The effects of the P2 receptor antagonists suramin and PPADS, the P2Y14 receptor antagonist PPTN, and the P2Y6 receptor antagonist MRS2578, were investigated. (nottingham.ac.uk)
Using the optimized circumstances, Michaelis-Menten constants (ideals for NTPDase1, 2 and 3 acquired for reactive blue 2, PPADS, suramin, and "type":"entrez-protein","attrs":"text message":"ARL67156″,"term_id":"1186396857″,"term_text message":"ARL67156″ARL67156, using the in-capillary electrophoresis technique. (bioinf.org)
For example, P2X7 inhibition studies by suramin, KN-62, oATP, PPADS, and BBG have IC50 values that vary by 10- to 20- fold based on the agonist used, and the extracellular conditions to which they are uncovered [48, 96, 120]. (afl-journal.org)
Receptor antagonist2
An inward current (Ix) was identified and this current was blocked by the P2 receptor antagonist, suramin, and inhibited by the ATP-degrading enzyme, apyrase. (ucl.ac.uk)
The response to ATP was inhibited by the nonselective P2X purinergic antagonist suramin and by oxidized ATP, a potent P2Z/P2X(7) receptor antagonist. (ac.be)
Tetrodotoxin1
To exemplify potential studies on ion channels, we characterized voltage-gated sodium channels and their inhibition by tetrodotoxin, saxitoxin and lidocaine, as well as their opening by the plant alkaloid veratridine and the food-relevant marine biotoxin ciguatoxin. (uni-konstanz.de)
Potentiation1
At rat P2X4, reduced extracellular sodium had a biphasic action (potentiation, then inhibition) on ATP signalling, which was insensitive to acidification but was intensified by adding calcium. (ucl.ac.uk)
Proteins3
The mechanism of action for suramin is unclear, but it is thought that parasites are able to selectively uptake suramin via receptor-mediated endocytosis of drug that is bound to low-density lipoproteins and, to a lesser extent, other serum proteins. (wikipedia.org)
Once inside parasites, suramin combines with proteins, especially trypanosomal glycolytic enzymes, to inhibit energy metabolism. (wikipedia.org)
Forskolin-induced VASP-phosphorylation was reduced in porcine coronary arteries exposed to UDP-glucose and MRS2690, consistent with P2Y14 receptor coupling to Gi/o proteins and inhibition of adenylyl cyclase activity. (nottingham.ac.uk)
IC501
Both analogs 6 and 9 are active at noncytotoxic doses, exhibit slightly higher potencies for the RT of HIV-2 over HIV-1, and demonstrate activities superior to the hexasulfonic acid derivative suramin (IC50 values of 9.4 and 15.5 microM for HIV-1 and HIV-2 RT, respectively). (neb.com)
Blockade1
The effects of blockade of purinoceptors with suramin, or blockade of HIF-1α hydroxylation by suppressing prolyl hydroxylase (PAH) activity on the endogenous NO release measured electrochemically by microsensor inserted into the isolated carotid body superfused with bicarbonate-buffer were examined. (openbiochemistryjournal.com)
Secretion2
2021, Jan). Targeting inhibition of CCR5 on improving obesity-associated insulin resistance and impairment of pancreatic insulin secretion in high fat-fed rodent models. (ndmctsgh.edu.tw)
Angiogenesis inhibitor through angiogenin secretion inhibition [10]. (adipogen.com)
Synthesis2
The synthesis of suramin itself and structural analogs is by successive formation of the amide bonds from their corresponding amine (aniline) and carboxyl (as acyl chloride) components. (wikipedia.org)
Synthesis and inhibition of HIV-1 induced cytopathogenesis and HIV-1 and HIV-2 reverse transcriptase activities. (neb.com)
Reactive1
Biological significance of these compounds include anti-bacterial, anti-thrombotic and vasodilatory, anti-mutagenic, lipoxygenase and cyclooxygenase inhibition, scavenging of reactive oxygen species, and anti-tumourigenic. (biomedcentral.com)
Affects2
Suramin uncommonly affects the eyes causing watery eyes, swelling around the eyes, photophobia, and changes or loss of vision. (wikipedia.org)
Inhibition of either FGFA, FGFR1 or FGFR2 function severely affects morphogenesis of the skeleton. (biologists.com)
Dose dependent2
The extract also showed a dose dependent growth inhibition of all tested cell lines, IC 50 values against HCT-116, HUVEC, CCD-18CO and HT-29 were 14, 23, 50 and 52 μg mL -1 , respectively. (scialert.net)
Suramin did not change the resting NO level under normoxic conditions but it significantly decreased the hypoxia-induced NO elevation in a dose-dependent manner. (openbiochemistryjournal.com)
Phenylephrine1
3 mM and 6 mM), FE + suramin (100 μM), FE + phenylephrine and FE + carbachol. (arccjournals.com)
Medication3
Suramin is a medication used to treat African sleeping sickness and river blindness. (wikipedia.org)
NF449, a sulfated compound produced from the antiparasitic medication suramin, once was reported to inhibit infection by enterovirus A71 (EV-A71). (mindunwindart.com)
Inhibition was noticed when NF449 was added in the beginning of illness, however, not after 2 hrs, recommending that the medication acts at an early on stage in the disease life routine. (mindunwindart.com)
Concentration2
Suramin does not distribute well into cerebral spinal fluid and its concentration in the tissues is equivalently lower than its concentration in the plasma. (wikipedia.org)
4% of compounds examined showed action greater than 50% inhibition at a concentration of two uM from the hypo xanthine incorporation assay at 48 hours. (faksignaling.com)
Molecule2
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)
Piritrexim is usually a dihydrofolate reductase inhibitor and lurtotecan a topoisomerase I inhibitor and neither molecule demonstrated a significant possible thera peutic window concerning inhibition on the parasite and inhibition of tumor derived cell lines. (faksignaling.com)
Prostate1
Noguchi K, Uemura H, Harada M et al (2001) Inhibition of PSA flare in prostate cancer patients by administration of flutamide for 2 weeks before initiation of treatment with slow-releasing LH-RH agonist. (springer.com)
Extract2
At 100 μg mL -1 , the extract showed 94±5.5% inhibition of the outgrowth of the blood vessels from the rat aorta rings. (scialert.net)
The presence of suramin and prazosin were not significantly increase the inhibition caused by the FE extract, while Ca 2+ and ATP significantly increased the inhibition by the FE extract. (arccjournals.com)
Drug2
This included receptor sub-typing and the characterization of the anti-parasitic drug suramin as modulator of the cellular response to ATP. (uni-konstanz.de)
Naviaux wants to plug the leaks in the cell wall using Suramin, which is an old anti-parasite drug made by Bayer, the giant German company. (epiphanyasd.com)
Reactions1
inhibition reduced and potentiated, respectively, 5-HT-induced reactions. (nonamimaho.com)
Human2
Suramin is used for treatment of human sleeping sickness caused by trypanosomes. (wikipedia.org)
Reversible inhibition of normal human prokeratinocyte proliferation by type beta transforming growth factor-growth inhibitor in serum-free medium. (academicinfluence.com)
Patients2
however, the pharmacokinetics of suramin can vary substantially between individual patients. (wikipedia.org)
The WHO has recommended that suramin not be used to treat onchocerciasis in individuals who are elderly or infirm or in patients with severe liver or renal disease. (medscape.com)
Growth1
These inhibitors act on a variety of SIRTs, strengthening the idea that the concomitant inhibition of several SIRTs may contribute to a reduction in malignant growth [ 23 ]. (biomedcentral.com)
Effects1
Suramin causes a fair number of side effects. (wikipedia.org)
Disease2
In regions of the world where the disease is common suramin is provided for free by the World Health Organization (WHO). (wikipedia.org)
Cobos, S.N and Torrente, M.P.^ Epidrugs in Amyotrophic Lateral Sclerosis and Frontotemporal Dementia: Contextualizing a Role for Histone Kinase Inhibition in Neurodegenerative Disease. (cuny.edu)
Made2
Suramin was made at least as early as 1916. (wikipedia.org)
Suramin was first made by the chemists Oskar Dressel, Richard Kothe and Bernhard Heymann at Bayer AG laboratories in Elberfeld, after research on a series of urea-like compounds. (wikipedia.org)
Treatment1
Randomized clinical trial of low dose suramin intravenous infusions for treatment of autism spectrum disorder. (ucdavis.edu)
Loss1
Suramin can also cause loss of appetite and irritability. (wikipedia.org)
Activity1
have reported anti-carcinogenic activity of both koetjapic acid and 3-oxo-olean-12-en-29-oic acid. (scialert.net)