Funny channels in the control of cardiac rhythm and mode of action of selective blockers

Pharmacological Research : the Official Journal of the Italian Pharmacological Society
Dario DiFrancesco

Abstract

"Funny" (f) channels underlie the cardiac "pacemaker"I(f) current, originally described as an inward current activated on hyperpolarization to the diastolic range of voltages in sino-atrial node myocytes [Brown, HF, DiFrancesco, D, Noble, SJ. How does adrenaline accelerate the heart? Nature 1979;280:235-236]. The involvement of funny channels in the generation and modulation of cardiac pacemaker activity has been amply demonstrated by thorough analysis since its discovery. The degree of funny current activation upon termination of an action potential determines the slope of diastolic depolarization, and hence pacemaker frequency; furthermore, I(f) is under cAMP-mediated control by beta-adrenergic and muscarinic stimulation and underlies the modulation of cardiac rate by the autonomous nervous system: it therefore represents a mechanism of fundamental physiological relevance. Their function in pacemaking makes funny channels an obvious target for drugs aiming at regulation of spontaneous activity and cardiac rate. This explains the recent development of "heart rate-reducing" drugs which act as selective f-channel inhibitors, and as such are capable of specifically slow cardiac frequency by decreasing the rate of diastolic depola...Continue Reading

Citations

Feb 1, 2011·Naunyn-Schmiedeberg's Archives of Pharmacology·Roman BogdanHartmut Ruetten
May 11, 2010·Clinical Research in Cardiology : Official Journal of the German Cardiac Society·Ralf KoesterThomas Meinertz
May 7, 2008·Bulletin of Experimental Biology and Medicine·T L ZefirovA L Zefirov
Jun 15, 2007·Journal of Biomedical Science·Mario Vassalle
Aug 24, 2013·Hypertension Research : Official Journal of the Japanese Society of Hypertension·Taku InoueYusuke Ohya
Nov 1, 2006·The Journal of General Physiology·Phillip PianSteven A Siegelbaum
Sep 19, 2008·Toxicological Sciences : an Official Journal of the Society of Toxicology·Valeria Dell'OvoAurelia Tubaro
Apr 15, 2011·Journal of Neurophysiology·Marie L GoeritzRonald M Harris-Warrick
Mar 5, 2013·Physiology·Oliver MonfrediEdward G Lakatta
Nov 1, 2007·Future Cardiology·Silvia SuffrediniElisabetta Cerbai
Nov 19, 2010·Radiology·Amir A MahabadiUNKNOWN Working group "Cardiac CT" of the German Cardiac Society
Aug 29, 2013·Heart Views : the Official Journal of the Gulf Heart Association·Hosam ZakyArif Al-Mulla
Sep 2, 2014·The New England Journal of Medicine·Kim FoxUNKNOWN SIGNIFY Investigators
Feb 24, 2009·Canadian Journal of Physiology and Pharmacology·Laura SartianiAlessandro Mugelli
Nov 22, 2011·Expert Opinion on Pharmacotherapy·Antonio Arrebola-MorenoJuan-Carlos Kaski
Jan 14, 2011·Expert Opinion on Emerging Drugs·Tarek A N AhmedJ Wouter Jukema
Mar 5, 2016·Trends in Cardiovascular Medicine·Jeffrey S Borer, Luigi Tavazzi
Feb 28, 2016·American Heart Journal·Robert Townsend Cole
Feb 8, 2014·European Journal of Heart Failure·Adriaan A VoorsUNKNOWN SHIFT investigators
Dec 24, 2011·Revista Española De Cardiología·Larraitz GaztañagaBrian P Betensky
Nov 22, 2008·Ageing Research Reviews·Gus Q Zhang, Weiguo Zhang
May 15, 2015·International Journal of Cardiology·Liyuan PengGang Wang
Apr 1, 2008·Annals of the New York Academy of Sciences·Andrea Barbuti, Dario DiFrancesco
Feb 8, 2007·Journal of Cardiovascular Electrophysiology·Andrea BarbutiDario DiFrancesco
Feb 23, 2012·Journal of Cardiovascular Electrophysiology·Eugene A Sosunov, Evgeny P Anyukhovsky
Jun 26, 2014·European Journal of Heart Failure·Michel KomajdaUNKNOWN SHIFT Investigators
Jul 23, 2013·Journal of Cardiovascular Electrophysiology·Francesca StillitanoElisabetta Cerbai
Oct 14, 2009·Pacing and Clinical Electrophysiology : PACE·Lucio CapulziniPedro Brugada
Jan 28, 2010·The American Journal of Cardiology·Jeffrey S Borer, Jean-Claude Tardif
Sep 29, 2009·American Heart Journal·Ralf KösterUNKNOWN REDUCTION Study Group
Apr 21, 2009·Journal of Molecular and Cellular Cardiology·Z Maggie HuangDayue Duan
Mar 14, 2014·JACC. Heart Failure·Eugene Braunwald

❮ Previous
Next ❯

Related Concepts

Related Feeds

Antianginal Drugs: Mechanisms of Action

Antianginal drugs, including nitrates, beta-blockers, and calcium channel blockers, are used in the treatment of angina pectoris. Here is the latest research on their use and their mechanism of action.

CREs: Gene & Cell Therapy

Gene and cell therapy advances have shown promising outcomes for several diseases. The role of cis-regulatory elements (CREs) is crucial in the design of gene therapy vectors. Here is the latest research on CREs in gene and cell therapy.

Bradyarrhythmias

Bradyarrhythmias are slow heart rates. Symptoms may include syncope, dizziness, fatigure, shortness of breath, and chest pains. Find the latest research on bradyarrhythmias here.