101620-15-9Relevant academic research and scientific papers
Design, synthesis and pharmacological characterization of analogs of 2-aminoethyl diphenylborinate (2-APB), a known store-operated calcium channel blocker, for inhibition of TRPV6-mediated calcium transport
Hofer, Alexandre,Kovacs, Gergely,Zappatini, Anna,Leuenberger, Michele,Hediger, Matthias A.,Lochner, Martin
, p. 3202 - 3213 (2013/07/11)
2-Aminoethyl diphenylborinate (2-APB) is a known modulator of the IP 3 receptor, the calcium ATPase SERCA, the calcium release-activated calcium channel Orai and TRP channels. More recently, it was shown that 2-APB is an efficient inhibitor of the epithelial calcium channel TRPV6 which is overexpressed in prostate cancer. We have conducted a structure-activity relationship study of 2-APB congeners to understand their inhibitory mode of action on TRPV6. Whereas modifying the aminoethyl moiety did not significantly change TRPV6 inhibition, substitution of the phenyl rings of 2-APB did. Our data show that the diaryl borinate moiety is required for biological activity and that the substitution pattern of the aryl rings can influence TRPV6 versus SOCE inhibition. We have also discovered that 2-APB is hydrolyzed and transesterified within minutes in solution.
New Prenylamine analogues: synthesis and Ca2+-entry blocking activity
Caldirola, PM,Goot, H van der,Timmerman, H
, p. 571 - 579 (2007/10/02)
The synthesis of a series of diphenylalkylamine derivatives related to prenylamine is reported.The amphetamine group in the prenylamine structure was replaced by other moieties.In addition to substitutions in the aromatic rings, heteroatoms such as sulphur and oxygen were introduced in the chain.The calcium-entry blocking activity was assayed in binding experiments on a guinea-pig brain membrane preparation by displacing -nitrendipine.
