glycine site

Neboglamine hydrochloride (CR-2249 hydrochloride) 是一种具有口服活性的 NMDA 受体正向调节剂，具有神经保护活性，可增强认知，可用于研究精神分裂症和红斑狼疮。

1-Aminocyclobutanecarboxylic acid (ACBC) 是一种NMDA 受体部分激动剂，作用于 NR1 甘氨酸位点。

CGP 78608 hydrochloride 是 NMDA 受体甘氨酸结合位点的特异性拮抗剂 (IC50 = 6 nM)。 CGP 78608 hydrochloride 具有抗惊厥活性。 CGP 78608 hydrochloride 增强 GluN1 GluN3A 介导的甘氨酸电流（估计 EC50 = 26.3 nM）。

AV-101 (4-Cl-KYN) 是 NMDA 受体甘氨酸位点的前药拮抗剂，具有抗抑郁活性，可减少 MPTP 猴子中左旋多巴诱导的运动障碍。

Rapastinel acetate 是 N-甲基-D-天冬氨酸 (NMDA) 受体的调节剂和甘氨酸位点的部分激动剂，具有长效抗抑郁作用。

7-Chlorokynurenic acid (7-chloro-4-hydroxy-2-carboxyquinoline) 是一种有效的选择性 NMDA 受体拮抗剂，对甘氨酸 B 激动剂位点的 IC50 为 0.56 μM。 7-Chlorokynurenic acid 抑制谷氨酸再摄取到突触小泡中，Ki 为 0.59 μM，并在神经轴输送后显示出镇痛作用。

Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) 是一种 NMDA 受体调节剂，具有甘氨酸位点部分激动剂性质，有研究抑郁症的潜力。

L-701324 是一种 NMDA 受体，对甘氨酸位点具有高亲和力和选择性，用作口服活性和长效抗惊厥药。

L-701252 是一种有效的甘氨酸位点 NMDA 受体拮抗剂，IC50 值为 420 nM。L-701252 对全脑缺血提供小范围的神经保护。

HA-966 HCl is an NMDA receptor complex glycine site antagonist.

RPR104632 是一种新型有效的位于 NMDA 甘氨酸位点的拮抗剂，具有神经保护活性。

FN-A208 是源自鼠层粘连蛋白 a1 的 A208 与纤连蛋白 (GRGDS) 活性位点和甘氨酸间隔区融合形成的生物活性肽。该肽能形成淀粉样原纤维，并有助于促进肌动蛋白应力纤维的形成，进而介导成纤维细胞附着，显示出其在组织再生和工程生物粘合剂方面的应用潜力。FN-A208 与 IKVAV 受体和整合素发生相互作用，而在 EDTA 存在下，其活性则会被破坏。

Obestatin is a 23 amino acid peptide hormone with a conserved C-terminal glycine residue and amidation site that is formed by cleavage of the ghrelin and obestatin prepropeptide.1It binds to the orphan receptor GPR39 (Kd= 1 nM) and stimulates cAMP production in CHO and HEK293 cells overexpressing human GPR39. Obestatin inhibits contraction of isolated mouse jejunum muscle strips induced by ghrelin .In vivo, obestatin (12.5-1,000 nmol/kg) suppresses food intake in a time- and dose-dependent manner and reduces body weight gain and gastric emptying in mice. Obestatin (0.22 g per animal) also reduces food intake and glucose response without affecting plasma insulin responses in fasted high-fat diet fed mice.2 1.Zhang, J.V., Ren, P.C., Avsian-Kretchmer, O., et al.Obestatin, a peptide encoded by the ghrelin gene, opposes ghrelin's effects on food intakeScience310(5750)996-999(2005) 2.Subasinghage, A.P., Green, B.D., Flatt, P.R., et al.Metabolic and structural properties of human obestatin {1-23} and two fragment peptidesPeptides31(9)1697-1705(2010)

GV-196771 selectively antagonize the glycine-binding site of the NMDA ionophore.

NMDA receptor antagonist6 (compound 13b) 为针对甘氨酸结合位点的NMDA 受体拮抗剂，其展现出对PC12 细胞的神经保护功能，能够抵御NMDA引起的细胞损伤及细胞凋亡。

L-689560 是 N-甲基-D-天冬氨酸受体（NMDA）的有效拮抗剂，抑制 NMDA 甘氨酸结合位点。它用于研究 NMDA 受体在正常神经系统过程以及疾病中的作用，也广泛用作结合研究中的放射性标记配体，也。

HA-966 trihydrate is an NMDA receptor complex glycine site antagonist.

MDL 100748 is a glycine site antagonist of NMDA receptor.

1-Aminocyclopropane-1-carboxylic acid (ACC) 是内源性代谢产物的一种。

H-Arg-Gly-Asp-Cys-OH is a tetrapeptide that contains the arginine-glycine-aspartate (RGD) motif, a sequence that acts as a recognition site for various adhesion proteins.1It inhibits the binding of fibrinogen to endothelial cells and ADP-stimulated platelets with IC50values of 320 and 35 μM, respectively.2Implantation of titanium rods coated with H-Arg-Gly-Asp-Cys-OH increases bone formation in rat femurs.3H-Arg-Gly-Asp-Cys-OH has been conjugated to polyethylenimine to improve gene transfection efficiency.4 1.Park, H.S., Kim, C., and Kang, Y.K.Preferred conformations of RGDX tetrapeptides to inhibit the binding of fibrinogen to plateletsBiopolymers63(5)298-313(2002) 2.Tranqui, L., Andrieux, A., Hudry-Clergeon, G., et al.Differential structural requirements for fibrinogen binding to platelets and to endothelial cellsJ. Cell Biol.108(6)2519-2527(1989) 3.Ferris, D.M., Moodie, G.D., Dimond, P.M., et al.RGD-coated titanium implants stimulate increased bone formation in vivoBiomaterials20(23-24)2323-2331(1999) 4.Kunath, K., Merdan, T., Hegener, O., et al.Integrin targeting using RGD-PEI conjugates for in vitro gene transferJ. Gene Med.5(7)588-599(2003)

Gavestinel sodium 是一种非竞争性的 NMDA 受体拮抗剂，具有有效性、选择性和口服活性。Gavestinel sodium可与 NMDA 受体的甘氨酸位点结合，其结合亲和力(pKi 值)为 8.5。Gavestinel sodium 可用于急性缺血性脑卒中研究。

RGD-4C（ACDCRGDCFC）是一种携带Arg-Gly-Asp（RGD）序列的肽，具备与αv整合素结合的能力，用于模拟细胞外基质蛋白的整合素识别特性。作为αv整合素的配体，它能够与生物活性分子进行偶联，进而在动物模型中展现出抗肿瘤活性。

GW-468816 is a glycine site NMDA receptor antagonist.

ACEA1011 is a glycine site NMDA receptor antagonist. It may have analgesic effects.

7-Chlorokynurenic acid sodium salt (7-CKA sodium salt) is a potent and selective antagonist of the glycine B coagonist site of the NMDA receptor (IC50: 0.56 μM). It is also a potent inhibitor of the reuptake of glutamate into synaptic vesicles (Ki: 0.59 μ

CGP-78608 is a glycine site-specific N-methyl-D-aspartate receptor antagonist prevents activation of the NMDA/NO/CGMP pathway by ammonia.

5,7-Dichlorokynurenic acid (5,7-dichlorokynurenic acid sodium) 是一种专门针对于NMDA 受体甘氨酸位点的竞争性拮抗剂(KB:65 nM)。它是犬尿酸的衍生物，可降低大鼠皮质细胞培养物中 NMDA 诱导的神经元损伤程度。

GV-196771A 一种新型的NMDA受体甘氨酸位点拮抗剂，具有强大的抗痛觉过敏活性。