PMID: 8584049Sep 1, 1995Paper

Extracellular site of action of phenylalkylamines on L-type calcium current in rat ventricular myocytes

Naunyn-Schmiedeberg's Archives of Pharmacology
J W Wegener, H Nawrath

Abstract

The effects of the phenylalkylamines verapamil, gallopamil, and devapamil on L-type calcium currents (ICa) were studied in ventricular myocytes from rat hearts using the whole-cell patch-clamp technique. In particular, the question was addressed, whether the pharmacological binding sites for these drugs were located at the inner and/or at the outer surface of the cell membrane. Therefore, tertiary verapamil, gallopamil, and devapamil and their corresponding quaternary derivatives were applied either from the outside or the inside of the cell membrane. Extracellular application of verapamil, gallopamil and devapamil (each at 3 microM) reduced ICa to 16.1 +/- 8.6%, 11 +/- 8.9%, and 9.3 +/- 6% of control, respectively. Intracellular application of the same substances, via the patch pipette filled with 30 microM of either verapamil, gallopamil, or devapamil, failed to depress ICa. The quaternary derivatives of the phenylalkylamines (30 microM) were ineffective both when applied extracellularly or intracellularly. It is suggested that phenylalkylamines block ICa in ventricular myocytes by acting on a binding site of the calcium channel molecule located at the outer surface of the cell membrane.

Citations

Dec 4, 1995·European Journal of Pharmacology·J W Wegener, H Nawrath
May 12, 1997·European Journal of Pharmacology·J W Wegener, H Nawrath
Aug 22, 2000·British Journal of Pharmacology·J W WegenerH Nawrath
Nov 1, 1996·British Journal of Pharmacology·S BerjukovJ Striessnig
Dec 15, 2010·Molecular Pharmacology·Pamela BergsonDorothy A Hanck
Dec 1, 1996·Naunyn-Schmiedeberg's Archives of Pharmacology·J W Wegener, H Nawrath
Jul 29, 2003·Journal of Cardiovascular Pharmacology·J W WegenerH Nawrath
Jul 24, 1998·Journal of Cardiovascular Pharmacology·J W WegenerH Nawrath
Jan 1, 1997·Annual Review of Pharmacology and Toxicology·G H HockermanW A Catterall
Jul 1, 1997·Pharmazie in unserer Zeit·K J Schleifer
May 15, 1997·Archives of Biochemistry and Biophysics·B S Zhorov, V S Ananthanarayanan

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