Indiplon

C₂₀H₁₆N₄O₂S

376.43

MFCD09264193

Indiplon (NBI 34060) is an orally active, high-affinity GABAA receptor positive allosteric modulator (PAM) with preferential labeling of alpha1 subunits-containing receptors (rat cerebellar/cerebral cortex membranes binding KD = 1.01/0.45 nM). Indiplon potentiates GABA-induced chloride conductance of cultured rat cortical neurons (EC50 = 11.6 nM vs 152 nM/630 nM) and exhibits sedative efficacy in mice (ED50 = 1 mg/kg/passive avoidance & 2.7 mg/kg/locomotor activity inhibition po.) and rats (ED50 = 2.5 mg/kg/locomotor activity inhibition & 3 mg/kg/vigilance impairment po.) in vivo. Indiplon shows greater affinity, in vitor and in vivo potency than zaleplon and zolpidem.

100

≥98% (HPLC)

powder

white to beige

DMSO: 2 mg/mL, clear

2-8℃

11 - Combustible Solids

WGK 3