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.
      • 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.
      • Sanna, E. et al. (2003) J. Neurosci. 23, 11711.
      • 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.
      • 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
      • 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: 21/07/2019

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

    For research purposes only, not for human use