288305-89-5Relevant academic research and scientific papers
CALCIUM CHANNEL AGONISTS
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, (2014/12/12)
Embodiments of calcium channel agonists, as well as methods of making and using the calcium channel agonists, are disclosed. The disclosed calcium channel agonists and corresponding salt forms have a structure according to general formula I wherein each bond depicted as " " is a single bond or a double bond as needed to satisfy valence requirements; Z1, Z2, Z3, Z4, and Z5 independently are nitrogen or carbon; R1 and R3 are alkyl; R2 is alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; and R4 is alkyl or hydroxyalkyl.
Synthesis and biological evaluation of a selective N- and P/Q-Type calcium channel agonist
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
, p. 985 - 990 (2013/02/23)
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 panel for their off-target effects. Among several novel compounds with diminished cdk activity, we identified a new lead structure with a 4-fold improved N-type Ca2+ channel agonist effect and a 22-fold decreased cdk2 activity as compared to (R)-roscovitine. This compound was selective for agonist activity on N- and P/Q-type over L-type calcium channels.
