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- JTV-519 abstract "JTV-519 (K201) is a 1,4-benzothiazepine derivative that interacts with many cellular targets. It has many structural similarities to diltiazem, a Ca2+ channel blocker used for treatment of hypertension, angina pectoris and some types of arrhythmias. JTV-519 acts in the sarcoplasmic reticulum (SR) of cardiac myocytes by binding to and stabilizing the ryanodine receptor (RyR2) in its closed state. It can be used in the treatment of cardiac arrhythmias, heart failure, catecholaminergic polymorphic ventricular tachycardia (CPVT) and store overload-induced Ca2+ release (SOICR). Currently, this drug has only been tested on animals and its side effects are still unknown. As research continues, some studies have also found a dose-dependent response; where there is no improvement seen in failing hearts at 0.3 μM and a decline in response at 1 μM.Treatment with JTV-519 involves stabilization of RyR2 in its closed state, decreasing its open probability during diastole and inhibiting a Ca2+ leak into the cell’s cytosol. By decreasing the intracellular Ca2+ leak, it is able to prevent Ca2+ sparks or increases in the resting membrane potential, which can lead to spontaneous depolarization (cardiac arrhythmias), and eventually heart failure, due to the unsynchronized contraction of the atrial and ventricular compartments of the heart. When Ca2+ sparks occur from the SR, the increase in intracellular Ca2+ contributes to the rising membrane potential which leads to the irregular heart beat associated to cardiac arrhythmias. It can also prevent SOICR in the same manner; preventing opening of the channel due to the increase of Ca2+ inside the SR levels beyond its threshold.".
- JTV-519 iupacName "3-(4-Benzyl-1-piperidinyl)-1-(7-methoxy-2,3-dihydro-1,4-benzothiazepin-4(5H)-yl)-1-propanone".
- JTV-519 thumbnail JTV-519.svg?width=300.
- JTV-519 wikiPageID "31181238".
- JTV-519 wikiPageLength "8553".
- JTV-519 wikiPageOutDegree "22".
- JTV-519 wikiPageRevisionID "670403243".
- JTV-519 wikiPageWikiLink Angina_pectoris.
- JTV-519 wikiPageWikiLink Arrhythmias.
- JTV-519 wikiPageWikiLink Calcium_channel_blocker.
- JTV-519 wikiPageWikiLink Cardiac_arrhythmia.
- JTV-519 wikiPageWikiLink Catecholaminergic_polymorphic_ventricular_tachycardia.
- JTV-519 wikiPageWikiLink Category:Articles_created_via_the_Article_Wizard.
- JTV-519 wikiPageWikiLink Category:Benzothiazepines.
- JTV-519 wikiPageWikiLink Category:Calcium_channel_blockers.
- JTV-519 wikiPageWikiLink Category:Phenol_ethers.
- JTV-519 wikiPageWikiLink Category:Piperidines.
- JTV-519 wikiPageWikiLink Diastole.
- JTV-519 wikiPageWikiLink Diltiazem.
- JTV-519 wikiPageWikiLink Endoplasmic_reticulum.
- JTV-519 wikiPageWikiLink Heart_failure.
- JTV-519 wikiPageWikiLink Hydrochloride.
- JTV-519 wikiPageWikiLink Hypertension.
- JTV-519 wikiPageWikiLink Phosphorylation.
- JTV-519 wikiPageWikiLink Protein_kinase_A.
- JTV-519 wikiPageWikiLink Ryanodine_receptor.
- JTV-519 wikiPageWikiLink Sarcoplasmic_reticulum.
- JTV-519 wikiPageWikiLink Spontaneous_depolarization.
- JTV-519 wikiPageWikiLink Thiazepine.
- JTV-519 wikiPageWikiLinkText "JTV-519".
- JTV-519 hasPhotoCollection JTV-519.
- JTV-519 imagefile "JTV-519.svg".
- JTV-519 imagesize "200".
- JTV-519 iupacname "3".
- JTV-519 othernames "K201".
- JTV-519 wikiPageUsesTemplate Template:Chembox.
- JTV-519 wikiPageUsesTemplate Template:Reflist.
- JTV-519 subject Category:Articles_created_via_the_Article_Wizard.
- JTV-519 subject Category:Benzothiazepines.
- JTV-519 subject Category:Calcium_channel_blockers.
- JTV-519 subject Category:Phenol_ethers.
- JTV-519 subject Category:Piperidines.
- JTV-519 hypernym Benzothiazepine.
- JTV-519 type Agent.
- JTV-519 type Article.
- JTV-519 type ChemicalCompound.
- JTV-519 type ChemicalSubstance.
- JTV-519 type Agent.
- JTV-519 type Antianginal.
- JTV-519 type Article.
- JTV-519 type Ether.
- JTV-519 type Heterocycle.
- JTV-519 type ChemicalObject.
- JTV-519 type Thing.
- JTV-519 type Q11173.
- JTV-519 comment "JTV-519 (K201) is a 1,4-benzothiazepine derivative that interacts with many cellular targets. It has many structural similarities to diltiazem, a Ca2+ channel blocker used for treatment of hypertension, angina pectoris and some types of arrhythmias. JTV-519 acts in the sarcoplasmic reticulum (SR) of cardiac myocytes by binding to and stabilizing the ryanodine receptor (RyR2) in its closed state.".
- JTV-519 label "JTV-519".
- JTV-519 sameAs جیتیوی-۵۱۹.
- JTV-519 sameAs JTV-519.
- JTV-519 sameAs m.0gh829s.
- JTV-519 sameAs JTV-519.
- JTV-519 sameAs JTV-519.
- JTV-519 sameAs Q6109096.
- JTV-519 sameAs Q6109096.
- JTV-519 wasDerivedFrom JTV-519?oldid=670403243.
- JTV-519 depiction JTV-519.svg.
- JTV-519 isPrimaryTopicOf JTV-519.