(-)[3H]amlodipine binding to rat cardiac membranes.

  title={(-)[3H]amlodipine binding to rat cardiac membranes.},
  author={Winifred Gwen Nayler and Xi'an Gu},
  journal={Journal of cardiovascular pharmacology},
  volume={17 4},
Amlodipine is a newly developed long-acting dihydropyridine-based calcium antagonist. To characterize the binding properties of this compound, saturation binding studies were undertaken, using (-)[3H]amlodipine and rat cardiac membrane fragments. (-)[3H]Amlodipine bound to a single population of high-affinity binding sites with a KD of 1.68 +/- 0.12 nM, a Bmax of 0.34 +/- 0.08 pmol/mg protein, and a Hill coefficient approaching unity. Binding required up to 5 h to reach asymptote, and was pH… CONTINUE READING

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