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Effect of disulfonic stilbene anion-channel blockers on the guinea-pig myocardium

 

作者: Arda-E-Viraf M. Minocherhomjee,   Basil D. Roufogalis,   John H. McNeill,  

 

期刊: Canadian Journal of Physiology and Pharmacology  (NRC Available online 1985)
卷期: Volume 63, issue 8  

页码: 912-917

 

ISSN:0008-4212

 

年代: 1985

 

DOI:10.1139/y85-151

 

出版商: NRC Research Press

 

数据来源: NRC

 

摘要:

The role of anions in the maintenance of tension in electrically driven left atria isolated from guinea pigs has been examined. The disulfonic stilbene anion-channel blockers SITS (4-acetamido-4′-isothiocyanostilbene 2′-disulfonate) and DIDS (4,4′-diisothiocyano-2,2′-stilbene disulfonate) decreased the contractile force developed in a time- and concentration-dependent manner. As in the red cell anion channel, DIDS was more potent than SITS, but the maximal inhibition of tension produced byN-(4-azido-2-nitrophenyl)-2-aminoethyl sulfonate (NAP-taurine) was considerably lower than the near maximal inhibition produced by SITS and DIDS. The inhibition by SITS and DIDS was irreversible, suggesting a covalent interaction, and could not be overcome by increasing the calcium concentration or the frequency of stimulation. Consistent with a requirement for chloride anion, substitution of chloride and bicarbonate by the impermeant anion gluconate did not support contraction, while only partial tension was maintained with the lipophilic anions acetate and thiocyanate. Incubation of atria with 400 μMSITS blocked both36Cl and45Ca uptake to a similar extent, whereas the efflux of both these ions was not affected by incubation of the atria with SITS. The blockade by disulfonic stilbene anion-channel blockers of the contraction of the guinea pig myocardium may result from impairment of excitation–contraction coupling.

 

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