glyr

D-Alanine ((R)-Alanine) 是一种GlyR 和PMBA 的弱激动剂，其对GlyR 的EC50=9 mM。

PSEM 89S TFA 是一种脑渗透性和选择性离子通道激动剂，分别对 Q79G 和 L141F 具有正交选择性。

Picrotin 是甘氨酸受体的抑制剂。 Picrotin 阻断 α2 GlyR、α1 GlyR 和 α3 GlyR，可用于神经传递研究。

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

LQVTDSGLYRCVIYHPP（LP17）是一种多肽和TREM-1(Triggering Receptor Expressed on Myeloid cells 1)抑制剂，序列来源于小鼠和人类TREM-1和TLT-1胞外结构域之间的高度保守序列，通过类似于诱饵受体的机制抑制肌动蛋白激活TREM-1，具有可穿透大脑屏障的优点，能够减轻神经元损伤和炎症反应。

Lqvtdsglyrcviyhpp TFA 是一种由17个氨基酸组成的多肽，是可穿透血脑屏障的触发受体1 (TREM-1) 抑制剂，具有潜在的抗癌活性，可用于研究皮肤癌和胰腺癌。

Broflanilide 是昆虫抗狄氏剂 GABA 受体拮抗剂，可代谢为 Desmethyl-Broflanilide，抑制斜纹夜蛾 RDL GABAR，IC50值为 1.3 nM。

MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan 是一种抗体偶联活性分子的一部分 (drug-linker conjugate for ADC)，包含 Exatecan 。Exatecan 是一种 DNA 拓扑异构酶 I (Topoisomerase I) 抑制剂 (IC50=2.2 μM)。

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).

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 是一种有效的、具有口服活性的甘氨酸受体 (GlyR) 增效剂 (hGlyRα3EC50=0.45 μM)。