PMID: 8584405Nov 1, 1995Paper

Dihydropyridines, phenylalkylamines and benzothiazepines block N-, P/Q- and R-type calcium currents

Pflügers Archiv : European journal of physiology
S DiochotJ Valmier

Abstract

We compared the effects of representative members of three major classes of cardiac L-type channel antagonists, i.e. dihydropyridines (DHPs), phenylalkylamines (PAAs) and benzothiazepines (BTZs) on high-voltage-activated (HVA) Ca2+ channel currents recorded from a holding potential of -100 mV in rat ventricular cells, mouse sensory neurons and rat motoneurons. Nimodipine (DHP), verapamil (PAA) and diltiazem (BTZ) block the cardiac L-type Ca2+ channel current (EC50: 1 microM, 4 microM and 40 microM, respectively). At these concentrations, the drugs could also inhibit HVA Ca2+ channel currents in both sensory and motor neurons. Large blocking effects (> 50%) could be observed at 2-10 times these concentrations. The omega -conotoxin-GVIA-sensitive (omega -CTx-GVIA, N-type), omega -agatoxin-IVA-sensitive (omega -Aga-IVA, P- and Q-types) and non-L-type omega -CTx-GVIA-, omega -Aga-IVA-insensitive (R-types) currents accounted for more than 90% of the global current. Furthermore, our data showed that omega -CTx-GVIA and omega -Aga-IVA spare L-type currents and have only additive blocking effects on neuronal HVA currents. We conclude that DHPs, PAAs and BTZs have substantial inhibitory effects on neuronal non-L-type Ca2+ channels. Inhi...Continue Reading

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Citations

Dec 5, 1998·Toxicon : Official Journal of the International Society on Toxinology·E KalapothakisP S Beirão
Jun 16, 1999·Progress in Neuro-psychopharmacology & Biological Psychiatry·H A Futuro-NetoJ G Pires
Oct 25, 2000·Neuroscience Letters·P BenquetF Tiaho
Sep 22, 2011·Neuron Glia Biology·Mounir A KoussaLynne A Oland
Oct 1, 1996·Journal of Autonomic Pharmacology·P M Lundy, R Frew
Jun 12, 2010·Journal of Virology·Svetlana V Scherbik, Margo A Brinton
Jan 1, 1997·Annual Review of Pharmacology and Toxicology·G H HockermanW A Catterall
Jan 15, 1997·The Journal of Clinical Investigation·J F QuignardS Richard
Dec 31, 2015·Assay and Drug Development Technologies·Rok CerneBirgit T Priest
May 3, 2000·The European Journal of Neuroscience·K P CarlinR M Brownstone
Jan 20, 2007·Molecular and Cellular Endocrinology·Y LiL C Freeman
May 4, 2013·British Journal of Pharmacology·V Nimmrich, A Eckert
Jun 8, 2012·British Journal of Pharmacology·V Nimmrich, G Gross
Aug 2, 2005·Antiviral Research·Elena V GazinaSteven Petrou
Jul 29, 2015·Comparative Biochemistry and Physiology. Toxicology & Pharmacology : CBP·Nikhil V PalandeArun G Jadhao
Jul 17, 2001·The European Journal of Neuroscience·D Chesnoy-Marchais, L Cathala
Jul 15, 2016·Hypertension Research : Official Journal of the Japanese Society of Hypertension·Nicolás R RoblesGuido Grassi
Sep 28, 1998·The European Journal of Neuroscience·G DesmadrylJ Valmier
Jul 25, 1997·The Journal of Biological Chemistry·B Z PetersonW A Catterall
Jan 30, 2009·American Journal of Physiology. Cell Physiology·Hidetada MatsuokaMasumi Inoue
Aug 13, 1998·Journal of Cardiovascular Pharmacology·S HoischenR H Schwinger

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