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  • Sigma receptor ligand haloperidol is a neuroleptic drug with adverse cardiovascular effects, mainly ventricular arrhythmias. Its effects on the time course of action potential and on the basic ionic currents (sodium current INa, calcium current ICa, and potassium currents Ito,, IK1 and IK,end - current at the end of 250 ms pulse) were studied on enzymatically isolated rat ventricular cardiomyocytes using the whole cell patch clamp technique at room temperature. Haloperidol induced reversible and concentration-dependent inhibition of all investigated membrane currents. 1 ľmol/l inhibited INa by 39 %, ICa by 19.5 %, Ito by 23 % and IK,end by 14%, 10 ľmol/l haloperidol - by 95 %, 22 % 80 % 37 %, respectively, and IK1 by 29 %. Reversible loss of action potential in haloperidol was observed. Inhibition of Ito-amplitude by the drug was accompanied by acceleration of apparent inactivation. Both were voltage-independent. The time course of Ito recovery from inactivation was decelerated in the drug and 9 % of
  • Sigma receptor ligand haloperidol is a neuroleptic drug with adverse cardiovascular effects, mainly ventricular arrhythmias. Its effects on the time course of action potential and on the basic ionic currents (sodium current INa, calcium current ICa, and potassium currents Ito,, IK1 and IK,end - current at the end of 250 ms pulse) were studied on enzymatically isolated rat ventricular cardiomyocytes using the whole cell patch clamp technique at room temperature. Haloperidol induced reversible and concentration-dependent inhibition of all investigated membrane currents. 1 ľmol/l inhibited INa by 39 %, ICa by 19.5 %, Ito by 23 % and IK,end by 14%, 10 ľmol/l haloperidol - by 95 %, 22 % 80 % 37 %, respectively, and IK1 by 29 %. Reversible loss of action potential in haloperidol was observed. Inhibition of Ito-amplitude by the drug was accompanied by acceleration of apparent inactivation. Both were voltage-independent. The time course of Ito recovery from inactivation was decelerated in the drug and 9 % of (en)
  • Ligand sigma receptorů haloperidol je neuroleptikum se závažnými vedlejšími kardiovaskulárními účinky, především ventrikulárními arytmiemi. Studovali jsme jeho účinky na průběh akčního potenciálu a na základní iontové proudy (sodíkový - INa, vápníkový - ICa a draslíkové proudy - Ito,, IK1 a IK,end - proud na konci 250 ms pulzu) u izolovaných komorových kardiomyocytů potkana, za použití whole cell patch clamp techniky, při pokojové teplotě. Haloperidol způsobil reverzibilní a koncentračně-závislou inhibici všech zkoumaných proudů. 1 umol/l inhiboval INa na 39 %, ICa na 19.5 %, Ito na 23 % a IK,end na 14%, 10 umol/l haloperidol - na 95 %, 22 % 80 % 37 %, a IK1 na 29 %. Byla také pozorována reverzibilní blokáda akčního napětí. Inhibice Ito-amplitudy byla doprovázena akcelerací zřejmé inaktivace, obojí napěťově závisle. Můžeme shrnout, že haloperidol inhibuje všechny hlavní iontové proudy v kardiomyocytu potkana, obzvláště markantně sodíkový proud což koresponduje s velkým efektem na akční napětí. Inhibic (cs)
Title
  • Effects of sigma receptor ligand haloperidol on ionic currents in rat cardiomyocyte
  • Effects of sigma receptor ligand haloperidol on ionic currents in rat cardiomyocyte (en)
  • Účinky ligandu sigma receptorů haloperidolu na iontové proudy u kardiomyocytu potkana (cs)
skos:prefLabel
  • Effects of sigma receptor ligand haloperidol on ionic currents in rat cardiomyocyte
  • Effects of sigma receptor ligand haloperidol on ionic currents in rat cardiomyocyte (en)
  • Účinky ligandu sigma receptorů haloperidolu na iontové proudy u kardiomyocytu potkana (cs)
skos:notation
  • RIV/00216224:14110/06:00015732!RIV08-GA0-14110___
http://linked.open.../vavai/riv/strany
  • 981
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • P(GA305/04/1385)
http://linked.open...iv/cisloPeriodika
  • 6
http://linked.open...vai/riv/dodaniDat
http://linked.open...aciTvurceVysledku
http://linked.open.../riv/druhVysledku
http://linked.open...iv/duvernostUdaju
http://linked.open...titaPredkladatele
http://linked.open...dnocenehoVysledku
  • 473373
http://linked.open...ai/riv/idVysledku
  • RIV/00216224:14110/06:00015732
http://linked.open...riv/jazykVysledku
http://linked.open.../riv/klicovaSlova
  • sigma receptor; haloperidol; ionic currents; cardiomyocyte (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • NL - Nizozemsko
http://linked.open...ontrolniKodProRIV
  • [D23ED35E9DB3]
http://linked.open...i/riv/nazevZdroje
  • Journal of Molecular and Cellular Cardiology
http://linked.open...in/vavai/riv/obor
http://linked.open...ichTvurcuVysledku
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http://linked.open...vavai/riv/projekt
http://linked.open...UplatneniVysledku
http://linked.open...v/svazekPeriodika
  • 40
http://linked.open...iv/tvurceVysledku
  • Bébarová, Markéta
  • Pásek, Michal
  • Nováková, Marie
  • Lacinová, Ľubica
  • Matejovič, Peter
  • Tarabová, Bohuslava
issn
  • 0022-2828
number of pages
http://localhost/t...ganizacniJednotka
  • 14110
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