Overview
- Hu, L.Y. et al. (1999) Bioorg. Med. Chem. Lett. 9, 2151.
Alomone Labs PD 173212 blocks N-type Ca2+ currents in Xenopus oocytes.A. Time course of N-type channel (CaV2.2+α2δ1+β1a) activity before and during applications of 10 μM PD 173212 (#P-105) (green) and upon wash. Holding potential was -100 mV and currents were elicited every 10 seconds by 100 ms ramp to +60 mV. B. Superimposed example current traces (plotted against the corresponding ramp voltage) before and during application of 10 μM PD 173212 in green (taken from the experiment described in A).
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 neurons1.
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 technique2. PD 173212 blocks also other CaV channels but to a lesser extent and only at higher concentrations2. In vivo, it prevents tonic seizures in the audiogenic seizure model.
