Bepridil: a pharmacological reappraisal of its potential beneficial effects in angina and tissue protection following ischemia

Cardiovascular Drugs and Therapy
R Massingham, P van Zwieten

Abstract

In this review the pharmacologic properties of the calcium antagonist bepridil have been reexamined, particularly the evidence for an intracellular locus of action for the drug. Physicochemical properties of bepridil show it to be highly lipophylic, rapidly and extensively taken up, and accumulated in certain tissues. Combined electrophysiologic and mechanical studies have provided convincing, but indirect, evidence for an intracellular action of bepridil in cardiac muscle. Bepridil also fulfills, to a greater or lesser extent, certain important pharmacologic criteria necessary for evoking an intracellular action of a drug in cardiac and vascular smooth muscle: 1. Responses to agonists known to utilize intracellular calcium in the response are inhibited to a similar extent to depolarization-induced K+ responses. 2. Phasic and tonic responses to noradrenaline in vascular tissues are not, or are only to a minor extent, differentially antagonized. 3. Responses to the calcium ionophore A 23187 are antagonized. 4. Activity is retained following removal of the cell membrane by surfactants. 5. Isolated enzyme systems (e.g., calmodulin, myosin light-chain kinase) are affected by the drug at similar concentrations to those that are effe...Continue Reading

References

Jan 1, 1977·Biochimie·A YounésM Habert
Jul 1, 1987·Journal of Cardiovascular Pharmacology·T HuizerP W Achterberg
May 1, 1987·Journal of Molecular and Cellular Cardiology·N Sperelakis
Mar 1, 1988·Journal of Cardiovascular Pharmacology·H W BoddekeP A van Zwieten
Nov 1, 1986·The Annals of Thoracic Surgery·J W de Jong
Aug 26, 1985·Life Sciences·R G Rahwan
Jul 1, 1985·The Proceedings of the Nutrition Society·T R Houpt
Jun 1, 1987·International Journal of Cardiology·W G Nayler
Jun 1, 1987·Drug Intelligence & Clinical Pharmacy·F P Zeller, S A Spinler
Apr 9, 1986·European Journal of Pharmacology·P SchaefferJ C Stoclet
Oct 1, 1986·Journal of Molecular and Cellular Cardiology·J A Watts
Nov 19, 1986·European Journal of Pharmacology·E WinslowR J Marshall
Jan 28, 1987·European Journal of Pharmacology·J WattsT Harwell
Nov 19, 1986·European Journal of Pharmacology·P C WongP B Timmermans
Jul 1, 1981·Journal of Cardiovascular Pharmacology·E Winslow, K A Kane
Jan 1, 1980·Journal of Cardiovascular Pharmacology·K A Kane, E Winslow
Sep 1, 1982·Journal of Cardiovascular Pharmacology·S Mras, N Sperelakis
Oct 1, 1980·Journal of Molecular and Cellular Cardiology·R E Weishaar, R J Bing
Jun 1, 1982·Pflügers Archiv : European journal of physiology·J HeschelerW Trautwein
Sep 1, 1983·Journal of Autonomic Pharmacology·J BouR Massingham
Feb 10, 1984·European Journal of Pharmacology·C LugnierJ C Stoclet
Apr 15, 1980·Biochemical Pharmacology·A Younes, M Constantin
Feb 18, 1983·European Journal of Pharmacology·D C Pang, N Sperelakis
Jan 15, 1983·Biochemical Pharmacology·G Cramb, J W Dow
Mar 1, 1984·Biochemical Pharmacology·D C Pang, N Sperelakis
Aug 1, 1983·Cardiovascular Research·D J HearseR Wyse
May 1, 1984·Journal of Molecular and Cellular Cardiology·A J Higgins, K J Blackburn
Jun 1, 1981·British Journal of Pharmacology·R J Marshall, A W Muir

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Citations

Jun 5, 1992·European Journal of Pharmacology·J LeboeufR Massingham
Nov 1, 1992·Journal of the Neurological Sciences·D M HiestandM S Kindy
Oct 1, 1989·Trends in Pharmacological Sciences·E BoddekeP van Zwieten
Apr 9, 1992·The American Journal of Cardiology·A GillM D Brannan
Aug 14, 1998·Journal of Medicinal Chemistry·A S BourlotJ Y Mérour

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