Zaleplon

Sonata®, Zerene, CL-284846, Zalaplon
An Agonist of GABA(A) Receptors
    Cat #: Z-140
    Alternative Name Sonata®, Zerene, CL-284846, Zalaplon
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 305.34
    Purity: >98%
    Effective concentration 10 nM – 10 µM.
      • Zaleplon
    Chemical name N-[3-(Cyanopyrazolo[1,5-a]pyrimidin-7-yl)phenyl]-N-ethylacetamide.
    Molecular formula C17H15N5O.
    CAS No.: 151319-34-5.
    PubChem CID 5719
    Activity A non-benzodiazepine pyrazolopyrimidine agonist at the benzodiazepine site of the GABAA receptors. Potentiates GABA-induced chloride currents at sub-micromolar concentrations1. Displaces [3H]Flunitrazepam from rat cerebellum and spinal cord membranes with IC50 values of 167 nM and 2.38 µM, respectively2.
      • Sanna, E. et al. (2003) J. Neurosci. 23, 11711.
      • Noguchi, H. et al. (2002) Eur. J. Pharmacol. 434, 21.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored desiccated at 4°C.
    Protect from light.
    Solubility Up to 100 mM in DMSO. Centrifuge all products before reconstitution (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C. It is recommended to aliquot reconstituted product for storage.
      • Zaleplon
        Alomone Labs Zaleplon inhibits specific binding of Flunitrazepam to rat brain GABA(A) receptors.
        Percent inhibition of specific binding of 1 nM [3H]Flunitrazepam to membranes from whole rat brain (except cerebellum) was plotted against concentrations of Zaleplon (#Z-140), (green circles) and of Diazepam (assay standard, black squares) and used to calculate IC50 and Ki values for Zaleplon (IC50 ≈ 0.55 μM, and Ki ≈ 0.45 μM).
    References - Scientific background
      • The GABA(A) receptor is a ligand-gated ion channel and is the major type of receptor for the GABA inhibitory neurotransmitter in the central nervous system1.

        Zaleplon (also known as Sonata, Zerene) is a synthetic non benzodiazepine (BZD) pyrazolopyrimidine agonist at the BZD site of the GABA(A) receptor. Zaleplon potentiates GABA induced chloride currents at submicromolar concentrations2 and displaces Flunitrazepam from rat cerebellum and spinal cord membranes with IC50 values of 167 nM and 2.38 µM respectively3. Zaleplon is widely used for the treatment of insomnia and has been shown to improve sleep variables compared to placebo. Like most hypnotic drugs, Zaleplon can be used for problems of sleep initiation at the beginning of the night but its shorter half-life (1.05±0.13h) enables patients to take it later in the night without residual effects the next morning4. Zaleplon is rapidly absorbed after oral administration and has an absolute bioavailability of 30.6±10.2%5. The most common adverse effects attributed to Zaleplon are headache, pain, somnolence and rhinitis. There is not difference between Zaleplon and placebo treatment in CNS adverse events6.

    Target GABA(A) receptors
    Last update: 01/09/2019

    Zaleplon (#Z-140) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use