-N,N,NN-TETRAMETHYL METHANEDIAMINE based in Mumbai, Maharashtra, India. ... 2S,2S)-(-)-2-Hydroxymethyl-1-[(1-methylpyrrolidine- 2-yl)-methyl]-pyrrolidine *L-Hydroxyproline ... N,N-DIMETHYL IMIDAZOLIDINONE GC. *2,6-DIMETHYL HYDROQUINONE. *ACETONITRILE AR. *DIMETHYL GLYOXIME DISODIUM SALT ... 1-tert-BUTOXY-N,N,NN-TETRAMETHYL METHANEDIAMINE (CAS No.5815-08-7) AL0941 ...
2S,2S)-(-)-2-Hydroxymethyl-1-[(1-methylpyrrolidine- 2-yl)-methyl]-pyrrolidine *L-Hydroxyproline ... N,N-DIMETHYL IMIDAZOLIDINONE GC. *DIETHYLENE GLYCOL MONO BUTYL ETHER. *2,4-DIMETHYLPHENOL ... 1-tert-BUTOXY-N,N,NN-TETRAMETHYL METHANEDIAMINE. *AL0942 *tert-BUTYL ACETATE ... 2S,4S)-(-)-N-BOC-4-Diphenylphosphino-2-diphenyl phospino methyl-pyrrolidine *(2R,4R)-(+)-4-Diphenylphosphino2-diphenylphosphino ...
Overall survival and histology-specific subgroup analyses from a phase 3, randomized controlled study of trabectedin or ... Five-year outcomes from a phase 3 METRIC study in patients with BRAF V600 E/K-mutant advanced or metastatic melanoma. Eur J ... Pooled Analysis of 4 Randomized Clinical Trials. JAMA Oncol. 2018 10 01; 4(10):1382-1388. ...
1-Butoxy-2-Propanol *1-Indanone *1-Iododecane *1-Piperidinecarboxylic Acid,4-[(2-Amino-4-Chlorophenyl)Amino]-,Ethyl Ester ...
  • This is reflected in notable pharmacological differences, in particular, a 100-1000-fold-lower affinity of the rat A 3 AR for certain xanthine compounds compared with the recombinant human and sheep receptors ( 1 , 5-7 ). (aspetjournals.org)
  • This invention relates to pyrazole compounds that inhibit or modulate the activity of cyclin dependent kinases (CDK) and glycogen synthase kinase-3 (GSK-3), to the use of the compounds in the treatment or prophylaxis of disease states or conditions mediated by cyclin dependent kinases and glycogen synthase kinase-3, and to novel compounds having cyclin dependent kinase or glycogen synthase kinase-3 inhibitory or modulating activity. (allindianpatents.com)
  • Although several studies have detailed the mechanisms underlying agonist-mediated desensitization of the rat A 3 AR, the regulation of the human A 3 AR, which displays only a 70% amino acid identity with the rat homologue, has not been addressed. (aspetjournals.org)
  • A recent report demonstrated that the rat A 3 AR mRNA is subject to an alternative splicing event within the coding sequence, resulting in the insertion of a 17-amino acid segment within the second intracellular loop ( 8 ). (aspetjournals.org)
  • Male Wistar rats were fed a liquid diet containing ethanol as 35% of total calories or pair-fed a control diet that isocalorically substituted maltose dextrins for ethanol for 4 wk. (dundee.ac.uk)
  • 5-aminoimidazole-4-carboxamide-1-beta-4-ribofuranoside attenuates experimental autoimmune encephalomyelitis via modulation of endothelial-monocyte interaction. (healthsciencessc.org)
  • We demonstrated previously that prolonged agonist exposure of CHO cells expressing a recombinant rat A 3 AR results in a desensitization of receptor function that is associated with the down-regulation of specific G protein subunits ( 9 ). (aspetjournals.org)
  • The purpose of this study was to examine the properties of TIPP at selected points of the signal transduction pathway (i.e., receptor binding, G-protein activation, and effector regulation) in GH 3 DORT cells (GH 3 cells expressing δ-opioid receptors) and compare them with that of an established δ-opioid agonist, [ d -Pen 2 , d -Pen 5 ]-enkephalin (DPDPE). (aspetjournals.org)
  • The EC50 (PDE4H) values of luteolin and Ro 20-1724, a selective PDE4 inhibitor, for displacing 2 nM [3H]-rolipram binding were 11.2 μM and 45.6 nM, respectively. (elsevier.com)
  • Psoriasis is a common chronic relapsing inflammatory skin disease which affects 1-3% of the population. (google.com)
  • Bai A, Yong M, Ma AG, Ma Y, Weiss CR, Guan Q, Bernstein CN, Peng Z. Novel anti-inflammatory action of 5-aminoimidazole-4-carboxamide ribonucleoside with protective effect in dextran sulfate sodium-induced acute and chronic colitis. (healthsciencessc.org)
  • Time course experiments revealed that the onset of sensitization was half-maximal between 2 and 3 hr but was not due to the synthesis of new proteins because cycloheximide treatment failed to inhibit sensitization. (aspetjournals.org)
  • Treatment of atopic dermatitis MNL with varying concentrations of the cAMP PDE inhibitor Ro 20-1724 resulted in progressively decreasing amounts of IgE synthesis, statistically significant at the 10 -4 M and 10 -5 M concentrations. (elsevier.com)
  • Cytotoxic effect of 5-aminoimidazole-4-carboxamide-1-beta-4-ribofuranoside (AICAR) on childhood acute lymphoblastic leukemia (ALL) cells: implication for targeted therapy. (healthsciencessc.org)
  • The inability of the sensitization process to alter the AC activity obtained in the presence of manganese chloride suggests that prolonged A 3 AR activation increases the coupling efficiency between G s and AC catalytic units. (aspetjournals.org)
  • these include cardioprotection and neuroprotection from prolonged ischemia, bronchoconstriction, mast cell and eosinophil activation, and induction of hypotension ( 1-3 ). (aspetjournals.org)
  • In assays measuring G-protein activation, TIPP failed to stimulate guanosine 5′- O -(3-[ 35 S]thio)triphosphate ([ 35 S]GTPγS) binding in membrane preparations, which is consistent with an antagonist profile. (aspetjournals.org)
  • The suppressor of cytokine signaling 3 inhibits leptin activation of AMP-kinase in cultured skeletal muscle of obese humans. (healthsciencessc.org)
  • Monocalcium Phosphate Monocalcium phosphate is a chemical compound with the formula Ca(H2PO4)2. (tradeindia.com)
  • and in said formula (f2-0-3), R 51 and R 52 each independently represents a hydrogen atom, a lower alkyl group of 1 to 5 carbon atoms, a fluorine atom or a fluorinated lower alkyl group, m f and n f each independently represents an integer of 0 to 5 (provided that m f +n f ≧1), and q' represents an integer of 0 to (patentsencyclopedia.com)
  • 5. A negative resist composition according to claim 4, wherein said fluorine-containing resin component (F) comprises said structural unit (f1), and a structural unit (f2-1), which is represented by said general formula (f2-0), in which at least one of said R 1 to R 4 is an alkali-soluble group represented by said general formula (f2-0-1). (patentsencyclopedia.com)
  • In addition to A 3 AR desensitization, a 1.5-2.5-fold increase was noted in the adenylyl cyclase (AC) activity achieved in the presence of GTP with or without forskolin. (aspetjournals.org)