Voltage-dependent blockers

There was some interest in the isobutylamides derived from various plant species including affinin (Figure 3.25) from Heliopsis longipes and pipercide (Figure 3.25) from Piper nigrum. These compounds are potent voltage-dependent blockers of the sodium channel but are too unstable to be used as products directly. 

Voltage-dependent Ca2+ Channels Ca2+ Channel Blockers Ryanodine Receptor... 

Voltage-dependent Ca2 Channels. Figure 1 Structure, identity and blockers of calcium channel subunits. 

Ca44 channel-blockers Nifedipine Inhibits voltage-dependent L-type Ca44 channels. 

Nelson We have seen Ca2+ channel blockers block the voltage dependence of the frequency of the STOCs. 

Witchel, H.J., Dempsey, C.E., Sessions, R.B., Perry, M., Milnes, J.T., Hancox, J.C. and Mitcheson, J.S. (2004) The low-potency, voltage-dependent HERG blocker propafenone-molecular determinants and drug trapping. Molecular Pharmacology, 66, 1201—... 

Available evidence suggests that a single unifying mechanism does not exist but rather that various vasodilators may act at different places in the series of processes that couple excitation of vascular smooth muscle cells with contraction. For example, the vasodilators known as calcium channel antagonists block or limit the entry of calcium through voltage-dependent channels in the membrane of vascular smooth muscle cells. In this way, the calcium channel blockers limit the amount of free intracellular calcium available to interact with smooth muscle contractile proteins (see Chapter 14). 

Derived from lamotrigine (Glaxo Wellcome), The compound is a potent voltage- and frequency-dependent blocker of TTX-resitant and TTX-sensitive sodium channels. The compound induces anti-hyperalgesic and anti-allodynic effects in animal models of chronic neuropathic and inflammatory pain... 

Carter, R. B., Vanover, K. E., Wilent, W., Xu, Z., Woodward, R. M., Illyin, V. I. Anti-allodynic and anti-hyperalgesic effects of the novel voltage-dependent sodium channel blocker Co102862 in a rat model of peripheral neuropathy, Adv. Ion Channel Res., San Francisco 1999, Abstract book, P-... 

Tetrodotoxin (TTX) a voltage-dependent Na+-channel blocker was infused directly into the prefrontal cortex through the dialysis fiber. TTX significantly decreased ACh spontaneous release by more than 40%, but the exposure to 100 mM potassium released similar amounts of ACh in the absence and in the presence of 0.5 pM TTX (figure 2). However, H3 receptor-induced inhibition is... 

Yarishkin OV, Ryu HW, Park JY, Yang MS, Hong SG, Park KH. 2008. Sulfonate chalcone as new class voltage-dependent K + channel blocker. Bioorg Med Chem Lett 18 137-140. 

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