Different modes of Ca channel gating behaviour favoured by dihydropyridine Ca agonists and antagonists

Single cardiac transmembranous Ca channels have three modes of gating behaviour in the absence of drugs, expressed as current records with brief openings (mode 1), with no openings because of channel unavailability (mode 0 or null mode) and with long-lasting openings and very brief closings that appear only rarely (mode 2). The dihydropyridine Ca agonist Bay K 8644 enhances Ca channel current by promoting mode 2, while the Ca antagonists nitrendipine and nimodipine inhibit the current by favouring mode 0.

[1]  J. Cooper,et al.  Thromboxane Synthesis by Sources Other Than Platelets in Association with Complement‐Induced Pulmonary Leukostasis and Pulmonary Hypertension in Sheep , 1983, Circulation research.

[2]  R. Kretsinger,et al.  Calcium in biological systems , 1976 .

[3]  R. Tsien,et al.  Mechanism of calcium channel blockade by verapamil, D600, diltiazem and nitrendipine in single dialysed heart cells , 1983, Nature.

[4]  N. Taira,et al.  Simultaneous assessment of effects of coronary vasodilators on the coronary blood flow and the myocardial contractility by using the blood-perfused canine papillary muscle. , 1976, Japanese journal of pharmacology.

[5]  H. Reuter,et al.  Ca2+ channel modulation by 8-bromocyclic AMP in cultured heart cells , 1983, Nature.

[6]  R. Tsien,et al.  β-Adrenergic modulation of calcium channels in frog ventricular heart cells , 1984, Nature.

[7]  M. Lazdunski,et al.  Determination of the molecular size of the nitrendipine-sensitive Ca2+ channel by radiation inactivation. , 1983, Biochemical and biophysical research communications.

[8]  H. Reuter Calcium channel modulation by neurotransmitters, enzymes and drugs , 1983, Nature.

[9]  R. Kao,et al.  The effects of insulin and anoxia on the metabolism of isolated mature rat cardiac myocytes. , 1980, Archives of biochemistry and biophysics.

[10]  W. Catterall,et al.  Solubilization of the calcium antagonist receptor from rat brain. , 1983, The Journal of biological chemistry.

[11]  H. Reuter,et al.  Dihydropyridine derivatives prolong the open state of Ca channels in cultured cardiac cells. , 1984, Proceedings of the National Academy of Sciences of the United States of America.

[12]  M. Sanguinetti,et al.  Photoalteration of calcium channel blockade in the cardiac Purkinje fiber. , 1984, Biophysical journal.

[13]  Y. Niimi,et al.  Prolongation of calcium channel open time by the dihydropyridine derivative BAY K 8644 in cardiac myocytes. , 1984 .

[14]  C. F. Stevens,et al.  Properties of single calcium channels in cardiac cell culture , 1982, Nature.

[15]  E Neher,et al.  Sodium and calcium channels in bovine chromaffin cells , 1982, The Journal of physiology.

[16]  A. Brown,et al.  The suction pipette method for internal perfusion and voltage clamp of small excitable cells , 1980, Journal of Neuroscience Methods.

[17]  T. Linn,et al.  Temperature‐dependent regulation of d‐cis‐[3H]diltiazem binding to Ca2+ channels by 1,4‐dihydropyridine channel agonists and antagonists , 1983, FEBS Letters.

[18]  M. Schramm,et al.  Novel dihydropyridines with positive inotropic action through activation of Ca2+ channels , 1983, Nature.

[19]  J. Venter,et al.  Molecular properties of the slow inward calcium channel. Molecular weight determinations by radiation inactivation and covalent affinity labeling. , 1983, The Journal of biological chemistry.

[20]  A. Fleckenstein Calcium antagonism in heart and smooth muscle , 1984 .

[21]  R. Tsien Calcium channels in excitable cell membranes. , 1983, Annual review of physiology.