PD 173212 is a dipeptidyl-amine that acts as a N-type CaV channels blocker. It is the most active small molecule for N-type calcium channel blockade as it inhibits this channel with an IC50 of 36 nM in IMR-32 cells, as measured by using fluorescent technique. PD 173212 blocks also other CaV channels but to a lesser extent and only at higher concentrations. in vivo, it prevents tonic seizures in the audiogenic seizure model.
产品描述
A Novel Blocker of N-type Cav Channels
产品形式
Native voltage-gated Ca2+ channels (VGCC, CaV) are pharmacologically classified into at least five different subclasses (L-, N-, P-, Q-, and R-type), the characteristics of which are determined by the pore-forming α1 subunit. The subunit CaV2.2 (α1B) forms N-type Ca2+ channels, which are located primarily on presynaptic nerve terminals of central and peripheral neurons.