GABAA Rα2 Inhibitors
The class of GABAA Rα2 inhibitors comprises a diverse range of compounds that either directly or indirectly modulate the function of GABAA receptors containing the α2 subunit. These receptors play a crucial role in regulating neuronal excitability and inhibitory signaling in the central nervous system. Flumazenil, Bicuculline, and Picrotoxin are direct inhibitors acting at the GABAA receptor level. Flumazenil competitively antagonizes the benzodiazepine binding site, disrupting GABAergic transmission. Bicuculline competitively blocks the ion channel pore, stopping chloride ion influx and reducing inhibitory signaling. Picrotoxin acts as a non-competitive antagonist, interfering with the ion channel function of GABAA receptors. Gaboxadol and SR-95531 (Gabazine) modulate GABAA receptors containing the α2 subunit directly. Gaboxadol is a selective agonist activating extrasynaptic receptors, enhancing inhibitory signaling. Gabazine competitively antagonizes the GABA binding site, blocking inhibitory effects on receptors with the α2 subunit.
CGP 35348 indirectly influences the inhibitory tone by acting as a competitive antagonist at GABAB receptors, affecting presynaptic GABAergic transmission. TPMPA is a selective antagonist of GABAC receptors, which indirectly modulates overall inhibitory tone, including that regulated by GABAA receptors with the α2 subunit. 3-Mercaptopropionic acid indirectly affects GABAA receptors containing the α2 subunit by chelating zinc ions, modulating their function. Bilobalide, an indirect inhibitor, modulates GABAergic transmission, influencing inhibitory tone. Allopregnanolone and Ethanol are positive allosteric modulators, indirectly enhancing GABAergic transmission and influencing neuronal excitability. Ro15-4513 competitively antagonizes the benzodiazepine binding site, directly interfering with the modulation of GABAA receptors containing the α2 subunit. The diverse mechanisms of action exhibited by these inhibitors highlight the intricate regulation of GABAA receptors with the α2 subunit in neuronal circuits, offering valuable tools for understanding their roles in normal physiology and pathological conditions.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Flumazenil (Ro 15-1788) | 78755-81-4 | sc-200161 sc-200161A | 25 mg 100 mg | $110.00 $370.00 | 10 | |
Flumazenil is a competitive antagonist of the benzodiazepine binding site on the GABAA receptor α2 subunit. By binding to this site, it prevents the binding of endogenous ligands, such as GABA, thereby inhibiting the activation of the receptor. This direct inhibition leads to a reduction in the inhibitory signaling mediated by GABAA receptors containing the α2 subunit, influencing neuronal excitability. | ||||||
(+)-Bicuculline | 485-49-4 | sc-202498 sc-202498A | 50 mg 250 mg | $82.00 $281.00 | ||
Bicuculline is a competitive antagonist that blocks the ion channel pore of GABAA receptors, including those containing the α2 subunit. By inhibiting the influx of chloride ions through the receptor channel, bicuculline hinders the hyperpolarization induced by GABA binding. This leads to an increase in neuronal excitability due to the reduced inhibitory input mediated by GABAA receptors with the α2 subunit. | ||||||
Picrotoxin | 124-87-8 | sc-202765 sc-202765A sc-202765B | 1 g 5 g 25 g | $67.00 $286.00 $1326.00 | 11 | |
Picrotoxin acts as a non-competitive antagonist of GABAA receptors, including those with the α2 subunit. It binds to a site distinct from the GABA binding site and interferes with the ion channel function, preventing the normal inhibitory response to GABA. This direct inhibition disrupts the chloride ion flow through the channel, altering the inhibitory tone regulated by GABAA receptors containing the α2 subunit. | ||||||
Gabazine | 105538-73-6 | sc-211552 | 10 mg | $714.00 | 3 | |
Gabazine is a competitive antagonist at the GABA binding site on GABAA receptors, including those containing the α2 subunit. By binding to the same site as GABA, it blocks the inhibitory effects of the neurotransmitter. This direct inhibition disrupts the normal functioning of GABAA receptors with the α2 subunit, leading to altered neuronal excitability. | ||||||
3-Mercaptopropionic acid | 107-96-0 | sc-256523 sc-256523A | 5 g 100 g | $38.00 $40.00 | ||
3-Mercaptopropionic acid is an indirect inhibitor that influences GABAA receptors containing the α2 subunit through modulation of endogenous zinc levels. It chelates zinc ions, which can modulate GABAergic transmission. By affecting the zinc-sensitive site on GABAA receptors, this compound indirectly modulates the receptor function and alters the inhibitory signaling mediated by GABAA receptors with the α2 subunit. | ||||||
Bilobalide | 33570-04-6 | sc-201061 sc-201061B sc-201061A sc-201061C | 10 mg 25 mg 50 mg 100 mg | $82.00 $163.00 $296.00 $444.00 | 3 | |
Bilobalide, found in Ginkgo biloba, is an indirect inhibitor that affects GABAA receptors containing the α2 subunit through modulation of GABAergic transmission. While its precise mechanism is not fully elucidated, bilobalide has been shown to influence GABAergic neurotransmission, impacting neuronal excitability. This indirect modulation can alter the inhibitory tone regulated by GABAA receptors with the α2 subunit. | ||||||