BUY PD 173212

PD 173212. A Novel N-type Cav Channel Blocker.

Native voltage-gated Ca²⁺ channels (VGCC, Ca_V) 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 alpha1 subunit. The subunit Ca_V2.2 (alpha1B) forms N-type Ca²⁺ channels, which are located primarily on presynaptic nerve terminals of central and peripheral neurons.
PD 173212 is a dipeptidyl-amine that acts as a N-type Ca_V 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 Ca_V channels but to a lesser extent and only at higher concentrations.in vivo, it prevents tonic seizures in the audiogenic seizure model.

Ion Channel Modulator; Voltage - Gated Ca²⁺ Channel Blockers