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January 21, 2008British Journal of PharmacologyOpen Access

S0859, anN‐cyanosulphonamide inhibitor of sodium‐bicarbonate cotransport in the heart

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Key result

Compound S0859 reversibly inhibited NBC-mediated intracellular pH recovery (Ki=1.7 μM) in isolated ventricular myocytes without affecting NHE or Cl-/HCO3- exchange.

Population

Guinea pig, rat and rabbit isolated ventricular myocytes

Comparison

Compound S0859, an N-cyanosulphonamide putative… vs Control conditions (absence of S0859)

Design

Preclinical

Authors

FCFrederick F.‐T. Ch'enUniversity of OxfordFVFrancisco C. VillafuerteUniversidad Peruana Cayetano HerediaPSPawel SwietachUniversity of Oxford

Discussion

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Implication

S0859 enables selective NBC studies in vitro; leaves open translation to cardioprotection in patients.

Structured PICO

P
Population
Guinea pig, rat and rabbit isolated ventricular myocytes
I
Intervention
Compound S0859 (C29H24ClN3O3S), an N-cyanosulphonamide putative sodium-bicarbonate cotransport (NBC) inhibitor
C
Comparator
Control conditions (absence of S0859)
O
Outcome
Intracellular pH (pHi) recovery from intracellular acidosis and electrically evoked cell shortening (contraction)surrogate

Compound S0859 is a selective, high-affinity generic NBC inhibitor that slows the recovery of intracellular pH and contraction during acidosis in ventricular myocytes.

Cite This Study

Ch'en et al. (2008) studied this question. Compound S0859 was evaluated on NBC-mediated intracellular pH recovery. Compound S0859 reversibly inhibited NBC-mediated intracellular pH recovery (Ki=1.7 μM) in isolated ventricular myocytes without affecting NHE or Cl-/HCO3- exchange.

synapsesocial.com/papers/6a6ab25701245da06ecb449fhttps://doi.org/10.1038/sj.bjp.0707667
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Also Consider

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  1. 1Protective effects of HOE642, a selective sodium-hydrogen exchange subtype 1 inhibitor, on cardiac ischaemia and reperfusion1995 · 422 citations
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  4. 4Effects of moderate hypothermia on sarcolemmal Na+/H+ exchanger activity and its inhibition by cariporide in cardiac ventricular myocytes2001 · 23 citations
  5. 5Na+/H+exchange inhibition attenuates hypertrophy and heart failure in 1-wk postinfarction rat myocardium2000 · 117 citations