A positive allosteric modulator of the GABAA receptor
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Indiplon

Item No. 11638

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-methyl-N-[3-[3-(2-thienylcarbonyl)pyrazolo[1,5-a]pyrimidin-7-yl]phenyl]-acetamide
CAS Number
325715-02-4
Synonyms
  • NBI 34060
Molecular Formula
C20H16N4O2S
Formula Weight
376.4
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 14 mg/ml
λmax
230, 312, 347 nm
SMILES
O=C(C1=CC=CS1)C2=C3N(N=C2)C(C4=CC=CC(N(C)C(C)=O)=C4)=CC=N3
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    10 mg

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    50 mg

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    Product Description

    Indiplon is a pyrazolopyrimidine that acts as a high-affinity positive allosteric modulator of the GABAA receptor, potentiating GABA-activated chloride currents in a dose-dependent and reversible manner.1,2 Indiplon is selective for α1 subunits (EC50 = 2.6 nM) as compared with α2, α3, or α5 (EC50 = 24, 60, and 77 nM).1,2 Through this action, indiplon has sedative and hypnotic effects that can improve sleep onset, maintenance, and duration.3,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Petroski, R.E., Pomeroy, J.E., Das, R., et al. Indiplon is a high-affinity positive allosteric modulator with selectivity for α1 subunit-containing GABAA receptors. J. Pharmacol. Exp. Ther. 317(1), 369-377 (2006).

    2. Sullivan, S.K., Petroski, R.E., Verge, G., et al. Characterization of the interaction of indiplon, a novel pyrazolopyrimidine sedative-hypnotic, with the GABAA receptor. J. Pharmacol. Exp. Ther. 311(2), 537-546 (2004).

    3. Foster, A.C., Pelleymounter, M.A., Cullen, M.J., et al. In vivo pharmacological characterization of indiplon, a novel pyrazolopyrimidine sedative-hypnotic. J. Pharmacol. Exp. Ther. 311(2), 547-559 (2004).

    4. Scharf, M.B., Black, J., Hull, S., et al. Long-term nightly treatment with indiplon in adults with primary insomnia: Results of a double-blind, placebo-controlled, 3-month study. Sleep 30(6), 743-752 (2007).