Overview
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).
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.
