Suramin: A polyanionic compound with an unknown mechanism of action. It is used parenterally in the treatment of African trypanosomiasis and it has been used clinically with diethylcarbamazine to kill the adult Onchocerca. (From AMA Drug Evaluations Annual, 1992, p1643) It has also been shown to have potent antineoplastic properties.Purinergic P2 Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.Receptors, Purinergic P2: A class of cell surface receptors for PURINES that prefer ATP or ADP over ADENOSINE. P2 purinergic receptors are widespread in the periphery and in the central and peripheral nervous system.Pyridoxal Phosphate: This is the active form of VITAMIN B 6 serving as a coenzyme for synthesis of amino acids, neurotransmitters (serotonin, norepinephrine), sphingolipids, aminolevulinic acid. During transamination of amino acids, pyridoxal phosphate is transiently converted into pyridoxamine phosphate (PYRIDOXAMINE).Uridine Triphosphate: Uridine 5'-(tetrahydrogen triphosphate). A uracil nucleotide containing three phosphate groups esterified to the sugar moiety.Adenosine Triphosphate: An adenine nucleotide containing three phosphate groups esterified to the sugar moiety. In addition to its crucial roles in metabolism adenosine triphosphate is a neurotransmitter.Receptors, Purinergic: Cell surface proteins that bind PURINES with high affinity and trigger intracellular changes which influence the behavior of cells. The best characterized classes of purinergic receptors in mammals are the P1 receptors, which prefer ADENOSINE, and the P2 receptors, which prefer ATP or ADP.Purinergic Antagonists: Drugs that bind to and block the activation of PURINERGIC RECEPTORS.Purinergic P2 Receptor Agonists: Compounds that bind to and stimulate PURINERGIC P2 RECEPTORS.Receptors, Purinergic P2X: A subclass of purinergic P2 receptors that signal by means of a ligand-gated ion channel. They are comprised of three P2X subunits which can be identical (homotrimeric form) or dissimilar (heterotrimeric form).Purinergic P2X Receptor Antagonists: Compounds that bind to and block the stimulation of PURINERGIC P2X RECEPTORS. Included under this heading are antagonists for specific P2X receptor subtypes.Parotid Gland: The largest of the three pairs of SALIVARY GLANDS. They lie on the sides of the FACE immediately below and in front of the EAR.Amylases: A group of amylolytic enzymes that cleave starch, glycogen, and related alpha-1,4-glucans. (Stedman, 25th ed) EC 3.2.1.-.Apyrase: A calcium-activated enzyme that catalyzes the hydrolysis of ATP to yield AMP and orthophosphate. It can also act on ADP and other nucleoside triphosphates and diphosphates. EC 3.6.1.5.Acinar Cells: Cells lining the saclike dilatations known as acini of various glands or the lungs.Salivary Glands: Glands that secrete SALIVA in the MOUTH. There are three pairs of salivary glands (PAROTID GLAND; SUBLINGUAL GLAND; SUBMANDIBULAR GLAND).Parotid Neoplasms: Tumors or cancer of the PAROTID GLAND.Nucleoside-Triphosphatase: An enzyme which catalyzes the hydrolysis of nucleoside triphosphates to nucleoside diphosphates. It may also catalyze the hydrolysis of nucleotide triphosphates, diphosphates, thiamine diphosphates and FAD. The nucleoside triphosphate phosphohydrolases I and II are subtypes of the enzyme which are found mostly in viruses.Receptors, AMPA: A class of ionotropic glutamate receptors characterized by their affinity for the agonist AMPA (alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid).Cerebral Cortex: The thin layer of GRAY MATTER on the surface of the CEREBRAL HEMISPHERES that develops from the TELENCEPHALON and folds into gyri and sulchi. It reaches its highest development in humans and is responsible for intellectual faculties and higher mental functions.Pyramidal Cells: Projection neurons in the CEREBRAL CORTEX and the HIPPOCAMPUS. Pyramidal cells have a pyramid-shaped soma with the apex and an apical dendrite pointed toward the pial surface and other dendrites and an axon emerging from the base. The axons may have local collaterals but also project outside their cortical region.Receptors, Purinergic P2X2: A purinergic P2X neurotransmitter receptor involved in sensory signaling of TASTE PERCEPTION, chemoreception, visceral distension and NEUROPATHIC PAIN. The receptor comprises three P2X2 subunits. The P2X2 subunits also have been found associated with P2X3 RECEPTOR subunits in a heterotrimeric receptor variant.Benzothiadiazines: Heterocyclic compounds of a ring with SULFUR and two NITROGEN atoms fused to a BENZENE ring. Members inhibit SODIUM-POTASSIUM-CHLORIDE SYMPORTERS and are used as DIURETICS.Receptors, Purinergic P2X4: A widely distributed purinergic P2X receptor subtype that plays a role in pain sensation. P2X4 receptors found on MICROGLIA cells may also play a role in the mediation of allodynia-related NEUROPATHIC PAIN.Patents as Topic: Exclusive legal rights or privileges applied to inventions, plants, etc.Stents: Devices that provide support for tubular structures that are being anastomosed or for body cavities during skin grafting.Radial Artery: The direct continuation of the brachial trunk, originating at the bifurcation of the brachial artery opposite the neck of the radius. Its branches may be divided into three groups corresponding to the three regions in which the vessel is situated, the forearm, wrist, and hand.Inventions: A novel composition, device, or process, independently conceived de novo or derived from a pre-existing model.Intellectual Property: Property, such as patents, trademarks, and copyright, that results from creative effort. The Patent and Copyright Clause (Art. 1, Sec. 8, cl. 8) of the United States Constitution provides for promoting the progress of science and useful arts by securing for limited times to authors and inventors, the exclusive right to their respective writings and discoveries. (From Black's Law Dictionary, 5th ed, p1014)Coronary Restenosis: Recurrent narrowing or constriction of a coronary artery following surgical procedures performed to alleviate a prior obstruction.Radial Nerve: A major nerve of the upper extremity. In humans the fibers of the radial nerve originate in the lower cervical and upper thoracic spinal cord (usually C5 to T1), travel via the posterior cord of the brachial plexus, and supply motor innervation to extensor muscles of the arm and cutaneous sensory fibers to extensor regions of the arm and hand.Fever: An abnormal elevation of body temperature, usually as a result of a pathologic process.Retrospective Studies: Studies used to test etiologic hypotheses in which inferences about an exposure to putative causal factors are derived from data relating to characteristics of persons under study or to events or experiences in their past. The essential feature is that some of the persons under study have the disease or outcome of interest and their characteristics are compared with those of unaffected persons.Bunyaviridae Infections: Virus diseases caused by the BUNYAVIRIDAE.Medical Records: Recording of pertinent information concerning patient's illness or illnesses.Bunyamwera virus: A species in the ORTHOBUNYAVIRUS genus of the family BUNYAVIRIDAE. A large number of serotypes or strains exist in many parts of the world. They are transmitted by mosquitoes and infect humans in some areas.UtahChoroideremia: An X chromosome-linked abnormality characterized by atrophy of the choroid and degeneration of the retinal pigment epithelium causing night blindness.Biological Science Disciplines: All of the divisions of the natural sciences dealing with the various aspects of the phenomena of life and vital processes. The concept includes anatomy and physiology, biochemistry and biophysics, and the biology of animals, plants, and microorganisms. It should be differentiated from BIOLOGY, one of its subdivisions, concerned specifically with the origin and life processes of living organisms.Salts: Substances produced from the reaction between acids and bases; compounds consisting of a metal (positive) and nonmetal (negative) radical. (Grant & Hackh's Chemical Dictionary, 5th ed)Sodium: A member of the alkali group of metals. It has the atomic symbol Na, atomic number 11, and atomic weight 23.Death Certificates: Official records of individual deaths including the cause of death certified by a physician, and any other required identifying information.Sodium Chloride: A ubiquitous sodium salt that is commonly used to season food.Birth Certificates: Official certifications by a physician recording the individual's birth date, place of birth, parentage and other required identifying data which are filed with the local registrar of vital statistics.Tellurium: Tellurium. An element that is a member of the chalcogen family. It has the atomic symbol Te, atomic number 52, and atomic weight 127.60. It has been used as a coloring agent and in the manufacture of electrical equipment. Exposure may cause nausea, vomiting, and CNS depression.Cadmium Compounds: Inorganic compounds that contain cadmium as an integral part of the molecule.Hepatitis, Infectious Canine: A contagious disease caused by canine adenovirus (ADENOVIRUSES, CANINE) infecting the LIVER, the EYE, the KIDNEY, and other organs in dogs, other canids, and bears. Symptoms include FEVER; EDEMA; VOMITING; and DIARRHEA.Dog Diseases: Diseases of the domestic dog (Canis familiaris). This term does not include diseases of wild dogs, WOLVES; FOXES; and other Canidae for which the heading CARNIVORA is used.HIV-1: The type species of LENTIVIRUS and the etiologic agent of AIDS. It is characterized by its cytopathic effect and affinity for the T4-lymphocyte.HIV Envelope Protein gp120: External envelope protein of the human immunodeficiency virus which is encoded by the HIV env gene. It has a molecular weight of 120 kDa and contains numerous glycosylation sites. Gp120 binds to cells expressing CD4 cell-surface antigens, most notably T4-lymphocytes and monocytes/macrophages. Gp120 has been shown to interfere with the normal function of CD4 and is at least partly responsible for the cytopathic effect of HIV.HIV Infections: Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).
The mechanism of action for suramin is unclear, however, it is thought that parasites are able to selectively uptake suramin ... Once inside parasites, suramin combines with proteins, especially trypanosomal glycolytic enzymes to inhibit energy metabolism ... Suramin was studied as a possible treatment for prostate cancer in a clinical trial. Suramin has been studied in a mouse model ... Suramin can also cause loss of appetite and irritability. Suramin causes non-harmful changes in urine during use, specifically ...
... is thought to work by selectively inhibiting the synthesis of microtubules in parasitic worms, and by destroying ... MBZ significantly inhibited cancer cell growth, migration, and metastatic formation of adrenocortical carcinoma, both in vitro ... Martarelli D, Pompei P, Baldi C, Mazzoni G (April 2008). "Mebendazole inhibits growth of human adrenocortical carcinoma cell ...
Suramin Selectively Inhibits Inducible Nitric Oxide Synthase at the Calmodulin Binding Site. ... These data suggest that suramin selectively inhibits iNOS over nNOS and that inhibition occurs by way of competition for the ... Previous studies with wild type CaM showed that suramin, a polysulfonated naphthylurea, inhibits iNOS at lower concentrations ... This study further investigates the nature of nNOS and iNOS inhibition by suramin by testing it in the presence of CaM with ...
1993) Suramin selectively inhibits the non-adrenergic non-cholinergic inhibitory junction potential in the guinea-pig stomach. ... Calcium-sensing receptor stimulates Cl−- and SCFA-dependent but inhibits cAMP-dependent HCO3− secretion in colon ... 1989) Adenosine analogs inhibit gastric acid secretion. Eur. J. Pharmacol. 160:275-281. ... pig stomach fundus a transmural nerve stimulation evoked an excitatory junction potential that could be blocked by suramin, ...
Suramin selectively inhibits carcinoma cell growth that is dependent on extracellular polyamines. Sandgren, Staffan LU and ...
The mechanism of action for suramin is unclear, however, it is thought that parasites are able to selectively uptake suramin ... Once inside parasites, suramin combines with proteins, especially trypanosomal glycolytic enzymes to inhibit energy metabolism ... Suramin was studied as a possible treatment for prostate cancer in a clinical trial. Suramin has been studied in a mouse model ... Suramin can also cause loss of appetite and irritability. Suramin causes non-harmful changes in urine during use, specifically ...
The low-amplitude mEPSCs were partially inhibited by PPADS (3 μM, Fig. 2 A) and suramin (10 μM, Fig. 2 B), which both block ... Cyclothiazide selectively prolongs larger mEPSCs. (A) A large mEPSC that is markedly prolonged by cyclothiazide (50 μM, red) ... smaller events were partially inhibited by P2X receptor antagonists suramin and PPADS. The decay of the larger events was ... 2, B and C). When added in the presence of NBQX and d-APV, suramin (10 μM) also reduced the amplitude (by 55 ± 8%, n = 7) and ...
The P2Y2-receptor is activated by UTP and ATP and blocked by suramin. The P2Y2-agonist diquafosol is used for the treatment of ... The receptor prefers UDP as agonist and is selectively blocked by 1,2-di-(4-isothiocyanatophenyl)ethane (MRS2567). The P2Y11- ... These P2Y12-antagonists are used in pharmacotherapy to inhibit platelet aggregation. The P2Y13-receptor is expressed in ... The human P2Y11-receptor is activated by ATP as naturally occurring agonist and it is blocked by suramin and reactive blue 2 ( ...
... suramin inhibits migration and proliferation by blocking PDGF-induced and/or mitogen activated protein kinase (MAPK-AP-1)- ... bFGF-saporin to selectively stop SMC proliferation among those cells with a large number of FGF-2 receptors (Chen et al, 1995, ... The material is preferable adapted to deliver an amount of the bioactive agent which is sufficient to inhibit restenosis at the ... 0023] The articulating mechanism(s) of the present invention which allow the stent to expand but inhibit stent recoil, may ...
Suramin Selectively Inhibits Inducible Nitric Oxide Synthase at the Calmodulin Binding Site  Jackson, Philip (Kalamazoo ...
In addition, suramin was able to inhibit wild-type CHIKV and Ebola virus replication in vitro. Inhibition occurred at early ... Suramin efficiently inhibited CHIKV and Ebola envelope-mediated gene transfer while vesicular stomatitis virus G protein ... Suramin, also known as Germanin or Bayer-205, is a market-authorized drug, however shows significant side effects, which ... As a competitive inhibitor of heparin, suramin has been described to have anti-viral activity. We tested the activity of ...
Furthermore, suramin, which selectively disrupts multiple Gα proteins, blocked endosomal maturation, suggesting that Gα may be ... A selective TSH receptor antagonist inhibits stimulation of thyroid function in female mice. Endocrinology 155, 310-314 (2014). ... Suramin analogues as subtype-selective G protein inhibitors. Mol. Pharmacol. 49, 602-611 (1996).. ... In contrast, gallein (54), a specific Gβγ inhibitor, did not substantially inhibit EE generation (Fig. 7A). These results ...
... concerned in a peroxidase and immunosuppressive drugs Cimetidine inhibits the cell superoxide dismutase activity and suramin. ... The few cases and is distrib- uted selectively in the immediate apnoea, dyslipidaemia, reducing the β2-agonist. Stretch ... Hypokalaemia - anti-dysrhythmic drugs inhibit the lower than in human cancers. Therapy consists of thyrox- ine, gastro- ...
View our Suramin sodium salt specific physical and chemical properties, and analytical data. ... COA of Suramin sodium salt contains the actual results obtained from testing performed as part of quality control. ... Suramin sodium salt is a polysulfonated naphthylurea that inhibits the binding of calmodulin to recognition sites on the ... ryanodine receptor-1 (IC50 = 4.9 μM), blocks G protein coupling to GPCRs, and non-selectively antagonizes P2 purinergic ...
Selectively inhibits microtubule synthesis and glucose uptake in nematodes, ovicidal ; For ascariasis, pinworm, whipworm ... Inhibits binding of VEGF to VEGFR leading to inhibiton of VEGF signalling, inhibits tumor vascular permeability but enhances ... Inhibits cell wall synthesis by binding to the D-Ala-D-Ala terminus of nascent peptidoglycan inhibit transglycosylation ... Inhibits with ergosterol synthesis by inhibiting fungal squalene oxidase leading to increased squalene which interferes with ...
In addition to inhibiting cell growth, these antagonists also inhibited estrogen-induced increases cialis before and after in ... Basal and stimulus-induced cytokine expression is selectively impaired in peripheral blood mononuclear cells of newborn foals. ... were treated with intraperitoneal suramin through a Tenckhoff catheter. Risk factors, help-seeking behavior, and quality of ... Cytochrome c and carbon monoxide inhibit the hydroxylation reaction, suggesting a cytochrome P-450-dependent mixed-function ...
Aurintricarboxylic acid and Evans Blue represent two different classes of anionic compounds which selectively inhibit the ... Balzarini J, Mitsuya H, De Clercq E and Broder S, Comparative inhibitory effects of suramin and other selected compounds on the ... Lifson JD, Hwang KM, Nara PL, Fraser B, Padgett M, Dunlop NM and Eiden LE, Synthetic CD4 peptide derivatives that inhibit HIV ... Schols D, Baba M, Pauwels R and De Clercq E, Flow cytometric method to demonstrate whether anti-HIV-1 agents inhibit virion ...
Clostridial botulinum C3 toxin is a mono-ADP-ribosyl transferase that selectively inhibits RhoA, RhoB, and RhoC by covalently ... whereas LPA-induced Ca2+ transients were suppressed by suramin, a nonselective P2Y receptor antagonist. Attenuation of ... Although CBX markedly inhibited PAR1-stimulated ATP release from 1321N1 cells (Figs. 7 and 8A), we were unable to correlate ... C3 toxin selectively inactivates RhoA, RhoB, and RhoC, whereas ToxB nonselectively inactivates all Rho-family GTPases (61). ...
P2X4-mediated currents are relatively insensitive to blockade by suramin or PPADS (IC50 , 500 μM), which inhibit other P2X ... P2X7 receptors are selectively expressed on cells of hematopoietic lineage, including mast cells, lymphocytes, erythrocytes, ... Ho BT, Huo YY, Lu JG, Newman RA, and Levin VA (1992) Analgesic activity of anticancer agent suramin. Anti-Cancer Drugs 3: 91-94 ... Whereas reduced pain sensation was noted in a suramin phase 1 cancer clinical trial (Ho et al., 1992), the clinical utility of ...
... i increase and cell proliferation were inhibited by a purinoceptor antagonist, suramin(10-4M).Thus, the present study indicates ... in vitro platelet aggregation and in vivo thrombus formation.NSP-513 selectively inhibited human platelet PDE 3 isozyme with an ... U-46619, a Selective Thromboxane A2 Mimetic, Inhibits the Release of Endogenous Noradrenaline From the Rat Hippocampus In Vitro ... inhibited the TG-induced [Ca2+]i elevation dose-dependently(0.1-1μM)and attenuated Mn2+ entry.Phorbol 12-myristate 13-acetate( ...
2) When blocking P2Y2 receptors by suramin or injection of P2Y2R antisense oligodeoxynucleotides both led to a time- and dose- ... which could be reversed by the P2 receptor antagonist suramin and the ERK antagonist U0126. In ION-CCI (chronic constriction ... 2) UTP significantly inhibited IA and the expression of Kv1.4, Kv3.4 and Kv4.2 subunits in TG neurons, ... Wu Y, Willcockson HH, Maixner W, Light AR: Suramin inhibits spinal cord microglia activation and long-term hyperalgesia induced ...
2005). Dipyridamole selectively inhibits inflammatory gene expression in platelet-monocyte aggregates. Circulation 111, 633-642 ... Liu, N., He, S., Tolbert, E., Gong, R., Bayliss, G., and Zhuang, S. (2012). Suramin alleviates glomerular injury and ... 2013). Benazepril inhibited the NF-kappaB and TGF-beta networking on LV hypertrophy in rats. Immunol. Lett. 152, 126-134. doi: ... 2013). Ketoprofen inhibits expression of inflammatory mediators in human dental pulp cells. J. Endod. 39, 764-767. doi: 10.1016 ...
... which are selectively inhibited by ZD7288. Indeed, injection of large hyperpolarizing currents (300 pA for 200 ms) evoked a ... 100 μm suramin; n = 3) receptors did not eliminate the burst or inward current. Blocking muscarinic acetylcholine receptors (10 ... However, inhibiting either CCK1/2 receptors (using 1 μm L365260; n = 3), NTS receptors (0.5 μm SR142948; n = 3), neurokinin ... SNc neurons synaptically inhibit CINs. Early clinical observations revealed that ACh levels rise as dopamine levels fall in ...
The present invention relates to compositions and methods for inhibiting unwanted angiogenesis, particularly those of ocular ... The basic concept of Vessel Painting is to selectively stain the inner lining of blood vessels with fluorescent dye. Blood ... analogues of suramin; VEGF trap molecules; Visudyne™ and other photosensitizers with photodynamic therapy (PDT); and laser ... Method of inhibiting choroidal neovascularization US12244655 US20090036479A1 (en) 2002-09-18. 2008-10-02. Method of inhibiting ...
Suramin, other than its P2 antagonism, was also shown to inhibit ecto-nucleotidases.[source] The question is if this effect is ... and those low levels make cyclophosphamide able to selectively kill Tregs, sparing other T cells. Yes, cyclophosphamide is the ... But then you also have the result that adding suramin greatly reduced the sickly response. Suramin is a non-selective P2 ... Now, Im not saying that suramin is a bad idea and we shouldnt try it in ME/CFS. My very uninformed guess is that overall the ...
Suramin, a potent inhibitor of HIV reverse transcriptase" was included as a standard. HIV-1 reverse transcriptase assay RESULTS ... In an effort to ascertain other ways of inhibiting viral infections, we have been investigating the effect of various inorganic ... Perhaps the most important successes have been the discovery of antiviral nucleosides which more or less selectively affect ... to inhibit viral cytopathogenicity by 50%. For HIV-l-induced cytopathogenicity in MT-4 cells, this activity was expressed as ...
The results indicate that suramin blocks the interaction between hFGF1 and FGFR2 (zeige FGFR2 Antikörper) D2. ... Although FGF1 transgenic mice had a normal phenotype with unperturbed kidney structure, they showed a severely inhibited kidney ... structures and suggest that it is now possible to chemoenzymatically synthesize precise HS polysaccharides that can selectively ...
  • Upon administration, ABC294640 competitively binds to and inhibits SK2, thereby preventing the phosphorylation of the pro-apoptotic amino alcohol sphingosine to sphingosine 1-phosphate (S1P), the lipid mediator that is pro-survival and critical for immunomodulation. (blogspot.com)
  • ivermectin binds selectively and with high affinity to glutamate-gated chloride ion channels in invertebrate muscle and nerve cells of the microfilaria. (msis.info)
  • Weaver JL, Gergeley P, Pine PS, Patzer E and Aszalos A, Polyionic compounds selectively alter availability of CD4 receptors for HIV coat protein rgp120. (springer.com)
  • 2) When blocking P2Y 2 receptors by suramin or injection of P2Y2R antisense oligodeoxynucleotides both led to a time- and dose-dependent reverse of allodynia in ION-CCI rats. (biomedcentral.com)
  • Using a combination of optogenetic, electrophysiological, and pharmacological approaches, we demonstrate that synaptically released dopamine inhibits CINs through type 2 dopamine receptors, while another unidentified transmitter mediates the delayed excitation. (jneurosci.org)
  • The effects of D-glucose and nucleotides on the number and activity of hENT1 and hENT1 mRNA were blocked by reactive blue 2 (nonspecific P2Y purinoceptor antagonist), suramin (G s protein inhibitor), or hexokinase but not by pyridoxal phosphate-6-azophenyl- 2 ,4 -disulfonic acid (nonselective P2 purinoceptor antagonist). (slideshare.net)
  • The present invention provides a locally deliverable composition for inhibiting pain/inflammation and spasm, comprising a combination of ketoprofen and a calcium channel antagonist in a carrier. (justia.com)
  • Ketoprofen and the calcium channel antagonist are each included in a therapeutically effective amount such that the combination inhibits pain/inflammation and spasm at a site of local delivery. (justia.com)
  • In a further aspect of the present invention, a locally deliverable composition for inhibiting pain/inflammation and spasm comprises a combination of a cyclooxygenase inhibitor and a calcium channel antagonist, propyl gallate as a stabilizing agent and a liquid carrier. (justia.com)
  • In a further aspect of the present invention, a locally deliverable composition for inhibiting pain/inflammation and spasm comprises a combination of a cyclooxygenase inhibitor and a calcium channel antagonist an aqueous liquid carrier, a cosolvent, at least one stabilizing agent and a buffer. (justia.com)
  • Like all benzimidazoles, albendazole acts by selectively binding to free â-tubulin in nematodes, inhibiting the polymerization of tubulin and the microtubule-dependent uptake of glucose. (gkhub.info)
  • Researchers activated these neurons so that they would secrete neurotransmitters - chemicals that excite or inhibit the transmission of electrical signals through the brain. (ucsd.edu)
  • Preservation of enteric neurons by inhibiting Panx1 in vivo prevented the onset of inflammation-induced colonic motor dysfunction. (pubmedcentralcanada.ca)
  • The effects of both drugs when they were used at the MICs at which 100% of isolates are inhibited were amoebistatic, but at higher doses they were amoebicidal as well as cysticidal. (asm.org)
  • modulation of CFTR channel, potentiating its opening at low concentration and inhibiting it a higher doses. (ipfs.io)
  • Balzarini J, Mitsuya H, De Clercq E and Broder S, Aurintricarboxylic acid and Evans Blue represent two different classes of anionic compounds which selectively inhibit the cytopathogenicity of human T-cell lymphotropic virus type III/lymphadenopathy-associated virus. (springer.com)
  • The invention also relates to a method of screening compounds for their ability to inhibit P2X.sub.7 activity and thereby for their usefulness in treating a variety of diseases/disorders, including arthritic and respiratory disorders and neurodegenerative diseases. (patentgenius.com)
  • This study further investigates the nature of nNOS and iNOS inhibition by suramin by testing it in the presence of CaM with mutations at calcium binding sites 1 and 3 (IQ mutant and 3Q mutant). (kzoo.edu)
  • These data suggest that suramin selectively inhibits iNOS over nNOS and that inhibition occurs by way of competition for the CaM binding site. (kzoo.edu)
  • Suramin, also known as Germanin or Bayer-205, is a market-authorized drug, however shows significant side effects, which probably prevents its use as a CHIKV drug, but due to the high lethality of Ebola virus infections, suramin might be valuable against Ebola infections. (biomedcentral.com)
  • inhibits viral RNA translation and induces MHC1 expression, increasing macrophage sensitivity towards and ability to eradicate virally infected cells. (memorize.com)
  • Suramin contains six aromatic systems - four benzene rings, sandwiched by a pair of naphthalene moieties - plus four amide functional groups (in addition to the urea) and six sulfonic acid groups. (wikipedia.org)
  • We tested the activity of suramin during CHIKV or Ebola virus infection, using CHIKV and Ebola envelope glycoprotein pseudotyped lentiviral vectors and wild-type CHIKV and Ebola virus. (biomedcentral.com)
  • Mitsuya H, Popovic M, Yarchoan R, Matsushita S, Gallo RC, Broder S. Suramin protection of T cells in vitro against infectivity and cytopathic effect of HTLV-III. (springer.com)
  • Although CBX was first characterized as an inhibitor of 11-β-hydroxysteroid dehydrogenase, it has also been used extensively to inhibit the activity of intercellular gap-junction channels and gap-junction hemichannels ( 18 ). (physiology.org)
  • Inhibiting P2X7Rs, Panx1, Asc or caspase activity prevents inflammation-induced neuron cell death. (pubmedcentralcanada.ca)
  • Each active agent is included in a therapeutically effective amount such that the combination inhibits pain/inflammation and spasm at a site of local delivery. (justia.com)
  • Once inside parasites, suramin combines with proteins, especially trypanosomal glycolytic enzymes to inhibit energy metabolism. (wikipedia.org)
  • It is also used as a research reagent to inhibit the activation of heterotrimeric G proteins in a variety of GPCRs with varying potency. (wikipedia.org)
  • Knockdown of Rictor resulted in inhibiting ventricular-like myocytes differentiation and induced arrhythmias symptom, which was accompanied by interfering the expression and distribution patterns of cell-cell junction proteins. (ijbs.com)
  • By being able to distinguish benign from malignant aging based on distinctive RNA splicing patterns, we can develop therapeutic strategies that selectively target leukemia stem cells while sparing normal hematopoietic stem cells," she said. (ucsd.edu)
  • Suramin efficiently inhibited CHIKV and Ebola envelope-mediated gene transfer while vesicular stomatitis virus G protein pseudotyped vectors were only marginally affected. (biomedcentral.com)
  • Meanwhile, phenylephrine-induced relaxation was inhibited by pretreatment with propranolol and calcitonin gene-related peptide (CGRP)-depletory capsaicin in UB strips with and without mucosa. (bvsalud.org)
  • Suramin is used for treatment of human sleeping sickness caused by trypanosomes. (wikipedia.org)
  • Previous studies showed that treatment of mES cells with suramin [ 9 ] or human ES cells with IWR-1 [ 10 ] could enhance cardiac specialization into sinus node-like or ventricular-like cells respectively. (ijbs.com)
  • Inhibiting mGluRl or mGluR5 reduces pain, as shown by in vivo treatment with antibodies selecti\e for either mGluRl or mGluR5. (allindianpatents.com)
  • Clostridium difficile toxin B and Clostridium botulinum C3 exoenzyme, which inhibit Rho-GTPases, attenuated the thrombin- and LPA-stimulated ATP release but did not decrease carbachol-stimulated release. (physiology.org)
  • Growth curve evaluations revealed that both drugs inhibit trophozoite growth in dose- and time-dependent ways. (asm.org)
  • This agent may inhibit the pathophysiologic effects of aldosterone produced in excess by various types of malignant and benign tumors. (blogspot.com)
  • In regions of the world where the disease is common suramin is provided for free by the World Health Organization. (wikipedia.org)
  • Suramin has been applied clinically to HIV/AIDS patients resulting in a significant number of fatal occurrences and as a result the application of this molecule was abandoned for this condition. (wikipedia.org)
  • however, the pharmacokinetics of suramin can vary substantially between individual patients. (wikipedia.org)
  • Patients with histologically verified cancer confined to the abdominal cavity, for which no effective therapy was canadian pharcharmy online cialis available, were treated with intraperitoneal suramin through a Tenckhoff catheter. (duefree.info)
  • It is needless to stress the need for a successful drug that would keep the liver functioning at its optimum or the one that would be selectively active against the currently known etiological agents of acute viral diseases of the liver. (allindianpatents.com)