Overview

Cat #: L-230

Alternative Name Ativan^®, Temesta, O-Chloroxazepam, O-Chlorooxazepam, Almazine

Lyophilized Powder yes

Source Synthetic

MW: 321.16

Purity: >99%

Effective concentration 1 nM – 10 µM.

Structure

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

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.

Our bioassay

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

Spyker, D.A. et al. (2015) Pharmacol. Res. Perspect. 3, 6.
Pomara, N. et al. (2015) Prog. Neuropsychopharmacol. Biol. Psychiatry. 56, 35.
Nohria, V. and Giller, E. (2007) Neurotherapeutics 4, 102.
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 GABA_A receptor is considered to be a major target of antiseizure drugs³.

Target GABA(A) receptors

Lyophilized Powder

Certificate of Analysis

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

Order Summary

Lorazepam

Overview

Applications

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Specifications

Scientific Background

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