Inhibition of Na+/Ca2+ exchange in pituitary plasma membrane vesicles by analogues of amiloride.

@article{Kaczorowski1985InhibitionON,
  title={Inhibition of Na+/Ca2+ exchange in pituitary plasma membrane vesicles by analogues of amiloride.},
  author={Gregory J. Kaczorowski and Francisco Barros and J K Dethmers and M J Trumble and Edward J. Cragoe},
  journal={Biochemistry},
  year={1985},
  volume={24 6},
  pages={1394-403}
}
Amiloride is a weak inhibitor of Na+/Ca2+ exchange in isolated plasma membrane vesicles prepared from GH3 rat anterior pituitary cells. However, substitution on either a terminal guanidino nitrogen atom or the 5-amino nitrogen atom can increase inhibitory potency ca. 100-fold (I50 approximately 10 microM). A structure-activity study indicates that defined structural modifications of guanidino substituents are associated with increases in inhibitory activity. In contrast, analogues bearing 5… CONTINUE READING

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