Lorazepam

Ativan®, Temesta, O-Chloroxazepam, O-Chlorooxazepam, Almazine
An Agonist of GABA(A) Receptors
    Cat #: L-230
    Alternative Name Ativan®, Temesta, O-Chloroxazepam, O-Chlorooxazepam, Almazine
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 321.16
    Purity: >99%
    Effective concentration 1 nM – 10 µM.
    Structure
    • Lorazepam
    Chemical name 7-chloro-5-(2-chlorophenyl)-3-hydroxy-1,3-dihydro-1,4-benzodiazepin-2-one.
    Molecular formula C15H10Cl2N2O2.
    CAS No.: 846-49-1.
    PubChem CID 3958
    Activity Lorazepam is a positive allosteric modulator of GABA(A) receptors at the benzodiazepine site. It potentiates GABA-induced chloride currents at sub-micromolar concentrations1. It displaces [3H]Flunitrazepam from GABA(A) receptors in rat cerebral cortex (IC50 = 4.8 nM)2.
    References-Activity
    1. Sanna, E. et al. (2003) J. Neurosci. 23, 11711.
    2. Möhler, H. et al. (1980) Proc. Natl. Acad. Sci. U. S. A. 77, 1666.
    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 at -20°C. Keep tightly sealed.
    Solubility Up to 100 mM in DMSO, up to 40 mM in ethanol. 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.
    Our bioassay
    • Lorazepam
      Alomone Labs Lorazepam 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 increasing concentrations of Lorazepam (#L-230). Full inhibition is achieved at over 1 µM.
    References - Scientific background
    1. Spyker, D.A. et al. (2015) Pharmacol. Res. Perspect. 3, 6.
    2. Pomara, N. et al. (2015) Prog. Neuropsychopharmacol. Biol. Psychiatry. 56, 35.
    3. Nohria, V. and Giller, E. (2007) Neurotherapeutics 4, 102.
    4. Möhler, H. et al. (1980) Proc. Natl. Acad. Sci. U. S. A. 77, 1666.
    Scientific background

    Lorazepam (also called Ativan), acts as a positive allosteric modulator of GABA(A) receptors at the benzodiazepine site. It is used to treat anxiety disorders and is a sedative and anticonvulsant drug. Lorazepam is one of the most common benzodiazepines used to control acute agitation and is commonly administered with antipsychotics1.

    Lorazepam has a better safety profile compared to other benzodiazepines2. The drug has IC50 values of 4.8 nM in rat cerebral cortex4.

    GABA(A) receptors are members of the Cys-loop superfamily of ligand-gated ion channels. They mediate GABA action, a major inhibitory neurotransmitter, through the central nervous system. The GABAA receptor is considered to be a major target of antiseizure drugs3.

    Target GABA(A) receptors
    Last update: 24/01/2020

    Lorazepam (#L-230) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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