GlyR α2 Inhibitors
GlyR α2 inhibitors constitute a diverse class of compounds that exert their modulatory effects on the glycine receptor (GlyR) α2, a ligand-gated ion channel crucial for inhibitory neurotransmission. Strychnine and picrotoxin exemplify direct inhibitors, binding to GlyR α2 and impeding its function. Sarcosine and SLC6A9 inhibitors indirectly modulate GlyR α2 by altering glycine availability, highlighting the intricate regulatory network involving glycine transporters. Ethanol, acting through GABAergic pathways, showcases indirect modulation, emphasizing the cross-talk between neurotransmitter systems. Positive allosteric modulators (PAMs) like NS-3763 and ivermectin enhance GlyR α2 activity, exemplifying a nuanced approach to potentiate inhibitory neurotransmission. GSK1016790A, through GPR40 activation, demonstrates a distinct indirect modulation, emphasizing the broader signaling cascades influencing GlyR α2. Zinc ions, exhibiting dual modulation, underscore the complex interplay of allosteric sites within GlyR α2. Amiloride, targeting ASIC1a, showcases the interconnectedness of ion channels in influencing GlyR α2-mediated inhibition.
Selective GlyT1 inhibitors like SSR504734 and those targeting GlyT2, such as dihydrokainic acid, offer indirect strategies by modifying glycine reuptake, emphasizing the significance of transporters in regulating GlyR α2 activity. This chemical class presents a comprehensive toolkit for dissecting and manipulating glycinergic neurotransmission, offering valuable insights into the intricate regulatory mechanisms governing inhibitory signaling mediated by GlyR α2 in diverse physiological contexts.
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| 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, a bicyclic sesquiterpene, serves as a GlyR α2 antagonist by binding to its ion channel and impeding chloride influx. This interference disrupts the inhibitory postsynaptic potentials mediated by GlyR α2, culminating in hyperexcitability and convulsive activity. | ||||||
Ivermectin | 70288-86-7 | sc-203609 sc-203609A | 100 mg 1 g | $56.00 $75.00 | 2 | |
Ivermectin, an antiparasitic agent in research, exhibits positive allosteric modulation of GlyR α2. By binding to a distinct allosteric site, Ivermectin augments the response to glycine, enhancing GlyR α2-mediated inhibition. This modulation can contribute to its neuroprotective effects observed in various experimental settings. | ||||||
GSK1016790A | 942206-85-1 | sc-255193 | 10 mg | $260.00 | 6 | |
GSK1016790A, a potent and selective agonist of GPR40, indirectly modulates GlyR α2. By activating GPR40, it initiates downstream signaling cascades that influence glycine release and availability, consequently impacting GlyR α2 activity and modulating inhibitory neurotransmission. | ||||||
Zinc | 7440-66-6 | sc-213177 | 100 g | $47.00 | ||
Zinc ions (Zn2+), essential trace elements, exhibit dual modulation of GlyR α2. While acting as a negative allosteric modulator (NAM) at high concentrations, Zn2+ at lower concentrations positively modulates GlyR α2 by enhancing glycine binding. This bimodal modulation provides intricate control over GlyR α2 activity in diverse cellular contexts. | ||||||
Amiloride | 2609-46-3 | sc-337527 | 1 g | $290.00 | 7 | |
Amiloride, a diuretic agent in research, indirectly influences GlyR α2 by inhibiting the acid-sensing ion channel (ASIC) 1a. This inhibition reduces excitotoxicity by suppressing ASIC1a-mediated currents, subsequently influencing glycine release and GlyR α2-mediated inhibition, highlighting the intricate interplay between different ion channels in neuronal signaling. | ||||||
Dihydrokainic acid | 52497-36-6 | sc-200442B sc-200442 sc-200442A | 1 mg 10 mg 50 mg | $108.00 $296.00 $896.00 | 3 | |
Dihydrokainic acid, a competitive inhibitor of the glycine transporter GlyT2, indirectly influences GlyR α2. By targeting GlyT2, it modulates the availability of glycine for GlyR α2 activation, offering a unique approach to fine-tune glycinergic neurotransmission and control the inhibitory tone mediated by GlyR α2. | ||||||