Key result
The R(-)-isomer of efonidipine specifically blocked T-type Ca(2+) channels, whereas the S(+)-isomer blocked both L- and T-type channels in expression systems.
Population
Expression systems using Xenopus oocytes and baby hamster kidney cells (BHK tk-ts13)
Design
Preclinical
Authors
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R(-)-efonidipine selectively blocks T-type Ca2+ channels; leaves open its cardiovascular utility pending in vivo and clinical validation.
The R(-)-isomer of efonidipine is identified as a specific blocker of the T-type Ca(2+) channel, distinguishing it from the S(+)-isomer and racemic mixture.
Furukawa et al. (2004) studied this question. Efonidipine and its R(-)- and S(+)-isomers was evaluated on Blocking actions on Ca(2+) channel subtypes (L-, T-, N-, P/Q-, and R-types). The R(-)-isomer of efonidipine specifically blocked T-type Ca(2+) channels, whereas the S(+)-isomer blocked both L- and T-type channels in expression systems.
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