GABA(A) Receptor Antagonist Explorer Kit

A Screening Package of GABA(A) Receptor Antagonists Economically Priced
  • New
  • Bioassay Tested
Cat #: EK-420
Sizes: 11 Vials

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Last update: 17/07/2019

GABA(A) Receptor Antagonist Explorer Kit (#EK-420) contains GABA(A) receptor antagonists, ideal for screening purposes.

For research purposes only, not for human use
Compounds
Product NameCat #Size
(-)-Bicuculline methiodide
B-136 1 x 5 mg
(-)-Bicuculline methochloride
B-137 1 x 5 mg
Etbicyphat
E-175 1 x 50 mg
GABA(A)-Compound 1b
CMG-004 1 x 5 mg
Gabazine
G-215 1 x 5 mg
Gabazine hydrobromide
G-216 1 x 5 mg
Oroxylin A
O-160 1 x 5 mg
Picrotoxin
P-325 1 x 500 mg
Tracazolate hydrochloride
T-230 1 x 5 mg
U 93631
U-120 1 x 5 mg
Waglerin-1
STW-001 1 x 1 mg
References
    • GABA (γ-aminobutyric acid) is the major inhibitory neurotransmitter in the brain. Its production, release, reuptake, and metabolism all occur in the nervous system1.

      The GABA transmitter interacts with two major types of receptors: ionotropic GABAAreceptors (GABAAR) and metabotropic receptors (GABABR). GABAARs belong to the ligand-gated ion channel superfamily2. GABA inhibits the activity of signal-receiving neurons by interacting with the GABAA receptor on these cells3. Binding of GABA to its GABAA receptor results in conformational changes that open a Clchannel, producing an increase in membrane conductance that results in inhibition of neural activity2.

      GABAARs are heteropentamers, in which all five subunits contribute to pore formation.  To date, eight subunit isoforms have been cloned: α, β, γ, δ, ε, π, θ, and ρ1. Six α subunit isoforms have been found to exist in mammals (α1-α6). In most cases, native GABAA receptors consists of 2α, 2β, and 1δ subunits. The α subunit is the most common and is expressed ubiquitously. It determines the affinities of GABAARs for allosteric ligands.

      Each subtype has a unique regional expression in the brain, and individual neurons often express multiple subtypes.4 The α1 subunit is highly expressed in adulthood while the α2 subunit is highly expressed very early in rat brain development. Failure to complete the normal transition between the α-subunits that are highly expressed in early development (α2, α3, and α5) and those expressed in adulthood (α1) is suggested to play a major role in the development of temporal lobe epilepsy5.

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