ArticleBritish journal of pharmacology1992
Effect of the hypoglycaemic drug (-)-AZ-DF-265 on ATP-sensitive potassium channels in rat pancreatic beta-cells.
Article in British journal of pharmacology, 1992. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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0 citing papers in PubMed, 18 citations in OpenAlex.
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4 authors at 1 institution in 1 country.
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Abstract
1. It has previously been shown that the hypoglycaemic drug (-)-AZ-DF-265 stimulates insulin release from mouse islets; in the presence of 3 mM glucose it also inhibits 86Rb-efflux from 86Rb-loaded islets. Based on these data we tested the hypothesis that (-)-AZ-DF-265 inhibits ATP-sensitive potassium channels. 2. We voltage-clamped the plasma membrane of single rat pancreatic beta-cells in the whole-cell configuration and measured the current flowing through ATP-sensitive potassium channels. (-)-AZ-DF-265 was applied to the outside of the cell; it inhibited the current half-maximally at a concentration of 1.2 +/- 0.2 nM with a Hill coefficient of 0.7 +/- 0.1. The inhibition was reversible on washing. 3. In intact RINm5F cells, the sulphonylurea [3H]-glibenclamide bound with an affinity of 0.24 +/- 0.01 nM and a Hill coefficient of 2.1 +/- 0.4. Treatment with (-)-AZ-DF-265 led to the displacement of [3H]-glibenclamide; this effect was half-maximal at 8.6 +/- 1.7 nM and displayed a Hill coefficient of 0.53 +/- 0.01. Meglitinide and tolbutamide, which represent, respectively, the benzamido and sulphonylurea moieties of glibenclamide, showed Hill coefficients of 0.8 +/- 0.1 and 0.9 +/- 0.1, respectively. 4. At pH 7.4 and with phosphate/borate buffer, (-)-AZ-DF-265 had an apparent octanol/water partition coefficient of about 53, which is intermediate between the partition coefficients of glibenclamide and glipizide. Nevertheless, (-)-AZ-DF-265 bound only to a minor degree to glass and plastic.5. In conclusion, (-)-AZ-DF-265 inhibits ATP-sensitive potassium channels and displaces [3H]-glibenclamide from the sulphonylurea receptor.
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