Biochemistry (Easton), 1985-01, Vol.24 (6), p.1394-1403
1985
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Details
- Autor(en) / Beteiligte
- Titel
- Inhibition of Na super(+)/Ca super(2+) exchange in pituitary plasma membrane vesicles by analogues of amiloride
- Ist Teil von
- Biochemistry (Easton), 1985-01, Vol.24 (6), p.1394-1403
- Erscheinungsjahr
- 1985
- Quelle
- Alma/SFX Local Collection
- Beschreibungen/Notizen
- Amiloride is a weak inhibitor of Na super(+)/Ca super(2+) exchange in isolated plasma membrane vesicles prepared from GH sub(3) 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. A structure-activity study indicates that defined structural modifications of guanidino substituents are associated with increases in inhibitory activity. The results suggest that the inhibitors function as Na super(+) analogues, interact at a Na super(+) binding site on the carrier (presumably the site at which the third Na super(+) binds), and reversibly tie up the transporter in an inactive complex. In addition to blocking pituitary exchange, these analogues are effective inhibitors of the bovine brain and porcine cardiac transport systems.