Jpn. J. Pharmacol. 82 (3), 269-271 (2000)

Inhibition of Microtubule Polymerization by SK&Fﾊ96365,
a Blocker of Receptor-Linked Ca²⁺ Entry

Minori Mitsui-Saito, Norimichi Nakahata*^,# and Yasushi Ohizumi


Department of Pharmaceutical Molecular Biology, Graduate School of Pharmaceutical Sciences, Tohoku University,
Aoba, Aramaki, Aoba-ku, Sendai 980-8578, Japan
*ﾊTo whom correspondence should be addressed.
^#ﾊPresent address for correspondence: Department of Cellular Signaling, Graduate School of Pharmaceutical Sciences, Tohoku University, Aoba, Aramaki, Aoba-ku, Sendai 980-8578, Japan

Abstract: SK&Fﾊ96365 (l-{b-[3-(4-methoxyphenyl)propoxyl]-4-methoxyphenethyl}-1H-imidazole hydrochloride) is widely used as an effective inhibitor of receptor-linked and capacitative Ca²⁺ entry. Since this inhibitor has additional effects such as inhibition of voltage-dependent Ca²⁺ channels, sarco- and endoplasmic reticula Ca²⁺ pumps and cell proliferation, its molecular mechanism of action remains to be solved. In the present study, we have investigated the effect of SK&Fﾊ96365 on microtubule protein isolated from bovine brain in vitro. SK&Fﾊ96365 depolymerized the polymerized microtubules in a concentration-dependent manner. This result suggests that SK&Fﾊ96365 directly depolymerizes microtubules, an effect that may contribute to the various actions of this compound.

Keywords: SK&Fﾊ96365, Microtubule, Ca²⁺ entry blocker