NS11394

SKU: orb1223536

Description

A potent, subtype-selective, orally available GABAA receptor positive modulator with Ki of 0.4, 0.8, 0.5 and 0.1 nM for α1, α2, α3 and α5 subunits together with β3γ2; displays 600 to 2000-fold over GABAA-α4 or GABAA-α6 containing receptors; exhibits in vivo anxiolytic efficacy, attenuates spontaneous nociceptive behaviors in response to hindpaw injection of formalin and capsaicin in rats.

Key Properties

• CAS Number: 951650-22-9
• MW: 353.4165
• Purity: >98% (HPLC)
• Formula: C₂₃H₁₉N₃O
• SMILES: N#CC1=CC=CC=C1C2=CC=CC(N3C4=CC=C(C(C)(O)C)C=C4N=C3)=C2
• Target: GAT
• Solubility: DMSO: ≥ 43 mg/mL

Bioactivity

• In Vivo:
  NS11394 (1-120 mg/kg) selectively attenuates injury-induced nociceptive behaviors in the formalin test. NS11394 (1–10 mg/kg) markedly attenuates the deficit in hindpaw weight bearing [F(4, 61) = 7.569, p < 0.001] in CFA rats. Animal model: Adult male Sprague-Dawley rats. Dosage: 1-120 mg/kg. Administration: Orally. Result: Significantly attenuated motor function compared with corresponding vehicle responses. Significantly reduced flinching behavior during interphase [F(3, 30) = 4.139, p < 0.05] and the second phase [F(3, 30) = 11.033, p < 0.001] of the formalin test compared with vehicle treatment indicative of a selective effect on injury-induced nociceptive transmission.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NS-11394

Quick Database Links

Gene Symbol

GAT