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

  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},
  volume={51 2},
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


Publications referenced by this paper.
Showing 1-10 of 36 references

Trans - fer of 1 , 4 - dihydropyridine sensitivity from L - type to class A ( BI ) calcium channels

  • M. Granner, Z. Wang, S. Hering, J. Striessnig, H. Glossmann
  • Neuron
  • 1996

Quaternary 1,5benzothiazepine derivative (DTZ417) acts only from extracellular side of the membrane in ventricular myocytes

  • J. Kurokawa, S. Adachi-Akahane, T. Nagao
  • Heart Vessels (Suppl. 10)
  • 1995
1 Excerpt

implications for pharmacokinetics and access to dihydropyridine binding site

  • Y. W. Kwan, R. Bangalore, M. Lakitsch, H. Glossmann, R. S. Kass. Inhibition of cardiac L-type calcium chan amlodipine
  • J. Mol. Cell Cardiol. 27:253–262
  • 1995
1 Excerpt

High affinity binding of DTZ 323 , a novel 1 , 5 - benzothiazepine derivative , to diltiazem binding site

  • T. Nagao, J. Kurokawa, S. Adachi-Akahane
  • Can . J . Physiol . Pharmacol
  • 1994

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