Voltage-dependent Ca2+ channels serve as the only link to transduce me
mbrane depolarization into cellular Ca2+-dependent reactions. A wide v
ariety of chemical substances that have the ability to modulate Ca2+ c
hannels have been demonstrated both for their clinic utility and for i
mportance in elucidating the molecular basis of various biological res
ponses. Recently, introduction of molecular biology to pharmacology ha
s brought a great deal of information about the molecular basis of dru
g action in Ca2+ channels. In this review, we attempt to overview rece
nt progress in understanding the interactions between Ca2+ channels an
d their blockers, namely Ca2+ antagonists, from a molecular and struct
ural point of view.