Archives of Physiology

Archives of Physiology

ISSN 2055-0898
Original Research

2-Aminoethyl diphenylborinate (2-APB) analogues: part 2. regulators of Ca2+ release and consequent cellular processes

Shoichiro Ozaki

Correspondence: Shoichiro Ozaki ozaki-0991@m.jcnnet.jp

Author Affiliations

Laboratory for Developmental Neurobiology, Brain Science Institute, RIKEN, 2-1 Hirosawa, Wako, Saitama 351-0198, Japan.

Abstract

In order to obtain compounds with modified 2-APB activities, we synthesized number of bis-boron 2-APB analogues and analyzed their inhibitory activities for SOCE and IICR. Adducts of amino acids with bis-borinic acid showed the highest activity. The IC50 of 2-APB for SOCE inhibition was 3 µM, while the IC50 of 2051 bis(4,4'(phenyllysineboryl)benzyl) ether was 0.2 µM. By using these compounds, we may be able to regulate Ca2+ release and consequent cellular processes more efficiently than with 2-APB.

Keywords: 2-APB, 2-APB analogue, regulator of Ca2+ release, regulator of cellular processes

ISSN 2055-0898
Volume 1
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