J Mol Cell Cardiol 32, 2279–2285 (2000) doi:10.1006/jmcc.2000.1259, available online at http://www.idealibrary.com on No Confirmation for a Causal Role of Volume-regulated Chloride Channels in Ischemic Preconditioning in Rabbits Gerd Heusch 1,2 , Guang S. Liu 1 , Jochen Rose 2 , Michael V. Cohen 1,3 and James M. Downey 1 1 Departments of Physiology and 3 Medicine, University of South Alabama College of Medicine, Mobile, AL, USA and the 2 Department of Pathophysiology, University of Essen Medical School, Essen, Germany (Received 17 July 2000, accepted in revised form 13 September 2000, published electronically 17 October 2000) G. H, G. S. L, J. R, M. V. C  J. M. D . No Confirmation for a Causal Role of Volume- regulated Chloride Channels in Ischemic Preconditioning in Rabbits. Journal of Molecular and Cellular Cardiology (2000) 32, 2279–2285. Volume-regulated chloride channels have recently been proposed to be end-effectors in ischemic preconditioning. The present study attempted to confirm this hypothesis by looking both at car- dioprotection and channel activity. In isolated rabbit cardiomyocytes, hypo-osmotic stress (167 mosm/l) induced a current with a magnitude of 2–5 pA/pF at 60mV. That current could be blocked by the selective chloride channel blockers 5-nitro–2–(3-phenylpropylamino) benzoic acid (NPPB) or indanyloxyacetic acid 94 (IAA-94), but only at 100 and 1 mrespectively. Lower concentrations were not effective. Because the channel-blocking concentrations were toxic in isolated perfused rabbit hearts, as evidenced by cessation of cardiac contraction and massive infarction, neither agent could be tested against preconditioning’s anti-infarct effect. NPPB and IAA-94 at 1 and 10 , respectively (the doses used in a previous report), did not affect coronary flow, heart rate and developed pressure, and also did not prevent the infarct size reduction of ischemic preconditioning with 5 min global ischemia/10 min reperfusion preceding 30 min of regional ischemia and 120 min of reperfusion [11.4(±3.6) and (11.1(±3.7)% infarction of risk area, respectively]. The volume-regulated chloride and organic osmolyte channel blocker 4,4-diisothiocyanostilbene-2,2-disulfonic acid (DIDS) at 100 blocked the hypo- osmotically induced current in myocytes, but again could not be used, since it induced total cessation of cardiac contraction and reduced infarct size in non-preconditioned hearts. Our data do not confirm a prior study on a causal role for volume-regulated chloride channels in the protection of ischemic preconditioning. This hypothesis remains to be adequately tested. 2000 Academic Press K W: Myocardial ischemia; Reperfusion; Infarction; Cardioprotection. recent studies have proposed the activation of mito- Introduction chondrial K ATP channels as the final step in the signal-transduction cascade, 4,5,6 but it remains un- One or several brief episodes of sublethal myocardial ischemia and reperfusion delay infarct development clear how activation of mitochondrial K ATP channels is ultimately cardioprotective. Alternatively, os- during a subsequent prolonged ischemia. 1 The mag- nitude of cardioprotection by such ischemic pre- motic swelling is a key feature of ischemia/re- perfusion injury to cardiomyocytes. 7,8 Indeed, conditioning is impressive, but its underlying signal cascade and mechanisms are still poorly un- preconditioned cardiomyocytes do show increased tolerance to osmotic swelling, 9 and increased sta- derstood. 2,3 In particular, the final end-effector of ischemic preconditioning is still unclear. Several bility of the actin cytoskeleton has been proposed Please address all correspondence to: James M. Downey, Department of Physiology, MSB 3024, University of South Alabama, College of Medicine, Mobile, AL 366 88, USA. Tel: +334-460-6818; Fax: +334-460-6464; E-mail: jdowney@usamail.usouthal.edu 0022–2828/00/122279+07 $35.00/0 2000 Academic Press