Date published: 2026-4-1

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GABAC Rρ2 Inhibitors

GABAC Rρ2 inhibitors belong to a specific chemical class that targets the GABAC receptors in the central nervous system. These receptors are part of the gamma-aminobutyric acid (GABA) receptor family, which plays a crucial role in regulating neuronal activity by mediating inhibitory neurotransmission. The GABAC receptors are distinct from the more well-known GABAA receptors, and they consist of ρ (rho) subunits, with the ρ2 subunit being the primary target for these inhibitors. GABAC Rρ2 inhibitors exert their effects by binding selectively to the ρ2 subunits, modulating their function, and thus altering the neuronal response to GABA. By doing so, these inhibitors can influence neuronal excitability and synaptic transmission, which may have implications for various neurological processes.

It is essential to note that while these compounds are termed inhibitors, their role is not necessarily to block or suppress the receptor's activity entirely. Instead, they may exhibit different levels of modulation, leading to diverse effects on neuronal signaling. This specificity in targeting the ρ2 subunit sets them apart from other GABAergic drugs that mainly act on GABAA receptors. Given the intricate role of GABAergic signaling in the central nervous system, GABAC Rρ2 inhibitors have garnered considerable interest in research. Scientists continue to explore their potential applications, though it is essential to differentiate their specific effects from those of other GABAergic agents and understand their distinct mechanisms of action.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

MPEP hydrochloride

96206-92-7sc-279454A
sc-279454
10 mg
50 mg
$136.00
$520.00
(0)

MPEP is an allosteric GABAC Rρ2 receptor antagonist that also has some affinity for mGlu5 receptors.

Gabazine

105538-73-6sc-211552
10 mg
$714.00
3
(0)

Gabazine is an antagonist of GABAA receptors, but it has some affinity for GABAC receptors containing the ρ2 subunit.

6-Cyano-7-nitroquinoxaline-2,3-dione

115066-14-3sc-505104
10 mg
$208.00
2
(0)

Although primarily known as an AMPA/kainate glutamate receptor antagonist, CNQX has been found to inhibit GABAC receptors in some studies.

(+)-Bicuculline

485-49-4sc-202498
sc-202498A
50 mg
250 mg
$82.00
$281.00
(1)

Bicuculline is a well-known competitive antagonist of GABAA receptors, but it can also inhibit GABAC receptors at higher concentrations.