I was slightly bored and wondered if anyone might be interested in the structure itself.Here you go, I think it’s correct. And just for (sad) kicks, the 3D structure, although it’s probably wildly inaccurate, I used a very basic modeller package. Interestingly the piperidine sits in a boat conformation…probably not *that *interesting.
Not quite. The primary accent is on the second syllable - pie PERR ah deen. The audio pronunciation confirms that. At least, for the US pronunciation.
And it smells gross, too.
Oddly enough you linked to the exact paper I did my presentation on.
As for clinical significance, the HERG channel controls how potassium enters back into the heart cells. Several other drugs exist that block this channel, which in turn means the cell takes longer to repolarize. If a cell isn’t repolarized, then it can’t beat when a depolarization signal is propogated to it. So you can end up having some cells depolarized and some cells not, but then the do depolarize later when they shouldn’t, a condition known as early afterdepolarization. If it gets severe enough, then it can lead to arrhythmias in the heart and possible death.
This is pretty much the first chemical ever found that activates the channel, so there’s a lot of potential to use it with these other drugs that have the side effect of blocking the channel to reduce the chance of an arrythmia.
Oh, and Andy, that looks pretty accurate. The actual structure printed in the paper is here.
