CX 717是一种AMPA受体的正变构调节剂。
Cas No.:867276-98-0
Sample solution is provided at 25 µL, 10mM.
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CX 717 is a positive allosteric modulator of the AMPA receptor. CX 717 exerts rapid antidepressant-like effects by increasing brain-derived neurotrophic factor (BDNF) and p11 levels[1-2]. CX 717 is primarily used in research related to attention deficit hyperactivity disorder (ADHD) and the reversal of opioid-induced respiratory depression[3-4].
In vitro, cortical neurons were treated with CX 717 (0.33mM or 10mM), and intracellular calcium levels were measured immediately. CX 717 exerted only a minimal effect on both the rapid, initial phase and the late, slow phase of AMPA-induced cytosolic calcium elevation[5]. Treatment of U87 glioblastoma cells with CX 717 (0-2.5mM) for 24 hours did not significantly alter cell viability. CX 717 failed to enhance the oncolytic effect of fluoxetine (FLX) when used in combination[6].
In vivo, CX 717 (15mg/kg) was intraperitoneally administered to anesthetized and mechanically ventilated 129SVE mice 10 minutes before exposure to intermittent hypoxia (IH). CX 717 significantly enhanced the long-term facilitation of inspiratory burst amplitude in the hypoglossal (XII) nerve induced by IH[7]. In adult male Sprague-Dawley rats, a single injection of CX 717 (20mM; 15μl; delivered over 60 seconds) was administered via an intrathecal catheter placed at the fourth cervical segment (C4). CX 717 treatment produced a gradual and sustained increase in phrenic nerve inspiratory burst amplitude[8].
References:
[1] Porrino LJ, Daunais JB, Rogers GA, et al. Facilitation of task performance and removal of the effects of sleep deprivation by an ampakine (CX717) in nonhuman primates. PLoS Biol. 2005 Sep;3(9):e299.
[2] Gordillo-Salas M, Pascual-Antón R, Ren J, et al. Antidepressant-Like Effects of CX717, a Positive Allosteric Modulator of AMPA Receptors. Mol Neurobiol. 2020 Aug;57(8):3498-3507.
[3] Radin DP, Cerne R, Smith JL, et al. Low-impact ampakine CX717 exhibits promising therapeutic profile in adults with ADHD - A phase 2A clinical trial. Eur J Pharmacol. 2025 Oct 15;1005:178047.
[4] Ren J, Ding X, Funk GD, et al. Ampakine CX717 protects against fentanyl-induced respiratory depression and lethal apnea in rats. Anesthesiology. 2009 Jun;110(6):1364-70.
[5] Radin DP, Zhong S, Cerne R, et al. High Impact AMPAkines Induce a Gq-Protein Coupled Endoplasmic Calcium Release in Cortical Neurons: A Possible Mechanism for Explaining the Toxicity of High Impact AMPAkines. Synapse. 2024 Sep;78(5):e22310.
[6] Radin DP, Purcell R, Lippa AS. Oncolytic Properties of Ampakines In Vitro. Anticancer Res. 2018 Jan;38(1):265-269.
[7] Thakre PP, Sunshine MD, Fuller DD. Spinally delivered ampakine CX717 increases phrenic motor output in adult rats. Respir Physiol Neurobiol. 2022 Feb;296:103814.
[8] Kara NZ, Flaisher-Grinberg S, Einat H. Partial effects of the AMPAkine CX717 in a strain specific battery of tests for manic-like behavior in black Swiss mice. Pharmacol Rep. 2015 Oct;67(5):928-33.
CX 717是一种AMPA受体的正变构调节剂。CX 717可通过增加脑源性神经营养因子（BDNF）和p11水平发挥快速抗抑郁效应[1-2]。CX 717主要被用于注意力缺陷多动障碍（ADHD）和逆转阿片类药物所致呼吸抑制的相关研究[3-4]。
在体外，CX 717（0.33mM或10mM）处理皮层神经元细胞，立即测定胞内钙离子水平。CX 717对AMPA诱导的胞质钙离子快速升高阶段和缓慢升高阶段均仅有最小的影响[5]。CX 717（0-2.5mM）U87胶质母细胞瘤细胞24小时，未显著改变细胞活力；与氟西汀（FLX）联合使用时，CX 717未能增强FLX的溶瘤效果[6]。
在体内，CX 717（15mg/kg）间歇性低氧（IH）暴露前10分钟腹腔注射于麻醉并机械通气的129SVE小鼠。CX 717显著增强IH诱导的舌下神经（XII）吸气爆发振幅的长期增强效应[7]。CX 717（20mM；15μl；60秒内推注）通过置于第四颈段（C4）的鞘内导管单次注射于成年雄性Sprague-Dawley大鼠。CX 717处理导致膈神经吸气爆发振幅产生逐渐且持续的增强[8]。
| Cell experiment [1]: | |
Cell lines | U87 glioblastoma cells |
Preparation Method | U87 cells were seeded and incubated overnight. Cells were then treated with CX 717 (0-2.5mM). |
Reaction Conditions | 0-2.5mM; 24 hours. |
Applications | CX 717 did not significantly alter the cell viability of U87 cells. CX 717 failed to enhance the oncolytic activity of fluoxetine (FLX) in U87 cells. |
| Animal experiment [2]: | |
Animal models | Adult male 129SVE mice |
Preparation Method | Mice were anesthetized with urethane, mechanically ventilated, and bilaterally vagotomized. Efferent inspiratory bursting was recorded from the hypoglossal (XII) nerve. Mice received an intraperitoneal (i.p.) injection of CX 717 10 minutes before being exposed to intermittent hypoxia (IH). |
Dosage form | 15mg/kg; i.p.; single injection. |
Applications | Pretreatment with CX 717 significantly potentiated intermittent hypoxia-induced long-term facilitation (LTF) of inspiratory burst amplitude recorded from the hypoglossal nerve. This enhancement was particularly evident when the initial baseline burst amplitude was low. |
References: | |
| Cas No. | 867276-98-0 | SDF | Download SDF |
| 别名 | 苯并[C][1,2,5]恶二唑-5-基(吗啉)甲酮 | ||
| 分子式 | C11H11N3O3 | 分子量 | 233.22 |
| 溶解度 | DMSO : 100 mg/mL (428.78 mM; Need ultrasonic) | 储存条件 | 4°C, protect from light |
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.2878 mL | 21.439 mL | 42.878 mL |
| 5 mM | 857.6 μL | 4.2878 mL | 8.5756 mL |
| 10 mM | 428.8 μL | 2.1439 mL | 4.2878 mL |
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