PD173212

SKU: orb1706835

Description

PD 173212 is a selective N-type voltage-gated calcium channel (Cav2.2) blocker. In vivo, it dose-dependently attenuates DNBS-induced visceral pain in mice following intraperitoneal administration, supporting its research use in neuropathic pain and visceral hypersensitivity studies.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 217171-01-2
• MW: 599.85
• Purity: 99.84% (May vary between batches)
• Formula: C₃₈H₅₃N₃O₃
• SMILES: CC(C)C[C@H](N(C)Cc1ccc(cc1)C(C)(C)C)C(=O)N[C@@H](Cc1ccc(OCc2ccccc2)cc1)C(=O)NC(C)(C)C
• Target: Calcium Channel
• Solubility: DMSO:90 mg/mL (150.04 mM);10% DMSO+90% Corn Oil:3.3 mg/mL (5.5 mM)

Bioactivity

• Target IC50:
  VSCC:36 nM
• In Vivo:
  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. In the audiogenic seizure model, PD173212 (30 mg/kg, i.v.) displays moderate efficacy in preventing tonic seizures.
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• In Vitro:
  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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

N-type Ca2+ channel, PD173212, PD-173212, PD 173212, Calcium Channel, CalciumChannel, VSCC

Compound Identifiers

PubChem CID

9916734