Allosteric interactions between the antagonist prazosin and amiloride analogs at the human alpha(1A)-adrenergic receptor.

@article{Leppik2000AllostericIB,
  title={Allosteric interactions between the antagonist prazosin and amiloride analogs at the human alpha(1A)-adrenergic receptor.},
  author={R. A. Leppik and A. Mynett and Sebastian Lazareno and Nigel J. M. Birdsall},
  journal={Molecular pharmacology},
  year={2000},
  volume={57 3},
  pages={
          436-45
        }
}
It has been demonstrated previously that amilorides can interact with a well defined allosteric site on the human alpha(2A)-adrenergic receptor. In this study, the question was explored as to whether the human alpha(1A)-adrenergic receptor also possesses an equivalent allosteric site. The six amilorides examined strongly increased the dissociation rate of the antagonist [(3)H]prazosin from the alpha(1A)-adrenergic receptor in a concentration-dependent manner. With the parent amiloride, the… CONTINUE READING
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