Guanidine derivative U-37883A, inhibits mitochondrial K+ uniport.
The activity of potassium uniport in rat liver mitochondria was measured using light scattering technique (mitochondrial swelling). It was shown, that guanidine derivative, U-37883A (4-morpholinecarboxamidine-N-1-adamantyl-N'-cyclohexylhyd rochloride), was able to inhibit A23187 induced potassium uniport activity. The inhibitory effect of U-37883A on mitochondrial swelling gave an IC50 an of 89 +/- microM. No inhibition was observed with U-37883A analog, U-42069D (4-morpholinecarboxamidine), which points to the specificity of U-37883A action. It was also shown, that U-37883A acted on a different binding site in rat liver mitochondria than glibenclamide, inhibitor of the ATP sensitive potassium channel.
Szewczyk
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Department of Muscle Biochemistry, Nencki Institute of Experimental Biology, Warszawa, Poland.
Wójcik
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Jabłonowska
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Nałecz
D000218:Adamantane / Q000031:analogs & derivatives* / Q000494:pharmacology; D000818:Animals; D001667:Binding, Competitive; D004232:Diuretics / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D008928:Mitochondria / Q000187:drug effects*; D009025:Morpholines / Q000494:pharmacology*; D011188:Potassium / Q000378:metabolism*; D015221:Potassium Channels / Q000187:drug effects*; D051381:Rats
D004232:Diuretics; D009025:Morpholines; D015221:Potassium Channels; C082658:U 37883A; D000218:Adamantane; D011188:Potassium