The Cys-loop class of LGICs forms a superfamily of ionotropic receptors that includes two types of anion-permeable channels, which are represented by receptors for the neurotransmitters GABA (gamma-aminobutyric acid) and glycine, and allow negatively charged chloride ions to migrate through the cell membrane. Activation of these receptors in general leads to rapid inhibitory synaptic transmission[1].
Upon activation, the GABAA receptor selectively conducts Cl- through its pore, resulting in hyperpolarization of the neuron. This causes an inhibitory effect on neurotransmission by diminishing the chance of a successful action potential occurring. Mild inhibition of neuronal firing by drugs acting at the GABAA receptor causes a reduction of anxiety in the patient (an anxiolytic effect) while more pronounced inhibition induces general anesthesia[2].
As a consequence of its high affinity binding to its natural inhibitor, strychnine, the GlyR was the first nicotinicoid receptor isolated from mammalian nervous tissue. Structurally and functionally, the glycine receptor is most closely related to the GABAA receptor. GlyRs are primarily expressed in spinal cord, brain stem, caudal brain, and retina. In adult neurons, the inhibitory chloride influx upon glycine receptor activation stabilizes the resting potential of the cell, rendering them electrically quiescent. Reduced channel expression and/or reduced activity of mutants often result in channelopathies involving muscle tone regulation, such as human startle disease (hyperekplexia)[3].

[1] Novel animal-health drug targets from ligand-gated chloride channels. V. Raymond, D.B. Sattelle. Nat. Rev. Drug Discov. 2002, 1, 427-436.
[2] Structure, Function, and Modulation of GABAA Receptors. E. Sigel M.E. Steinmann. J. Biol. Chem. 2012, 287, 40224-40231.
[3] Structure and Function of the Glycine Receptor and Related Nicotinicoid Receptors. M. Cascio. J. Biol. Chem. 2004, 279, 19383-19386.

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Axon ID Name Description From price
1594 (+)-Pagoclone GABAA-α2 and GABAA-α3 agonist €135.00
2784 (R)-(-)-N-Desmethyl-PK 11195 Radioligand precursor of the benzodiazepine antagonist (R)-(-)-PK 11195 €150.00
2785 (R)-(-)-PK 11195 Benzodiazepine antagonist. €130.00
3698 AC-5216 Selective translocator protein (TSPO) ligand €90.00
3042 AZD6280 Selective, orally active, allosteric GABA-A α2/3 receptor modulator €125.00
3087 AZD7325 Potent, selective GABAA-α2 and GABAA-α3 modulator €90.00
1604 CP 615003 mesylate GABAA agonist €90.00
3406 Demoxepam Metabolite of Chlordiazepoxide €120.00
3388 Etifoxine PAM of GABAA €90.00
3331 Etifoxine hydrochloride PAM of GABAA €110.00
4047 Fluralaner GABA/L-glutamate gated chloride channel inhibitor €80.00
1301 Gabapentin GABA modulator; Anti-convulsant €65.00
1196 L 838417 GABAA-α1 antagonist €90.00
3390 L-655,708 Selective inverse agonist of GABAA-α5 €120.00
2833 N-Desmethyl-PK 11195 Radioligand precursor of the benzodiazepine antagonist PK 11195 €105.00
1121 NBI 34060 PAM of GABAA-α1 €95.00
1457 NS 11394 PAM of GABAA €110.00
1208 PK 11195 Benzodiazepine antagonist €65.00
1195 SL 651498 GABAA-α2 agonist €80.00
3119 Stiripentol PAM of GABAA €70.00
1422 TP003 GABAA-α3 agonist €80.00
1646 Zaleplon GABAA-α1 agonist €70.00
1197 Zopiclone Benzodiazepine agonist €70.00

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