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Chemical Compound Review

Cariporide     N-(diaminomethylidene)-3- methylsulfonyl-4...

Synonyms: SureCN39639, HOE642, CHEMBL436559, AG-L-22195, SureCN1648723, ...
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Disease relevance of Cariporide

  • In conclusion, selective inhibition of the Na(+)/H(+) exchanger by cariporide may represent an effective therapeutic strategy in the treatment of hepatic fibrosis [1].
  • Selective Na+/H+ exchange inhibition by cariporide reduces liver fibrosis in the rat [1].
  • After the desired duration of acidosis, NHE was reactivated (by reintroduction of [Na+]o or removal of cariporide), and the rate of recovery of pHi (dpHi/dt) was measured as the index of NHE activity [2].
  • In contrast, recent clinical studies with the NHE inhibitors cariporide and eniporide in patients with evolving myocardial infarction (MI) and those at risk of MI have provided mixed and somewhat contradictory data [3].
  • METHODS: Twenty-six isolated rat hearts and 23 in situ porcine hearts were submitted to no-flow ischemia followed by reperfusion, with or without pre-treatment with cariporide (7 microM in rats and 3 mg/kg in pigs) [4].

Psychiatry related information on Cariporide

  • At day 36, patients treated with cariporide 120 mg demonstrated a 10% risk reduction in death or MI compared with placebo (p = 0.12) [5].

High impact information on Cariporide

  • Treatment with cariporide reduced the degree of liver injury, as determined by alanine aminotransferase (ALT) values, also when administered after the induction of hepatic damage [1].
  • Inhibition of NHE by amiloride or cariporide resulted in a similar reduction of secretin-stimulated bile flow and bicarbonate secretion [6].
  • Preincubation of the cells with zinc was followed by robust activation of Na+/H+ exchange, which was eliminated by cariporide (0.5 microm); indicating that zinc enhances the activity of NHE1 [7].
  • Thus, in the GUARDIAN trial, the cardioprotective efficacy of cariporide was limited to the subset of high-risk patients who underwent coronary artery bypass graft surgery, in whom both prerequisites could be readily fulfilled [3].
  • (d) Small effects of incubation in cariporide and S3705 at low pHe to increase the net cell kill after treatment with melphalan [8].

Chemical compound and disease context of Cariporide

  • We tested if combining treatment with cariporide, an Na(+)/H(+) exchange inhibitor, and diazoxide, a mitochondrial ATP-sensitive K(+) (K(ATP)) channel opener, would reduce myocardial infarct size (IS) to a greater extent than either intervention alone [9].
  • After hypoxia, relaxation to acetylcholine was preserved in adult rings treated with cariporide (-22.3% vs. -9.3% of baseline value in control and treated groups respectively, P<0.05) but not in senescents [10].
  • CONCLUSIONS: Pretreatment with cariporide in the setting of ischemia-reperfusion injury provides greater protection against the development of diastolic abnormalities than probucol when Celsior solution is used for both arrest and preservation [11].
  • We tested whether pharmacologic pre-conditioning with adenosine and the Na(+)/H(+) exchanger inhibitor, cariporide, combined with controlled reperfusion, would prevent injury in porcine hearts that had sustained 30 minutes of hypoxia/ischemia in closed-chest animals [12].
  • These animals exhibited focal myocardial fibrosis and increased ejection fraction, in association with a tendency to increased left ventricular wall thickness and heart weight, after six months of follow-up, both bosentan and cariporide prevented these responses [13].

Biological context of Cariporide

  • RESULTS: The two doses of cariporide did not differ in their effects after 1 month of treatment, since both induced a slight decrease in systolic blood pressure (SBP) of approximately 6 mmHg and regression of the heart weight to body weight ratio (mg/g) from 3.28+/-0.05 to 3.04+/-0.05 (0.3 mg) and 2.99+/-0.10 (3.0 mg, P<0.05) [14].
  • Blockade of impulse propagation (transmembrane action potentials in rat hearts) was also markedly delayed by cariporide (from 14+/-1 to 20+/-1 min, P<0.001) [4].
  • Hydrogen peroxide induced impairment of post-ischemic ventricular function is prevented by the sodium-hydrogen exchange inhibitor HOE 642 (cariporide) [15].
  • A rapid ischemia-induced apoptosis in isolated rat hearts and its attenuation by the sodium-hydrogen exchange inhibitor HOE 642 (cariporide) [16].
  • 1. Specific inhibitors of the sarcolemmal Na(+)/H(+) exchanger (NHE) such as cariporide are being evaluated for cardioprotective therapy during cardiac surgery [17].

Anatomical context of Cariporide

  • RESULTS: Human ventricular myocytes exhibited readily detectable sarcolemmal NHE activity after the induction of intracellular acidosis, and this activity was suppressed by the NHE1-selective inhibitor HOE-642 (cariporide) at 1 micromol/L [18].
  • RESULTS: Pre-treatment with cariporide delayed ATP depletion (luminescence assay in rat myocardium) and onset of rigor contracture (tension recordings or ultrasonic crystals) during ischemia both in rat and pig hearts (P<0.05) [4].
  • Using intracellular acidifications in the presence of 3 mM external sodium on the CR5 fibroblasts, we isolated two revertants which exhibited a complete recovery for sodium affinity but were still resistant to cariporide [19].
  • Cariporide counteracts atherosclerosis-related functions in monocytes from obese and normal individuals [20].
  • Fifteen Sprague-Dawley rats were randomized to receive bolus injections of cariporide or placebo in a dose of 3 mg/kg into the right atrium either 5 mins before or at 8 mins after onset of ventricular fibrillation [21].

Associations of Cariporide with other chemical compounds


Gene context of Cariporide


Analytical, diagnostic and therapeutic context of Cariporide

  • The lack of an effect of additional IB4 treatment may indicate that GSH/cariporide retroinfusion itself affects leukocyte-dependent reperfusion injury [28].
  • BACKGROUND: The aim of this study was to determine the efficacy of cariporide (a sodium-hydrogen exchanger inhibitor), BMS180448 (a pharmacologic ischemic preconditioning agent), and the combination thereof, as adjuvant therapies for extended cardiac allograft preservation [29].
  • The aorta was endoclamped, and in situ perfusion of the aortic root was maintained with University of Wisconsin solution and cariporide [30].
  • METHODS: Treatment with cariporide was commenced either 1 week pre or 30 min, 3 h, 24 h or 7 days after ligation of the left ventricular artery and was continued until haemodynamic parameters were obtained 6 weeks after MI in conscious rats [31].
  • CONCLUSION: In this porcine model of extended cardiac allograft preservation, cariporide was more effective than BMS180448 as an adjuvant to our usual preservation solution [29].


  1. Selective Na+/H+ exchange inhibition by cariporide reduces liver fibrosis in the rat. Di Sario, A., Bendia, E., Taffetani, S., Marzioni, M., Candelaresi, C., Pigini, P., Schindler, U., Kleemann, H.W., Trozzi, L., Macarri, G., Benedetti, A. Hepatology (2003) [Pubmed]
  2. Stimulation of the plasma membrane Na+/H+ exchanger NHE1 by sustained intracellular acidosis. Evidence for a novel mechanism mediated by the ERK pathway. Haworth, R.S., McCann, C., Snabaitis, A.K., Roberts, N.A., Avkiran, M. J. Biol. Chem. (2003) [Pubmed]
  3. Na(+)/H(+) exchange inhibitors for cardioprotective therapy: progress, problems and prospects. Avkiran, M., Marber, M.S. J. Am. Coll. Cardiol. (2002) [Pubmed]
  4. Pre-treatment with the Na+/H+ exchange inhibitor cariporide delays cell-to-cell electrical uncoupling during myocardial ischemia. Rodríguez-Sinovas, A., García-Dorado, D., Padilla, F., Inserte, J., Barrabés, J.A., Ruiz-Meana, M., Agulló, L., Soler-Soler, J. Cardiovasc. Res. (2003) [Pubmed]
  5. A review of the GUARDIAN trial results: clinical implications and the significance of elevated perioperative CK-MB on 6-month survival. Chaitman, B.R. Journal of cardiac surgery. (2003) [Pubmed]
  6. Sodium, hydrogen exchange type 1 and bile ductular secretory activity in the guinea pig. Hübner, C., Stremmel, W., Elsing, C. Hepatology (2000) [Pubmed]
  7. Extracellular zinc triggers ERK-dependent activation of Na+/H+ exchange in colonocytes mediated by the zinc-sensing receptor. Azriel-Tamir, H., Sharir, H., Schwartz, B., Hershfinkel, M. J. Biol. Chem. (2004) [Pubmed]
  8. Reduction of intracellular pH as a strategy to enhance the pH-dependent cytotoxic effects of melphalan for human breast cancer cells. Wong, P., Lee, C., Tannock, I.F. Clin. Cancer Res. (2005) [Pubmed]
  9. Effect of combined K(ATP) channel activation and Na(+)/H(+) exchange inhibition on infarct size in rabbits. Hale, S.L., Kloner, R.A. Am. J. Physiol. Heart Circ. Physiol. (2000) [Pubmed]
  10. Protection of endothelial-derived vasorelaxation with cariporide, a sodium-proton exchanger inhibitor, after prolonged hypoxia and hypoxia-reoxygenation: effect of age. Besse, S., Tanguy, S., Boucher, F., Huraux, C., Riou, B., Swynghedauw, B., de Leiris, J. Eur. J. Pharmacol. (2006) [Pubmed]
  11. Na+/H+ exchange inhibition and antioxidants lack additive protective effects after reperfusion injury in the working heterotopic rat heart isograft. Rabkin, D.G., Curtis, L.J., Weinberg, A.D., Spotnitz, H.M. J. Heart Lung Transplant. (2005) [Pubmed]
  12. Pharmacologic pre-conditioning and controlled reperfusion prevent ischemia-reperfusion injury after 30 minutes of hypoxia/ischemia in porcine hearts. Fedalen, P.A., Piacentino, V., Jeevanandam, V., Fisher, C., Greene, J., Margulies, K.B., Houser, S.R., Furukawa, S., Singhal, A.K., Goldman, B.I. J. Heart Lung Transplant. (2003) [Pubmed]
  13. Contributions of endothelin-1 and sodium hydrogen exchanger-1 in the diabetic myocardium. Hileeto, D., Cukiernik, M., Mukherjee, S., Evans, T., Barbin, Y., Downey, D., Karmazyn, M., Chakrabarti, S. Diabetes Metab. Res. Rev. (2002) [Pubmed]
  14. Regression of cardiomyocyte hypertrophy in SHR following chronic inhibition of the Na(+)/H(+) exchanger. Camilión de Hurtado, M.C., Portiansky, E.L., Pérez, N.G., Rebolledo, O.R., Cingolani, H.E. Cardiovasc. Res. (2002) [Pubmed]
  15. Hydrogen peroxide induced impairment of post-ischemic ventricular function is prevented by the sodium-hydrogen exchange inhibitor HOE 642 (cariporide). Myers, M.L., Farhangkhoee, P., Karmazyn, M. Cardiovasc. Res. (1998) [Pubmed]
  16. A rapid ischemia-induced apoptosis in isolated rat hearts and its attenuation by the sodium-hydrogen exchange inhibitor HOE 642 (cariporide). Chakrabarti, S., Hoque, A.N., Karmazyn, M. J. Mol. Cell. Cardiol. (1997) [Pubmed]
  17. Effects of moderate hypothermia on sarcolemmal Na(+)/H(+) exchanger activity and its inhibition by cariporide in cardiac ventricular myocytes. Hoshino, K., Avkiran, M. Br. J. Pharmacol. (2001) [Pubmed]
  18. Sarcolemmal Na+/H+ exchanger activity and expression in human ventricular myocardium. Yokoyama, H., Gunasegaram, S., Harding, S.E., Avkiran, M. J. Am. Coll. Cardiol. (2000) [Pubmed]
  19. Second-site revertants of a low-sodium-affinity mutant of the Na+/H+ exchanger reveal the participation of TM4 into a highly constrained sodium-binding site. Touret, N., Poujeol, P., Counillon, L. Biochemistry (2001) [Pubmed]
  20. Cariporide counteracts atherosclerosis-related functions in monocytes from obese and normal individuals. Kaloyianni, M., Zolota, Z., Paletas, K., Tsapas, A., Koliakos, G. Obes. Res. (2005) [Pubmed]
  21. Pharmacologic defibrillation. Wann, S.R., Weil, M.H., Sun, S., Tang, W., Pellis, T. Crit. Care Med. (2002) [Pubmed]
  22. Contribution of NHE-1 to cell length shortening of normal and failing rabbit cardiac myocytes. van Borren, M.M., Zegers, J.G., Baartscheer, A., Ravesloot, J.H. J. Mol. Cell. Cardiol. (2006) [Pubmed]
  23. Na(+)/H(+) exchange inhibition attenuates hypertrophy and heart failure in 1-wk postinfarction rat myocardium. Yoshida, H., Karmazyn, M. Am. J. Physiol. Heart Circ. Physiol. (2000) [Pubmed]
  24. Na(+)/H(+) exchange inhibition reduces hypertrophy and heart failure after myocardial infarction in rats. Kusumoto, K., Haist, J.V., Karmazyn, M. Am. J. Physiol. Heart Circ. Physiol. (2001) [Pubmed]
  25. Potent and selective inhibition of the human Na+/H+ exchanger isoform NHE1 by a novel aminoguanidine derivative T-162559. Kawamoto, T., Kimura, H., Kusumoto, K., Fukumoto, S., Shiraishi, M., Watanabe, T., Sawada, H. Eur. J. Pharmacol. (2001) [Pubmed]
  26. The role of the sodium hydrogen exchanger-1 in mediating diabetes-induced changes in the retina. Cukiernik, M., Hileeto, D., Downey, D., Evans, T., Khan, Z.A., Karmazyn, M., Chakrabarti, S. Diabetes Metab. Res. Rev. (2004) [Pubmed]
  27. Enhanced activity of the myocardial Na+/H+ exchanger NHE-1 contributes to cardiac remodeling in atrial natriuretic peptide receptor-deficient mice. Kilic, A., Velic, A., De Windt, L.J., Fabritz, L., Voss, M., Mitko, D., Zwiener, M., Baba, H.A., van Eickels, M., Schlatter, E., Kuhn, M. Circulation (2005) [Pubmed]
  28. Selective retroinfusion of GSH and cariporide attenuates myocardial ischemia-reperfusion injury in a preclinical pig model. Kupatt, C., Hinkel, R., Horstkotte, J., Deiss, M., von Brühl, M.L., Bilzer, M., Boekstegers, P. Cardiovasc. Res. (2004) [Pubmed]
  29. Sodium-hydrogen exchanger inhibition, pharmacologic ischemic preconditioning, or both for extended cardiac allograft preservation. Ryan, J.B., Hicks, M., Cropper, J.R., Garlick, S.R., Kesteven, S.H., Wilson, M.K., Feneley, M.P., Macdonald, P.S. Transplantation (2003) [Pubmed]
  30. Emergency donor heart protection: application of the port access catheter technique using a pig heart transplantation model. Scheule, A.M., Beierlein, W., Zurakowski, D., Jost, D., Haas, J., Vogel, U., Miller, S., Wendel, H.P., Ziemer, G. Transplantation (2004) [Pubmed]
  31. Cardioprotective effects of the Na(+)/H(+)-exchange inhibitor cariporide in infarct-induced heart failure. Spitznagel, H., Chung, O., Xia, Q., Rossius, B., Illner, S., Jähnichen, G., Sandmann, S., Reinecke, A., Daemen, M.J., Unger, T. Cardiovasc. Res. (2000) [Pubmed]
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