SML3009

Indiplon

≥98% (HPLC)

• Synonym(e): CL 285,489, CL 285489, CL-285,489, CL-285489, CL285,489, CL285489, N-Methyl-N-(3-(3-(thiophene-2-carbonyl)pyrazolo[1,5-a]pyrimidin-7-yl)phenyl)acetamide, N-Methyl-N-[3-[3-(2-thienylcarbonyl)pyrazolo[1,5-a]pyrimidin-7-yl]phenyl]acetamide, NBI 34060, NBI-34060, NBI34060
• Empirische Formel (Hill-System): C₂₀H₁₆N₄O₂S
• CAS-Nummer: 325715-02-4
• Molekulargewicht: 376.43
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD09264193
• Assay: ≥98% (HPLC)
• Form: powder

Eigenschaften

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 2-8°C
• SMILES string: [s]1c(ccc1)C(=O)c2c3[n](nc2)C(=CC=N3)c4cc(ccc4)N(C)C(=O)C
• InChI: 1S/C20H16N4O2S/c1-13(25)23(2)15-6-3-5-14(11-15)17-8-9-21-20-16(12-22-24(17)20)19(26)18-7-4-10-27-18/h3-12H,1-2H3
• InChI key: CBIAWPMZSFFRGN-UHFFFAOYSA-N

Beschreibung

Biochem/physiol Actions

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.

Orally active, high-affinity GABA(A) receptor positive allosteric modulator (PAM) with in vivo sedative-hypnotic efficacy.

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable