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Valium®, Diazemuls, Relanium, Ansiolisina, Apaurin, Ro 5-2807

An Agonist of GABA(A) Receptors

Cat #: D-215
Alternative Name Valium®, Diazemuls, Relanium, Ansiolisina, Apaurin, Ro 5-2807
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 284.74
    Purity: >98%
    Effective concentration 1 nM – 10 µM.
    Chemical name 7-chloro-1-methyl-5-phenyl-3H-1,4-benzodiazepin-2-one.
    Molecular formula C16H​13ClN2O.
    CAS No.: 439-14-5
    PubChem CID 3016
    Activity Diazepam is a positive allosteric modulator of GABAA receptors at the benzodiazepine site, shown to increase single channel conductance1. Potentiates GABA induced chloride current (EC50=10-8 M in frog pituitary melanotrophs)2. Displaces [3H]Flunitrazepam from synaptosomal membranes of rat cerebellum, striatum and spinal cord (pIC50 > 7.5)3.
    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 to protect from contact with air.
    Solubility Up to 100 mM in DMSO, up to 25 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 Diazepam inhibits specific binding of Flunitrazepam to rat brain GABA(A) receptors.
      Alomone Labs Diazepam inhibits specific binding of Flunitrazepam to rat brain GABA(A) receptors.
      Percent inhibition of the specific binding of 1 nM [3H]Flunitrazepam to membranes from whole rat brain (except cerebellum) was plotted against concentrations of Diazepam (#D-215), (green circles) and of Diazepam standard (black squares) and used to calculate IC50 and Ki values for Diazepam (IC50 ≈ 36 nM, and Ki ≈ 29 nM).
    References - Scientific background
    1. Eghbali, M. et al. (1997) Nature 388, 71.
    2. Louiset, E. et al. (2000) Endocrinology 141, 1083.
    3. Massotti, M. et al. (1991) J. Pharmacol. Exp. Ther256, 1154.
    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.

    Diazepam (also known as Valium, Relanium) is a synthetic positive allosteric modulator of the GABA(A) receptor at the benzodiazepine (BZD). Diazepam inhibits specific binding of Flunitrazepam to rat brain GABA(A) receptors with an IC50 = 36 nM and a Ki = 29 nM. Diazepam potentiates GABA induced chloride currents with an EC50 = 10-8 in from pituitary melanotrophs2.

    In the cerebellum, cortex and olfactory bulb membranes the density of high affinity binding sites for Diazepam is similar to those of other benzodiazepines, however in the striatum Diazepam has a substantially higher density of binding sites than clonazepam or Zolpidem3.

    Diazepam, like other BZD, is used as an anxiolytic and hypnotic drug. Notably, it can cause adverse effects especially in the elderly. Some of these adverse effects, such as impaired motor and cognitive function, can be improved after discontinuation of the drug. Carbamazepine has been found useful for assisting discontinuation of long-term BDZ use4.

    Target GABA(A) receptors
    Last update: 25/04/2021

    Diazepam (#D-215) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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