Effects of Bifemelane on the Calcium Level and ATP Release of the Human Origin Astrocyte Clonal Cell

Journal of Pharmacological Sciences

Haruno Kumagai¹  Remi Tsuchiya¹  Mitsuhiro Morita¹  Yoshiumi Ohkubo¹  Yoshitoku Yoshida¹  Yoshihisa Kudo¹  Hiroyoshi Miyakawa¹ 

[1] School of Life Science, Tokyo University of Pharmacy and Life Science, Japan

关键词: human astrocyte;    bifemelane;    ATP release;    store operated Ca2+ entry;    intracellular Ca2+ store;   

DOI  :  10.1254/jphs.FP0060471

学科分类：药学

来源: Nihon Yakuri Gakkai Henshuubu / Japanese Pharmacological Society

【 摘 要 】

References(23)Cited-By(2)The effect of bifemelane hydrochloride (bifemelane) was examined on human origin astrocyte clonal cells (Kings-1). Bifemelane (125 – 1000 μM) induced a dose-dependent increase in the intracellular calcium concentration ([Ca2+]i). In the highest concentration (1000 μM), the drug caused the second large increase in [Ca2+]i during the washing. The increase that occurred during the administration partially remained in the Ca2+-free medium and was blocked by 2-aminoethoxydiphenyl borate (2-APB), an IP3-receptor blocker, indicating that the source of Ca2+ for the increase could be ascribed to the intracellular store. The increase in [Ca2+]i was not observed during washing with Ca2+-free medium, but was observed when the washing was performed with Ca2+-containing medium. Bifemelane caused a dose-dependent ATP release, but histamine and carbachol, which induced a large increase in [Ca2+]i, had no effects on the ATP release. The effects on the [Ca2+]i were blocked by pretreatment with pyridoxal phosphate-6-azophenyl-2',4' disulfonic acid, a P2-receptor antagonist. Although the mechanisms of ATP release induced by the drug have not been elucidated yet, the present results demonstrate that the increase in [Ca2+]i induced by bifemelane is not due to its direct effect on the cells, but is dependent upon the ATP released from the cells.

【 授权许可】

Unknown