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Vol. 291, Issue 2, 464-473, November 1999

Selectivities of Dihydropyridine Derivatives in Blocking Ca2+ Channel Subtypes Expressed in Xenopus Oocytes1

Taiji Furukawa, Takeshi Yamakawa, Takayuki Midera, Toshio Sagawa, Yasuo Mori and Toshihide Nukada

Department of Medicine, Teikyo University School of Medicine, Tokyo, Japan (T.F., T.Y., T.M., T.S.); Department of Information Physiology, National Institute for Physiological Sciences, Okazaki, Japan (Y.M.); and Department of Neurochemistry, Tokyo Institute of Psychiatry, Tokyo, Japan (T.N.)

Some dihydropyridines (DHPs), such as amlodipine and cilnidipine, have been shown to block not only L-type but also N-type Ca2+ channels; therefore, DHPs are no longer considered as L-type-specific Ca2+ channel blockers. However, selectivity of DHPs for Ca2+ channel subtypes including N-, P/Q-, and R-types are poorly understood. To address this issue at the molecular level, blocking effects of 10 DHPs (nifedipine, nilvadipine, barnidipine, nimodipine, nitrendipine, amlodipine, nicardipine, benidipine, felodipine, and cilnidipine) on four subtypes of Ca2+ channels (L-, N-, P/Q-, and R-types) were investigated in the Xenopus oocyte expression system with the use of the two-microelectrode voltage-clamp technique. L-type Ca2+ channels expressed as alpha 1Calpha 2beta 1a combination were profoundly blocked by all DHPs examined, whereas blocking actions of these DHPs on R-type (alpha 1Ealpha 2beta 1a) channels were equally weak. In contrast, 5 of the 10 DHPs (amlodipine, benidipine, cilnidipine, nicardipine, and barnidipine) significantly blocked N-type (alpha 1Balpha 2beta 1a) and P/Q-type (alpha 1Aalpha 2beta 1a) Ca2+ channels. These selectivities of DHPs in blocking Ca2+ channel subtypes would provide useful pharmacological and clinical information on the mode of action of the drugs including side effects and adverse effects.

0022-3565/99/2912-0464$03.00/0
THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
Copyright © 1999 by The American Society for Pharmacology and Experimental Therapeutics


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