1,5-benzothiazepine binding domain is located on the extracellular side of the cardiac L-type Ca2+ channel.

@article{Kurokawa199715benzothiazepineBD,
  title={1,5-benzothiazepine binding domain is located on the extracellular side of the cardiac L-type Ca2+ channel.},
  author={Junko Kurokawa and Satomi Adachi-Akahane and Taku Nagao},
  journal={Molecular pharmacology},
  year={1997},
  volume={51 2},
  pages={262-8}
}
To determine whether 1,5-benzothiazepine Ca2+ channel blocker approaches its binding domain within the cardiac L-type Ca2+ channel from inside or outside of the membrane, we tested the effects of a novel potent 1,5-benzothiazepine derivative (DTZ323) and its quaternary ammonium derivative (DTZ417) on guinea pig ventricular myocytes by using the whole-cell patch-clamp technique. The extracellular application of DTZ417 suppressed the L-type Ca2+ channel currents (I[Ca(L)]) with an IC50 value of 1… CONTINUE READING

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