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Tertiapin Inhibitor for inward-rectifier K+ channels  

[Novel high-affinity inhibitor for inward-rectifier K⁺ channels]

Inward-rectifier K⁺ channels accomplish many important and diversified biological roles. Thus far, there are no high-affinity inhibitors that directly target any inward-rectifier K⁺ channels.

Only Lq2, scorpion toxin, blocks the ROMK1 inward-rectifier K⁺ channel, but the affinity is rather low (Kd = 0.4 mM) [Biochemistry, 36, 6936 (1997)].

Recently, a novel high-affinity inhibitor, Tertiapin has reported [Biochemistry, 37, 13291 (1998)]. This peptide blocks a G protein-gated channel (GIRK1/4) and the ROMK1 channel with nanomolar affinity.

About selectivity, tertiapin is insensitive to IRK1-channel, a closely related channel to GIRK1/4 and the ROMK1. Tertiapin will be a very useful tool for studying the physiological and the structure-function relationship of these channels.

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