PD 173212 is a blocker that blocks N-type voltage sensitive calcium channel (Cav2.2). PD173212 (0.0017-1.7 μmol/kg, Intraperitoneal Injection.) dose-dependently reduced DNBS-induced visceral hypersensitivity in mice.

VSCC:36 nM

PD 173212 blocked recombinant B-class (N-type) Ca+2 channels with a IC50 of 74 nM (N = 2), and blocked Na+ channels by 8% at 1 μM (N = 4), and blocked K+ channels by 10% at 1 μM (N = 4) in superior cervical ganglion neurons. PD 173212 effectively blocks recombinant B-class (N-type) calcium channel currents 78±7.8% (IC50: 74 nM), by whole-cell voltage-clamp techniques[1].

This study evaluated the effect of acute administration of the selective N-type Cav2.2 blocker PD17321238 in their visceral pain model. The test (VMR assessment) was performed on day 14 after DNBS injection. PD173212 (0.0017-1.7 μmol·kg−1, i.p.) dose-dependently reduced the visceral hypersensitivity induced by DNBS. The compound started to be effective at a dose of 0.017 μmol·kg−1 and completely relieved abdominal pain when administered at a ten-fold higher dose[2]. In the audiogenic seizure model, PD173212 (30 mg/kg, i.v.) displays moderate efficacy in preventing tonic seizures[1].