PT - JOURNAL ARTICLE AU - JAMES P. CHOVAN AU - ELLIOTT C. KULAKOWSKI AU - STEVEN SHEAKOWSKI AU - STEPHEN W. SCHAFFER TI - Calcium Regulation by the Low-Affinity Taurine Binding Sites of Cardiac Sarcolemma DP - 1980 May 01 TA - Molecular Pharmacology PG - 295--300 VI - 17 IP - 3 4099 - http://molpharm.aspetjournals.org/content/17/3/295.short 4100 - http://molpharm.aspetjournals.org/content/17/3/295.full SO - Mol Pharmacol1980 May 01; 17 AB - Several lines of evidence are presented indicating that taurine binding to the low-affinity sites of cardiac sarcolemma is responsible for many previously observed, taurine-mediated pharmacological effects. First, verapamil inhibits taurine binding to the cell membrane in a dose-dependent manner. Second, verapamil reverses taurine enhancement of Ca2+ binding to the sarcolemma at concentrations at which verapamil itself has no significant effect on Ca2+ binding. Third, maximal reversal of the negative inotropic effect of both low Ca2+ and verapamil perfusion occurs at taurine concentrations above the apparent K0.5 of the low-affinity sites. Fourth, hypotaurine is a potent inhibitor of taurine binding to the low-affinity sites and exerts taurine-like pharmacological effects. This is contrasted with two less potent inhibitors of taurine binding which possess no significant pharmacological activity. It is concluded that binding to low-affinity sarcolemmal sites is a fundamental step in the mechanism underlying the actions of taurine on the heart. The possibility that low-affinity taurine binding affects the Na2+/Ca2+ exchange system of the sarcolemma is discussed. ACKNOWLEDGMENTS The authors wish to thank Jay Kramer for his technical assistance and Mary Ann Elgin for the typing of the manuscript.