Synthesis and biological evaluation of a selective N-and P/Q-type calcium channel agonist

…, TB Tarr, K Bravo-Altamirano, G Valdomir…

Index: Liang, Mary; Tarr, Tyler B.; Bravo-Altamirano, Karla; Valdomir, Guillermo; Rensch, Gabriel; Swanson, Lauren; Destefino, Nicholas R.; Mazzarisi, Cara M.; Olszewski, Rachel A.; Wilson, Gabriela Mustata; Meriney, Stephen D.; Wipf, Peter ACS Medicinal Chemistry Letters, 2012 , vol. 3, # 12 p. 985 - 990

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Citation Number: 6

Abstract

The acute effect of the potent cyclin-dependent kinase (cdk) inhibitor (R)-roscovitine on Ca2+ channels inspired the development of structural analogues as a potential treatment for motor nerve terminal dysfunction. On the basis of a versatile chlorinated purine scaffold, we have synthesized ca. 20 derivatives and characterized their N-type Ca2+ channel agonist action. Agents that showed strong agonist effects were also characterized in a kinase ...

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