GABAA Rα3 Inhibitors
GABAA Rα3 inhibitors are chemicals that either directly antagonize the GABAA Rα3 subunit or modulate the signaling pathways and cellular processes that indirectly affect its function. This class of inhibitors includes both competitive and non-competitive antagonists that act on different sites of the GABAA receptor, as well as compounds that indirectly influence the receptor's activity through various neuronal mechanisms. Direct inhibitors like Picrotoxin and Bicuculline act by binding to specific sites on the GABAA receptor and blocking its function. Picrotoxin blocks the chloride channel associated with the receptor, while Bicuculline competes with GABA for binding to the receptor. Other direct inhibitors, such as Flumazenil and FG-7142, modulate the receptor's activity through the benzodiazepine site, influencing the receptor dynamics and its inhibitory neurotransmission.
Indirect inhibitors, on the other hand, affect GABAA Rα3 by altering the overall balance of excitatory and inhibitory neurotransmission in the brain. Compounds like Tertiapin-Q, Penicillin, Zinc Sulfate, Strychnine, and Thujone influence GABAA receptors or related inhibitory pathways. For example, Tertiapin-Q's action on GIRK channels and Penicillin's interference with GABA binding lead to changes in neuronal excitability, which can indirectly modulate GABAA Rα3 function. PTX, Dihydro-β-erythroidine, and Caffeine, through their respective actions on phosphodiesterases, nicotinic acetylcholine receptors, and adenosine receptors, also contribute to the indirect modulation of GABAA Rα3. In summary, GABAA Rα3 inhibitors encompass a diverse range of chemicals that act through various mechanisms to inhibit or modulate the function of the GABAA Rα3 subunit. These inhibitors play a crucial role in influencing inhibitory neurotransmission in the central nervous system, affecting the balance between excitation and inhibition through both direct antagonism of the receptor and indirect modulation of related neuronal pathways.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
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 receptor's chloride channel and blocks it, inhibiting the flow of chloride ions. This action directly antagonizes the inhibitory effect of GABA on neurons. For the GABAA Rα3 subunit, Picrotoxin's binding can hinder its normal function, leading to a reduction in the inhibitory neurotransmission that GABAA receptors typically mediate. | ||||||
(+)-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 directly inhibits the function of the GABAA Rα3 subunit, thereby reducing the inhibitory effect of GABA on neurons. | ||||||
Flumazenil (Ro 15-1788) | 78755-81-4 | sc-200161 sc-200161A | 25 mg 100 mg | $108.00 $363.00 | 10 | |
Flumazenil is a competitive antagonist of the benzodiazepine site on GABAA receptors. While its primary action is to antagonize the effects of benzodiazepines, it can also modulate the receptor's activity. Flumazenil's binding can influence the functioning of the GABAA Rα3 subunit, leading to altered receptor dynamics and potentially reduced inhibitory neurotransmission. | ||||||
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 | |
Penicillin, at high concentrations, acts as a GABAA receptor antagonist. It can interfere with GABA binding and inhibit the receptor's function, including the GABAA Rα3 subunit. This effect can reduce the inhibitory action of GABAA receptors in the central nervous system. | ||||||
Zinc | 7440-66-6 | sc-213177 | 100 g | $47.00 | ||
Zinc ions can modulate GABAA receptor activity. Zinc binds to a specific site on the receptor, distinct from the GABA binding site, and can inhibit its function. This action can affect the GABAA Rα3 subunit, leading to a decrease in the receptor's inhibitory effect on neuronal signaling. | ||||||
Pentoxifylline | 6493-05-6 | sc-203184 | 1 g | $20.00 | 3 | |
PTX is a phosphodiesterase inhibitor that raises intracellular cAMP levels. Elevated cAMP can lead to changes in neuronal signaling pathways, potentially affecting GABAA receptor function, including the GABAA Rα3 subunit. This indirect influence can modulate the receptor's inhibitory role in the central nervous system. | ||||||
Caffeine | 58-08-2 | sc-202514 sc-202514A sc-202514B sc-202514C sc-202514D | 50 g 100 g 250 g 1 kg 5 kg | $32.00 $66.00 $95.00 $188.00 $760.00 | 13 | |
Caffeine is an adenosine receptor antagonist and can influence neuronal excitability and neurotransmission. By antagonizing adenosine receptors, caffeine can indirectly modulate the balance of excitatory and inhibitory signals in the brain, potentially affecting the function of GABAA Rα3 subunits. | ||||||