Epithelial sodiumInhibitorPotent sodium channel blockerCalcium channelVoltage-gated sodiumAngiotensinInhibitorsBeta-blockerPotassiumSelectiveBioactive compoundNeurotoxicityIonsInhibitsMolecularAnticoagulationMutationsNovel compoundsCurrentsBenzimidazoleSubunitFungicidesInfluxInhibitionIUPACSubsetMagnesiumNav1.7CardiacChemical compoundPoreAlgaeDrugsElementalBindNav1.5UrineAbsorptionTargetsMoleculesActivityStructuresHydrogenSynonymsGeneElectrophysiologicalCompositionBiotechOrganicInvolvesClinicalComplexPeripheralAminoRational designSevere
Epithelial sodium4
- The aerosol-based therapy uses a specific epithelial sodium channel-blocking agent called GS-9411, which prevents sodium from being absorbed across the airway, allowing the surface to remain moist. (news-medical.net)
- This study was performed during the pre-clinical stage of development to compare GS-9411 to an established epithelial sodium channel blocker, called amiloride. (news-medical.net)
- Amiloride blocks the epithelial sodium channel (ENaC) in the late distal tubule, connecting tubule, and collecting duct of the nephron, which both reduces absorption of sodium ion from the lumen of the nephron and reduces excretion of potassium ion into the lumen. (worldsbest.rehab)
- Some people with the Liddle phenotype have Liddle syndrome, which involves a genetic mutation resulting in upregulation of the epithelial sodium channel (ENaC), located in the apical membrane of polarized epithelial cells in the late distal tubule and collecting duct of the kidney. (worldsbest.rehab)
Inhibitor3
- Wald and Law called their drug the Polypill, a combination of several powerful cardiovascular medications-a statin, an ACE inhibitor, a beta-blocker and a thiazide-as well as aspirin. (protomag.com)
- For people with resistant hypertension, already taking a thiazide diuretic, an angiotensin converting enzyme inhibitor (ACE-i) or an angiotensin II receptor blocker (ARB), and a calcium channel blocker, the addition of amiloride (or spironolactone) was better at reducing blood pressure than adding a beta-blocker (bisoprolol) or an alpha-1 blocker (doxazosin). (worldsbest.rehab)
- Because Liddle phenotype usually involves an upregulation of ENaC channels, leading to retention of sodium and water and to hypokalemia, amiloride is useful as an ENaC channel inhibitor due to its promotion of sodium excretion and its potassium-sparing effects, restoring potassium to normal levels. (worldsbest.rehab)
Potent sodium channel blocker2
- Being the most potent sodium channel blocker among its group, it causes severe cardiotoxicity (eg, wide QRS complex, hypotension) without producing significant antimuscarinic symptoms. (medscape.com)
- INTRODUCTION: Tetrodotoxin (TTX) is a potent sodium channel blocker, with significant neurotoxicity, found in marine animals like pufferfish and blue-ringed octopus. (cdc.gov)
Calcium channel1
- Amlodipine/valsartan/hydrochlorothiazide may be used as add-on/switch therapy for patients not adequately controlled on any two of the following antihypertensive classes: calcium channel blockers, angiotensin receptor blockers, and diuretics. (nih.gov)
Voltage-gated sodium7
- Voltage-gated sodium channels are important targets for the development of pharmaceutical drugs, because mutations in different human sodium channel isoforms have causal relationships with a range of neurological and cardiovascular diseases. (rcsb.org)
- Structure of a bacterial voltage-gated sodium channel pore reveals mechanisms of opening and closing. (rcsb.org)
- To evaluate the Swarm screening system, we optimized a series of heterologous optogenetic spiking HEK293 cell assays for several voltage-gated sodium channel subtypes including Nav1.2, Nav1.5, and Nav1.7. (frontiersin.org)
- The targets that many researchers are aiming at are called voltage-gated sodium ion channels, which are common in pain-sensing nerve cells. (scientificamerican.com)
- The voltage gated sodium channel Na V 1.8 has been postulated to play a key role in the transmission of pain signals. (ncl.ac.uk)
- These agents block the excitability of nerves, principally by blocking voltage-gated sodium channels. (asra.com)
- It increases the duration of ventricular and atrial muscle action by inhibiting POTASSIUM CHANNELS and VOLTAGE-GATED SODIUM CHANNELS. (bvsalud.org)
Angiotensin1
- Amlodipine/valsartan/hydrochlorothiazide is a combination tablet of amlodipine, a dihydropyridine calcium channel blocker (DHP CCB), valsartan, an angiotensin II receptor blocker (ARB), and hydrochlorothiazide, a thiazide diuretic. (nih.gov)
Inhibitors2
- Clinical data are currently available for sodium channel isoform-specific antagonists, anti-nerve growth factor molecules, and fatty acid amide hydrolase inhibitors. (hindawi.com)
- The main groups include sodium channel blockers, calcium current inhibitors, gamma-aminobutyric acid (GABA) enhancers, glutamate blockers, carbonic anhydrase inhibitors, hormones, and drugs with unknown mechanisms of action (see the image below). (medscape.com)
Beta-blocker1
- Together these 4 plus just one beta blocker has been enough to drop my BP from 200/100 down to 125/60 . (deeprootsathome.com)
Potassium2
- I use celery as a diuretic and banana to deal with the potassium/sodium balance. (deeprootsathome.com)
- That's an indication of muscle overuse and inadequate electrolytes (potassium, sodium and magnesium), and too much calcium (which triggers muscle contractions). (maxcelint.com)
Selective3
- Although most novel drugs are still developed using the "magic bullet" paradigm, which involves highly selective profiles, chemical compounds are naturally promiscuous in practice. (frontiersin.org)
- Snake venom is also a source of selective channel blockers. (scientificamerican.com)
- Subsequent optimization allowed the identification of compound 9 , PF-06305591, as a potent, highly selective blocker with an excellent preclinical in vitro ADME and safety profile. (ncl.ac.uk)
Bioactive compound2
- Dr Johan Svenson, Cawthron Institute's Science Leader for Algae and Bioactives research says this is a globally significant scientific innovation that demonstrates Cawthron Institute's world leading expertise in algal biotechnology and bioactive compound extraction and purification. (aquahoy.com)
- Producing commercial quantities of algae is a complex business - figuring out how to grow it is challenging enough, but then you still need the capability to extract and purify the bioactive compound, and in the case of neosaxitoxin, there was a chemical conversion step that we have developed and patented to achieve the level of purity required. (aquahoy.com)
Neurotoxicity1
- Jamaicamide A belongs to a family of compounds collectively called jamaicamides, which are sodium channel blockers with potent neurotoxicity in a cellular model. (wikipedia.org)
Ions4
- During an action potential, these channels exist in the active state and allow influx of sodium ions. (medscape.com)
- In order to illustrate the potential of the updated Geomfinder version, we show a case of use in which similar 3D patterns were detected in the cardiac ions channels NaV1.5 and TASK-1. (frontiersin.org)
- It has been proven that the influx of sodium ions contributes to the increase in the number of cells falling victim to necrosis and apoptosis. (ifit.ee)
- MS/MS data from a training set of 142 fentanyl analogs were used to select the four product ions and six neutral losses that together provided the most complete coverage (97.2%) of the training set compounds. (cdc.gov)
Inhibits1
- Phenytoin is a sodium channel blocker that inhibits the spread of seizure activity in the brain. (inchikey.info)
Molecular1
- Phenylhydantoin is an organic compound with the molecular formula C10H13NO2. (inchikey.info)
Anticoagulation1
- No ongoing clinical trials are at the moment comparing any of screening compounds the new anticoagulation agents with one another. (liverxreceptor.com)
Mutations4
- In silico docking studies indicate the full extent of the blocker binding site, and electrophysiology studies of NavMs channels with mutations at adjacent residues validate the location. (rcsb.org)
- Finally, it seems appropriate to consider the "sodium channel syndrome" (mutations in the gene of the α subunit of the sodium channel, SCN5A gene) as a single clinical entity that may manifest in a wide range of phenotypes, to thus have a better insight on these cardiac syndromes and potential outcomes for their clinical treatment. (bvsalud.org)
- Mutations in the genes encoding a calcium channel (Ca V 1.1) and a sodium channel (Na V 1.4) have been identified in HypoPP families. (jci.org)
- The hyperkalemic form is due to mutations in the gene that encodes the alpha-subunit of the skeletal muscle sodium channel ( SCN4A ). (msdmanuals.com)
Novel compounds2
- The present invention relates to novel compounds of general formula: and to the cosmetic or pharmaceutical use thereof. (justia.com)
- Researchers at UIC who wish to deposit novel compounds or natural product fractions into our collection are encouraged to do so. (agilent.com)
Currents2
- Title: Inflammatory-pathway.indd Created Date: 7/18/2018 1:38:17 PM Small-diameter sensory neurons express a variety of sodium channel transcripts as well as a repertoire of electrophysiological and pharmacologically distinct type of sodium currents. (newmedia1.net)
- The effects of the novel analogs were tested on sodium currents of native myofibers. (uniba.it)
Benzimidazole2
- The tri-component synthesis of novel chiral benzimidazole Mannich bases, by reaction between benzimidazole, aqueous 30% formaldehyde and an amine, the biological evaluation and DFT studies of the new compounds are reported here. (biomedcentral.com)
- Core hopping from our previously reported phenylimidazole leads has allowed the identification of a novel series of benzimidazole Na V 1.8 blockers. (ncl.ac.uk)
Subunit1
- In the hypokalemic form, 70% of affected people have a mutation in the alpha-subunit of the voltage-sensitive muscle calcium channel gene on chromosome 1q (HypoPP type I). In some families, the mutation is in the alpha-subunit of the sodium channel gene on chromosome 17 (HypoPP type II). (msdmanuals.com)
Fungicides2
- Patent Document 1 discloses a harmful organism control composition containing a cyclic amine compound having a specific structure and at least one selected from the group consisting of neonicotinoid compounds, organophosphorus insecticides, carbamate insecticides, synthetic pyrethroid insecticides, IGR insecticides, other insecticides/acaricides and agricultural/horticultural fungicides. (justia.com)
- This present disclosure is related to the field of to N-(substituted)-5-fluoro-4-imino-3-methyl-2-oxo-3,4-dihydropyrimidine-1(2H)-carboxamide compounds and their derivatives and to the use of these compounds as fungicides. (justia.com)
Influx1
- The transporters mediate the simultaneous efflux of a hydrogen ion and the influx of a sodium ion across the plasma membrane, the driving force being the inwardly directed electrochemical Na + gradient. (tocris.com)
Inhibition2
- This compound also displayed low micromolar inhibition of sodium channel-blocking activity at 5 µM. (wikipedia.org)
- We also present in silico result of compounds that bind to γ-tubulin under the ambit of centrosomal clustering inhibition. (blogspot.com)
IUPAC1
- IUPAC nomenclature provides a standardized method for naming chemical compounds. (inchikey.info)
Subset2
- ChemDiv PPI library (10,000 compounds): A 10K subset of the ChemDiv protein-protein interaction library, curated to follow rules 1-4 above. (agilent.com)
- With this approach, lower reportable limits for fentanyl and a subset of fentanyl-related compounds range from 0.25 to 2.5 ng/mL in urine and 0.5 to 5.0 ng/mL in plasma. (cdc.gov)
Magnesium2
- The revolutionary Compound Complex ™ process potentiates all of the active ingredients in Potentiated Magnesium ( pMg ) and Go To The MAX ( MAX ), bringing each of them to their full potential. (maxcelint.com)
- Because of the new and patented Compound Complex process, pMg is the only form of magnesium in oral supplement form that has successfully overcome the inherent hydrophilic nature of magnesium (thus eliminating magnesium's usual laxative effect), and as a result has 100% Uptake - not just bioavailability but actual uptake . (maxcelint.com)
Nav1.71
- Plugging one particular type of channel, known as NaV1.7, keeps the cell from passing a pain message to other parts of the body, as discussed in the accompanying article. (scientificamerican.com)
Cardiac1
- Functional states of the sodium channel (closed, open, and inactivated) and their structure help to understand the cardiac regulation processes. (bvsalud.org)
Chemical compound2
- CAS number (Chemical Abstracts Service Registry Number) is a unique identifier is assigned to every chemical compound indexed in the CAS database. (inchikey.info)
- Sodium cyanoborohydride CAS 25895-60-7 is the chemical compound with the formula NaBH3CN. (kmubk.com)
Pore1
- Crystal complexes of the NavMs pore with several brominated blocker compounds depict a common antagonist binding site in the cavity, adjacent to lipid-facing fenestrations proposed to be the portals for drug entry. (rcsb.org)
Algae2
- Cawthron Institute has decades of experience producing compounds from algae for a range of scientific purposes. (aquahoy.com)
- Company Description Ideal Health Biotechnology researches and develops dietary supplements made from plant-based compounds, including products derived from grape seed extract and algae for digestion, eye disease and diabetes. (ncbiotech.org)
Drugs5
- Even when plants themselves don't produce a useful compound, they often have chemicals that inspire more potent synthetic drugs. (labonline.com.au)
- The Amazon is home to unique wildlife that contains potent compounds that scientists can use to synthesise new drugs. (labonline.com.au)
- These results suggest that the NavMs channel can be a valuable tool for screening and rational design of human drugs. (rcsb.org)
- Some antiepileptic drugs work by acting on combination of channels or through some unknown mechanism of action. (medscape.com)
- These channels are quite different in terms of structure, sequence and function and both have been regarded as important targets for drugs aimed at treating atrial fibrillation. (frontiersin.org)
Elemental1
- The 1 H-NMR, 13 C-NMR, FTIR spectra and elemental analysis confirm the structures of the new compounds. (biomedcentral.com)
Bind2
- Provided herein are compounds that bind to dCK and methods for treating cancer. (justia.com)
- It has been documented that compounds with guanidine-like structures may bind to imidazoline receptors [ 11 ]. (hindawi.com)
Nav1.51
- Finally, we describe the in vitro effects of tafluprost (a drug currently used to treat glaucoma, which was identified as a novel putative ligand of NaV1.5 and TASK-1) upon both ion channels' activity and discuss its possible repositioning as a novel antiarrhythmic drug. (frontiersin.org)
Urine1
- Hepatorenal syndrome is diagnosed when a creatinine clearance rate of less than 40 mL/min is present or when a serum creatinine level of greater than 1.5 mg/dL, a urine volume of less than 500 mL/day, and a urine sodium level of less than 10 mEq/L are present. (medscape.com)
Absorption1
- 80% absorption) and less soluble compounds potentially persisting within the lungs (ATSDR 2001e). (cdc.gov)
Targets2
- In the last few years, new medical treatments for neuropathic pain have been tested, including compounds acting on new pain targets [ 1 ]. (hindawi.com)
- Optogenetic assays provide a flexible, scalable, and information rich approach to probe compound effects for ion channel drug targets in both heterologous expression systems and associated disease relevant cell types. (frontiersin.org)
Molecules4
- ChEMBL (Compound Bioactivity Data): ChEMBL is a database of bioactivity data for small molecules, including information on their properties and structures. (inchikey.info)
- The planarity of the molecules, specific bond lengths and localization of HOMO-LUMO orbitals is responsible for the best biological activities of the compounds. (biomedcentral.com)
- Neosaxitoxin is the first member of the class of molecules called site 1 sodium channel blockers to be used in human clinical trials as a local anaesthetic. (aquahoy.com)
- The mambalgins, as the molecules are called, plug a particular set of acid-sensing ion channels in peripheral nerve cells that, like sodium channels, help the cells send pain signals. (scientificamerican.com)
Activity6
- All synthesized compounds were screened by qualitative and quantitative methods for their in vitro antibacterial activity against 4 bacterial strains. (biomedcentral.com)
- Astemizole-related compounds demonstrated anti-prion activity for treatment of Creutzfeldt-Jakob disease, while albendazole compounds are currently used as medication for the treatment of a variety of parasitic worm infestations. (biomedcentral.com)
- In 1938, Houston Merrit and Tracy Putnam described animal models for screening multiple compounds for antiepileptic activity in the Journal of the American Medical Association. (medscape.com)
- Certain venom components have just the right shape and chemical activity to latch onto a part of the channel called a voltage sensor, and that action shuts the channel. (scientificamerican.com)
- The antioxidant activity of selected compounds was assayed with 1,1-diphenyl-2-picrylhydrazyl. (beilstein-journals.org)
- In addition to repeated activity, the increased levels of certain compounds lead to sensitization, as well. (eclecticme.org)
Structures1
- Many structures and processes are involved in the development of a seizure, including neurons, ion channels, receptors, glia, and inhibitory and excitatory synapses. (medscape.com)
Hydrogen2
- and (by direct contact) compounds containing aspirin, hydrogen peroxide, or phenol. (medscape.com)
- Sodium-hydrogen exchangers (Na + /H + exchangers, NHE) are ATP-independent membrane glycoprotein transporters that are involved in the regulation of intracellular pH, cell volume and the cellular response to hormones and mitogens. (tocris.com)
Synonyms2
- One common source of synonyms for chemical compounds is the common or trivial names, assigned on the basis of appearance, properties, or origin of the molecule. (inchikey.info)
- In addition to common and historical names, chemical compounds may also have synonyms that are specific to a particular field or industry. (inchikey.info)
Gene2
- To address the question of specificity for the allele encoding the Na V 1.4-R669H variant as a cause of HypoPP and to produce a model system in which to characterize functional defects of the mutant channel and susceptibility to paralysis, we generated knockin mice carrying the ortholog of the gene encoding the Na V 1.4-R669H variant (referred to herein as R669H mice). (jci.org)
- Each form of familial periodic paralysis involves a different gene and electrolyte channel. (msdmanuals.com)
Electrophysiological1
- In this study, functional electrophysiological studies show that the prokaryotic sodium channel from Magnetococcus marinus (NavMs) binds and is inhibited by eukaryotic sodium channel blockers in a manner similar to the human Nav1.1 channel, despite millions of years of divergent evolution between the two types of channels. (rcsb.org)
Composition1
- Disclosed are a compound and a pharmaceutical composition that exhibit an excellent drug efficacy against a tumor, in particular a tumor which has acquired resistance to gemcitabine. (justia.com)
Biotech1
- Thanks to improvements in biotech, scientists no longer have to exploit animals to extract these valuable compounds. (labonline.com.au)
Organic1
- Metabolites are intermediate organic compounds or are steming from metabolism. (alsachim.com)
Involves1
- One of the mechanisms causing airways to not clear mucous correctly in these patients involves the body's natural homeostasis of sodium which, when absorbed too quickly from the surface of the airway, causes moisture to become absorbed too quickly. (news-medical.net)
Clinical1
- Novel classes of compounds have emerged for treating chronic constipation, with promising clinical trial data. (medscape.com)
Complex1
- See "Maxcelint Uptake" and "Compound Complex" for more details. (maxcelint.com)
Peripheral1
- An embryonic channel (Nav1.3) is also upregulated in damaged peripheral nerves and associated with increased electrical excitability in neuropathic pain states. (newmedia1.net)
Amino1
- At least 279 microcystins have been identified, and most of these compounds share a common amino acid, the Adda side chain. (cdc.gov)
Rational design1
- Previously identified potent and/or use-dependent mexiletine (Mex) analogs were used as template for the rational design of new Nav-channel blockers. (uniba.it)
Severe1
- Following exposure to radioactive strontium compounds, the most severe non carcinogenic effects seen are the result of incorporation of radioactive strontium, an emitter of beta radiation, into the skeleton, with subsequent irradiation of surrounding tissues (ATSDR 2001e). (cdc.gov)