glyr

PSEM 89S TFA is a brain-penetrant and selective ion channels agonist, and is orthogonally selective for Q79G and L141F, respectively.

Picrotin is an inhibitor of glycine receptors. Picrotin blocks α2 GlyR, α1 GlyR, and α3 GlyR and can be used in studies about neurotransmission.

Alanine is a nonessential amino acid made in the body from the conversion of the carbohydrate pyruvate or the breakdown of DNA and the dipeptides carnosine and anserine. D-Alanine ((R)-Alanine) is a weak GlyR (inhibitory glycine receptor) and PMBA agonist, with an EC50 of 9 mM for GlyR.

GlyRS-IN-1 is an inhibitor of glycyl-tRNA synthase (GlyRS). It can inhibit the growth of bacteria.

LQVTDSGLYRCVIYHPP (LP17) is a peptide and TREM-1 (Triggering Receptor Expressed on Myeloid cells 1) inhibitor derived from a highly conserved sequence between the extracellular structural domains of mouse and human TREM-1 and TLT-1.LP17 inhibits TREM-1 activation through a decoy receptor LP17 inhibits TREM-1 activation by actin through a decoy receptor mechanism, which has the advantage of penetrating the brain barrier and attenuating neuronal damage and inflammatory responses.

LQVTDSGLYRCVIYHPP (LP17) TFA is a TREM-1 (triggering receptor expressed on myeloid cells) inhibitory peptide that significantly reduces ischemic infarction and neuronal damage, with the ability to penetrate the brain to inhibit TREM-1 [1].

Anti-PGLYRP1/PGRP-S Antibody is a CHO-expressed human antibody targeting PGLYRP1/PGRP-S. It features a huIgG4SP heavy chain and a huκ light chain, with an estimated molecular weight (MW) of 150 kDa. For isotype control, refer to Human IgG4 kappa, Isotype Control.

Broflanilide is an insecticide-resistant GABA receptor antagonist for dieldrin. Its metabolite, Desmethyl-Broflanilide, can inhibit the RDL GABAR of the striped night moth, with an IC50 value of 1.3 nM.

NFPS exerts neuroprotection via glyR alpha1 subunit in the rat model of transient focal cerebral ischaemia and reperfusion. NFPS is a selective and non-competitive glycine transporter-1 (GlyT1) inhibitor (IC50s: 2.8 nM and 9.8 nM for hGlyT1 and rGlyT1, respectively).

uPSEM792 hydrochloride is an agonist of PSAM4-GlyR.

uPSEM792 is a pharmacologically selective agonist molecule (PSEM) for PSAM4-GlyR, with an affinity Ki of 0.7 nM. It acts as a substrate for efflux transporters in both wild-type mice brains and in P-gp and BCRP double knockout mice. Additionally, uPSEM792 may serve as a lead compound in the development of PET radioligands for PSAM4-GlyR.

Ultrapotent PSEM (uPSEM) agonist for PSAM4-GlyR and PSAM4-5HT3 (Ki = 0.7 nM for PSAM4-GlyR and <10 nM for PSAM4-5HT3). Exhibits >10,000-fold agonist selectivity for PSAM4-GlyR over α7-GlyR, α7-5HT3, and 5HT3-R, and 230-fold selectivity over α4β2 nAChR. Also weak partial agonist (~10 %) at α4β2 nAChR. Retains the potency of varenicline (Cat.No. 3754) for PSAM4-GlyR with enhanced chemogenetic selectivity. Does not act as a substrate for P-glycoprotein pumps. Silences neurons in vivo. Brain-penetrant. Magnus et al (2019) Ultrapotent chemogenetics for research and potential clinical applications. Science doi: 10.1126/science PMID:30872534

Selective ultrapotent PSEM (uPSEM) agonist for α7L131G,Q139L,Y217F-GlyR (PSAM4-GlyR) and PSAM4-5-HT3 chimeric ion channel agonist (EC50 values are 0.3 and 0.5 nM, respectively). Suppresses firing of layer 2/3 cortical neurons expressing PSAM4-GlyR in brain slices. Increases contralateral rotation in mice expressing PSAM4-GlyR unilaterally in the substantia nigra reticulata (LED 0.1 mg/kg). Magnus et al (2019) Ultrapotent chemogenetics for research and potential clinical applications. Science 364 PMID:30872534

PSAM (pharmacologically selective actuator module) agonist. Activates PSAML141F-GlyR chimeric ion channels. Inhibits activity of neurons expressing PSAML141F-GlyR in vivo and activates locus coeruleus noradrenergic neurons expressing PSAML141F,Y115F-5-HT3 ion channels. Recommended concentration for use in mice is 5 mg/kg or lower. Plasmid vectors for the transfection of cells with PSAML141F-GlyR and PSAML141F,Y115F-5-HT3 are available from Addgene. Lovett-Barron et al (2012) Regulation of neuronal input transformations by tunable dendritic inhibition. Nat.Neurosci. 15 423 PMID:22246433 |Satoh et al (2016) Context-dependent gait choice elicited by EphA4 mutation in Lbx1 spinal interneurons. Neuron 89 1046 PMID:26924434 |Atasoy et al (2012) Deconstruction of a neural circuit for hunger. Nature 488 172 PMID:22801496 |Hirschberg et al (2017) Functional dichotomy in spinal- vs prefrontal-projecting locus coeruleus modules splits descending noradrenergic analgesia from ascending aversion and anxiety in rats. Elife 6 e29808 PMID:29027903

AM1488 is a potent, orally active glycine receptor (GlyR) potentiator with an effective concentration (hGlyRα3 EC50) of 0.45 µM [1] [2].