AR-M 1896是一种新型的、具有高度选择性的甘丙肽2型受体（GalR2）激动剂（IC50=1.76nM）。
Cas No.:367518-31-8
Sample solution is provided at 25 µL, 10mM.
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AR-M 1896 is a novel, highly selective galanin type 2 receptor (GalR2) agonist (IC₅₀=1.76nM)[1-2]. AR-M 1896 modulates neuropeptide signaling pathways by specifically activating the GalR2 receptor, thereby exerting neuroprotective, anti-inflammatory, and pain-modulating effects. AR-M 1896 can be used in research related to acute myocardial infarction, neuropathic pain, and epilepsy[3-4].
In vitro, treatment of primary cultured cortical neurons ischemia model with AR-M 1896 (1nM to 10μM) for 15min did not increase neuronal viability or reduce lactate dehydrogenase (LDH) release in a dose-dependent manner, unlike galanin[5]. Treatment of rat pheochromocytoma (PC12) cells stably transfected with GFP-labeled galanin type 2 receptor (GalR2) with AR-M 1896 (100nM) for 24h induced caspase-dependent apoptosis, inhibited the PI3K/Akt signaling pathway, and caused cell cycle arrest in the sub‑G1 phase[6].
In vivo, AR-M 1896 (0.1μM/paw) was administered to rats via plantar injection on days 5 and 7 after median nerve chronic constriction injury (CCI). AR‑M 1896 slightly aggravated CCI-induced mechanical allodynia and significantly increased the number of c‑Fos‑positive neurons in the cuneate nucleus (CN) after electrical stimulation of the injured nerve[7]. AR‑M 1896 (3pmol) and calcitonin gene-related peptide (CGRP; 10pmol) were co-administered to CD-1 mice via intradermal injection; AR‑M 1896 significantly suppressed CGRP-induced inflammatory skin edema (plasma extravasation)[8].
References:
[1] Liu HX, Brumovsky P, Schmidt R, et al. Receptor subtype-specific pronociceptive and analgesic actions of galanin in the spinal cord: selective actions via GalR1 and GalR2 receptors. Proc Natl Acad Sci U S A. 2001 Aug 14;98(17):9960-4.
[2] Serebryakova L, Pal'keeva M, Studneva I, et al. Galanin and its N-terminal fragments reduce acute myocardial infarction in rats. Peptides. 2019 Jan;111:127-131.
[3] Pirondi S, Fernandez M, Schmidt R, et al. The galanin-R2 agonist AR-M1896 reduces glutamate toxicity in primary neural hippocampal cells. J Neurochem. 2005 Nov;95(3):821-33.
[4] Kerekes N, Mennicken F, O'Donnell D, et al. Galanin increases membrane excitability and enhances Ca(2+) currents in adult, acutely dissociated dorsal root ganglion neurons. Eur J Neurosci. 2003 Dec;18(11):2957-66.
[5] Li Y, Mei Z, Liu S, et al. Galanin Protects from Caspase-8/12-initiated Neuronal Apoptosis in the Ischemic Mouse Brain via GalR1. Aging Dis. 2017 Feb 1;8(1):85-100.
[6] Tofighi R, Joseph B, Xia S, et al. Galanin decreases proliferation of PC12 cells and induces apoptosis via its subtype 2 receptor (GalR2). Proc Natl Acad Sci U S A. 2008 Feb 19;105(7):2717-22.
[7] Chen SH, Lue JH, Hsiao YJ, et al. Elevated galanin receptor type 2 primarily contributes to mechanical hypersensitivity after median nerve injury. PLoS One. 2018 Jun 21;13(6):e0199512.
[8] Schmidhuber SM, Rauch I, Kofler B, et al. Evidence that the modulatory effect of galanin on inflammatory edema formation is mediated by the galanin receptor 3 in the murine microvasculature. J Mol Neurosci. 2009 Feb;37(2):177-81.
AR-M 1896是一种新型的、具有高度选择性的甘丙肽2型受体（GalR2）激动剂（IC50=1.76nM）[1-2]。AR-M 1896通过特异性激活GalR2受体来调节神经肽信号传导，从而发挥神经保护、抗炎和调节疼痛感知等作用。AR-M 1896可用于急性心肌梗死、神经性疼痛以及癫痫的相关研究[3-4]。
在体外，AR-M 1896（1nM至10μM）处理原代培养皮层神经元缺血模型15分钟。AR-M 1896未能像甘丙肽那样以剂量依赖方式提高神经元存活率或降低乳酸脱氢酶（LDH）释放 [5]。AR-M 1896（100nM）处理稳定转染了GFP标记的甘丙肽2型受体（GalR2）的大鼠嗜铬细胞瘤（PC12）细胞24小时，能诱导caspase依赖的细胞凋亡，抑制PI3K/Akt信号通路，并导致细胞周期停滞于亚G1期[6]。
在体内，AR-M 1896（0.1μM/paw）于正中神经慢性压迫损伤（CCI）后第5天和第7天通过足底注射给予大鼠。AR-M 1896略微加重了CCI诱导的机械性痛觉过敏，并显著增加了电刺激损伤神经后楔束核（CN）中c-Fos阳性神经元的数量[7]。AR-M 1896（3pmol）和降钙素基因相关肽（CGRP；10pmol）共同通过皮内注射给予CD-1小鼠，AR-M 1896能显著抑制由CGRP诱导的皮肤炎症性水肿[8]。
| Cell experiment [1]: | |
Cell lines | Rat pheochromocytoma (PC12) cells stably transfected with GFP-tagged galanin receptor subtype 2 (GalR2) and non-transfected (native) PC12 cells |
Preparation Method | PC12 and GFP-GalR2-transfected PC12 cells were cultured. Cells were exposed to AR-M 1896 (100nM; 24h). |
Reaction Conditions | 100μM; 24h. |
Applications | In GFP-GalR2-transfected cells, AR-M 1896 induced caspase-dependent apoptotic cell death, as shown by a significant increase in apoptotic nuclei and caspase-3-like activity. AR-M 1896 also led to a down-regulation of phosphorylated Akt (pAkt) and phosphorylated Bad (pBad), indicating inhibition of the PI3K/Akt survival pathway. In contrast, in non-transfected native PC12 cells, AR-M 1896 did not significantly induce apoptosis. Flow cytometry analysis indicated that treatment in transfected cells resulted in a significant population of cells in the sub-G1 phase, indicative of cell death. |
| Animal experiment [2]: | |
Animal models | Sprague-Dawley rats with median nerve chronic constriction injury (CCI) |
Preparation Method | Rats received intraplantar injection of AR-M 1896 (0.1µM/paw) on day 5 and day 7 after CCI. The forepaw withdrawal threshold was assessed using von Frey filaments, and neuronal activation (c-Fos expression) in the cuneate nucleus (CN) was examined after electrical stimulation of the injured nerve on day 7. |
Dosage form | 0.1µM/paw; intraplantar injection; Two doses (on day 5 and day 7 post-CCI). |
Applications | AR-M 1896 administration slightly aggravated CCI-induced mechanical allodynia (tactile hypersensitivity). Furthermore, AR-M 1896 significantly increased the number of c-Fos-positive neurons in the cuneate nucleus following electrical stimulation of the injured median nerve. |
References: | |
| Cas No. | 367518-31-8 | SDF | |
| Canonical SMILES | CC(C[C@@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/C/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](N)([H])CC1=CNC2=CC=CC=C12)([H])[C@@](O)([H])C)([H])CC(C)C)([H])CC(O)=N)([H])CO)([H])C)([H])CC3=CC=C(O)C=C3)([H])CC(C)C)([H])C(O)=N)C | ||
| 分子式 | C54H81N13O14 | 分子量 | 1136.31 |
| 溶解度 | Soluble to 1 mg/ml in 20% formic acid | 储存条件 | Desiccate at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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1 mg | 5 mg | 10 mg |
| 1 mM | 880 μL | 4.4002 mL | 8.8004 mL |
| 5 mM | 176 μL | 880 μL | 1.7601 mL |
| 10 mM | 88 μL | 440 μL | 880 μL |
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