Date published: 2025-12-24

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GABAA Rα5 Inhibitors

GABAA receptors are a class of neurotransmitter receptors found in the central nervous system that play a pivotal role in inhibitory neurotransmission. These receptors are ion channels composed of five subunits, and various subunit combinations exist within the GABAA receptor family. The GABAA Rα5 inhibitors refer to a specific class of compounds that target and modulate the activity of the GABAA receptors containing the α5 subunit. These inhibitors exert their effects by binding to the α5 subunit, leading to changes in receptor function.

The α5 subunit is one of the several subunits that can combine to form functional GABAA receptors. When GABAA receptors incorporate the α5 subunit, they tend to be located predominantly in specific regions of the brain, such as the hippocampus. This subunit's involvement in receptor assembly and localization makes it an attractive target for drug development, and inhibitors specifically designed for GABAA Rα5 subunits can alter the receptor's activity. By inhibiting the α5 subunit, these compounds can modulate the functioning of GABAA receptors in a highly selective manner, leading to altered inhibitory neurotransmission and influencing neural signaling processes in the brain. Understanding the pharmacological properties of GABAA Rα5 inhibitors is crucial for elucidating their impact on neural circuits and neurotransmission, which may have implications for research into various neurological and neuropsychiatric conditions.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Flumazenil (Ro 15-1788)

78755-81-4sc-200161
sc-200161A
25 mg
100 mg
$108.00
$363.00
10
(1)

Flumazenil is a benzodiazepine antagonist which can bind to GABAA receptors and may affect the expression of its various subunits, including alpha 5.

Picrotoxin

124-87-8sc-202765
sc-202765A
sc-202765B
1 g
5 g
25 g
$66.00
$280.00
$1300.00
11
(3)

Picrotoxin is a noncompetitive antagonist of GABAA receptors. It binds irreversibly to the receptor chloride channels and could influence their subunit composition.

(+)-Bicuculline

485-49-4sc-202498
sc-202498A
50 mg
250 mg
$80.00
$275.00
(1)

Bicuculline is a competitive antagonist of GABA and blocks GABAA receptors, potentially altering the expression of its subunits.

THIP hydrochloride

64603-91-4sc-204342
50 mg
$152.00
2
(0)

THIP is a GABA agonist with selectivity for delta-containing GABAA receptors but might also affect alpha 5-containing receptor expression through complex interactions.

Tetracaine

94-24-6sc-255645
sc-255645A
sc-255645B
sc-255645C
sc-255645D
sc-255645E
5 g
25 g
100 g
500 g
1 kg
5 kg
$66.00
$309.00
$500.00
$1000.00
$1503.00
$5000.00
(0)

Tetracaine is a local anesthetic that inhibits sodium channels, but also could interact with GABA receptors, influencing their subunit expression.