The D3-dopaminergic agonist 7-hydroxy-dipropylaminotetralin (7-OH-DPAT) increases cardiac action potential duration and blocks human ether-a-go-go-related gene K channel
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The D3-dopaminergic agonist (±) 7-hydroxy- dipropylaminotetralin (7-OH-DPAT) prolonged cycle length and action potential duration, depolarized maximum diastolic potential, and reduced the upstroke velocity of the action potential of rabbit sinoatrial node cells. These effects were not mediated by D3-dopaminergic receptors. In cat Purkinje fibers, the drug increased action potential duration. In voltage-clamped cat ventricular myocytes, 7-OH-DPAT blocked the rapid component of the delayed rectifier potassium current, IKr. This effect was corroborated in experiments studying the effect of the drug on human Ether-a-go-go-related Gene channels expressed in Xenopus oocytes and in HEK293 cells. We conclude that the direct electrophysiologic effects of 7-OH-DPAT on cardiac tissues are caused by the blockade of the rapid component of the delayed rectifier potassium current, IKr. Copyright © 2006 by Lippincott Williams %26amp; Wilkins.
The D3-dopaminergic agonist (±) 7-hydroxy- dipropylaminotetralin (7-OH-DPAT) prolonged cycle length and action potential duration, depolarized maximum diastolic potential, and reduced the upstroke velocity of the action potential of rabbit sinoatrial node cells. These effects were not mediated by D3-dopaminergic receptors. In cat Purkinje fibers, the drug increased action potential duration. In voltage-clamped cat ventricular myocytes, 7-OH-DPAT blocked the rapid component of the delayed rectifier potassium current, IKr. This effect was corroborated in experiments studying the effect of the drug on human Ether-a-go-go-related Gene channels expressed in Xenopus oocytes and in HEK293 cells. We conclude that the direct electrophysiologic effects of 7-OH-DPAT on cardiac tissues are caused by the blockade of the rapid component of the delayed rectifier potassium current, IKr. Copyright © 2006 by Lippincott Williams & Wilkins.
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7-OH-DPAT; Cardiac action potential; hERG; IKr; Sinoatrial node 2 dipropylamino 7 hydroxytetralin; dopamine receptor stimulating agent; potassium channel HERG; voltage gated potassium channel; 7 hydroxy 2 N,N dipropylaminotetralin; 7-hydroxy-2-N,N-dipropylaminotetralin; dopamine 3 receptor; KCNH2 protein, human; potassium channel HERG; tetralin derivative; animal cell; article; cat; controlled study; diastolic blood pressure; gene expression regulation; heart electrophysiology; heart muscle potential; heart stroke volume; human; human cell; human tissue; nonhuman; potassium current; priority journal; Purkinje cell; rabbit; sinus node; velocity; action potential; animal; cell line; drug antagonism; drug effect; drug potentiation; heart; heart muscle cell; in vitro study; long QT syndrome; oocyte; physiology; Purkinje fiber; Xenopus; Action Potentials; Animals; Cats; Cell Line; Dopamine Agonists; Ether-A-Go-Go Potassium Channels; Heart; Humans; Long QT Syndrome; Myocytes, Cardiac; Oocytes; Purkinje Fibers; Rabbits; Receptors, Dopamine D3; Sinoatrial Node; Tetrahydronaphthalenes; Xenopus
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