GABAA Rα4 Inhibitors
The chemical class of GABAA Rα4 inhibitors is characterized by a diverse range of compounds that modulate the activity of the GABAA receptor, including the Rα4 subunit. These inhibitors act through various mechanisms, such as competitive antagonism at the GABA binding site, non-competitive antagonism at the chloride channel, and allosteric modulation at different receptor sites. Compounds like Bicuculline and Gabazine are competitive antagonists that disrupt GABA from activating the receptor, thereby inhibiting its function. Picrotoxin and TBPS are examples of non-competitive antagonists that bind to the chloride channel associated with the receptor, blocking ion flow and inhibiting receptor activity. Other compounds, like Flumazenil, FG-7142, and β-Carboline, function as inverse agonists or modulators at the benzodiazepine site, influencing the receptor's response to GABA and its overall activity.
These inhibitors not only act directly on the receptor but also can influence the receptor indirectly. For example, Tertiapin-Q's action on GIRK channels and Zinc's modulation of GABAA receptors highlight the indirect pathways through which the GABAA Rα4 subunit's activity can be influenced. These diverse mechanisms of action reflect the intricate regulation of inhibitory neurotransmission in the central nervous system and underscore the involvement of these compounds in influencing the function of GABAA receptors, including those containing the Rα4 subunit.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
(+)-Bicuculline | 485-49-4 | sc-202498 sc-202498A | 50 mg 250 mg | $80.00 $275.00 | ||
Bicuculline is a competitive antagonist of GABAA receptors. It binds to the GABA binding site on the receptor, preventing GABA from activating the receptor. This blockade can affect all subtypes of GABAA receptors, potentially including those with the Rα4 subunit. | ||||||
Picrotoxin | 124-87-8 | sc-202765 sc-202765A sc-202765B | 1 g 5 g 25 g | $66.00 $280.00 $1300.00 | 11 | |
Picrotoxin is a non-competitive antagonist of GABAA receptors. It binds to the chloride channel associated with the receptor, blocking ion flow and inhibiting receptor activity. This action can influence all GABAA receptor subtypes, potentially including those with Rα4 subunits. | ||||||
Flumazenil (Ro 15-1788) | 78755-81-4 | sc-200161 sc-200161A | 25 mg 100 mg | $108.00 $363.00 | 10 | |
Flumazenil is a benzodiazepine antagonist that binds to the benzodiazepine site on GABAA receptors. While it primarily antagonizes the effects of benzodiazepines, it can also modulate GABAA receptor activity, potentially affecting subunits including Rα4. | ||||||
Gabazine | 105538-73-6 | sc-211552 | 10 mg | $714.00 | 3 | |
Gabazine, also known as SR-95531, is a competitive antagonist of GABAA receptors. It binds to the GABA binding site, preventing GABA from activating the receptor. This action can affect various GABAA receptor subtypes, including those with the Rα4 subunit. | ||||||
Penicillin G sodium salt | 69-57-8 | sc-257971 sc-257971A sc-257971B sc-257971C sc-257971D | 1 mg 10 mg 1 g 5 g 100 g | $25.00 $36.00 $46.00 $168.00 $260.00 | 1 | |
At high concentrations, Penicillin acts as a non-specific antagonist of GABAA receptors. It can interfere with GABA binding and inhibit receptor function, which may include effects on receptors containing the Rα4 subunit. | ||||||
Zinc | 7440-66-6 | sc-213177 | 100 g | $47.00 | ||
Zinc ions can modulate GABAA receptor activity by binding to a site distinct from the GABA binding site, potentially inhibiting receptors including those with Rα4 subunits. | ||||||